Slides
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Q2 2026 Financial Results Presentation August 4 , 2026 rigel .
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Please visit www.VEPPANU.com for Full Prescribing Information. Please visit www.TAVALISSE.com for Full Prescribing Information. Please visit www.REZLIDHIA.com for Full Prescribing Information, including Boxed WARNING. Please visit www.GAVRETO.com for Full Prescribing Information, including Boxed WARNING. 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, projections of financial perform ance and outlook for 2026, expectations for growing our commercial business and successfully executing our commercial strategy, continued enrollment of our R289 study, presentation of study data, expectation of clinical outcomes, continued ability to develop and commercialize VEPPANU, TAVALISSE, GAVRETO, REZLIDHIA and R289 domestically and in certain in ternational markets, the Company's ability to fund its existing and future clinical development programs, and expectations for our partnering, licensing, commercialization and collaboration efforts. Any statements contained in this presentation that are not statements of historical fact may be deemed to be forward -looking statements and as such are intended to be covered by the safe harbor for “forward-looking statements” provided by the PSLRA. Forward-looking statements can be identified by words such as “plan”, “potential”, “may”, “outlook”, “anticipates”, “expects”, “will”, “promising” and similar expressions in reference to future periods. Forward -looking statements are neither historical facts nor assurances of future performance. Instead, they are based on Rigel’s current beliefs, expectations, and assumptions and hence they inherently invo lve significant risks, uncertainties and changes in circumstances that are difficult to predict and many of which are outside of Rigel’s control. Therefore, you should not rely on any of these forward-looking statements. Actual results and the timing of events could differ materially from those anticipated in such forward -looking statements as a result of these risks and uncertainties, which include, without limitation, anticipated financial performance and profitability for 2026; expected product sales and commercial growth; the anticipated t iming, progress and results of clinical development activities for R289, including enrollment, dose selection and data readouts; the Company's ability to fund its existing and f uture clinical development programs; the anticipated commercial launch and commercialization of VEPPANU, including expectations regarding its market opportunity, physician adoption, commercial performance and potential contribution to Rigel’s commercial portfolio; the Company's ability to successfully execute its commercial strategy; and its par tnering, licensing, commercialization, collaboration and potential business development activities. Actual results and the timing of events could differ materially from those anticipated in such forward looking statements a s a result of these risks and uncertainties, which include, without limitation, risks and uncertainties associated with the commercialization and marketing of VEPPANU, TAVALISSE, GAVRETO and REZLIDHIA, including uncertainties relating to physician adoption, patient demand, market acceptance, reimbursement and pricing; risks that the FDA, European Medicines Agency, PMDA or other regulatory authorities may make adverse decisions regarding VEPPANU, TAVALISSE, GAVRETO, REZLIDHIA or R289; operational, regulatory or other risks that can affect the timing of enrollment and data availability for R289 clinical development; risks that clinical trials may not be predictive of real- world results or of results in subsequent clinical trials; risks that VEPPANU, TAVALISSE, GAVRETO, REZLIDHIA or R289 may have unintended side effects, adverse reactions or incidents of misuse; the availability of resources to develop or market Rigel’s product candidates; market competition; product demand variability; pricing/reimbursement dynamics; unanticipated business needs and other develo pments, including potential partnering, licensing or other collaboration arrangements, which could impact Rigel's funding needs or other internal resourc e demands, as well as other risks detailed from time to time in Rigel’s reports filed with the Securities and Exchange Commission, including its Quarterly Report on Form 10-Q for the quarter ended June 30, 2026 and subsequent filings . Any forward-looking statement made by us in this presentation is based only on information currently available to us and speaks only as of the date on which it is made. Rigel does not undertake any obligation to update forward-looking statements, whether written or oral, that may be made from time to time, whether as a result of new information, future developments or otherwise, and expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein, except as required by law. Forward-Looking Statements 2
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Dean Schorno Executive Vice President & Chief Financial Officer Dave Santos Executive Vice President & Chief Commercial Officer Ray Furey, J.D. Executive Vice President, General Counsel & Corporate Secretary Raul Rodriguez President & Chief Executive Officer Alison Hannah, M.D. Executive Vice President & Chief Medical Officer 3 Rigel Participants
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Rigel’s Transformational Growth Strategy 4 Grow Commercial Business Maintain Financial Discipline Advance Development Pipeline In-Licensing / Business Development
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In-License of VEPPANUTM (Vepdegestrant) VEPPANU will be commercially available in mid-August 5 2L+, second line-plus; ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; FDA, U.S. Food and Drug Administration; PROTAC, PROteolysis TArgeting Chimera; HCP, healthcare provider. Please visit www.VEPPANU.com for Full Prescribing Information. • 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 breast cancer, effective June 11, 2026 – VEPPANU is the first and only FDA-approved oral PROTAC • VEPPANU has a novel mechanism of action and differentiated data; has the potential to become a market-leading treatment • Rigel has engaged with HCPs for early awareness and is ready to drive rapid adoption to execute a successful commercial launch
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Rigel’s Transformation to Accelerated Growth 6 Grow Commercial Business Maintain Financial Discipline Advance Development Pipeline In-Licensing / Business Development • Growth of four commercial products • Growth from potential in-licensing / M&A transactions • Transformational development pipeline, including R289 portfolio and other potential opportunities 2 • One commercial product • Limited development pipeline • Three commercial products • Development pipeline opportunity advancement, including R289 in lower-risk MDS • Profitable with a cash balance of $155M at the end of 2025 1 2020 2025 2030s MDS, myelodysplastic syndrome. 1. Cash, cash equivalents & short-term investments. 2. Investigational compounds in these indications and not approved by the FDA.
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Grow Commercial Business
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8 Please see Indications and Important Safety Information on slides 39-44. Please visit www.TAVALISSE.com for Full Prescribing Information. Please visit www.REZLIDHIA.com for Full Prescribing Information, including Boxed WARNING. Please visit www.GAVRETO.com for Full Prescribing Information, including Boxed WARNING.
