Slide 1: Rigel Corporate Presentation
Rigel Corporate Presentation August 4, 2026 1
Slide 2: Forward-Looking Statements
Forward-Looking Statements This presentation contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 ("PSLRA") relating to, among other things, expected commercial launches and commercial availability, commercial, financial and clinical results,
Slide 3: Rigel's Transformational Growth Strategy
Rigel’s Transformational Growth Strategy Grow Commercial In-Licensing / Business Business Development Maintain Financial Advance Development Discipline Pipeline 3
Slide 4: In-License of VEPPANU (Vepdegestrant)
In-License of VEPPANUTM (Vepdegestrant) VEPPANU will be commercially available in mid-August • Entered into exclusive, global license agreement with Arvinas and Pfizer to develop, manufacture and commercialize VEPPANUTM (vepdegestrant) for the treatment of 2L+ ER+/HER2-, ESR1m advanced or metastatic
Slide 5: Rigel's Transformation to Accelerated Growth
Rigel’s Transformation to Accelerated Growth Grow Commercial In-Licensing / Business Business Development Maintain Financial Advance Development Discipline Pipeline 2030s 2025 • Growth of four commercial products • Growth from potential in-licensing / 2020 • Three commercial products M&A transaction
Slide 6: Future Transformational Revenue Growth Opportunities
Future Transformational Revenue Growth Opportunities Annual Net Product Sales ($M) 1 260.0 232.0 144.9 104.3 76.7 2022 2023 2024 2025 2026 Guidance Future Potential TAVALISSE REZLIDHIA GAVRETO Mid-Point Opportunity CAGR, compound annual growth rate. 6 1. 2026 net product sales guidance excludes VEPP
Slide 7: Grow Commercial Business
Grow Commercial Business rigel.
Slide 8: Q2 2026 Commercial Performance
Q2 2026 Commercial Performance Net Portfolio Sales grew $8.1M (14%) vs. Q2 2025 Net Product Sales ($M) TAVALISSE GAVRETO REZLIDHIA $47.4M 18% Growth vs. 67.0 Q2 2026 Net Product Sales Q2 2025 58.9 8.9 7.0 10.7 11.8 $10.7M (10)% Growth vs. Axis Title Q2 2026 Net Product Sales Q2 2025 47.4 40.1 $8.9M
Slide 9: TAVALISSE indication and safety information
Kinase inhibitor indicated for the treatment of thrombocytopenia in adult patients with chronic immune thrombocytopenia (cITP) who have had an insufficient response to a previous treatment Select Important Safety Information Adverse Reactions: • Serious adverse drug reactions in the ITP double-blind
Slide 10: Creating Opportunities to Gain Market Share
Creating Opportunities to Gain Market Share 81,300 U.S. Adult cITP Patients1 37,000 20,000 11,400 44,300 Patients Actively Treated2 Watchful Waiting 1st Line 2nd Line • 24,300 patients are 2L or later 6,900 Patients Need Additional 3rd Line Treatment Options as They Move through Therapies 3,500 4th
Slide 11: Efficacy Across All Post-Steroid Lines of Therapy
Efficacy Across All Post-Steroid Lines of Therapy Post-hoc Data Analysis Demonstrated Use as 2nd-Line Durable Efficacy was Observed in Therapy Resulted in Higher Response Rates1,2 Responders to TAVALISSE in the FIT Studies (combined results from FIT-1, FIT-2, and FIT-3)3 Response Median Platelet Cou
Slide 12: REZLIDHIA approved and available in the U.S.
APPROVED AND AVAILABLE IN THE U.S. REZLIDHIA is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible IDH1 mutation as detected by an FDA-approved test Please see Important Safety Information on slides 68 & 69, including Boxed WARNI
Slide 13: mIDH1 Relapsed/Refractory AML Background
mIDH1 Relapsed/Refractory AML Background mIDH1 AML • AML will be diagnosed in nearly 23K patients and result in nearly 11.5K deaths in 20261 Fit (~65%)4 Unfit (~35%)4 Treated with Treated with • IDH1 mutations are found in 6-9%2,3 of AML Intensive Therapy Non-Intensive Consolidation → Transplant The
Slide 14: REZLIDHIA Phase 2 Clinical Trial Highlights
REZLIDHIA Phase 2 Clinical Trial Highlights1 • Elderly population (median age 71) with a median of 2 (1-7) prior treatments (all naïve to m1DHI inhibitor) • CR+CRh rate of 35%, with a median duration of response of 25.3 months • 92% of CR+CRh responders were CR, with a median duration of response of
Slide 15: GAVRETO approved and available in the U.S.
