Idorsia Ltd. · SIX:IDIA
Idorsia — Investor Presentation (October 2020)
186 slides from Idorsia's investor presentation, October 2020
Slide 1: Idorsia – Reaching out for more
Idorsia – Reaching out for more
Slide 2: Forward-looking statements
The following information contains certain “forward-looking statements”, relating to the company’s business, which can be identified by the use of forward-looking terminology such as “estimates”, “believes”, “expects”, “may”, “are expected to”, “will”, “will continue”, “should”, “would be”, “seeks”,
Slide 3: 15 June 2017
15 June 2017 3 Idorsia - Reaching out for more | October 2020
Slide 4: The purpose of Idorsia
The purpose of Idorsia is to discover, develop and bring more, innovative medicines to patients. We have more ideas, we see more opportunities and we want to help more patients. 4 Idorsia - Reaching out for more | October 2020
Slide 5: Highlights
Highlights Positive pivotal results with daridorexant for insomnia 20 NINE-MONTH First pivotal study 20 of daridorexant presented at SLEEP 2020 Issuance of 23.8 On target for NDA filing million new of daridorexant around shares raises the end of 2020 CHF 535.5 million 5 Idorsia - Reaching out for mo
Slide 6: Idorsia Today
Idorsia Today >800 Highly qualified 12 professionals Compounds in the pipeline, with four in the final stage of development Strong balance sheet > 550 State-of-the-art laboratory workspaces 6 Idorsia - Reaching out for more | October 2020
Slide 7: Our Strategic Priorities
Our Strategic Priorities Our mid-term key priorities to 2 Build and integrate a commercial organization achieve long-term 3 Bring Idorsia to success: sustainable profitability 1 Deliver at least three products to market in the mid-term 4 Create a pipeline with a sales potential of CHF 5 billion 5 Ut
Slide 8: Idorsia's potential first revenue stream
Idorsia’s potential first revenue stream Ponesimod for the treatment of adults with relapsing multiple sclerosis (MS) • Ponesimod is an investigational highly- selective phingosine-1-phosphate receptor 1 (S1P1) modulator that functionally inhibits S1P receptor Phase 3 data presented by Janssen activ
Slide 9: Clinical development pipeline
Insomnia Clinical development pipeline Resistant hypertension management Daridorexant Dual orexin receptor Aprocitentan* antagonist Dual endothelin receptor Status: Filing in preparation antagonist Fabry disease Status: Phase 3 Systemic lupus Suspected acute erythematosus myocardial infarction Lucer
Slide 10: Lucerastat in Fabry disease
Lucerastat in Fabry disease Lucerastat is investigational, in development and not approved or marketed in any country. 10 Idorsia - Reaching out for more | October 2020
Slide 11: Fabry disease
Fabry disease Fabry disease is a rare inherited lysosomal storage disorder in which a particular lipid (a fat-like substance) can’t be broken down by the body, leading to its build-up in the cells of the body organs which results in cell and organ damage Fabry disease is often undetected or misdiagn
Slide 12: What is the role of lipids in the body?
What is the role of lipids in the body? • Lipids are fat-like substances What happens in patients with lysosomal storage disorders? such as fatty acids, oils, waxes Normal breakdown of lipids and steroids. A well-known example is cholesterol • Lipids are stored naturally in the body’s cells and orga
Slide 13: Fabry disease biochemical mechanism
Fabry disease Biochemical mechanism cis-Golgi SM Dysfunctional or absent GCS α-galactosidase A Cer GlcCer Gb3 results in accumulation of Gb3 in various organs Gb3 Sph Plasma α-GalA Membrane Sph Gb3 Cer ceramide GCS glucosylceramide synthase GlcCer glucosylceramide Gb3 globotriaosylceramide lysoGb3 g
Slide 14: Inheritance pattern in Fabry disease
Inheritance pattern in Fabry disease X-linked recessive genetic disease • GLA gene mutation results in defective lysosomal enzyme α-GalA • In turn, this results in Gb3 accumulation Random X-inactivation in Fabry female ‘carriers’: both genders affected Male have generally Females have higher classic
Slide 15: Clinical manifestations of Fabry disease
Clinical manifestations of Fabry disease Large spectrum of clinical, heterogeneous manifestations Neuropathic pain Pain resulting from damage to or dysfunction Kidneys of the nervous system • Gradually progressing Cysts, reduced kidney Eyes function, progressive The appearance in severity from of th
Slide 16: Diagnosis of Fabry disease
Diagnosis of Fabry disease Clinical symptoms Clinical events Pedigree analysis Neuropathic pain, GI, Stroke, cardiac Family members hearing loss, and renal events (between children hypohydrosis and parents) Enzyme assay Genotyping Biomarkers Leukocyte α-GalA >830 mutations Gb3 in plasma and urine 16
Slide 17: Epidemiology of Fabry disease
Epidemiology of Fabry disease Patients diagnosed with Fabry disease 2018 patients, n in EU-5 and US in 2018 EU-5 3,507 UK 890 Italy 828 Germany 692 France 562 Spain 535 US 3,875 Total 7,382 Delveinsight, Fabry Disease – Market Insight, Epidemiology and Market Forecast – 2028 17 Idorsia - Reaching ou
Slide 18: Current therapies in Fabry disease
Current therapies in Fabry disease No curative Symptomatic Etiological therapies limited therapy treatments not satisfactory Enzyme replacement Chaperone therapy therapy • Fabrazyme (agalsidase beta) • Galafold (migalastat) for (US and EU) patients with amenable • Replagal (agalsidase alfa) mutation
Slide 19: Lucerastat in Fabry disease
Lucerastat in Fabry disease Bioavailability Orally available, highly soluble small molecule with rapid and complete absorption Tissue penetration Access to most tissues, including peripheral and central nervous system For all mutations Potential to treat all Fabry patients irrespective of the underl
Slide 20: Lucerastat mode of action
Lucerastat in Fabry disease Mode of action lucerastat cis-Golgi SM By inhibiting GCS, GCS lucerastat reduces the Cer GlcCer Gb3 precursor of Gb3 (GlcCer) and Gb3 itself Gb3 Sph Plasma α-GalA Membrane Sph Gb3 Cer ceramide GCS glucosylceramide synthase GlcCer glucosylceramide Gb3 globotriaosylceramide
Slide 21: Lucerastat has the potential to reduce Gb3 levels in target organs
Lucerastat has the potential to reduce Gb3 levels in target organs Dorsal root Kidneys Heart ganglia *ANOVA with Bonferroni’s multiple Male and female Fabry mice treated testing correction. for 20 weeks with lucerastat at 1200 mg/kg/day as food admix and Idorsia data on file. Data collected in anima
Slide 22: Mutation sensitivity
Mutation sensitivity Proven reduction in Gb3 in all tested mutation types Effect of different concentrations of lucerastat on GlcCer, Gb3, lysoGb3 lipid levels, and LysoTracker staining in cultured Fabry patients’ fibroblasts after 9 days of treatment. Each point is the mean of duplicates (±SD) Luce
Slide 23: Lucerastat clinical development plan
Lucerastat in Fabry disease Clinical development plan • Better understand medical need from Pediatric patient perspective study Confirmatory • Plan agreed Patient survey study with EMA Exploratory • MODIFY study Clinical pharmacology • Safety and proof of studies mechanism study • SAD and MAD studie
Slide 24: Lucerastat clinical pharmacology
Lucerastat in Fabry disease Clinical pharmacology Half-life: approximately 6 hours – twice daily dosing Negligible Dose-proportional food effect exposure Dose adjustment required in Low potential subjects with renal function impairment for drug-drug interaction eGFR Dosing regimen (mL/min/1.73 m2) (
Slide 25: Exploratory study design