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$8.9M Q2 2026 Net Product Sales Growth vs. Q2 2025 27% Q2 2026 Commercial Performance Net Portfolio Sales grew $8.1M (14%) vs. Q2 2025 9 Net Product Sales ($M) 40.1 47.4 11.8 10.77.0 8.9 58.9 67.0 Q2 2025 Q2 2026 Axis Title TAVALISSE GAVRETO REZLIDHIA $47.4M Q2 2026 Net Product Sales Growth vs. Q2 2025 18% $10.7M Q2 2026 Net Product Sales Growth vs. Q2 2025 (10)%
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Expanding Commercial Availability in Global Markets 10 NDA, New Drug Application. 1. Forma, now Novo Nordisk, is entitled to a certain portion of Rigel’s sublicensing revenue from olutasidenib. 2. Dr. Reddy’s territory includes Latin America, South Africa, certain countries in the Commonwealth of Independent States (CIS), India, certain countries in Southeast Asia and North Africa, Australia and New Zealand. Q2 2026 Collaboration Revenues • Kissei $5.8M • Grifols $5.0M • Medison $0.3M • Others $0.6M TAVALISSE Commercial Launch • Knight announced launch of TAVALISSE in Mexico in May TAVALISSE Regulatory Approval • Knight announced regulatory approval in Brazil in May REZLIDHIA Opportunity1 • Executing on ex-U.S. opportunities for development and commercialization ‒ Expanded relationship with Kissei to include REZLIDHIA in Japan, South Korea, and Taiwan ‒ Kissei submitted NDA in Japan in May ‒ Entered relationship with Dr. Reddy’s in Latin America and other territories 2 TAVALISSE is commercially available in key European countries (TAVLESSE), Japan, South Korea, Canada and Israel
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12 Please see Important Safety Information on slide 44 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 progression following at least one line of endocrine therapy. APPROVED IN THE U.S.
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has the Potential to Transform Rigel’s Commercial Portfolio 13 FDA, U.S. Food and Drug Administration; PROTAC, PROteolysis TArgeting Chimera degrader; 2L, second line; 3L, third line; ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2- negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated. 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 commercial and medical infrastructure and expertise are enabling us to quickly and successfully launch The potential to drive portfolio growth and become Rigel’s largest revenue producer
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PROteolysis TArgeting Chimera (PROTAC) The FIRST in a novel class of drugs called heterobifunctional protein degraders 14 The novel bifunctional design of PROTAC represents a major innovation in ER degradation VEPPANU binds to an estrogen receptor and recruits an E3 ligase complex to tag the receptor with a chain of ubiquitin proteins The ubiquitin-tagged estrogen receptor is then recognized and eliminated by the proteasome Because VEPPANU bonds transiently and reversibly to both the E3 ligase complex and the ER, it is able to repeat this process multiple times until metabolized
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ER+/HER2-, ESR1m mBC Patient Opportunity 15 ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutation; mBC, metastatic breast cancer; CDK4/6i, cyclin- dependent kinase 4/6 inhibitor; 2L, second line; 3L, third line; ctDNA, circulating tumor DNA. 1. Internal market research. 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- patients with ESR1m are in the 2L and later setting due to exposure to endocrine and CDK4/6 therapy The largest segment of metastatic breast cancer ~20,0001 patients with 2L/3L ER+/HER2-, ESR1m mBC represent potential $1B+ market in the U.S.
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2L, second line; 3L, third line; ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; MBC, metastatic breast cancer; SERD, Selective Estrogen Receptor Degrader. 1. Internal Market Research Apr 2026 Will Enter a Dynamic Market Where Most Patients are Treated in the Community Setting Current Therapies in 2L/3L ER+/HER2-, ESR1m mBC1 16 Market Opportunity • Oral SERDs have been rapidly adopted, and are used in the majority of patients in 2L and ~30% of patients in 3L • Chemotherapy and other therapies still represent more than 25% of patients in 2L and 60% of patients in 3L • Approximately 80% of patients are treated at community oncology practices, where nearly half of patients still do not receive oral SERDs in the 2L setting % Market Share 2L 8% 8% 1 Legend Chemotherapy/Other Fulvestrant Oral SERDs 57% 75% 54% 7% 2% 8% 36% 23% 38% Overall Academic Community 3L 29% 32% 29% 7% 5% 7% 64% 63% 64% Overall Academic Community
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2L+, second line-plus; ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; GI, gastrointestinal; 2L, second line; 3L, third line; CDK4/6i, cyclin-dependent kinase 4/6 inhibitor; ET, endocrine therapy; NCCN, National Comprehensive Cancer Network® (NCCN®). 1. NCCN Clinical Practice Guidelines in Oncology® for Breast Cancer V.5.2026. Accessed July 30, 2026. has the Potential to Become a Market-leading Treatment in 2L+ ER+/HER2-, ESR1m Metastatic Breast Cancer (mBC) 17 Demonstrated Tolerability • Patient characteristics of those enrolled in VERITAC-2 were representative of real-world 2L+ setting, with 100% receiving prior CDK4/6i + ET Proven Efficacy • Improved median Progression Free Survival (mPFS), Objective Response Rate (ORR) and Clinical Benefit Rate (CBR) vs. fulvestrant • Improved mPFS 2.4-fold, or 2.9 months (5.0 months vs. 2.1 months), ORR (19% vs. 4%) and CBR (42% vs. 20%) vs. fulvestrant • Manageable safety profile with low rates and severity of GI-related events • Low rates of treatment discontinuation (3%) and dose reductions (2%) Real-World Applicability Breast Cancer NCCN Guidelines® include vepdegestrant as a Category 2A Targeted Therapy treatment option for HR-positive/HER2-negative ESR1 mutation for recurrent unresectable or stage IV (M1) disease1