APPROVED AND AVAILABLE IN THE U.S. GAVRETO is indicated for the treatment of adult patients with metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer as detected by an FDA-approved test, and adult and pediatric patients 12 years of age and older with advanced or
Slide 16: Growing Our Oncology Targeted Therapy Portfolio
Growing Our Oncology Targeted Therapy Portfolio A Compelling and Synergistic Opportunity 1L Treatment of RET Fusion-Positive NSCLC Patients1 • Enables entry into a well-identified subset of large solid tumor market ~5% – Immediately recognizable population of RET fusion-positive patients ~20% – Chal
Slide 17: Pralsetinib Has a Differentiated Value Proposition
Pralsetinib Has a Differentiated Value Proposition • The only once daily, oral, RET inhibitor approved for patients with NSCLC and thyroid cancer with RET gene fusions • High and durable response rates regardless of prior treatment history1 • Promising intracranial efficacy in patients with brain me
Slide 18: Expanding Commercial Access Globally
Expanding Commercial Access Globally 18
Slide 19: Expanding Commercial Availability in Global Markets
Expanding Commercial Availability in Global Markets TAVALISSE is commercially available in key European countries (TAVLESSE), Japan, South Korea, Canada and Israel Q2 2026 Collaboration Revenues • Kissei $5.8M • Grifols $5.0M • Medison $0.3M • Others $0.6M TAVALISSE Commercial Launch • Knight announ
Slide 20: In-Licensing / Business Development
In-Licensing / Business Development
Slide 21: In-Licensing / Business Development Strategy
In-Licensing / Business Development Strategy • Acquired global rights to REZLIDHIA in 2022; first commercial sale in patients with R/R mIDH1 AML in Q4 2022 Differentiated asset(s) • Acquired U.S. rights to GAVRETO in 2024; first commercial sale in patients with in hematology, oncology RET+ NSCLC and
Slide 22: Vepdegestrant
vepdegestrant ‘som; rigel.
Slide 23: VEPPANU approved in the U.S.
APPROVED IN THE U.S. VEPPANU is indicated for the treatment of adults with estrogen receptor-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-), estrogen receptor 1 (ESR1)-mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progress
Slide 24: Potential to Transform Rigel's Commercial Portfolio
has the Potential to Transform Rigel’s Commercial Portfolio The first and only FDA-approved PROTAC, a new class of targeted agents A novel and unique mechanism of action with the potential to be an important new therapy for 2L and 3L ER+/HER2-, ESR1m metastatic breast cancer Rigel’s proven commercia
Slide 25: PROteolysis TArgeting Chimera (PROTAC)
PROteolysis TArgeting Chimera (PROTAC) The FIRST in a novel class of drugs called heterobifunctional protein degraders The novel bifunctional design of PROTAC represents a major innovation in ER degradation VEPPANU binds to an The ubiquitin-tagged Because VEPPANU bonds estrogen receptor and estrogen
Slide 26: PROTAC Degraders Are Differentiated From SERDs
PROTAC Degraders Are Differentiated From SERDs SERD (Selective Estrogen Receptor PROTAC Degrader (Targeted Protein Degrader) Degrader/Downregulator) • SERDs bind to the estrogen SERD binds ER PROTAC binds 1 1 receptor (ER), destabilizing ER SERD (blocks ER E3 ER + an E3 the ER, making it more signal
Slide 27: Vepdegestrant Addresses Significant Unmet Medical Need
Vepdegestrant Addresses Significant Unmet Medical Need 27
Slide 28: ER+/HER2-, ESR1m mBC Patient Opportunity