Lucerastat in Fabry disease Exploratory study design Phase 1b study Prospective, single-center, open-label, randomized, study in 14 male/female adult patients with Fabry disease receiving enzyme replacement therapy (ERT) Screening Treatment Period Follow-up + 2 Days Phone Call Admission for patients
Slide 26: Exploratory study objectives
Lucerastat in Fabry disease Exploratory study objectives Phase 1b study Primary objective • To assess the safety and tolerability of lucerastat 1000 mg b.i.d. for 12 weeks Secondary objectives • To investigate the effect of lucerastat on plasma biomarker levels following a 12-week treatment • To ass
Slide 27: Exploratory study patient demographics
Lucerastat in Fabry disease Exploratory study patient demographics Phase 1b study Medical history: • All patients had Lucerastat group comorbidities, most of Control group them manifestations • 6 females, 4 males of Fabry disease • 4 males • Mean age (SD): 47.7 (15.0), • None of these affected • Mea
Slide 28: Exploratory study safety results
Lucerastat in Fabry disease Exploratory study safety results Phase 1b study Lucerastat was safe and well tolerated in patients with Fabry disease over 12 weeks on top of ERT One Serious Adverse Event, unrelated to lucerastat: Re-occurrence of atrial fibrillation in a patient with underlying hypertro
Slide 29: Exploratory study results: reduction in Gb3
Lucerastat in Fabry disease Exploratory study results: rapid and additional reduction in Gb3 Phase 1b when added to enzyme replacement therapy study Mean % (SD) biomarker reduction from baseline at week 12 Plasma Plasma Urinary Lucerastat was safe and well tolerated GB3 Gb3 GlcCer LacCer LysoGB3 i
Slide 30: Fabry patients survey goals
Fabry patients survey Goals Better understand Investigate key Complement patients’ disease and aspects of Phase 3 existing needs from the study MODIFY with information/data patient perspective respect to symptoms: from the literature neuropathic pain and gastrointestinal 1 symptoms 2 3 In addition,
Slide 31: Fabry patients survey key results
Fabry patients survey Key results Moderate • Fabry patients experience to severe significant Neuropathic Pain pain 51.5% (189/367) of patients 74.7% (274/367) of patients • Combining intensity, report frequent pain AND moderate/severe pain report pain in hands & feet AND moderate/severe pain frequen
Slide 32: Designing the confirmatory study
Lucerastat in Fabry disease Designing the confirmatory study Phase 3 study MODIFY • Informed design based on patients survey • Development of endpoint measurement – neuropathic pain, based on Brief Pain Inventory instrument, modified for Fabry’s neuropathic pain according to FDA guidelines for PRO −
Slide 33: Confirmatory study objectives
Lucerastat in Fabry disease Confirmatory study objectives Phase 3 study MODIFY Primary objective • To determine the effect of lucerastat on neuropathic pain in patients with Fabry disease Secondary objectives • To determine the effect of lucerastat on gastro-intestinal symptoms (abdominal pain and d
Slide 34: Confirmatory study design
Lucerastat in Fabry disease Confirmatory study design Phase 3 study MODIFY Screening 6-7 weeks Treatment 6 months Open, uncontrolled, Extension Randomization Primary/secondary 2:1 efficacy endpoints Lucerastat Placebo Site visits Stratification by Lucerastat dose Screening, Randomization, • Sex • 10
Slide 35: Confirmatory study patient population
Lucerastat in Fabry disease Confirmatory study patient population Phase 3 study MODIFY Last ERT Randomization Switched patients ERT bi-weekly for at least 12 months (stable dose regimen during the last 3 months) Placebo Pseudo-naïve patients ERT bi-weekly No ERT in at least the last 6 months Screeni
Slide 36: Confirmatory study endpoints
Lucerastat in Fabry disease Confirmatory study endpoints Phase 3 study MODIFY Primary efficacy endpoint • The primary efficacy endpoint is a response to study treatment on neuropathic pain, defined as a reduction from baseline to Month 6 of at least 30% in the “modified” BPI-SF3 score of “neuropathi
Slide 37: Lucerastat in Fabry disease summary
Lucerastat in Fabry disease A glucosylceramide synthase Phase 3 study ongoing inhibitor,developed as an oral • Lucerastat acts by reducing the monotherapy,offering a new damaging build-up of lipids which is treatment approach for all responsible for all the symptoms of patientsliving with Fabry Fabr
Slide 38: Daridorexant in insomnia
Daridorexant in insomnia Daridorexant is investigational, in development and not approved or marketed in any country. 38 Idorsia - Reaching out for more | October 2020
Slide 39: Insomnia: A disease of the night and the day
Insomnia: A disease of the night and the day High unmet need for effective, safe medications to treat insomnia ≥ 3 nights/week • Estimated approximatively 20 million (10%1) ≥ 3 months adults in the US suffer from chronic insomnia Difficulty staying asleep • Insomnia has a significant impact on patie
Slide 40: Who gets insomnia and what is the impact?
Who gets insomnia and what is the impact ? Insomnia is a Impact common problem • Physically and mentally fatigued, anxious and irritable • Increased the risk of malaise, Risk factors fall, accidents, and injury • Age (more common with ageing) • Impaired daytime functioning • Gender (women > men) • D
Slide 41: How is insomnia treated, what are the limitations?
How is insomnia treated, what are the limitations? Sleep hygiene Cognitive Pharmacological therapy • Active behavioral therapy • Many have significant limitations patient • Recommended first- • Insufficient acute effect: participation line therapy but lack of sustained effect through the night requi
Slide 42: The orexin system and wakefulness
The orexin system is crucial for the regulation of wakefulness Orexin stimulates orexin many wake-promoting pathways Dopamine (VTA) Histamine Acetylcholine (LDT, PPT) (TMN) LHA / PH Orexin Serotonin (raphe) LC OX1R Norepinephrine (LC) TMN OX2R Raphe OX1R and OX2R LTD / PPT OX1R and OX2R VTA OX1R and
Slide 43: Daridorexant in insomnia: rationale
Daridorexant in insomnia Rationale • There remains a need for effective and safe treatments for insomnia Daridorexant • Accumulating evidence for the role of the orexin (OX) system to regulate wake drive • a potent and selective dual orexin has led to the development of new receptor antagonist (DORA
Slide 44: The optimization process
The optimization process Potent DUAL OX1 and OX2 receptor blockade in vitro No major drug- drug interaction High brain penetration Optimal in Optimized duration of vivo efficacy action (fast onset, no next-day hangover) > 25,000 1,361 236 83 12 Daridorexant compounds synthesized in the Human orexin
Slide 45: Translation
Translation Preclinical healthy subjects patients Desired profile High in vitro potency in vivo efficacy Quick absorption and short half-life fast onset of action, “appropriate” duration of action to act throughout the night, and to avoid next morning residual effect Safety is key • No deterioration
Slide 46: Clinical development
Clinical development Clinical pharmacology program Today Entry into man Phase 2 studies studies Phase 3 • Single and multiple • Two studies, in adults confirmatory ascending dose and elderly patients studies • Adults and elderly subjects with insomnia • Night time administration • All information re
Slide 47: Ideal pharmacokinetic profile
Ideal pharmacokinetic profile Entry into man studies Plasma 1000 25 mg concentrations (ng/ml) 800 • Fast absorption 600 • Short half life • No accumulation over time 400 200 0 0 24 48 72 96 120 144 168 Time (h) Daridorexant is investigational, in development and not approved or marketed in any count
Slide 48: Fast and time limited pharmacodynamic effect