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Commercialization Plans Now Being Implemented Executing activities to ensure successful launch upon product availability 18 KOLs, key opinion leaders; GPOs, group purchasing organizations; ASCO, American Society of Clinical Oncology Annual Meeting. Collaboration Enabling Expedited Product Availability Strong relationships with partners and execution against detailed transition plans have ensured we are ON TRACK to have VEPPANU in our specialty distribution channel and available to patients and clinics in mid-August Coordinated Engagement with Key Customers Meetings with Breast Cancer KOLs, Payers, GPOs and other key customers have been ongoing since ASCO to prepare for launch Key accounts and top customer targets have been identified and refined through analytics and ongoing market research Leveraged Capabilities to Immediately Operationalize VEPPANU.COM live immediately upon June 16th deal close Sales Force fully deployed on June 17th to spread VEPPANU awareness Rigel ONECARE Patient Services hub, Copay Card services, and Specialty Pharmacy network now able to serve providers and patients, enabling patients access to VEPPANU upon availability Commercial Launch Readiness Activities
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• Websites: VEPPANU.com, rigelonecare.com, rigelmedinfo.com, • Initial Sales Force Materials: USPI, Now Approved promotional materials Phase 1: Now Approved Since Deal Close Phase 2: Now Available Upon Product Availability Phase 3: Branded Campaign Post-Launch (Q4) 1 2 3 • Expand Awareness and Adoption through an Omnichannel Approach • Dedicated HCP and Patient websites • Additional Promotional Materials for HCPs and Patients • Additional Materials to Facilitate Patient Starts Publication Overview, Dosing and Admin Guide, Getting Started Patient Brochure, Distribution Guide Commercial Launch Phases ON TRACK 19 USPI, U.S. Prescribing Information; HCP, healthcare provider. HCP Campaign Drive patient identification, utilization Patient Campaign Drive request, activation and support positive outcomes
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Advance Development Pipeline
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Vepdegestrant Clinical Overview 21
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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) 22 ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; CDK4/6i, cyclin-dependent kinase 4/6 inhibitor; ET, endocrine therapy; SERD, selective estrogen receptor degrader; IM, intramuscularly; BICR, blinded independent central review. 1. ESR1m status was assessed in ctDNA by Foundation Medicine, except in China, where Origmed testing was used. Primary Endpoints • Progression-free survival by BICR in: - ESR1m population - All patients Secondary Endpoints • Overall survival (key secondary) • Clinical benefit rate and objective response rate by BICR • Adverse events Data cutoff date: Jan 31, 2025 28-day Treatment CyclesKey Eligibility Criteria • Age ≥18 years old • ER+/HER2- advanced or metastatic breast cancer • Prior therapy: - 1 line of CDK4/6i + ET - ≤1 additional ET - Most recent ET for ≥6 months - No prior SERD (e.g. fulvestrant, elacestrant) - No prior chemotherapy for advanced or metastatic disease - Radiologic progression during or after the last line of therapy Vepdegestrant (n=313) 200 mg orally (once daily) Fulvestrant (n=311) 500 mg IM (days 1 and 15 of cycle 1; day 1 of subsequent cycles) Stratification Factors: • ESR1 mutation1 (yes vs. no) • Visceral disease (yes vs. no) Randomize
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Vepdegestrant Met the Primary Endpoint with a ~3-Month mPFS Improvement in Patients with Tumors Harboring ESR1 Mutations 23 Source: Hamilton. ASCO 2025. Abstr LBA1000. Note: Vepdegestrant did not meet the primary endpoint in the intention-to-treat (ITT) population. mPFS, median progression-free survival; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; PFS, progression-free survival; CI, confidence interval; Vepdeg, vepdegestrant; Fulv, fulvestrant; BICR, blinded independent central review; HR, hazard ratio. Parameter Vepdeg (n = 136) Fulv (n = 134) Median follow up, months 7.4 6.0 Events, n (%) 79 (58) 95 (71) Median PFS by BICR, months (95% CI) 5.0 (3.7-7.4) 2.1 (1.9-3.5) Stratified HR (95% CI) 0.57 (0.42-0.77) 2-sided P <.001 6-month PFS (95% CI): 45.2% (36.1–53.9) 22.7% (15.1–31.2) 0 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 0 10 20 30 40 50 60 70 80 90 100 Time (Months) P F S (%) Vepdegestrant Fulvestrant No. at risk Vepdegestrant Fulvestrant 136 134 134 125 87 62 78 52 55 30 53 29 38 15 37 12 22 8 15 7 14 2 10 1 8 1 4 1 3 1 2 0 0 0 22 8 3 0
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Vepdegestrant Showed Statistically Significant Improvements in CBR and ORR in the ESR1m Population 24 Source: Hamilton. ASCO 2025. Abstr LBA1000. CBR, clinical benefit rate; ORR, objective response rate; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; CI, confidence interval; CR, complete response; PR, partial response; SD, stable disease. 1. CBR was defined as the rate of confirmed CR or PR at any time, or SD, non-CR, or non-progressive disease for ≥24 weeks and was estimated in CBR-evaluable patients (those enrolled for ≥24 weeks prior to data cutoff or those with confirmed CR or PR). 2. ORR was defined as the rate of confirmed CR or PR and was estimated in patients with measurable disease at baseline. 3. Nominal P-value. 0 10 20 30 40 50 60 70 80 Vepdegestrant Fulvestrant Patients With ESR1m Odds ratio: 2.88 (95% CI: 1.57–5.39) P<0.0013 % ± 95% CI 42.1 20.2 CBR1 Vepdegestrant Fulvestrant ORR2 Odds ratio: 5.45 (95% CI: 1.69–22.73) P=0.0013 18.6 4.0 % ± 95% CI
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Vepdegestrant Was Generally Well Tolerated, with Low Rates of Discontinuation and Dose Reductions 25 Source: Hamilton. ASCO 2025. Abstr LBA1000. TEAEs, treatment-emergent adverse events; tx, treatment; QTcF, Fridericia-corrected QT interval; Gr, grade; ALT, alanine aminotransferase; AST, aspartate aminotransferase. a. Includes fatigue and asthenia. b. No between-group differences were observed for ALT/AST increases or anemia based on laboratory values. c. Includes anemia, hemoglobin decreased, and iron deficiency anemia. d. Includes neutropenia and neutrophil count decreased. No events led to dose reductions or treatment discontinuation in either treatment group. There were no events of febrile neutropenia in the vepdegestrant group and 1 event of grade 2 febrile neutropenia in the fulvestrant group. e. One patient with grade 4 event. f. Based on a concentration-QTc population modeling analysis. Adverse Events, % Vepdegestrant (n = 312) Fulvestrant (n = 307) TEAEs Any Grade ≥3 Serious Leading to tx discontinuation Leading to dose reduction 87 23 10 3 2 81 18 9 1 NA TRAEs Any Grade ≥3 57 8 40 3 TEAEs in >10% of Patients in Either Group, % Vepdegestrant (n = 312) Fulvestrant (n = 307) Any Gr 3/4 Any Gr 3/4 Fatiguea 27 1 16 1 ALT increasedb 14 1 10 1 AST increased 14 1 10 3 Nausea 13 0 9 1 Anemiab,c 12 2 8 3 Neutropeniad 12 2e 5 1e Back pain 11 1 7 <1 Arthralgia 11 1 11 0 Decreased appetite 11 <1 5 0 QT Prolongation • TEAEs: 10% in vepdegestrant and 1% in fulvestrant • A QT interval substudy (n = 88) confirmed a mild increase (11.1 ms) from baseline in QTcF, with upper 90% CI (13.7 ms) <20 ms,f indicating no large QT-prolonging effect
