Slide 1: Corporate Presentation
Corporate Presentation May 5, 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, continued development and expansion of our business, projected financial performance including sales
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: Rigel's Transformational Growth Strategy 2030s
Rigel’s Transformational Growth Strategy Grow Commercial In-Licensing / Business Business Development Maintain Financial Advance Development Discipline Pipeline 2030s 2025 • Growth of three commercial products • Three commercial products 2020 • Growth from potential in-licensing / • Development pipe
Slide 5: Future Transformational Revenue Growth Opportunities
Future Transformational Revenue Growth Opportunities Annual Net Product Sales ($M) 260.0 232.0 144.9 104.3 76.7 2022 2023 2024 2025 2026 Guidance Future Potential TAVALISSE REZLIDHIA GAVRETO Mid-Point Opportunity 5 CAGR, compound annual growth rate.
Slide 6: Grow Commercial Business
Grow Commercial Business rigel.
Slide 7: Q1 2026 Commercial Performance
Q1 2026 Commercial Performance Net Portfolio Sales grew $11.3M (26%) vs. Q1 2025 Net Product Sales ($M) TAVALISSE GAVRETO REZLIDHIA 54.9 $37.3M 31% Growth vs. Q1 2026 Net Product Sales Q1 2025 8.0 43.6 9.6 $9.6M 6.1 7% 9.0 Axis Title Growth vs. Q1 2026 Net Product Sales Q1 2025 37.3 28.5 $8.0M 31% G
Slide 8: TAVALISSE: Kinase inhibitor for chronic immune thrombocytopenia
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 9: 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 10: 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 11: 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 47 & 48, including Boxed WARNI
Slide 12: 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 13: 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 14: 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 15: 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 16: 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 17: Expanding Commercial Access Globally
Expanding Commercial Access Globally 17
Slide 18: 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 Q1 2026 Collaboration Revenues • Grifols $1.8M • Kissei $1.8M • Medison $0.3M TAVALISSE Regulatory Approvals • Knight announced regulato
Slide 19: In-Licensing / Business Development
In-Licensing / Business Development 19
Slide 20: In-Licensing / Business Development Strategy
In-Licensing / Business Development Strategy • Acquired global rights to REZLIDHIA in 2022; first commercial sale in Differentiated asset(s) patients with R/R mIDH1 AML in Q4 2022 in hematology, oncology • Acquired U.S. rights to GAVRETO in 2024; first commercial sale in patients or related areas wi
Slide 21: Advance Development Pipeline
Advance Development Pipeline 21
Slide 22: 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, designations by the FDA 2 MDS, CCUS, CMML
Slide 23: R289 IRAK1/4 Inhibitor in Lower-Risk MDS
R289 IRAK1/4 Inhibitor in Lower-Risk MDS 23
Slide 24: 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 25: 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 26: R835 Proof-of-Mechanism in Healthy Volunteer Study
R8351 Proof-of-Mechanism in Healthy Volunteer Study2 Cytokine Response After LPS Challenge TNF 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 27: 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 28: 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 treated 2 Unmet Medical • Therapies for previously-treated transfusion dependent lower-risk MDS patients Need are lacking • Dysregulated inflammatory signaling is associated with MDS Novel
Slide 29: 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 30: Safety and Efficacy Results from a Phase 1b Study of R289
Safety and Efficacy Results from a Phase 1b Study of R289 in Patients with Relapsed/Refractory Lower-Risk MDS 30
Slide 31: 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 32: 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 33: 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 34: 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 35: 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 36: 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 37: 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 38: Olutasidenib mIDH1 Inhibitor
Olutasidenib mIDH1 Inhibitor 38
Slide 39: Strategic Alliance with MD Anderson Cancer Center
Strategic Alliance with MD Anderson Cancer Center to Advance Olutasidenib in AML and Other Cancers1 Five studies are open for enrollment Rigel and The University of Texas MD Anderson Cancer Center are evaluating and supporting olutasidenib in combination with other agents to treat newly-diagnosed an
Slide 40: 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 41: Potential to Evaluate Olutasidenib in MyeloMATCH Precision Medicine 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 42: Maintain Financial Discipline
Maintain Financial Discipline 42
Slide 43: Q1 2026 Highlights
Q1 2026 Highlights Q1 2026 Net Product Sales: Net Product Sales ($M) $54.9M TAVALISSE GAVRETO REZLIDHIA 64.1 65.4 • TAVALISSE $37.3M 58.9 9.6 • GAVRETO $9.6M 8.3 54.9 7.0 • REZLIDHIA $8.0M 46.5 11.1 10.2 8.0 43.6 11.8 38.9 7.4 9.6 Q1 2026 Contract Revenues: 6.1 Axis Title 33.5 5.5 $3.9M 8.1 9.0 5.2
Slide 44: Q1 2026 Financial Overview
Q1 2026 Financial Overview (in thousands) Three Months Ended March 31, 2026 2025 2026 Financial Outlook1 Revenues • Total revenues of ~$275 to $290M Net Product Sales $ 54,923 $ 43,550 Contract revenues from collaborations 3,895 9,783 • Net product sales of ~$255M to $265M Total revenues 58,818 53,3
Slide 45: 2026 Key Priorities
2026 Key Priorities Grow Commercial Business In-Licensing / Business Development Expand adoption of commercial portfolio Pursue late-stage assets which leverage current capabilities and capacity Maintain Financial Discipline Advance Development Pipeline 2026 Outlook:1 • R289 Phase 1b study in lower-
Slide 46: 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 47: 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 48: 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 49: 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 a
Slide 50: 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 51: Thank You
Thank You www.rigel.com rigel.