ER+/HER2-, ESR1m mBC Patient Opportunity The largest segment of metastatic breast cancer As patients become more exposed to endocrine and CDK4/6 inhibitor therapy, ESR1m resistance develops ctDNA testing is increasing the proportion of patients diagnosed and treated in 2L The majority of ER+/HER2- p
Slide 29: Will Enter a Dynamic Market Treated in the Community Setting
Will Enter a Dynamic Market Where Most Patients are Treated in the Community Setting Current Therapies in 2L/3L ER+/HER2-, ESR1m mBC1 Market Opportunity • Oral SERDs have been rapidly 2L 3L adopted, and are used in the majority of patients in 2L and ~30% of patients in 3L 23% 36% 38% 2% • Chemothera
Slide 30: Potential to Become a Market-leading Treatment in 2L+ mBC
has the Potential to Become a Market-leading Treatment in 2L+ ER+/HER2-, ESR1m Metastatic Breast Cancer (mBC) • Improved median Progression Free Survival (mPFS), Objective Response Proven Rate (ORR) and Clinical Benefit Rate (CBR) vs. fulvestrant Efficacy • Improved mPFS 2.4-fold, or 2.9 months (5.0
Slide 31: Commercialization Plans Now Being Implemented
Commercialization Plans Now Being Implemented Executing activities to ensure successful launch upon product availability Collaboration Enabling Expedited Product Availability Strong relationships with partners and execution against detailed transition plans have ensured we are ON TRACK to have VEPPA
Slide 32: Commercial Launch Phases ON TRACK
Commercial Launch Phases ON TRACK Phase 1: Now Approved Phase 2: Now Available Phase 3: Branded Campaign Since Deal Close Upon Product Availability Post-Launch (Q4) • Websites: VEPPANU.com, • Expand Awareness and • Additional Materials to 3 rigelonecare.com, Adoption through an Facilitate Patient St
Slide 33: Advance Development Pipeline
Advance Development Pipeline
Slide 34: Vepdegestrant Clinical Overview
Vepdegestrant Clinical Overview 34
Slide 35: VERITAC-2 Phase 3 Clinical Trial Design
VERITAC-2 Phase 3 Clinical Trial Design Randomized, open-label, multi-center trial evaluating efficacy and tolerability of vepdegestrant vs. fulvestrant in patients with ER+/HER2-, ESR1m advanced or metastatic breast cancer (NCT05654623) Key Eligibility Criteria 28-day Treatment Cycles Primary Endpo
Slide 36: Baseline Characteristics of the VERITAC-2 Population
Baseline Characteristics of the VERITAC-2 Population Representative of the Real-World 2L Setting in the U.S. Patients With ESR1m All Patients Patients With ESR1m All Patients Characteristic, % Vep Fulv Vep Fulv Characteristic, % Vep Fulv Vep Fulv (n = 136) (n = 134) (n = 313) (n = 311) (n = 136) (n
Slide 37: Vepdegestrant Met the Primary Endpoint in ESR1m Patients
Vepdegestrant Met the Primary Endpoint with a ~3-Month mPFS Improvement in Patients with Tumors Harboring ESR1 Mutations 100 Vepdeg Fulv Vepdegestrant Parameter (n = 136) (n = 134) 90 Fulvestrant Median follow up, 80 7.4 6.0 months 70 Events, n (%) 79 (58) 95 (71) 6-month PFS (95% CI): Median PFS by
Slide 38: Consistent PFS Benefit Across Subgroups in the ESR1m Population
Consistent PFS Benefit Across Pre-Specified Prognostic Characteristics / Baseline Disease Demographics in the ESR1m Population Events/n Subgroup Vepdegestrant Fulvestrant HR (95% CI) All patients (stratified) 79/136 95/134 0.57 (0.42–0.77) Age, years <65 50/86 66/88 0.51 (0.35–0.74) ≥65 29/50 29/46
Slide 39: Statistically Significant Improvements in CBR and ORR
Vepdegestrant Showed Statistically Significant Improvements in CBR and ORR in the ESR1m Population Patients With ESR1m CBR1 ORR2 80 Odds ratio: 2.88 70 (95% CI: 1.57–5.39) P<0.0013 60 42.1 Odds ratio: 5.45 50 (95% CI: 1.69–22.73) P=0.0013 40 % ± 95% CI 30 20.2 18.6 % ± 95% CI 20 4.0 10 0 Vepdegestra
