Corporate Presentation

March 2024

1

Forward Looking Statements

This presentation contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1955 ("PSLRA") relating to, among other things, expected commercial and financial results; Rigel's ability to earn and receive milestone payments; expectations related to the potential and market opportunity of REZLIDHIA® (olutasidenib) as therapeutics for relapsed or refractory acute myeloid leukemia (AML) and other conditions; the potential and market opportunity for TAVALISSE® (fostamatinib) as therapeutics for chronic ITP and other conditions; the regulatory approval and commercialization of fostamatinib or olutasidenib in the U.S. and international markets; and Rigel's ability to further develop its clinical stage and early-stage product candidates and Rigel's partnering and collaboration/alliance efforts, including the progress of the Phase 1b clinical trial of R289 for the treatment of lower-risk myeloid dysplastic syndrome (MDS), the advancement of the Phase 2a clinical trial of R552 for the treatment of rheumatoid arthritis, and the development of olutasidenib as a therapy for a broad range of mIDH1+ cancers, including but not limited to AML, MDS, and glioma, and Rigel's partnering efforts and ability to achieve regulatory and commercial milestones and earn and receive milestone payments; and the potential benefits of Rigel's acquisition of U.S. rights to GAVRETO (pralsetinib), including opportunities in NSCLC and DTC, Rigel's ability to leverage its existing commercial infrastructure to market and distribute pralsetinib, Rigel's ability to transition pralsetinib to its distribution network and provide patients with access to pralsetinib, the payment and timing of milestone and royalty payments and Rigel's ability to start recognizing product sales in the third quarter of 2024 and the market opportunity for pralsetinib.

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", "expects", "will" 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 involve 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, risks and uncertainties associated with the commercialization and marketing of fostamatinib, olutasidenib or pralsetinib; risks that the FDA, European Medicines Agency, PMDA or other regulatory authorities may make adverse decisions regarding fostamatinib, olutasidenib or pralsetinib; risks that clinical trials may not be predictive of real-world results or of results in subsequent clinical trials; risks that fostamatinib, olutasidenib or pralsetinib may have unintended side effects, adverse reactions or incidents of misuses; the availability of resources to develop, manufacture and commercialize Rigel's product candidates; market competition; and those other risks detailed from time to time in Rigel's reports filed with the Securities and Exchange Commission, including its Annual Report on Form 10-K for the year ended December 31, 2023 and subsequent filings. Any forward-looking statement made by us in this press release 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.

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

2 information.

Growing Our Hematology and Oncology Business

Commercial Execution

Expansion & Development

In-Licensing and Product Acquisition

GAVRETO®(pralsetinib) added to existing commercial and medical affairs operations

New late-stage assets which leverage current capabilities and capacity

Development Programs1

Evaluate REZLIDHIA in a broad range of IDH1-mutant cancers including AML, MDS and glioma

R289 IRAK1/4 inhibitor Phase 1b trial in lower-risk MDS

ITP

mIDH1 R/R AML

ITP, immune thrombocytopenia; IDH1, isocitrate dehydrogenase-1; mIDH1, mutated IDH1; R/R, relapsed or refractory; AML, acute myeloid leukemia; MDS, myelodysplastic syndrome; IRAK1/4, interleukin

3 receptor-associated kinases 1 and 4. 1. Investigational compounds in these indications and not approved by the FDA. Please see Important Safety Information on slides 50-54. 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.

Acquired U.S. Rights to GAVRETO®

GAVRETO (pralsetinib) is a once daily, small molecule, oral, kinase inhibitor of wild-type RET (rearranged during transfection) and oncogenic RET fusions

Highly synergistic with Rigel's current product portfolio and existing commercial infrastructure and expertise

Generated ~$28M in U.S. net product sales in 20231

Patents that have issued or are expected to issue covering GAVRETO will have statutory expiration dates between 2036 and 2041

  • Established U.S. marketed product
  • Blueprint will receive a purchase price of $15.0M
    • $10.0M payable upon first commercial sale by Rigel
    • $5.0M payable on the first anniversary of the closing date, subject to certain conditions
  • Blueprint is also eligible to receive up to $97.5M in future commercial milestone payments and up to $5.0M in future regulatory milestone payments, in addition to tiered royalties ranging from 10% to 30%
  • Rigel expects to add GAVRETO to its operations and start recognizing product sales in Q3, 2024

RET, rearranged during transfection.

4

1. U.S. Net sales provided by Blueprint Medicines as reported by Genentech, a member of the Roche group. Please see Important Safety Information on slides 53 & 54. Please visit www.GAVRETO.com for Full

Prescribing information.

APPROVED IN THE U.S.

GAVRETO is indicated for the treatment of adult patients with metastatic rearranged during transfection (RET)

fusion-positivenon-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 metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate)*

Please see Important Safety Information on slides 53 & 54

* This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval

5 for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).