Fast and time limited pharmacodynamic effect Entry into man studies Speed of eye 25 mg movements (degree/sec) Adult Healthy Volunteer – Daytime dosing Elderly Healthy Volunteer – Daytime dosing Time (h) Person performing eye movement test Daridorexant is investigational, in development and not appro
Slide 49: No pharmacodynamic effect on next morning
No pharmacodynamic effect on next morning Entry into man studies Karolinska Sleepiness Placebo 25 mg Scale Score 9 Very sleepy 8 7 Sleepy, but no effort keeping awake 6 Neither alert nor 5 sleepy 4 Alert, 3 normal level 2 1 Very alert Time after first dose (h) – measures 8 hours after dosing Daridor
Slide 50: Phase 2 studies – Purpose and objectives
Phase 2 studies – Purpose and objectives Phase 2 studies Purpose Objectives To provide necessary information To characterize the dose response to adequately design the confirmatory on objective and subjective sleep trials parameters To document the safety profile Focus in particular including advers
Slide 51: Two Phase 2 studies completed
Two Phase 2 studies completed Phase 2 studies Adult study: classical parallel group design Elderly study: cross over design • 4-week treatment to assess durability of effect • 2-night treatment • Short treatment withdrawal at the end • 4 dose levels identical to adults • 4 dose levels (5 mg, 10 mg,
Slide 52: Adult study design
Adult study design Phase 2 studies 14–28 days 29 days 30 days Screening Double-blind treatment Safety follow-up PSG measurements Sleep diary Zolpidem 10 mg Placebo Daridorexant 5 mg Daridorexant 10 mg Screening Run-in period period Daridorexant 25 mg Single-blind placebo run-in (2 nights) Daridorexa
Slide 53: Adult study patient disposition
Adult study patient disposition Phase 2 studies Entry 1005 screened Sleep diary Subjective confirmation of 664 enrolled in chronic insomnia 36% placebo PSG run-in Polysomnography Objective confirmation of 360 randomized chronic insomnia (359 treated) 344 completed treatment Daridorexant is investiga
Slide 54: Demographics and baseline characteristics
Demographics and baseline characteristics Adult study (N = 359) Phase 2 studies Baseline sleep parameters Mean (SD) Demographic characteristic WASO, min 97.5 (38.6) Female, n (%) 230 (64) LPS, min 71.8 (39.3) Mean age, years (SD) 45 (11) TST, min 318.5 (56.6) Mean BMI, kg/m2 (SD) 25 (3) sWASO, min 8
Slide 55: Wake after sleep onset (WASO)
Wake after sleep onset (WASO) Adult study Phase 2 studies 0 Days 1 & 2 Days 28 & 29 -10 P<0.001 -20 Change from baseline in WASO (min) -30 -40 -50 P=0.050 -60 Placebo 5 10 25 50 Zolpidem 10 mg Daridorexant dose (mg) Data shown as mean (SE) Daridorexant is investigational, in development and not appr
Slide 56: Latency to persistent sleep (LPS)
Latency to persistent sleep (LPS) Adult study Phase 2 studies 0 Days 1 & 2 Days 28 & 29 P<0.001 -10 -20 Change from baseline in LPS (min) -30 -40 -50 P=0.042 -60 Placebo 5 10 25 50 Zolpidem 10 mg Daridorexant dose (mg) Data shown as mean (SE) Daridorexant is investigational, in development and not a
Slide 57: Subjective WASO & LSO
Subjective WASO & LSO Adult study Phase 2 studies sWASO sLSO Change from baseline in sWASO (min) Change from baseline in sLSO (min) 0 Week 2 0 Week 2 Week 4 P=0.547 Week 4 -10 -10 P=0.074 -20 -20 P=0.107 -30 -30 P=0.045 -40 -40 Zolpidem Zolpidem Placebo 5 10 25 50 Placebo 5 10 25 50 10 mg 10 mg Dari
Slide 58: Total sleep time (TST) & subjective TST
Total sleep time (TST) & subjective TST Adult study Phase 2 studies TST sTST Change from baseline in sTST (min) Change from baseline in TST (min) P<0.001 80 80 P=0.006 60 60 40 40 P<0.001 P=0.069 20 20 Days 1 & 2 Week 2 Days 28 & 29 Week 4 0 0 Zolpidem Zolpidem Placebo 5 10 25 50 Placebo 5 10 25 50
Slide 59: Normal sleep architecture preserved
Normal sleep architecture preserved Adult study Phase 2 studies Total Sleep S1 S2 SWS REM Time (min) placebo 10.7 57.4 12.6 19.3 357 5 mg daridorexant 10 55.1 15 19.9 371 10 mg daridorexant 10.7 56.8 12.5 20 384 25 mg daridorexant 9.8 55.4 12.5 22.3 387 50 mg daridorexant 10 56.2 13 20.8 403 zolpide
Slide 60: Treatment emergent adverse events
Treatment emergent adverse events Adult study Phase 2 studies Daridorexant Zolpidem Placebo 5 mg 10 mg 25 mg 50 mg 10 mg n (%) (n=60) (n=60) (n=58) (n=60) (n=61) (n=60) Participants with ≥1 TEAE 18 21 22 23 21 24 AEs leading to treatment discontinuation Angioedema 0 0 0 0 1 0 Anxiety 0 0 0 0 0 1 Art
Slide 61: Karolinska sleepiness scale (morning assessment)
Karolinska sleepiness scale (morning assessment) Adult study Phase 2 studies Extremely sleepy, 9 fighting sleep 8 Mean KSS score (±SD)* 7 6 Baseline *9-point scale; Days 1 & 2 5 = Neither alert nor sleepy Lower scores indicate less 5 Days 15 & 16 sleepiness 4 Days 28 & 29 3 2 Extremely alert 1 Place
Slide 62: Elderly study design
Elderly study design Phase 2 studies Screening Double-blind treatment Safety follow-up Treatment periods 1 2 3 4 5 Washout Washout Washout Washout Screening Placebo Randomization period nights Two consecutive polysomnography nights Daridorexant is investigational, in development and not approved or
Slide 63: Elderly study patient disposition
Elderly study patient disposition Phase 2 studies Entry 149 screened Sleep diary Subjective confirmation of 101 enrolled in chronic insomnia 39% placebo PSG run-in Polysomnography Objective confirmation of chronic insomnia 58 randomized 54 completed treatment Daridorexant is investigational, in deve
Slide 64: Demographics and baseline characteristics
Demographics and baseline characteristics Elderly study (N = 58) Phase 2 studies Baseline sleep parameters Mean (SD) Demographic characteristic WASO, min 116.9 (40.2) Median age (range), years 69 (65-85) LPS, min 75.1 (50.0) Sex, n (%) – Male 19 (33) TST, min 295.8 (57.6) Sex, n (%) – Female 39 (67)
Slide 65: Wake after sleep onset (WASO)
Wake after sleep onset (WASO) Elderly study Phase 2 studies 0 -10 -20 p < 0.001 Change from baseline -30 in WASO (min) -40 -50 -60 -70 Placebo 5 10 25 50 Daridorexant dose (mg) Dots: LSMean changes from baseline; bars: 95% CIs; dotted line = 95% CI of curve Daridorexant is investigational, in develo
Slide 66: WASO by quarter of the night
WASO by quarter of the night Elderly study Phase 2 studies 5 Dose-dependent effects were observed for WASO 0 throughout the night -5 Change from baseline -10 in WASO (min) -15 Placebo -20 Daridorexant 5 mg Daridorexant 10 mg -25 Daridorexant 25 mg -30 Daridorexant 50 mg 1st Quarter 2nd Quarter 3rd Q
Slide 67: Latency to persistent sleep (LPS)
Latency to persistent sleep (LPS) Elderly study Phase 2 studies 0 -10 -20 p = 0.004 Change from baseline in LPS (min) -30 -40 -50 -60 Placebo 5 10 25 50 Daridorexant dose (mg) Dots: LSMean changes from baseline; bars: 95% CIs; dotted line = 95% CI of curve Daridorexant is investigational, in develop
Slide 68: Subjective WASO & LSO
Subjective WASO & LSO Elderly study Phase 2 studies 20 sWASO 0 sLSO Baseline mean (overall) = 99.6 min Baseline mean (overall) = 65.7 min Mean change from baseline 0 -10 (min, 95% CI) -20 -20 -40 -30 -60 -40 Placebo 5 10 25 50 Placebo 5 10 25 50 Daridorexant dose (mg) Daridorexant dose (mg) Daridore
Slide 69: Total sleep time (TST) & subjective TST
Total sleep time (TST) & subjective TST Elderly study Phase 2 studies 150 100 TST sTST Baseline mean (overall) = 295.8 min Baseline mean (overall) = 301.7 min 80 Mean change from baseline 100 (min, 95% CI) 60 40 50 20 0 0 Placebo 5 10 25 50 Placebo 5 10 25 50 Daridorexant dose (mg) Daridorexant dose
Slide 70: Safety results