Slide 40: Generally Well Tolerated, Low Discontinuation and Dose Reductions
Vepdegestrant Was Generally Well Tolerated, with Low Rates of Discontinuation and Dose Reductions Vepdegestrant Fulvestrant Vepdegestrant Fulvestrant Adverse Events, % TEAEs in >10% of Patients in (n = 312) (n = 307) (n = 312) (n = 307) Either Group, % TEAEs Any Gr 3/4 Any Gr 3/4 Any 87 81 Fatiguea
Slide 41: Vepdegestrant Development
Vepdegestrant Development Current Clinical Studies Development Plans The following studies are active, not • Pfizer and Arvinas remain responsible enrolling, except for the hepatic study: for current clinical studies2 • VERITAC-21 • Combination studies are expected to • Combination studies provide a
Slide 42: Hematology and Oncology Focus Areas
Hematology and Oncology Focus Areas1 R289 IRAK1/4 Inhibitor • Evaluating in a Phase 1b study for • Strategic collaborations: patients with R/R lower-risk MDS – MD Anderson: Monotherapy or – Granted Fast Track and Orphan Drug combination therapy in mIDH1 AML and designations by the FDA2 other hematol
Slide 43: R289 IRAK1/4 Inhibitor in Lower-Risk MDS
R289 IRAK1/4 Inhibitor in Lower-Risk MDS 43
Slide 44: Targeting Inflammatory Pathways in Lower-Risk MDS
Targeting Inflammatory Pathways in Lower-Risk MDS Dysregulation of immune/inflammatory signaling is associated with MDS • IRAK1/4 are critical for downstream signaling of the IL-1R family and most TLRs, leading to a proinflammatory marrow environment and persistent cytopenias in patients with lower-
Slide 45: Targeting IRAK1 & IRAK4 Pathways in Inflammatory Disease
Targeting IRAK1 & IRAK4 Pathways in Inflammatory Disease Dual inhibition of IRAK1 and IRAK4 provides stronger suppression of inflammatory cytokines compared to IRAK4-selective inhibitor alone in preclinical studies1 Kinase Assays IRAK4-Selective Inhibitor IRAK1/IRAK4 Dual Inhibitor IRAK4 P Substrate
Slide 46: R835 Proof-of-Mechanism in Healthy Volunteer Study
R8351 Proof-of-Mechanism in Healthy Volunteer Study2 Cytokine Response After LPS Challenge TNFα IL6 Cytokine Concentration Cytokine Concentration First-In-Human study (n=82) Placebo • R835 was well tolerated Group • Linear PK profile and dose proportional exposure Time (hour) Time (hour) Placebo Dos
Slide 47: Lower-Risk MDS Treatment Landscape
Lower-Risk MDS Treatment Landscape • MDS is a clonal disorder of hematopoietic stem cells (HSCs) leading to dysplasia and ineffective hematopoiesis – Consequences: Cytopenias (anemia), infections, iron overload and organ dysfunction, progression to AML • Primary goal of therapy: Reduce/limit transfu
Slide 48: R289 Program Value Proposition for Lower-Risk MDS
R2891 Program Value Proposition for Lower-Risk MDS • ~12,200 lower-risk MDS patients that have been previously treated2 Unmet Medical • Therapies for previously-treated transfusion dependent lower-risk MDS patients Need are lacking • Dysregulated inflammatory signaling is associated with MDS Novel •
Slide 49: R289: Phase 1b Study in Relapsed/Refractory Lower-Risk MDS
R2891: Phase 1b Study in Relapsed/Refractory Lower-Risk MDS Open-label, multicenter study to evaluate the safety, tolerability, PK and preliminary efficacy of R289 in patients with LR-MDS (NCT05308264) Key Eligibility Criteria • R/R LR-MDS or inadequate response to prior Dose Escalation Phase Dose E
Slide 50: Safety and Efficacy Results from the Dose Escalation Phase