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Vepdegestrant Development 26 1. VERITAC-2 study ongoing for time to event timepoints such as duration of response, progression-free survival and overall survival. 2. Rigel will contribute up to $40 million over the next 4 years. The following studies are active, not enrolling, except for the hepatic study: • VERITAC-21 • Combination studies • Abemaciclib • Ribociclib • Samuraciclib • Atirmociclib • Japanese bridging study • Hepatic impairment study • Pfizer and Arvinas remain responsible for current clinical studies2 • Combination studies are expected to provide additional safety and efficacy data • Rigel will evaluate future development opportunities for vepdegestrant Current Clinical Studies Development Plans
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Hematology and Oncology Focus Areas1 27 • Evaluating in a Phase 1b study for patients with R/R lower-risk MDS – Granted Fast Track and Orphan Drug designations by the FDA2 • Other potential indications under consideration • Strategic collaborations: – MD Anderson: Monotherapy or combination therapy in mIDH1 AML and other hematologic malignancies – CONNECT: Combination therapy in mIDH1 high-grade glioma – MyeloMATCH: Combination therapy in mIDH1 AML and MDS R289 IRAK1/4 Inhibitor Olutasidenib mIDH1 Inhibitor IRAK1/4, interleukin receptor-associated kinases 1 and 4; R/R, relapsed/refractory; MDS, myelodysplastic syndrome; FDA, U.S. Food and Drug Administration; IDH1, isocitrate dehydrogenase-1; mIDH1, mutated IDH1; AML, acute myeloid leukemia. 1. Investigational compounds in these indications and not approved by the FDA. 2. R289 granted Fast Track designation for previously-treated transfusion dependent lower-risk MDS and Orphan Drug designation for MDS by the U.S. FDA.
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R289 IRAK1/4 Inhibitor in Lower-Risk MDS 28
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Lower-Risk MDS Treatment Landscape 29 MDS, myelodysplastic syndrome; AML, acute myeloid leukemia; ESAs, erythropoiesis-stimulating agents; TD, transfusion dependent; LR-MDS, lower-risk myelodysplastic syndrome; R/R, relapsed or refractory. 1. Investigational compound not approved by the FDA. • 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 transfusion-dependency • Modest efficacy thus far with available therapies; there is room for improvement New therapies needed for previously-treated TD LR-MDS patients that are R/R or ineligible for ESAs Non-del(5q) Del(5q) First Line Post-ESA/ESA-Ineligible Relapsed/Refractory Disease Luspatercept Imetelstat Hypomethylating agent R2891 potential indications ESAs Luspatercept Lenalidomide
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• ~12,200 lower-risk MDS patients that have been previously treated2 • Therapies for previously-treated transfusion dependent lower-risk MDS patients are lacking • Dysregulated inflammatory signaling is associated with MDS • Co-targeting IRAK1/4 may suppress inflammation and LSPC function and restore hematopoiesis • Blocks TLR and IL-1R signaling in vitro; active in preclinical models of inflammation3 • Markedly suppressed LPS-induced cytokine release was observed in a randomized controlled trial in healthy volunteers4 • Fast Track designation for previously-treated transfusion dependent LR-MDS (Nov 2024) • Orphan Drug designation for treatment of myelodysplastic syndromes (Jan 2025) • Promising preliminary safety and efficacy in a Phase 1b study in elderly, heavily pre-treated patients with R/R LR-MDS (n=33) (presented at ASH 2025)5 R2891 Program Value Proposition for Lower-Risk MDS 30 MDS, myelodysplastic syndrome; LR-MDS, lower-risk myelodysplastic syndrome; ESAs, erythropoiesis-stimulating agents; LSPC, liver stem/progenitor cells; TLR, toll-like receptor; IL-1R, interleukin 1 receptor; LPS, lipopolysaccharide; R/R, relapsed or refractory. 1. Investigational compound not approved by the FDA. 2. Rigel data analysis on file. Patient population represents previously-treated patients. 3. Sallman DA, et al. Front Oncol. 2016;6. 4. Yan L et al. Ann Rheum Dis 2020;79 (suppl 1). 5. Garcia-Manero et al. Blood (2025) 146 (Supplement 1): 489. Unmet Medical Need Clinical Proof of Concept Regulatory Designations Encouraging Clinical Profile Novel Mechanism of Action
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R2891: Phase 1b Study inRelapsed/Refractory Lower-Risk MDS 31 MDS, myelodysplastic syndrome; LR-MDS, lower-risk MDS; PK, pharmacokinetics; QD, daily; BID, twice daily; RP2D, recommended Phase 2 dose; Tx, treatment; Hb, hemoglobin; TD, transfusion dependent; TI, transfusion independence; HI-E, hematologic improvement - erythroid; PD, pharmacodynamics; FACIT-Fatigue scale, The Functional Assessment of Chronic Illness Therapy – Fatigue Scale. 1. Investigational compound not approved by the FDA. 2. Jaki T et al. Cancer Chemother Pharmacol. 2013; 71. 3. Split dose: 500 mg q AM, 250 mg q PM. 4. Platzbecker U et al. Blood 2019;133(10). 5. Cheson BD et al. Blood 2006;108. 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 therapies. Del(5q): R/R to lenalidomide • Symptomatic anemia (Hb ≤9.0 g/dL) or TD (≥2u RBCs/16wks) in dose escalation; TD in dose expansion Assessments • Hematologic responses [TI and HI-E] per IWG 2018 criteria4 and other responses per IWG 2006 criteria5, from 8 weeks Primary Endpoints • Incidence of adverse events and dose-limiting toxicities Secondary Endpoints • Transfusion independence, hematologic improvement, response rates • PK / PD • Patient-reported outcomes (FACIT-Fatigue scale) Updated data presented at ASH 2025 Dose Expansion PhaseDose Escalation Phase Modified 3+3 Design2 Dose level 2 500 mg QD Dose level 4 250 mg BID Dose level 1 250 mg QD Dose level 3 750 mg QD Dose level 5 500/250 mg3 Dose level 6 500 mg BID 500 mg QD (n= up to 20) 500 mg BID (n= up to 20) Post-ESA, Tx naïve LR-MDS (n=10) Once RP2D selected, open exploratory cohort of 1L LR-MDS Randomize
