In June 2011, Rigel entered into an exclusive, worldwide research, development and commercialization agreement with BerGenBio for its investigational AXL receptor tyrosine kinase (AXL) inhibitor, R428 (now referred to as bemcentinib).

Bemcentinib is a potent, selective and orally bioavailable AXL inhibitor and the furthest along in clinical trials.

BerGenBio is a clinical-stage oncology company focused on developing transformative drugs targeting AXL as a potential cornerstone of therapy for aggressive diseases, including immune-evasive, therapy resistant cancers.  In preclinical studies, bemcentinib was shown to have an effect as a single agent therapeutic in the prevention and reversal of acquired resistance to standard of care cytotoxics and targeted therapies and may also slow or prevent tumor metastasis.

Rigel received an upfront payment and is eligible for milestone payments, potential sublicensing revenue as well as tiered royalties on any future net sales of commercialized products.

Development of bemcentinib:

  • Phase 2 adaptive platform trial to assess efficacy and safety of multiple candidate agents for the treatment of COVID-19 in hospitalized UK NHS patients
  • Six clinical trials are ongoing across oncology indications with high unmet medical need including acute myeloid leukemia (AML), non-small cell lung cancer (NSCLC), triple negative breast cancer (TNBC), and melanoma
  • AML
    • Phase 2 clinical trial in combination with low-dose chemotherapy
    • Phase 2 clinical trial in combination with KEYTRUDA® (partnered with Merck)
    • Phase 2 clinical trial in combination with TARCEVA®
    • Phase 2 clinical trial in combination with chemotherapy
  • TNBC
    • Phase 2 clinical trial in combination with KEYTRUDA (partnered with Merck)
  • Melanoma
    • Phase 2 clinical trial in combination KEYTRUDA or chemotherapy

KEYTRUDA is a trademark of Merck Sharp & Dohme Corp
Tarceva is a trademark of OSI Pharmaceuticals