Drug intelligence / Profile preview

agerafenib

Development stage
Phase 1
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Agerafenib is an orally bioavailable, selective multikinase inhibitor that targets mutant forms, fusions, and rearrangements involving the proto-oncogene receptor tyrosine kinase RET (rearranged during transfection), as well as the serine/threonine-protein kinase BRAF and epidermal growth factor receptor (EGFR). It is a small molecule developed for its potential antineoplastic activity in solid tumors. Agerafenib specifically inhibits mutated BRAF (notably V600E), RET, and EGFR kinases, thereby blocking downstream signaling through the RAF/MEK/ERK pathway. This inhibition leads to decreased proliferation of tumor cells harboring these mutations or alterations. The drug has been investigated primarily for cancers with RET alterations and other solid tumors such as malignant melanoma and colorectal cancer[1][2][3][4][5][7].

Other names
agerafenib hydrochloride
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)BRAF (B-Raf proto-oncogene, serine/threonine kinase)EPHA2 (Ephrin type-A receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RAF1 (c-Raf-1 (Y340D/Y341D))PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

Beyond the preview

Go deeper on agerafenib.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on agerafenib.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call