Safety results Elderly study Phase 2 studies SB- Daridorexant Placebo Placebo 5 mg 10 mg 25 mg 50 mg n, (%) (N=58) (N=54) (N=56) (N=54) (N=55) (N=56) • No SAE, no deaths Participants with ≥1 6 8 13 12 10 16 • No narcolepsy-like events adverse event Adverse event for • No suicidal ideation ≥2 partici
Slide 71: Karolinska sleepiness score (morning assessment)
Karolinska sleepiness score (morning assessment) Elderly study Phase 2 studies Extremely sleepy, 9 fighting sleep 8 7 Mean KSS score (SD) 9-point scale: 6 5 = Neither alert nor sleepy. Lower score indicates Baseline 5 improvement. Next morning after 4 treatment 3 2 Extremely alert 1 Placebo 5 10 25
Slide 72: Phase 2 conclusion
Phase 2 conclusion Phase 2 studies Efficacy • Daridorexant dose-dependently improved sleep onset, sleep maintenance, and total sleep time in adult and elderly chronic insomnia patients Safety (in the limit of the study design) • No sign of rebound or withdrawal symptoms • No clinically relevant next
Slide 73: Daridorexant registration program
Daridorexant registration program Robust program in adult and elderly insomnia patients Phase 3 program Following completion of Phase 2 studies, two similar pivotal studies of 3-month duration in moderate and severe insomnia Efficacy • Objective and subject sleep parameters (onset and maintenance) b
Slide 74: Phase 3 program overview
Phase 3 program overview Phase 3 program Main studies (12 weeks) Extension study (40 weeks) 301: placebo, 25 mg & 50 mg 303: placebo, 10 mg, 25 mg & 50 mg 302: placebo, 10 mg & 25 mg Design Duration • 3 double-blind, randomized, placebo-controlled, • 3-month treatment in main studies, 301 & 302, mul
Slide 75: Study design
Study design Phase 3 Screening 20-31days Treatment Period 84 days Safety Follow-up 30 days program Single-blind Placebo or 25 mg or 10 mg daridorexant Single- placebo run-in Double-blind blind placebo run-out Randomization 1st month 2nd month 3rd month EOT EOS V1 V2 V3 V4 V5 V6 V7 EODBT V8 V9 V10 V1
Slide 76: Phase 3 extension – Study Design
Phase 3 extension – Study Design Phase 3 program Screening Treatment Period 40 weeks Safety Follow up 30 days Run out period Either Placebo, 10, 25 or 50mg daridorexant Run out No treatment Double-blind No blinding Randomization Week 2 Week 13 Week 26 Week 40 Week 41 Week 44 V1 V2 V3 V4 EODBT, V5 EO
Slide 77: Key assessments
Key assessments Phase 3 program Objective sleep Patient’s oriented outcome assessment daily recorded Objective measures of night Subjective measures of night Assessment of impact of parameters by parameters by the sleep diary insomnia during the day by the polysomnography (PSG) in questionnaire (SDQ
Slide 78: Objective sleep assessments
Objective sleep assessments Repeated polysomnography recordings in a sleep lab in all patients Phase 3 program • Assess insomnia objectively • Ensure well-characterized insomnia patients are randomized Sensors • Establish solid baseline during placebo run-in measure brain activity, eye • Measure pri
Slide 79: Sleep diary questionnaire (SDQ)
Sleep diary questionnaire (SDQ) Daily recording Phase 3 program Morning questionnaire Evening questionnaire • 10 questions related to medication, • 2 questions related to napping quantification of sleep, awakenings • 2 visual analog scales related to • 3 visual analog scales related to alertness and
Slide 80: Subjective assessment of daytime functioning
Subjective assessment of daytime functioning Insomnia Daytime Symptoms and Impacts Questionnaire (IDSIQ) validated according to FDA guidelines Measures Items are ranked on a numeric rating scale from 0-10 19:30 1 Clear-Headed 2 Concentrate “Alert/cognition” 3 Forgetful domain score 4 Worried (0-60)
Slide 81: Study objectives
Study objectives 1st study, 50, 25 mg; 2nd study, 25, 10 mg Phase 3 program Primary objective • To evaluate the efficacy of daridorexant on objective sleep parameters in patients with insomnia. Secondary objective • To evaluate the efficacy of daridorexant on subjective sleep parameters and daytime
Slide 82: Primary and secondary endpoints
Primary and secondary endpoints Study-wise type 1 error controlled at 0.05 (across 16 comparisons to placebo) Phase 3 program Primary endpoints (night) Two dose levels − Wakening after sleep onset by PSG − High dose vs. placebo − Latency to persistent sleep by PSG − Low dose vs. placebo Secondary en
Slide 83: Statistical design and hypothesis testing
Statistical design and hypothesis testing α /2 α = 0.05 α/2 Phase 3 program H1 H2 WASO LPS H9 H10 H3 WASO LPS 1/2 1/2 sTST High dose H11 vs placebo 1/2 sTST 1/2 Low dose 1/2 1/2 1/2 Month 1 vs 1/4 1/4 1/2 1/2 placebo 1/2 H4 1/4 1/4 Month 1 IDSIQ H12 IDSIQ 1/2 1/2 H5 H6 1/2 1/2 WASO H7 LPS H13 H14 1/
Slide 84: Baseline characteristics
Baseline characteristics Phase 3 program Well-characterized moderate and severe insomnia patients Self-reported insomnia at entry Confirmed by polysomnography at baseline Sleep induction ≥ 30 minutes to fall asleep Mean LPS ≥ 20 min Sleep maintenance Wake time during sleep ≥ 30 minutes Mean WASO ≥ 3
Slide 85: Study patient disposition
Study patient disposition 1st study entry 2nd study entry 3326 screened 3683 screened Sleep diary & polysomnography 28% placebo run-in Subjective & objective confirmation placebo run-in 25% of chronic insomnia 930 randomized 924 randomized 92% 93% 853 completed 856 completed treatment treatment 847
Slide 86: Demographic characteristics
Demographic characteristics 1st pivotal study 2nd pivotal study Demographic characteristic N 930 924 Female, n (%) 624 (67.1) 638 (69.0) Mean age, years (SD) 55.4 (15.3) 56.7 (14.2) BMI < 25 39.5% 45.0% 25 – ≤ 30 41.7% 38.2% >30 18.8% 16.8% Median time from diagnosis, years 7.1 8.1 The first study w
Slide 87: Objective sleep parameters
Objective sleep parameters At 25 mg vs. placebo: highly consistent effect with that of the first pivotal study The studies demonstrated the efficacy of daridorexant in objective sleep parameters 50 mg vs 25 mg vs 25 mg vs 10 mg vs 1st pivotal study placebo placebo 2nd pivotal study placebo placebo s
Slide 88: Subjective sleep parameters
Subjective sleep parameters SDQ The studies demonstrated the efficacy of daridorexant in increasing patient’s assessed total sleep time 50 mg vs 25 mg vs 25 mg vs 10 mg vs 1st pivotal study placebo placebo 2 nd pivotal study placebo placebo significant significant significant numerical At 1 month sT
Slide 89: Daytime functioning
Daytime functioning IDSIQ sleepiness domain Daridorexant 50 mg showed statistical improvement of patient’s daytime functioning 50 mg vs 25 mg vs 25 mg vs 10 mg vs 1st pivotal study placebo placebo 2 nd pivotal study placebo placebo significant numerical numerical numerical At 1 month IDSIQ At 1 mont
Slide 90: Overview of treatment emergent adverse events
Overview of treatment emergent adverse events 1st pivotal study 2nd pivotal study Daridorexant Placebo Daridorexant Placebo 50 mg 25 mg 25 mg 10 mg n = 308 n = 310 n = 309 n = 308 n = 306 n = 306 Subjects with at least one event n (%) n (%) n (%) n (%) n (%) n (%) AE during the double-blind study pe
Slide 91: Most frequent adverse events
Most frequent adverse events* 1st pivotal study 2nd pivotal study Daridorexant Placebo Daridorexant Placebo 50 mg 25 mg 25 mg 10 mg n = 308 n = 310 n = 309 n = 308 n = 306 n = 306 Preferred Term n (%) n (%) n (%) n (%) n (%) n (%) Subjects with at least one event 117 (37.7) 116 (37.7) 105 (34.0) 121
Slide 92: Clinically relevant adverse events
Clinically relevant adverse events* 1st pivotal study 2nd pivotal study Daridorexant Placebo Daridorexant Placebo 50 mg 25 mg 25 mg 10 mg n = 308 n = 310 n = 309 n = 308 n = 306 n = 306 Adjudicated by Independent Safety Board n (%) n (%) n (%) n (%) n (%) n (%) Subjects with at least one event 2 (0.