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Phase 1b Study Dose Escalation Phase Data Summary Elderly, heavily pre-treated patient population with a high baseline transfusion burden 32 • R289 was generally well tolerated with a low incidence of Grade 3/4 cytopenias and infections • 6/18 (33%) evaluable TD patients receiving ≥500 mg QD achieved RBC-TI >8 weeks ; 4 >16 weeks; 3 >24 weeks • Median duration of treatment: 5.5 months (range: 0.9 - 27.7 months) • Median time to onset of RBC-TI: 1.9 months • Median duration of RBC- TI: 22.9 weeks (9 - 104.3) Note: Patients listed in order of enrollment. TD, transfusion dependent; QD, once daily; RBC, red blood cell; RBC-TI, red blood cell transfusion independence; BID, twice daily; HI-E, hematologic improvement-erythroid. Source: Garcia-Manero et al. Blood (2025) 146 (Supplement 1): 489. 500 mg QD (n=6) 500 mg BID (n=6) 500/250 mg QD (n=6) 250 mg BID (n=6) 250 mg QD (n=3) Study week Evaluable for HI-E responses RBC-TI ≥8 weeks On-going RBC transfusion day 750 mg QD (n=6) 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 RBC Transfusion Events by Dose Group
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R289 Development Next Steps 33 MDS, myelodysplastic syndrome; ESA, erythropoiesis-stimulating agent; FDA, U.S. Food and Drug Administration. 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 naïve patients following selection of recommended Phase 2 dose • Upon completion of Phase 1b study, follow-up with FDA about a potential registrational study Other Potential Indications • Evaluate R289 in other potential indications
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Maintain Financial Discipline
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Q2 2026 Highlights 35 Net Product Sales ($M) 21.1 26.4 26.3 31.0 28.5 40.1 44.7 45.6 37.3 47.4 1.9 7.1 8.1 9.0 11.8 11.1 10.2 9.6 10.7 4.9 5.2 5.5 7.4 6.1 7.0 8.3 9.6 8.0 8.9 26.0 33.5 38.9 46.5 43.6 58.9 64.1 65.4 54.9 67.0 Q124 Q224 Q324 Q424 Q125 Q225 Q325 Q425 Q126 Q226 Axis Title TAVALISSE GAVRETO REZLIDHIA Q2 2026 Net Product Sales: $67.0M • TAVALISSE $47.4M • GAVRETO $10.7M • REZLIDHIA $8.9M Q2 2026 Contract Revenues: $11.7M • Kissei $5.8M • Grifols $5.0M • Medison $0.3M • Others $0.6
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Q2 2026 Financial Overview (in thousands) 36 Note: Q2 2025 and full-year 2025 contract revenues from collaborations and total revenue included $40M in non-cash contract revenues related to Rigel’s agreement with Eli Lilly. 2026 Financial Outlook • Total revenues of ~$285M to $295M • Net product sales of ~$255M to $265M • Contract revenues of ~$30M (previously ~$20M to $25M) • Revenue guidance excludes VEPPANU • Anticipate will report positive net income for the full year 2026, while funding existing and new clinical development programs 2026 2025 2026 2025 Revenues Net Product Sales $ 67,015 $ 58,948 $ 121,938 $ 102,498 Contract revenues from collaborations and other 11,688 42,737 15,583 52,520 Total revenues 78,703 101,685 137,521 155,018 Costs and expenses: Cost of product sales 8,525 4,504 13,131 8,913 Research and development 13,961 6,821 25,637 15,257 Selling, general and administrativ e 32,642 29,257 63,293 56,972 Total costs and expenses 55,128 40,582 102,061 81,142 Income from operations 23,575 61,103 35,460 73,876 Interest income 789 753 1,994 1,344 Interest expense and other (779) (1,874) (2,212) (3,727) Income before income tax 23,585 59,982 35,242 71,493 Provision for income tax 6,295 369 9,298 434 Net income $ 17,290 $ 59,613 $ 25,944 $ 71,059 June 30, 2026 December 31, 2025 Cash, Cash Equivalents and Short-term Investments $ 95,329 $ 154,955 Three Months Ended June 30, Six Months Ended June 30, As of
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Exclusive Global License Agreement to Develop, Manufacture and Commercialize VEPPANUTM (vepdegestrant) 37 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 payments: $320M ⎻ Regulatory Milestones: $60M ⎻ Commercial Milestones: $260M • Tiered Royalties: Mid-teens to mid-twenties • Pfizer and Arvinas remain responsible for current clinical trials ⎻ Rigel will contribute up to $40 million over the next 4 years
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2026 Progress and Key 2H 2026 Priorities 38 PROTAC, PROteolysis TArgeting Chimera; 2L+, second line-plus; ER+/HER2-, estrogen receptor-positive, human epidermal growth factor receptor 2-negative; ESR1, estrogen receptor 1 gene; ESR1m, ESR1 mutated; MDS, myelodysplastic syndrome; RP2D, recommended Phase 2 dose; FDA, U.S. Food and Drug Administration. 1. Revenue guidance excludes VEPPANU. Grow Commercial Business • Immediately initiated VEPPANUTM (vepdegestrant) launch activities upon close of transaction; to become commercially available in mid-August • Drive rapid awareness and adoption of VEPPANU Maintain Financial Discipline • Leverage existing commercial and operating infrastructure during integration of VEPPANU to drive financial synergies • 2026 Outlook: Total revenues: ~$285M to $295M1 - Net product sales of ~$255M to $265M - Contract revenues of ~$30M (previously $20M to $25M) In-Licensing / Business Development • In-license of VEPPANUTM (vepdegestrant), an oral PROTAC with the potential to be an important new treatment option for patients with 2L+ ER+/HER2-, ESR1m advanced or metastatic breast cancer Advance Development Pipeline • R289 Phase 1b study in lower-risk MDS: - Complete dose expansion and select RP2D for future clinical studies (2H 2026) - Share updated top-line data by end of 2026 - Upon completion of the Phase 1b study, follow- up with FDA about a potential registrational study • Evaluate R289 in other potential indications
