-Verastem Oncology (Nasdaq: VSTM), a biopharmaceutical company committed to advancing new medicines for patients with RAS/MAPK pathway-driven cancers, announced that the first patient has been dosed in the TARGET-D 203 Phase 2 registration-directed trial evaluating VS-7375, an investigational oral KRAS G12D (ON/OFF) inhibitor with best-in-class potential, to treat patients with KRAS G12D-mutated metastatic colorectal cancer (mCRC). The Company has now initiated treatment across all three of its TARGET-D registration-directed Phase 2 clinical trials evaluating VS-7375 in patients with KRAS G12D-mutated pancreatic, colorectal, and lung cancers.

“KRAS G12D is the most common KRAS mutation found in colorectal cancer and is associated with a worse prognosis for patients compared with KRAS wildtype – underscoring the need for an FDA-approved treatment option specifically for KRAS G12D-mutated cancers. We believe VS-7375 with EGFR blockade has the potential to significantly improve outcomes for patients with KRAS G12D-mutated metastatic colorectal cancer due to its differentiated profile and encouraging preliminary data from our ongoing Phase 1/2 trial,” said Michael Kauffman, M.D., Ph.D., president of development at Verastem Oncology. “VS-7375 has demonstrated preliminary anti-tumor activity in combination with full dose cetuximab with no unexpected toxicities. Dosing the first patient in TARGET-D 203 marks an important milestone in our clinical development program as we continue to advance VS-7375 and build on the encouraging data generated to date.”

TARGET-D 203 (NCT07659795) is a Phase 2, open-label, multi-center study to evaluate VS-7375 at 900 mg once daily (QD) both as monotherapy and in combination with anti-EGFR therapies, including cetuximab or panitumumab, in previously treated KRAS G12D-mutated mCRC. The study is also evaluating VS-7375 in combination with cetuximab and chemotherapy in the first line setting in patients with KRAS G12D-mutated mCRC.

In June 2025, Verastem initiated TARGET-D 101, its Phase 1/2 dose escalation, dose expansion, and combination clinical trial evaluating the safety and efficacy of VS-7375 in patients with KRAS G12D-mutated metastatic pancreatic ductal carcinoma (mPDAC), mCRC, advanced non-small cell lung cancer (NSCLC), and other solid tumor cancers. In a recent update, the Company shared that VS-7375 demonstrated encouraging anti-tumor activity across multiple KRAS G12D-driven tumor types, including mPDAC, mCRC, and advanced NSCLC, with evidence of dose-dependent activity, favorable pharmacokinetics supporting target exposure, and a favorable and manageable safety and tolerability profile. Patient follow-up continues to mature across monotherapy and combination cohorts, and the Company expects to share an update in the second half of 2026.