Slide 93: Two positive pivotal studies enable filing
Two positive pivotal studies enable filing Remarkable consistency between studies 1st pivotal study 2nd pivotal study Daridorexant 50 mg Daridorexant 25 mg Daridorexant 25 mg Daridorexant 10 mg 1 month 3 months 1 month 3 months 1 month 3 months 1 month 3 months Primary WASO √ √ √ √ √ √ NS* NS* endpo
Slide 94: Program conclusion
Program conclusion The program with daridorexant demonstrated statistically significant and clinically meaningful improvements at month 1 and at month 3 Efficacy during the night and the day Safety and tolerability profile consistent between both pivotal studies Sleep • No dose-dependent treatment e
Slide 95: Preparing for a successful launch
Preparing for a successful launch Targeted for 2022 Smart Differentiated Disruptive partnering profile impact Potential to improve Opportunity to Strong regional sleep and daytime transform and partners to reach functioning without modernize broad primary care compromising safety insomnia market aud
Slide 96: Collaboration with Syneos Health
Collaboration with Syneos Health Selected as commercialization partner to launch daridorexant in the US • Idorsia will build the core capabilities needed to successfully launch daridorexant • Syneos Health selected as commercialization partner in order to effectively reach the primary care market, w
Slide 97: License agreement with Mochida
License agreement with Mochida Supply, co-development and co-marketing of daridorexant in Japan • Idorsia entitled to: − initial payment of 1 billion JPY (approx. CHF 9 million) − three additional development and regulatory milestones − sales milestones and tiered royalty payments based on net sales
Slide 98: Aprocitentan in resistant hypertension management
Aprocitentan in resistant hypertension management Aprocitentan is investigational, in development and not approved or marketed in any country. 98 Idorsia - Reaching out for more | October 2020
Slide 99: What is resistant hypertension?
What is resistant hypertension? Definition Resistant or “difficult to Not resistant hypertension control” hypertension Pseudo-resistant hypertension due to: Patients whose blood pressure • White coat effect remains high, despite receiving • Medical inertia at least three antihypertensive • Poor adhe
Slide 100: Resistant hypertension: medical need
Resistant hypertension Medical need • Hypertension is one of the most common cardiovascular risk factors, and its prevalence continues to rise • There are more than 1 billion people living with hypertension worldwide1 • Left uncontrolled, hypertension can lead to life-threatening conditions such as
Slide 101: Resistant hypertension: clinical phenotypes
Resistant hypertension Clinical phenotypes Typical characteristics of patients Poorer prognosis: higher incidence with resistant hypertension of major cardiovascular events Older age; REACH Registry n = 53,530 High baseline blood especially Excessive pressure and chronicity > 75 years dietary of unc
Slide 102: Resistant hypertension: therapeutic options
Resistant hypertension Therapeutic options Current (2018) Medical Treatment Principles Pharmacological therapy • Check that each drug is used at the maximum tolerated level • Optimize diuretic treatment • Add antihypertensive drugs with different mechanism of action • Aldosterone receptor antagonist
Slide 103: Aprocitentan rationale: endothelin system
Aprocitentan in resistant hypertension Rationale Endothelin (ET) System is involved in resistant hypertension ET system is activated in Resistant hypertension is hypertension and especially often a salt- and volume- in salt-and volume- dependent hypertension dependent hypertension ET-1 increase is E
Slide 104: Aprocitentan rationale
Aprocitentan in resistant hypertension Rationale Orally-active, potent dual ETA and ETB receptor antagonist Low potential for drug-drug Synergistic effect with interaction other antihypertensive drugs (RAAS blockers) in animal models Evidence of blockade of both receptors in vivo in humans Demonstra
Slide 105: Collaboration with Janssen Biotech, Inc.
Collaboration with Janssen Biotech, Inc. • Idorsia received up-front payment of USD 230 million • Idorsia to receive tiered royalties on annual net sales (20% up to $500 million, 30% from $500 million up to $2,000 million, and 35% above $2,000 million) • Both parties have joint development rights ov
Slide 106: Aprocitentan clinical development
Aprocitentan in resistant hypertension Clinical development • To characterize the RHT patient population SPIRIT survey • To identify sites where these patients are managed Today Clinical Phase 2 Phase 3 pharmacology study confirmatory study • Confirmation of dual ETA and ETB • Clinically relevant, d
Slide 107: Aprocitentan Phase 2 study design
Aprocitentan in resistant hypertension Phase 2 studies Design Patient population Prospective, multi-center, double-blind, double- • Mild-to-moderate essential hypertension dummy, randomized, monotherapy, placebo- and (Systolic BP/Diastolic BP ≥ 140/90 to < 180/110) active-reference, parallel group,
Slide 108: Aprocitentan dose-dependently decreases blood pressure
Aprocitentan in resistant hypertension Aprocitentan dose-dependently decreases blood pressure Phase 2 studies Diastolic Blood Pressure Systolic Blood Pressure -5 -4 Mean change from baseline in DBP (mmHg) Mean change from baseline in SBP (mmHg) -6 -10 -8 -10 -15 -12 -20 -14 5 10 25 50 20 5 10 25 50
Slide 109: Phase 2 safety results
Aprocitentan in resistant hypertension Phase 2 safety results Phase 2 studies Placebo group Aprocitentan group Lisinopril group Safety population / in patients 82 327 81 Discontinuation from study 6.1% 1.2% – 3.7% 3.7% treatment due to an adverse event Dose – 5 mg 10 mg 25 mg 50 mg 20 mg Cases of in
Slide 110: Phase 2 conclusion
Aprocitentan in resistant hypertension Phase 2 conclusion Phase 2 studies Efficacy • Dose response was consistent across all parameters measured • Efficacy observed at 10 and 25 mg, with no additional effect at 50 mg • The effect of aprocitentan covers the 24 h period Safety (in the limit of the stu
Slide 111: Aprocitentan – Confirmatory study
Aprocitentan – Confirmatory study Benefitting from consultation with regulatory agencies Phase 3 study PRECISION PRECISION will assess the short-term efficacy of aprocitentan as well as the durability of the effect. It will provide replication of clinical evidence in a single study Aprocitentan is i
Slide 112: Confirmatory study design
Aprocitentan in resistant hypertension Confirmatory study design Phase 3 study PRECISION RHT confirmation Efficacy and safety Standardization of aprocitentan Stabilization 1 to 8 weeks 4 weeks 4 weeks 4 weeks 32 weeks Withdrawal 12 weeks 30 days Safety Screening Screening Run-in Part I Part II Part
Slide 113: Confirmatory study objectives
Aprocitentan in resistant hypertension Confirmatory study objectives Phase 3 study PRECISION Part I Part II Part III • Double-blind treatment • Single-blind treatment • Double-blind, randomized, • 12.5 mg aprocitentan or 25 mg • 25 mg aprocitentan withdrawal treatment aprocitentan or placebo • Perio
Slide 114: Confirmatory study patient population
