Drug intelligence / Profile preview

encorafenib + binimetinib + infigratinib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**Encorafenib + binimetinib + infigratinib** is a hypothetical combination regimen comprised of three small-molecule inhibitors—**encorafenib** (a RAF kinase inhibitor), **binimetinib** (a MEK inhibitor), and **infigratinib** (a selective FGFR1-3 inhibitor). Encorafenib and binimetinib are indicated in combination for the treatment of adult patients with unresectable or metastatic melanoma and metastatic non-small cell lung cancer (NSCLC) harboring BRAF V600E/K mutations[1][2][4][7][8], with proven efficacy in halting tumor growth by inhibiting the MAPK pathway. Infigratinib is approved as a single agent for cholangiocarcinoma and is under investigation for other FGFR-driven cancers; it targets FGFR1, FGFR2, and FGFR3. At present, no clinical evidence or regulatory approval exists for the combined use of all three agents together. This entry describes the theoretical pharmacology of their combination: encorafenib inhibits mutant BRAF, binimetinib suppresses downstream MEK1/2 signaling, and infigratinib blocks FGFR-mediated cell growth—all leading to inhibition of tumor cell proliferation and survival in cancers with corresponding mutations.

02

Targets

MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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