Drug intelligence / Profile preview

VS-6766 + everolimus

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

Overview

VS-6766 is a small molecule RAF/MEK clamp that reduces p-MEK and p-ERK, while everolimus is an mTOR inhibitor. The combination of VS-6766 and everolimus has shown preclinical synergy in KRAS-mutant non-small cell lung cancer (NSCLC) cell lines. This drug combination aims to simultaneously block two key pathways (RAF/MEK and mTOR) that KRAS-driven cancers rely on for growth, potentially delaying the development of resistance. Clinical trials have evaluated intermittent dosing schedules for safety and efficacy, with promising early results in patients with KRAS-mutant NSCLC who have exhausted other treatment options.

Other names
RAF/MEK clamp VS-6766 plus everolimusVS-6766 and everolimus combinationVS6766 and everolimus combinationVS 6766 and everolimus combination
02

Targets

Mechanistic target of rapamycin complex 1MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))Mechanistic target of rapamycin kinase complex 2

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