GFH375/VS-7375

May 7, 2026: Verastem Oncology (NASDAQ: VSTM) reported Q1 2026 results and provided program updates. AVMAPKI® FAKZYNJA® CO-PACK (avutometinib + defactinib) generated $18.7M net product revenue in Q1 2026. The company highlighted new two-year median follow-up from the Phase 2 RAMP 201 trial in recurrent low-grade serous ovarian cancer (LGSOC), presented at the Society of Gynecologic Oncology 2026 meeting, showing durable benefit across KRAS-mutant and KRAS–wild-type patients and supporting the approved dose via exposure-response analysis. In Japan (RAMP 201J; data cutoff Jan 30, 2026), confirmed ORR was 38% (6/16); 57% (4/7) in KRAS-mutant and 22% (2/9) in KRAS–wild-type.

VS-7375 (oral KRAS G12D ON/OFF inhibitor): The company initiated three Phase 2 registration-directed trials—TARGET-D 201 (2L PDAC; monotherapy and with cetuximab; also evaluating 1L PDAC combo), TARGET-D 202 (2L/3L NSCLC; includes asymptomatic untreated brain metastases), and TARGET-D 203 (previously treated CRC; monotherapy and with EGFR inhibitors; also chemo combinations in 1L mCRC). In TARGET-D 101 (Phase 1/2), dosing includes 1200 mg QD evaluation and 900 mg QD + cetuximab; PK update indicated 900 mg QD achieves target plasma levels; safety update (n=23 at 400/600/900 mg QD; cutoff Jan 30, 2026) reported no drug-related LFT abnormalities and no drug-related neutropenia > Grade 2.

Upcoming catalysts: TARGET-D 101 early data in 1H 2026 and an additional update in 2H 2026; first patient dosed in TARGET-D 201/202/203 expected mid-2026; RAMP 205 (1L metastatic pancreatic cancer combo with chemotherapy) expansion cohort safety/efficacy update in Q2 2026; RAMP 301 Phase 3 primary endpoint topline in mid-2027. GenFleet (partner; GFH375 in China) received China breakthrough therapy designations for KRAS G12D-mutant metastatic pancreatic cancer (April) and KRAS G12D-mutant NSCLC (March). Verastem appointed Daniel Lyons as Chief Commercial Officer and ended Q1 2026 with $181.7M cash, projecting runway into 1H 2027.