Safety and Efficacy Results from the Dose Escalation Phase of the Phase 1b Study of R289 in Patients with R/R Lower-Risk MDS 50
Slide 51: Patient Characteristics
Patient Characteristics Elderly, heavily pre-treated patient population with a high baseline transfusion burden Data cutoff: October 28, 2025 All Patients (n=33) Median age, years (range) 75 (50 - 84) ≥ 75 years 19 (58%) Sex (M : F) 70% : 30% IPSS-R Classification (Low: Intermediate: Ring sideroblas
Slide 52: Safety
Safety R289 was generally well tolerated with a low incidence of Grade 3/4 cytopenias and infections TEAEs Occurring in at Least 18% (≥6) of Patients by Dose Level1 Total 250 mg QD 500 mg QD 750 mg QD 250 mg BID 500/250 mg 500 mg BID • All dose levels were generally well (N = 33) (N = 3) (N = 6) (N
Slide 53: Pharmacokinetics
Pharmacokinetics R835 plasma concentrations (administered as R289) by dose level (Cycle 2 Day 11) • R835 exposure increased with increasing R289 dose Observed R835 concentrations (ng/mL) * • At doses ≥500 mg once daily * * (QD), R835 steady state plasma concentrations reached or Time, hour Time, hou
Slide 54: RBC Transfusion Events by Dose Group
RBC Transfusion Events by Dose Group 250 mg QD 1 2 • Median duration of (n=3) 3 4 treatment: 5.5 months 5 6 (range: 0.9 - 27.7 500 mg QD (n=6) 7 8 months) 9 10 11 • 6/18 (33%) evaluable 750 mg QD 12 13 TD patients receiving (n=6) 14 15 ≥500 mg QD achieved 16 17 RBC-TI >8 weeks; 4 >16 250 mg BID (n=6
Slide 55: Summary of Patients Achieving RBC-TI
Summary of Patients Achieving RBC-TI Pt Sex, Dose Response BL RBCs Prior Therapies ID Age Level Duration Peak hemoglobin Darbopoetin, 500 mg Canakinumab, increases ranging from 7 76, M QD HTB ALK2 inhibitor, 24.0 m→ 2.9 - 6.1 g/dL vs baseline Decitabine occurred in patients Azacitidine, 750 mg achie
Slide 56: ASH 2025 Data Summary
ASH 2025 Data Summary • Elderly, heavily pre-treated lower-risk MDS patient population, the majority of R289 was Generally whom were high transfusion at baseline Well Tolerated - The incidence of Grade 3/4 cytopenias and infections was low • RBC-TI was achieved by 33% (6/18) of evaluable transfusion
Slide 57: R289 Development Next Steps
R289 Development Next Steps Lower-Risk MDS • Complete enrollment of the dose expansion phase and selection of the recommended Phase 2 dose for future clinical studies (2H 2026) – Share updated top-line data from dose expansion phase by end of 2026 – Open exploratory cohort of post-ESA, treatment naï
Slide 58: Olutasidenib mIDH1 Inhibitor
Olutasidenib mIDH1 Inhibitor 58
Slide 59: Strategic Alliance with UT MD Anderson to Advance Olutasidenib
Strategic Alliance with UT MD Anderson to Advance Olutasidenib in AML and Other Cancers1 Rigel and The University of Texas MD Anderson Cancer Center are evaluating and supporting olutasidenib in combination with other agents to treat newly-diagnosed and relapsed/refractory patients with IDH1-mutated
Slide 60: Advancing Olutasidenib into mIDH1 Glioma
Advancing Olutasidenib into mIDH1 Glioma1 CONNECT’s TarGeT Phase 2 Clinical Study • Gliomas account for 29-35% of CNS tumors in children, adolescents & young adults2 • As part of CONNECT’s “TarGeT” study in HGG, olutasidenib is being evaluated in combination with temozolomide as a maintenance regime
Slide 61: Potential to Evaluate Olutasidenib in MyeloMATCH Trial
Potential to Evaluate Olutasidenib in First-Line AML and MDS in MyeloMATCH Precision Medicine Trial NIH and NCI’s MyeloMATCH is a group of precision medicine clinical trials for MDS and AML • Patients will complete initial screening and will be assigned to a trial evaluating therapies that target th