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TAVALISSE® (fostamatinib disodium hexahydrate) Tablets INDICATION • TAVALISSE® (fostamatinib disodium hexahydrate) tablets is indicated for the treatment of thrombocytopenia in adult patients with chronic immune thrombocytopenia (ITP) who have had an insufficient response to a previous treatment. IMPORTANT SAFETY INFORMATION | WARNINGS AND PRECAUTIONS • Hypertension can occur with TAVALISSE treatment. Patients with pre-existing hypertension may be more susceptible to the hypertensive effects. Monitor blood pressure every 2 weeks until stable, then monthly, and adjust or initiate antihypertensive therapy for blood pressure control maintenance during therapy. If increased blood pressure persists, TAVALISSE interruption, reduction, or discontinuation may be required. • Elevated liver function tests (LFTs), mainly ALT and AST, can occur with TAVALISSE. Monitor LFTs monthly during treatment. If ALT or AST increase to ≥3 x upper limit of normal, manage hepatotoxicity using TAVALISSE interruption, reduction, or discontinuation. • Diarrhea occurred in 31% of patients and severe diarrhea occurred in 1% of patients treated with TAVALISSE. Monitor patients for the development of diarrhea and manage using supportive care measures early after the onset of symptoms. If diarrhea becomes severe (≥Grade 3), interrupt, reduce dose or discontinue TAVALISSE. • Neutropenia occurred in 6% of patients treated with TAVALISSE; febrile neutropenia occurred in 1% of patients. Monitor the ANC monthly and for infection during treatment. Manage toxicity with TAVALISSE interruption, reduction, or discontinuation. • TAVALISSE can cause fetal harm when administered to pregnant women. Advise pregnant women the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for at least 1 month after the last dose. Verify pregnancy status prior to initiating TAVALISSE. It is unknown if TAVALISSE or its metabolite is present in human milk. Because of the potential for serious adverse reactions in a breastfed child, advise a lactating woman not to breastfeed during TAVALISSE treatment and for at least 1 month after the last dose. DRUG INTERACTIONS • Concomitant use of TAVALISSE with strong CYP3A4 inhibitors increases exposure to the major active metabolite of TAVALISSE (R406), which may increase the risk of adverse reactions. Monitor for toxicities that may require a reduction in TAVALISSE dose. • It is not recommended to use TAVALISSE with strong CYP3A4 inducers, as concomitant use reduces exposure to R406. • Concomitant use of TAVALISSE may increase concentrations of some CYP3A4 substrate drugs and may require a dose reduction of the CYP3A4 substrate drug. • Concomitant use of TAVALISSE may increase concentrations of BCRP substrate drugs (eg, rosuvastatin) and P-Glycoprotein (P-gp) substrate drugs (eg, digoxin), which may require a dose reduction of the BCRP and P-gp substrate drug. ADVERSE REACTIONS • Serious adverse drug reactions in the ITP double-blind studies were febrile neutropenia, diarrhea, pneumonia, and hypertensive crisis, which occurred in 1% of TAVALISSE patients. In addition, severe adverse reactions occurred including dyspnea and hypertension (both 2%), neutropenia, arthralgia, chest pain, diarrhea, dizziness, nephrolithiasis, pain in extremity, toothache, syncope, and hypoxia (all 1%). • Common adverse reactions (≥5% and more common than placebo) from FIT -1 and FIT-2 included: diarrhea, hypertension, nausea, dizziness, ALT and AST increased, respiratory infection, rash, abdominal pain, fatigue, chest pain, and neutropenia. To report side effects of prescription drugs to the FDA, visit https://www.fda.gov/medwatch or call 1-800-FDA-1088 (1-800-332-1088) 39 Please see https://www.tavalisse.com/ for full Prescribing Information
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About REZLIDHIA® (olutasidenib) INDICATION REZLIDHIA is an isocitrate dehydrogenase-1 (IDH1) inhibitor indicated for the treatment of adult patients with relapsed or refra ctory acute myeloid leukemia (AML) with a susceptible IDH1 mutation as detected by an FDA-approved test. IMPORTANT SAFETY INFORMATION WARNING: DIFFERENTIATION SYNDROME Differentiation syndrome, which can be fatal, can occur with REZLIDHIA treatment. Symptoms may include dyspnea, pulmonary infiltrates/pleuropericardial effusion, kidney injury, hypotension, fever, and weight gain. If differentiation syndrome is suspected, withhold REZLIDHIA and initiate treatment with corticosteroids and hemodynamic monitoring until symptom resolution. WARNINGS AND PRECAUTIONS Differentiation Syndrome REZLIDHIA can cause differentiation syndrome. In the clinical trial of REZLIDHIA in patients with relapsed or refractory AML, differentiation syndrome occurred in 16% of patients, with grade 3 or 4 differentiation syndrome occurring in 8% of patients treated, and fatalities in 1% of patients. Differentiation syndrome is associated with rapid proliferation and differentiation of myeloid cells and may be life-threatening or fatal. Symptoms of differentiation syndrome in patients treated with REZLIDHIA included leukocytosis, dyspnea, pulmonary infiltrates/pleuropericardial effusion, kidney injury, fever, edema, pyrexia, and weight gain. Of the 25 patients who experienced differentiation syndrome, 19 (76%) recovered after treatment or after dose interruption of REZLIDHIA. Differentiation syndrome occurred as early as 1 day and up to 18 months af ter REZLIDHIA initiation and has been observed with or without concomitant leukocytosis. If differentiation syndrome is suspected, temporarily withhold REZLIDHIA and initiate systemic corticosteroids (e.g., dexamet hasone 10 mg IV every 12 hours) for a minimum of 3 days and until resolution of signs and symptoms. If concomitant leukocytosis is observed, initiate treatment with hydroxyurea, as clinically indicated. Taper corticosteroids and hydroxyurea after resolution of symptoms. Differentiation syndrome may recur with premature discontinuation of corticosteroid s and/or hydroxyurea treatment. Institute supportive measures and hemodynamic monitoring until improvement; withhold dose of REZLIDHIA and consider dose reduction based on recurr ence. Hepatotoxicity REZLIDHIA can cause hepatotoxicity, presenting as increased alanine aminotransferase (ALT), increased aspartate aminotransfer ase (AST), increased blood alkaline phosphatase, and/or elevated bilirubin. Of 153 patients with relapsed or refractory AML who received REZLIDHIA, hepatotoxicity occurred in 23% of patients; 13% experienced grade 3 or 4 hepatotoxicity. One patient treated with REZLIDHIA in combination with azacitidine in the clinical trial, a combination for w hich REZLIDHIA is not indicated, died from complications of drug-induced liver injury. The median time to onset of hepatotoxicity in patients with relapsed or refractory AML treated with R EZLIDHIA was 1.2 months (range: 1 day to 17.5 months) after REZLIDHIA initiation, and the median time to resolution was 12 days (range: 1 day to 17 months). The most common hepatotoxicities were elevations of ALT, AST, blood alkaline phosphatase, and blood bilirubin 40