Aprocitentan in resistant hypertension Confirmatory study patient population: Phase 3 study True resistant hypertension patients on standardized triple therapy PRECISION Entry into screening Entry into run-in Randomization Mean systolic Confirmed diagnosis of Mean systolic blood pressure ≥ 140 mmHg
Slide 115: Confirmatory study endpoints
Aprocitentan in resistant hypertension Confirmatory study endpoints Phase 3 study PRECISION Primary endpoint • Change from baseline to week 4 of double-blind treatment in mean trough sitting systolic blood pressure by AOBPM Key secondary endpoint • Change from week 36 (start of withdrawal period) to
Slide 116: Aprocitentan in resistant hypertension summary
Aprocitentan in resistant hypertension An orally active dual endothelin receptor antagonist, which is being Phase 2 data presented investigated for patients whose • Oral presentation at the European blood pressure is uncontrolled Society of Cardiology (ESC) despite the use of at least three Congress
Slide 117: Clazosentan in cerebral vasospasm post-aSAH
Clazosentan in cerebral vasospasm post-aneurysmal subarachnoid hemorrhage Clazosentan is investigational, in development and not approved or marketed in any country. 117 Idorsia - Reaching out for more | October 2020
Slide 118: Aneurysmal subarachnoid hemorrhage (aSAH)
Aneurysmal subarachnoid hemorrhage (aSAH) A sudden life-threatening bleeding occurring in the subarachnoid space • Caused by the rupture of an aneurysm – a Scalp weak, bulging spot on the wall of a cerebral Skull artery • Prevalence: between 6 and 9 in 100’000 Subarachnoid worldwide1,2 space • Emerg
Slide 119: Two options for the treatment of aSAH
Two options for the treatment of aSAH Pre-treatment Brain surgery: Catheter intervention: Clipping of the aneurysm Releasing of platinum coils Ruptured aneurysm Coil Clip Catheter Brain artery 119 Idorsia - Reaching out for more | October 2020
Slide 120: Cerebral vasospasm post-aSAH
Cerebral vasospasm post-aSAH Can occur between 4 and 14 days after aSAH securing Artery spasm • Cerebral vasospasm is a strong contraction of the arteries in the brain surrounding the hemorrhage Blood • Narrowing of the blood vessel limits blood flow decreasing the amount of blood supplied to the br
Slide 121: Symptoms of vasospasm
Symptoms of vasospasm From asymptomatic detected by systematic angiography to serious neurological symptoms Loss of Numbness or weakness consciousness of the face, arm or leg, Blurred or double especially on one side of the vision body, or in more severe cases, paralysis Mood change, Cerebral Confus
Slide 122: Long-term consequence of vasospasm
Long-term consequence of vasospasm Brain infarct due to vasospasm • Necrosis of an area of brain tissue • Physical deficit • Social and emotional impact, affecting all aspects of someone’s life 122 Idorsia - Reaching out for more | October 2020
Slide 123: Available therapy for vasospasm
Available therapy for vasospasm Hemodynamic therapy Rescue therapy No pharmacological therapy • Inducing high blood pressure • Invasive neurovascular intervention for cerebral vasospasm in an attempt to force a blood • Except for fasudil in Japan − balloon angioplasty supply to the brain region and
Slide 124: Endothelin release
Endothelin release Role in cerebral vasospasm Patients with cerebral vasospasm show high levels Cerebral vasospasm is of endothelin in their caused by the release of cerebral spinal fluid vasoactive mediators after a bleed on the brain triggering vessels to Endothelin is one of contract the most pow
Slide 125: Clazosentan in cerebral vasospasm
Clazosentan in cerebral vasospasm ETA selective ERA >1’800 patients treated with clazosentan Highly soluble providing significant experience in vasospasm post-aSAH and a well documented safety profile Suited for intravenous administration Fast onset of action Clazosentan is investigational, in devel
Slide 126: Learning from clazosentan program
Learning from clazosentan program Vasospasm ≈ day 4 to 14 Initial SAH Aneurism Asymptomatic Vasospasm- Hospital Delayed, event secured vasospasm related symptoms discharge 3 to 6 month outcome CONSCIOUS REVERSE From this program, we know: • Which patients would benefit most • What dose should be giv
Slide 127: What we have learned through our experience with clazosentan
What we have learned through our experience with clazosentan… Clazosentan is investigational, in development and not approved or marketed in any country. 127 Idorsia - Reaching out for more | October 2020
Slide 128: Dose-dependent prevention of vasospasm
Clazosentan in cerebral vasospasm Dose-dependent prevention of vasospasm Phase 2 study CONSCIOUS-1 Phase 2 study – 80 All patients (per-protocol) angiographic endpoint 70 • Clazosentan 1 to 15 mg/h versus Patients with moderate/severe 60 placebo post-clipping and coiling *p = 0.0027 vasospasm (%) 50
Slide 129: 5mg/hr dose is not high enough
Clazosentan in cerebral vasospasm 5mg/hr dose is not high enough Phase 3 study CONSCIOUS-2 Overall incidence of death and vasospasm-related morbidity Phase 3 study – clinical morbidity / mortality endpoint • Patients who received surgical clipping treated with 5mg/hr clazosentan Event rate (%) The L
Slide 130: 15mg/hr showed significant effect on morbidity / mortality
Clazosentan in cerebral vasospasm 15mg/hr showed significant effect on morbidity / mortality Phase 3 study CONSCIOUS-3 Overall incidence of death and vasospasm-related morbidity Phase 3 study – clinical morbidity / mortality endpoint • Patients who received endovascular coiling treated with 5 or 15m
Slide 131: 15mg/hr showed significant effect on primary endpoint
Clazosentan in cerebral vasospasm 15mg/hr showed significant effect on primary endpoint Phase 3 study CONSCIOUS-3 Incidence of death and each component Phase 3 study – of vasospasm-related morbidity clinical morbidity / mortality endpoint • Consistent effect at 15 mg/hr on all 25 morbidity events 21
Slide 132: 10mg/hr dose in Japanese patients
Clazosentan in cerebral vasospasm 10mg/hr dose showed similar results to CONSCIOUS-3 Japanese in Japanese patients study Overall incidence of death and vasospasm-related morbidity Phase 2 study – exploratory endpoint • Clazosentan significantly reduced vasospasm-related morbidity and mortality event
Slide 133: In patients with established vasospasm
Clazosentan in cerebral vasospasm In patients with established vasospasm Pilot study REVERSE Pilot study – angiographic endpoint Key findings: • Clazosentan acts on some large brain arteries but the real benefit is in the Indicates moderate effect on smaller arteries not vasospasm accessible to endo
Slide 134: Well documented safety profile
Clazosentan in cerebral vasospasm Well documented safety profile Side effects of clazosentan Risk mitigation Hypotension Blood pressure control with vasopressors in ICU Lung complications Euvolemia, (pulmonary edema) iv fluid restriction Peripheral edema Euvolemia, iv fluid restriction > 1’800 patie
Slide 135: Which patients are at highest risk of vasospasm?
Which patients are at highest risk of vasospasm? Patients with “thick and diffuse” clot • Characterized by large amount of subarachnoid blood on hospital admission cerebral CT scan • Represents approximately 50% of overall aSAH population Normal CT Thick and diffuse SAH Clazosentan is investigationa
Slide 136: Which patients are at highest risk of vasospasm?