Growing Our Oncology Targeted Therapy Portfolio

GAVRETO U.S. Net Sales ($M)1

30.0

27.7

25.0

22.8

20.0

14.5

15.0

10.0

5.0

0.9

0.0

2020

2021

2022

2023

Q1

Q2

Q3

Q4

A compelling and synergistic opportunity

  • Enables entry into a well-identified subset of large solid tumor market
    • Immediately recognizable population of RET fusion-positive patients
    • Challenging to treat with platinum-based chemotherapy and checkpoint inhibitors
  • Leverages patient access
    • Efficient product distribution
    • Responsive Rigel ONECARE patient services
    • Strong coverage and reimbursement
  • Complementary to our field capabilities
    • Commercial and Medical Affairs teams in both academic and community settings

6 RET, rearranged during transfection. 1. US Net sales provided by Blueprint Medicines as reported by Genentech, a member of the Roche group.

NSCLC and Treatment of RET fusion-positive Patients

~235K Lung cancer patients in 20241

1L therapy for treatment eligible patients3

~41K

~3K RET fusion- positive patients2

~194K

~20%

~15%

~60%

~5%

MKIs*

Chemo+ICI**

GAVRETO

treated with RET inhibitor

* Multi-Kinase Inhibitors

** Immune Checkpoint Inhibitors(anti PD-1/PD-L1)

NSCLC, non-small cell lung cancer; SCLC, small cell lung cancer; RET, rearranged during transfection. 1. American Cancer Society Key Statistics for Lung Cancer https://www.cancer.org/cancer/types/lung-

7 cancer/about/key-statistics.html2. Kato, S. et al. RET aberrations in diverse cancers: next-generation sequencing of 4,871 patients. Clin Cancer Res. 2017;23(8):1988-1997 doi: 10.1158/1078-0432.CCR-16- 1679 3. Market Research conducted in Q2 2023 with 60 oncologists managing RET fusion-positive patients.

Pralsetinib Clinical Data Overview

RET-altered Solid Tumors Have Been Underserved Historically1,2,3,4,5

Disease Overview

  • RET is one of the first oncogenic kinase fusions cloned from an epithelial tumor, an oncogenic driver primarily in solid tumors
  • Two primary mechanisms: Fusions and activating mutations
  • RET alterations are prevalent across a range of tumors:

Papillary

NSCLC1,2

thyroid

cancers3

RET fusions

~1-2%

~20%

US annual patient incidence

~3K

~1K

Historical Medical Need

Non-selective therapies in RET+ NSCLC have poor outcomes with an ORR <30%

Sub-optimal inhibition impacts the durability of responses with non-selectivemulti-kinase inhibitors

Drug-related toxicity due to non-selective inhibitors has been evidenced by poor tolerability

Up to 75% of patients dose reduce due to poor tolerability of non-selective inhibitors

NSCLC, non-small cell lung cancer; RET, rearranged during transfection; ORR, overall response rate.

9 1. Lipson, et al. Nat Med 2012 2. Takeuchi, et al. Nat Med 2012 3. Santoro, et al. J Clin Invest 1992 4. Romei, et al. Oncotarget 2018 5. Gainor JF. et al., BLU-667 ASCO 2019 Presentation

MKIs, Platinum-based Therapies and Immunotherapies are Associated with Suboptimal Response Rates and PFS

Studies Evaluating Kinase Inhibitors in Patients with RET Fusion-positive NSCLC

Outcomes

ORR (%)

Median PFS (months)

MKI

Vandetanib, Cabozantinib, Lenvatinib,

0 - 28%

4.5-7.3

Sorafenib1,2,3,4,5

Anti-PD1/PD-L1 directed immune

6%

2.1

checkpoint inhibitors (ICI) 6

Pemetrexed/platinum-based therapy

49%

6.4

(n=66)7

Platinum based chemotherapy (n=84)7

51%

7.8

NOTE: Data is from independent studies, not comparative trials.

Multi-kinase inhibitors: Discontinuation rate 8-24% and rate of AEs grade ≥ 3, 28-92%

MKI, multi-kinase inhibitors; ICI, immune checkpoint inhibitors; PFS, progression-free survival; ORR, overall response rate; NSCLC, non-small cell lung cancer; RET, rearranged during transfection.

1. Drilon A et al. Nat Rev Clin Oncol 15, 151-167 (2018). 2. Lee SH et al. Annals of Oncology. 2017;28(2):292-297.3. Drilon A et al. Lancet Oncology. 2016;17(12):1653- 1660. 4. Hida T et al. Lung Cancer. 2019;138:124-136.

10 5. Horiike A et al. Lung Cancer. 2016;93:43-46. doi:10.1016/j.lungcan.2015.12.011. 6. Mazieres J, Drilon AE, Mhanna L, et al. Efficacy of immune-checkpoint inhibitors (ICI) in non-small cell lung cancer (NSCLC) patients harboring activating molecular alterations (ImmunoTarget).Journal of clinical oncology 7. Gautschi O, et al. Targeting RET in Patients With RET-Rearranged Lung Cancers: Results From the Global, Multicenter RET Registry. J Clin Oncol. 2017;35(13):1403. Epub 2017 Mar 13.

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Rigel Pharmaceuticals Inc. published this content on 15 April 2024 and is solely responsible for the information contained therein. Distributed by Public, unedited and unaltered, on 15 April 2024 23:44:02 UTC.