GFH375 (VS-7375)

Jun 3, 2026 — Verastem Oncology (Nasdaq: VSTM) announced the U.S. FDA granted Fast Track Designation for VS-7375, an oral investigational selective KRAS G12D “ON/OFF” inhibitor, for adult patients with KRAS G12D–mutated unresectable locally advanced or metastatic NSCLC who have received platinum chemotherapy and an anti–PD-(L)1 antibody. VS-7375 previously received Fast Track Designation for KRAS G12D–mutated advanced/metastatic pancreatic cancer.

Verastem has initiated the Phase 2, open-label, registration-directed TARGET-D 202 trial in 2L/3L advanced NSCLC, evaluating VS-7375 900 mg once daily, including patients with asymptomatic untreated brain metastases based on supportive preclinical intracranial models. The Phase 1/2 TARGET-D 101 trial (advanced KRAS G12D solid tumors) is ongoing; dose escalation from 400–900 mg QD has shown no dose-limiting toxicities or major safety concerns to date, and March 2026 data from 23 patients indicated general tolerability with no drug-related LFT abnormalities or Grade >2 neutropenia (Jan 30, 2026 cutoff). Early updates are expected in 1H 2026 and more mature data in 2H 2026. Clinically, the designation may speed development for a mutation with no FDA-approved targeted therapies.