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IMPORTANT SAFETY INFORMATION (Cont.) WARNINGS AND PRECAUTIONS Hepatotoxicity Monitor patients frequently for clinical symptoms of hepatic dysfunction such as fatigue, anorexia, right upper abdominal dis comfort, dark urine, or jaundice. Obtain baseline liver function tests prior to initiation of REZLIDHIA, at least once weekly for the first two months, once every other week for the third month, once in the fourth month, and once every other month for the duration of therapy. If hepatic dysfunction occurs, withhold, reduce, or permanently discontinue REZLIDHIA base d on recurrence/severity. ADVERSE REACTIONS The most common (≥20%) adverse reactions, including laboratory abnormalities, were aspartate aminotransferase increased, alan ine aminotransferase increased, potassium decreased, sodium decreased, alkaline phosphatase increased, nausea, creatinine increased, fatigue/malaise, arthralgia, const ipation, lymphocytes increased, bilirubin increased, leukocytosis, uric acid increased, dyspnea, pyrexia, rash, lipase increased, mucositis, diarrhea and transaminitis. DRUG INTERACTIONS • Avoid concomitant use of REZLIDHIA with strong or moderate CYP3A inducers. • Avoid concomitant use of REZLIDHIA with sensitive CYP3A substrates unless otherwise instructed in the substrates prescribing information. If concomitant use is unavoidable, monitor patients for loss of therapeutic effect of these drugs. LACTATION Advise women not to breastfeed during treatment with REZLIDHIA and for 2 weeks after the last dose. GERIATRIC USE No overall differences in effectiveness were observed between patients 65 years and older and younger patients. Compared to pati ents younger than 65 years of age, an increase in incidence of hepatotoxicity and hypertension was observed in patients ≥65 years of age. HEPATIC IMPAIRMENT In patients with mild or moderate hepatic impairment, closely monitor for increased probability of differentiation syndrome. You may report side effects to the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 41 Please see https://www.REZLIDHIA.com/ for full Prescribing Information, including Boxed WARNING.
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42 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 age and older with advanced or metastatic RET fusion -positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate)* *This indication is approved under accelerated approval based on overall response rate and duration of response. Continued appro val for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s). IMPORTANT SAFETY INFORMATION WARNING: SERIOUS INFECTIONS, INCLUDING OPPORTUNISTIC INFECTIONS GAVRETO may increase the risk for serious infections, including bacterial, fungal, viral and opportunistic infections, which can lead to hospitalization or death. Withhold, reduce the dose or permanently discontinue GAVRETO based on severity. WARNINGS AND PRECAUTIONS • Serious Infections, including Opportunistic Infections: GAVRETO may increase the risk for serious infections, including fatal and opportunistic infections. In the AcceleRET-Lung trial, infections occurred in 72% of patients who received GAVRETO, including 18% with Grade 3 and 3.7% with Grade 4 and 7% with fat al outcomes. Among the patients who received chemotherapy/immunotherapy, infections occurred in 52%, including 10% with Grade 3. Infections in the GAVRETO arm included pn eumonia, urinary tract infection, opportunistic infections (such as pneumocystis jirovecii pneumonia, and fungal infections) and others. Monitor patients for signs and symptoms of infection and treat appropriately. W ithhold, reduce the dose, or permanently discontinue GAVRETO based on severity. • Interstitial Lung Disease (ILD)/Pneumonitis: Severe, life-threatening, and fatal interstitial lung disease (ILD)/pneumonitis can occur in patients treated with GAVRETO. Pneu monitis occurred in 12% of patients who received GAVRETO, including 3.3% with Grade 3 -4, and 0.2% with fatal reactions. Monitor for pulmonary symptoms indicative of ILD/pneumonitis. Withhold GAVRETO and promptly investigate for ILD in any patient who presents with acute or worsening of respiratory symptoms which may be indicative of ILD (e.g., dyspnea, cough, and fever). Withhold, reduce dose or permanently discontinue GAVRETO based on severity of confirmed ILD. • Hypertension: Hypertension occurred in 35% of patients, including Grade 3 hypertension in 18% of patients. Overall, 8% had their dose inter rupted and 4.8% had their dose reduced for hypertension. Treatment-emergent hypertension was most commonly managed with anti-hypertension medications. Do not initiate GAVRETO in patients with uncontrolled hypertension. Optimize blood pressure prior to initiating GAVRETO. Monitor blood pressure after 1 week, at least monthly thereafter and as clinically indicated. Initiate or adjust anti-hypertensive therapy as appropriate. Withhold, reduce dose, or permanently discontinue GAVRETO based on the severity. • Hepatotoxicity: Serious hepatic adverse reactions occurred in 1.5% of patients treated with GAVRETO. Increased AST occurred in 49% of patient s, including Grade 3 or 4 in 7% and increased ALT occurred in 37% of patients, including Grade 3 or 4 in 4.8%. The median time to first onset for increased AST w as 15 days (range: 5 days to 2.5 years) and for increased ALT was 24 days (range: 7 days to 3.7 years). Monitor AST and ALT prior to initiating GAVRETO, every 2 weeks during the first 3 months, then monthly thereafter and as clinically indicated. Withhold, reduce dose or permanently discontinue GAVRETO based on severity.