Slide 62: Maintain Financial Discipline
Maintain Financial Discipline
Slide 63: Q2 2026 Highlights
Q2 2026 Highlights Q2 2026 Net Product Sales: Net Product Sales ($M) $67.0M TAVALISSE GAVRETO REZLIDHIA • TAVALISSE $47.4M 65.4 67.0 • GAVRETO $10.7M 64.1 • REZLIDHIA $8.9M 58.9 8.9 8.3 9.6 54.9 7.0 10.7 46.5 11.1 10.2 8.0 Q2 2026 Contract Revenues: 43.6 11.8 Axis Title 38.9 7.4 9.6 $11.7M 33.5 6.1
Slide 64: Q2 2026 Financial Overview
Q2 2026 Financial Overview (in thousands) Three Months Ended June 30, 2026 2025 Six Months Ended June 30, 2026 2025 2026 Financial Outlook Revenues • Total revenues of ~$285M to Net Product Sales $ 67,015 $ 58,948 $ 121,938 $ 102,498 Contract revenues from collaborations and other 11,688 42,737 15,5
Slide 65: Exclusive Global License Agreement for VEPPANU Key Terms
Exclusive Global License Agreement to Develop, Manufacture and Commercialize VEPPANUTM (vepdegestrant) Key Transaction Terms Arvinas and Pfizer will receive: • $70M upfront fee (paid in Q2 2026) • $15M upon the successful completion of certain transition activities • Additional potential milestone p
Slide 66: 2026 Progress and Key 2H 2026 Priorities
2026 Progress and Key 2H 2026 Priorities Grow Commercial Business In-Licensing / Business Development • Immediately initiated VEPPANUTM (vepdegestrant) • In-license of VEPPANUTM (vepdegestrant), an oral launch activities upon close of transaction; to PROTAC with the potential to be an important new
Slide 67: TAVALISSE Important Safety Information
TAVALISSE® (fostamatinib disodium hexahydrate) Tablets DRUG INTERACTIONS • Concomitant use of TAVALISSE with strong CYP3A4 inhibitors increases exposure to the INDICATION major active metabolite of TAVALISSE (R406), which may increase the risk of adverse • TAVALISSE® (fostamatinib disodium hexahydra
Slide 68: About REZLIDHIA (olutasidenib)
About REZLIDHIA® (olutasidenib) INDICATION REZLIDHIA is an isocitrate dehydrogenase-1 (IDH1) inhibitor indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible IDH1 mutation as detected by an FDA-approved test. IMPORTANT SAFETY INFORMA
Slide 69: Important Safety Information (Cont.)
IMPORTANT SAFETY INFORMATION (Cont.) WARNINGS AND PRECAUTIONS Hepatotoxicity Monitor patients frequently for clinical symptoms of hepatic dysfunction such as fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice. Obtain baseline liver function tests prior to initiation of REZL
Slide 70: About GAVRETO (pralsetinib)
About GAVRETO® (pralsetinib) INDICATIONS GAVRETO (pralsetinib) is indicated for the treatment of: • Adult patients with metastatic rearranged during transfection (RET) fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test • Adult and pediatric patients 12 years of ag
Slide 71: Important Safety Information (Cont.)
IMPORTANT SAFETY INFORMATION (Cont.) • Hemorrhagic Events: Serious, including fatal, hemorrhagic events can occur with GAVRETO. Grade ≥ 3 hemorrhagic events occurred in 4.1% of patients treated with GAVRETO including one patient with a fatal hemorrhagic event. Permanently discontinue GAVRETO in pati
Slide 72: About VEPPANU (vepdegestrant)
About VEPPANUTM (vepdegestrant) INDICATION VEPPANU is indicated for the treatment of adults with estrogen receptor (ER)–positive, The most common (≥10%) adverse reactions, including laboratory abnormalities, were human epidermal growth factor receptor 2 (HER2)–negative, estrogen receptor–1 (ESR1)– d
Slide 73: Thank You
Thank You www.rigel.com rigel.