Which patients are at highest risk of vasospasm? CONSCIOUS-2 CONSCIOUS-3 Patients with “thick and diffuse” clot • Data from previous CONSCIOUS program demonstrates the high event Rescue Therapy rates for vasospasm and related ischemic complications DIND New Cerebral Infarcts Death 0% 10% 20% 30% Pro
Slide 137: In high-risk patient population
Clazosentan in cerebral vasospasm In high-risk patient population CONSCIOUS-2 CONSCIOUS-3 Clot size impacts the absolute treatment effect (individual morbidity / mortality components) Phase 3 studies – clinical morbidity / mortality endpoint Thick and Diffuse Clots 40% Proportion of patients with an
Slide 138: REACT study design incorporates these learnings
REACT study design incorporates these learnings Phase 3 study REACT Selection of Selection of Selection of Optimized patient the high-risk the dose the best measure management patient to demonstrate guidelines to ensure population efficacy patient safety Clazosentan is investigational, in developmen
Slide 139: Study objectives
Clazosentan in cerebral vasospasm Study objectives Phase 3 study REACT Primary objective • To determine the efficacy of clazosentan in preventing clinical deterioration due to delayed cerebral ischemia, in patients with aSAH Secondary objectives • To evaluate the effect of clazosentan on the inciden
Slide 140: Study design
Clazosentan in cerebral vasospasm Study design Phase 3 study REACT 400 patients (200 placebo/200 clazosentan) from 100 trial sites across 15 countries Observation: 14 days post-study drug initiation Placebo Treatment & Observation 24h Safety Screening Follow-up Extended Follow-up Clazosentan 15mg/h
Slide 141: Target patient population
Target patient population Elevated risk of developing delayed cerebral ischemia (DCI) Phase 3 study REACT High-risk for developing Early vasospasm without cerebral vasospasm Objective to prevent neurological deterioration DCI, subsequent • “thick and diffuse” clot on clinical deterioration, • clazos
Slide 142: Primary endpoint – highly relevant
Clazosentan in cerebral vasospasm Primary endpoint – highly relevant Phase 3 study REACT The occurrence of clinical deterioration due to DCI, from study drug initiation up to 14 days post-study drug initiation • Worsening of 2 points on neurological scales, lasting for at least 2 hours • Entirely or
Slide 143: Secondary endpoints
Clazosentan in cerebral vasospasm Secondary endpoints Phase 3 study REACT • Occurrence of all-cause new or worsened cerebral infarction ≥ 5 cm3 at Day 16 post-study drug initiation • Long-term clinical outcome assessed by the GOSE at Week 12 post-aSAH, dichotomized into poor (score ≤ 4) and good out
Slide 144: Japanese registration program
Japanese registration program • Two identically designed studies (one in clipped patients, one in coiled patients) evaluating the effect of clazosentan 10 mg/h versus placebo on vasospasm-related morbidity and mortality and all-cause morbidity and mortality − Death, new cerebral infarcts, delayed is
Slide 145: Clazosentan in cerebral vasospasm summary
Clazosentan in cerebral vasospasm A selective ETA receptor antagonist being developed Registration studies in Japan as an intravenous infusion • Evaluating reduction of vasospasm, for the prevention of clinical and vasospasm-related morbidity and deterioration due to mortality following aSAH vasospa
Slide 146: Cenerimod in systemic lupus erythematosus
Cenerimod in systemic lupus erythematosus Cenerimod is investigational, in development and not approved or marketed in any country. 146 Idorsia - Reaching out for more | October 2020
Slide 147: Systemic lupus erythematosus (SLE)
Systemic lupus erythematosus (SLE) Complex, systemic, autoimmune disease of unknown cause Normal immune response Autoimmune response Foreign threat Antibodies Antibodies Immune Antibodies Antibodies invades attack and continue to system forms attack the remain in the remove protect body antibodies b
Slide 148: SLE symptoms
Systemic lupus erythematosus (SLE) Symptoms Skin: rashes, Fatigue sensitivity to light Liver and Joint and • Tissue damage spleen: enlarged muscles: aches and pains across multiple organ systems Blood and circulation: Nervous • Severe organ swollen glands, poor circulation Lupus system: headaches, d
Slide 149: SLE: high medical need
Systemic lupus erythematosus (SLE) High medical need • Lupus can range from mild to severe depending on how it affects the body • Limited treatment options with a high need for new Mild Moderate Severe joint and skin inflammation of other inflammation causing severe approaches problems, parts of the
Slide 150: SLE epidemiology
Systemic lupus erythematosus (SLE) Epidemiology 5 million people worldwide have a form of lupus 10% male More common in people of Afro-Caribbean and Asian origin compared to 90% Caucasians female Peak incidence between Lupus Foundation of America Center for Disease Control and Prevention 15 and 40 y
Slide 151: S1P1 receptor modulation in SLE
S1P1 receptor modulation in SLE Rationale • T and B lymphocytes are considered the key immune cells that contribute to the symptoms of the disease • T and B lymphocytes have receptors on the surface called “Sphingosine-1-phosphate receptor 1” (S1P1) • S1P1 senses the gradient of sphingosine-1-phosph
Slide 152: Cenerimod in SLE
Cenerimod in SLE S1P1 Receptor Modulation S1P1 is on the surface of T and B lymphocytes, and the modulation Oral leads to internalization of the drug receptor Novel Lymphocytes can no longer approach to sense S1P and are held in the the treatment lymph nodes of SLE Tolerability Profile The evolving
Slide 153: Phase 2 safety study
Cenerimod in SLE Study presented at ACR2019 Phase 2 safety study Phase 2 safety study 67 patients were enrolled Randomized, double-blind, placebo- to receive either placebo or controlled, dose-response study to 0.5, 1, 2 or 4 mg/day of investigate the biological activity, cenerimod over a treatment
Slide 154: Study design
Cenerimod in SLE Study design Phase 2 safety study Randomization EOT EOS Placebo 12 pts Part A Cenerimod 0.5 mg 12 pts Cenerimod 1.0 mg 12 pts Cenerimod 2.0 mg 12 pts Visit 1 2 3 4 5 6 7 8 9 Week Day -30 Day 1 2 4 8 12 18 23 28 Screening Treatment period Follow-up Phone calls FU 30 days 12 weeks 6 w
Slide 155: Dose-response for total lymphocyte count
Cenerimod in SLE Dose-response for total lymphocyte count Phase 2 safety study Absolute change Placebo (n=16) from baseline to EOT 0.5 mg (n=12) in total lymphocyte 1 mg (n=10) count (109/L) –0.5 2 mg (n=13) 4 mg (n=9) –1.0 P<0.001 for dose-response Placebo 0.5 1 2 4 Dashed line represents the 95% C
Slide 156: Modified SLEDAI-2K over time
Cenerimod in SLE Modified SLEDAI-2K over time Phase 2 safety study Mean mSLEDAI-2K 10 score ± SE 8 6 Placebo (n=16) 0.5 mg (n=12) 4 1 mg (n=10) 2 mg (n=13) 2 4 mg (n=9) 0 Baseline W4 W8 W12 W18 EOT EOS Analysis Set: Modified Pharmacodynamic Set modified SLEDAI-2K, Systemic Lupus Erythematosus Diseas
Slide 157: Phase 2 conclusion
Cenerimod in SLE Phase 2 conclusion Phase 2 safety study Dose-response • Dose-dependent, sustained reduction in circulating lymphocyte counts • Reversible after treatment Safety (in the limit of the study design) • Well tolerated at all dose levels • The occurrence of adverse events was similar in a
Slide 158: Multi-dose efficacy & safety study
Cenerimod in SLE Efficacy & safety study Multi-dose efficacy & safety study Patients will be enrolled Multicenter, randomized, double-blind, to receive either placebo or placebo-controlled, parallel-group 0.5, 1, 2 or 4 mg/day of cenerimod study to evaluate the efficacy and for up to 12 months safet
Slide 159: Study design