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43 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 patients with severe or life -threatening hemorrhage. • Tumor Lysis Syndrome: Cases of tumor lysis syndrome (TLS) have been reported in patients with medullary thyroid carcinoma receiving GAVRETO. Patien ts may be at risk of TLS if they have rapidly growing tumors, a high tumor burden, renal dysfunction, or dehydration. Closely monitor patients at risk, c onsider appropriate prophylaxis including hydration, and treat as clinically indicated. • Risk of Impaired Wound Healing: Impaired wound healing can occur in patients who receive drugs that inhibit the vascular endothelial growth factor (VEGF) sig naling pathway. Therefore, GAVRETO has the potential to adversely affect wound healing. Withhold GAVRETO for at least 5 days prior to electiv e surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of GAVRETO after resolution of wound healing complications has not been established. • Embryo-Fetal Toxicity: Based on findings from animal studies and its mechanism of action, GAVRETO can cause fetal harm when administered to a pregna nt woman. Oral administration of pralsetinib to pregnant rats during the period of organogenesis resulted in malformations and embryolethality at maternal exposures below the human exposure at the clinical dose of 400 mg once daily. Advise pregnant women of the potential risk to a fetus. Advise females of reproduc tive potential to use effective non-hormonal contraception during treatment with GAVRETO and for 2 weeks after the last dose. Advise males with female partners of reprodu ctive potential to use effective contraception during treatment with GAVRETO and for 1 week after the last dose. ADVERSE REACTIONS • The most common adverse reactions (≥ 25%) were musculoskeletal pain, constipation, hypertension, diarrhea, fatigue, edema, pyrexia and cough. The most common Grade 3-4 laboratory abnormalities (≥ 2%) were decreased lymphocytes, decreased neutrophils, decreased hemoglobin, decreased phosphate, decreased leukocytes, decreased sodium, increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), decreased calcium (corrected), decreased platelets, increased alkaline phosphatase, increased potassium, decreased potassium and increased bilirubin. DRUG INTERACTIONS • Strong or moderate CYP3A inhibitors and/or P-gp inhibitors: Concomitant use with a strong or moderate CYP3A inhibitor and/or a P-gp inhibitor increases pralsetinib exposure, which may increase the risk of adverse reactions related to GAVRETO. Avoid coadministration of GAVRETO with a strong or moder ate CYP3A and/or P-gp inhibitor. If coadministration with any of the above inhibitors cannot be avoided, reduce the GAVRETO dose. • Strong or moderate CYP3A inducers: Concomitant use with a strong CYP3A inducer decreases pralsetinib exposure, which may decrease efficacy of GAVRETO. Avoid concomitant use of GAVRETO with strong or moderate CYP3A inducers. If coadministration of GAVRETO with strong or moderate CYP 3A inducers cannot be avoided, increase the GAVRETO dose. USE IN SPECIFIC POPULATIONS • Lactation: Advise not to breastfeed during treatment with GAVRETO and for 1 week after the last dose. • Pediatric Use: The safety and effectiveness of GAVRETO have not been established in pediatric patients with RET fusion -positive NSCLC or in pediatric patients younger than 12 years old with RET fusion positive thyroid cancer. You may report side effects to the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Please see https://www.GAVRETO.com/ for full Prescribing Information, including Boxed WARNING.
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About VEPPANUTM (vepdegestrant) INDICATION VEPPANU is indicated for the treatment of adults with estrogen receptor (ER)–positive, human epidermal growth factor receptor 2 (HER2)–negative, estrogen receptor–1 (ESR1)– mutated advanced or metastatic breast cancer, as detected by an FDA -authorized test, with disease progression following at least one line of endocrine therapy. IMPORTANT SAFETY INFORMATION WARNINGS AND PRECAUTIONS QTc Interval Prolongation VEPPANU can cause QT (QTc) interval prolongation. Correct electrolyte abnormalities, including hypokalemia and hypomagnesemia, prior to and during treatment with VEPPANU. Perform an ECG prior to initiation of treatment with VEPPANU and do not initiate VEPPANU in patients with QTc >470 msec. Repeat ECG approximately 4 weeks after initiating treatment and as clinically indicated. Avoid concomitant use of VEPPANU with strong CYP3A inhibitors or drugs known to prolong the QTc interval. Embryo-Fetal Toxicity Based on findings from animal studies and its mechanism of action, VEPPANU can cause fetal harm when administered to a pregnant woman. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose. ADVERSE REACTIONS Serious adverse reactions occurred in 9% of patients who received VEPPANU. The serious adverse reactions included any fracture (1.3%), fall, hypercalcemia, hepatic injury, pneumonia, musculoskeletal pain (0.6% each), and QTc prolonged (0.3%). Fatal adverse reactions occurred in 1.0% of patients who received VEPPANU, including dyspnea, cerebral ischemia, and unknown cause (one patient each). Permanent discontinuation of VEPPANU due to an adverse reaction occurred in 2.9% of patients, dosage interruptions of VEPPANU due to an adverse reaction occurred in 14% of patients, and dosage reductions of VEPPANU due to an adverse reaction occurred in 1.9% of patients. The most common (≥10%) adverse reactions, including laboratory abnormalities, were decreased white blood cells, increased AST, musculoskeletal pain, fatigue, decreased hemoglobin, decreased neutrophils, increased ALT, increased alkaline phosphatase, nausea, decreased blood potassium, increased bilirubin, decreased appetite, electrocardiogram QT prolonged, decreased platelets, and constipation. Clinically relevant adverse reactions in <10% of patients who received VEPPANU included headache, hot flush, diarrhea, vomiting, bradycardia, and urinary tract infection. DRUG INTERACTIONS • Strong CYP3A Inhibitors: Avoid concomitant use of VEPPANU with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce VEPPANU dosage. • Strong CYP3A Inducers: Avoid concomitant use with strong CYP3A inducers in patients receiving VEPPANU. If concomitant use cannot be avoided, increase VEPPANU dosage. • Certain P-gp Substrates: Avoid concomitant use with certain P-gp substrates where minimal increases in concentration may lead to serious adverse reactions. • Certain UGT1A9 Substrates: Refer to the Prescribing Information for UGT1A9 substrates where minimal increases in the concentration may lead to serious adverse reactions. Avoid concomitant use of VEPPANU with other drugs with a known potential to prolong the QTc interval. LACTATION Advise lactating women not to breastfeed during treatment with VEPPANU and for 2 weeks after the last dose. To report side effects of prescription drugs to the FDA, visit https://www.fda.gov/medwatch or call 1-800-FDA-1088 (1-800-332-1088) 44 Please see https://www.VEPPANU.com/ for full Prescribing Information. RIGL_FRN-26047
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Thank You www.rigel.com 45