Pipeline

Commercialized Products

TAVALISSE® (fostamatinib)1

Adult Chronic Immune Thrombocytopenia
Target: Spleen tyrosine kinase (SYK)

Pre-Clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-Clinical Complete
Phase 1 Complete
Phase 2 Complete
REGISTRATIONAL Complete
Approved Complete

REZLIDHIA® (olutasidenib)2

R/R mIDH1 Acute Myeloid Leukemia
Target: Mutant isocitrate dehydrogenase–1 (mIDH1)

Pre-clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-clinical Complete
Phase 1 Complete
Phase 2 Complete
REGISTRATIONAL Complete
Approved Complete

GAVRETO® (pralsetinib)3

RET+ Non-Small Cell Lung Cancer & Advanced Thyroid Cancer
Target: Rearranged During Transfection (RET)

Pre-clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-clinical Complete
Phase 1 Complete
Phase 2 Complete
REGISTRATIONAL Complete
Approved Complete

Clinical Trials

R289*

Lower-Risk Myelodysplastic Syndrome
Target: Interleukin receptor-associated kinases 1 and 4 (IRAK1/4)

Pre-clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-clinical Complete
Phase 1 Complete
Phase 2 Not Started
REGISTRATIONAL Not Started
Approved Not Started

Partnered Programs4

Ocadusertib* (Systemic) – Eli Lilly

Rheumatoid Arthritis
Target: Receptor-interacting serine/threonine-protein kinase 1 (RIPK1)

Pre-clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-clinical Complete
Phase 1 Complete
Phase 2 In Progress
REGISTRATIONAL Not Started
Approved Not Started

Rxxx (CNS penetrant) – Eli Lilly5

CNS Diseases
Target: RIPK1

Pre-clinical Phase 1 Phase 2 REGISTRATIONAL Approved
Pre-clinical In Progress
Phase 1 Not Started
Phase 2 Not Started
REGISTRATIONAL Not Started
Approved Not Started

KEY:

Company-sponsored Trials Partnered Programs

1 Please see the TAVALISSE Full Prescribing Information

2 Please see the REZLIDHIA Full Prescribing Information, including Boxed WARNING

3 Please see the GAVRETO Full Prescribing Information

4 Rigel also has partnerships with BerGenBio (bemcentinib) and Daiichi Sankyo (milademetan)

5 In early October, Rigel received notification from Lilly that it will terminate the central nervous system (CNS) disease program related to the collaboration between the two companies, which will become effective 60 days following notification.

* Investigational compound - has not been submitted for approval by FDA