Cenerimod in SLE Study design Efficacy & safety study Randomization Re-randomization of 4 mg to 5 groups (1:1:1:1:1) placebo and 2 mg (1:1) EOT EOS Echocardiography Placebo 100 pts ancillary study • 125 subjects Cenerimod 0.5 mg 100 pts echocardiography at screening and 6 months Cenerimod 1.0 mg 100
Slide 160: Large efficacy & safety study “CARE”
Cenerimod in SLE Large efficacy & safety study in patients with SLE “CARE” Efficacy & safety study Primary Objective • Assess the efficacy (disease activity) of 6 months cenerimod treatment given at 4 different dose levels in subjects with moderate to severe systemic lupus erythematosus Secondary Ob
Slide 161: Cenerimod in SLE summary
Cenerimod in SLE A potent, selective sphingosine-1- phosphate receptor 1 (S1P1) Phase 2 data presented modulator, which potentially offers a • Oral and poster presentations novel approach for systemic lupus at the annual meeting 2019 of erythematosus (SLE) – a disease the American College of Rheumat
Slide 162: Selatogrel for suspected acute myocardial infarction (AMI)
Selatogrel for suspected acute myocardial infarction (AMI) Selatogrel is investigational, in development and not approved or marketed in any country. 162 Idorsia - Reaching out for more | October 2020
Slide 163: Acute myocardial infarctions (AMI)
Acute myocardial infarctions (AMI) Early intervention is crucial for survival • Each year more than 600,000 persons living in the US will suffer their first heart attack and around 200,000 will suffer a recurring heart attack1 • Although the management of AMI has improved in the last decades, morbid
Slide 164: Selatogrel to prevent AMI
Selatogrel to prevent AMI Potent, fast-acting, reversible, and highly-selective P2Y12 receptor antagonist • Two Phase 2 studies in patients with stable Selatogrel has a rapid PD effect following subcutaneous injection coronary artery disease and acute myocardial infarction (AMI), respectively, have
Slide 165: Collaboration with Antares Pharma, Inc
Collaboration with Antares Pharma, Inc • With almost 20 years of experience, Antares has a proven track record in developing and commercializing complex drug device products that are tailored to the patient and the therapeutic need • The companies will develop a novel drug-device product combining I
Slide 166: Selatogrel to prevent AMI
Selatogrel to prevent AMI In development for single Epidemiology subcutaneous self-administration • Each year >600,000 persons Global agreement with Antares Pharma in the US will suffer their to develop a novel drug-device product first heart attack and ~200,000 will suffer a recurring heart attack
Slide 167: Idorsia's other clinical development assets
Idorsia’s other clinical development assets 167 Idorsia - Reaching out for more | October 2020
Slide 168: ACT-774312
ACT-774312 CRTH2 receptor antagonist for the treatment of nasal polyposis There is a need for new oral therapies to treat allergic and type 2 inflammatory responses Current evidence suggests that disease pathogenesis in nasal polyposis involves type-2 inflammatory processes and that a CRTH2 antagoni
Slide 169: ACT-539313
ACT-539313 Selective orexin 1 receptor antagonist (SORA) for psychiatric disorders In development for the potential treatment of psychiatric disorders • Potent antagonist, brain-penetrating • Shown anxiolytic (anxiety inhibiting) effects after oral administration in four different preclinical models
Slide 170: Sinbaglustat
Sinbaglustat GBA2/GCS inhibitor for rare lysosomal storage disorders Sinbaglustat is a GBA2/GCS inhibitor in development for lysosomal storage disorders (LSDs) • Based on a non-clinical program and completed Phase 1 studies, Idorsia considers developing sinbaglustat in rare LSDs. • To collect diseas
Slide 171: Other early-stage pipeline assets
Other early-stage pipeline assets • ACT-1004-1239 is a new cancer immunotherapy / immunology compound in Phase 1 development • ACT-1014-6470 is a new immunological compound in Phase 1 development • ACT-541478 is a new CNS compound in Phase 1 development ACT-709478 is investigational, in development
Slide 172: ACT-709478
ACT-709478 T-type calcium channel blocker for epilepsy In development for the treatment of a rare form of pediatric epilepsy • ACT-7091478 is a potent, selective, orally-active, and brain penetrating T-type calcium channel blocker • The Investigational New Drug (IND) application was accepted by the
Slide 173: More science – Bursting with ideas
More science – Bursting with ideas 173 Idorsia - Reaching out for more | October 2020
Slide 174: Idorsia's drug discovery approach
Idorsia’s drug discovery approach Single-center approach Few platforms of expertise Fully integrated research informatics Multiple therapeutic areas Focus on High medical input small molecules 174 Idorsia - Reaching out for more | October 2020
Slide 175: Our drug discovery process
More joy – Transforming the horizon Our drug discovery process Preclinical Development Clinical Development Registration Launch Molecular-Biology Biochemistry (High Structural Biology (Target Finding) Throughput Screening) And Molecular Modeling Targets Hits Research Information Medicinal Management
Slide 176: Financial information
Financial information 176 Idorsia - Reaching out for more | October 2020
Slide 177: US GAAP net results
US GAAP net results 20 NINE-MONTH in CHF millions, rounding differences may occur 20 Non-GAAP US GAAP Financial results as of September 30, 2020 177 Idorsia - Reaching out for more | October 2020
Slide 178: Non-GAAP operating expenses
Non-GAAP operating expenses 20 NINE-MONTH in CHF millions, rounding differences may occur 20 -5 -13 0 -9 -86 -75 -35 -42 -162 -221 -302 -347 9M 2019 9M 2020 Research Development Selling G&A Milestones Non-GAAP operating expenses Financial results as of September 30, 2020 178 Idorsia - Reaching out f
Slide 179: Cash flow
Cash flow 20 NINE-MONTH in CHF millions, rounding differences may occur 20 Financial results as of September 30, 2020 179 Idorsia - Reaching out for more | October 2020
Slide 180: Liquidity
Liquidity 20 NINE-MONTH in CHF millions, rounding differences may occur 20 816 816 9 739 Cash deposits 179 Other FX > 12 months 476 668 Cash deposits USD < 12 months 628 Cash and CHF Cash equivalents 263 148 Liquidity @ Liquidity @ Liquidity @ Dec 31, 2019 1 Sep 30, 2020 2 Sep 30, 2020 2 Financial r
Slide 181: Financial Guidance for 2020
Financial Guidance + + + 20 for 2020 ++ + NINE-MONTH 20 US GAAP operating expenses around CHF 500 million and non-GAAP operating expenses around CHF 460 million Both measures exclude unforeseen events, potential milestone payments and any potential payments related to the Axovan arbitration (October
Slide 182: More experience – Driving innovation
More experience – Driving innovation 182 Idorsia - Reaching out for more | October 2020
Slide 183: Idorsia has a strong and visionary leadership team
Idorsia has a strong and visionary leadership team with the power and drive to create more remarkable innovations and more new medicines 183 Idorsia - Reaching out for more | October 2020
Slide 184: Idorsia Executive Committee
Idorsia Executive Committee Jean-Paul Clozel Martine Clozel Guy Braunstein Chief Executive Officer Chief Scientific Officer Head of Global Clinical Development Simon Jose André C. Muller Chief Commercial Officer Chief Financial Officer 184 Idorsia - Reaching out for more | October 2020
Slide 185: Idorsia Leadership Team
Idorsia Leadership Team Andrew C. Weiss Head of Investor Relations & Alex Khatuntsev Oliver Peinelt Olivier Lambert Corporate Communications Head of Human Resources General Counsel Head of Pharmaceutical Development Ulrich Mentzel Stefan Abele Christoph Boss Head of Pharmacology & Preclinical Markus
Slide 186: Be prepared for more
Be prepared for more 186 Idorsia - Reaching out for more | October 2020