Phase 2 Trial Begins Testing VS-6766, Defactinib Combo in Low-grade Serous Ovarian Cancer

Phase 2 Trial Begins Testing VS-6766, Defactinib Combo in Low-grade Serous Ovarian Cancer
Verastem Oncology has started a Phase 2 clinical trial evaluating its inhibitors, VS-6766 and defactinib, for the treatment of people with recurrent low-grade serous ovarian cancer (LGSOC), the company announced. The trial seeks to recruit up to 100 female patients — more information is available here — and will investigate the company's RAF/MEK inhibitor VS-6766, either alone or in combination with defactinib, a FAF inhibitor. “Results to date have demonstrated the clinical activity of VS-6766 and defactinib in KRAS mutant cancers, signaling potentially promising clinical results in low-grade serous ovarian cancer and in KRAS-G12V mutant non-small cell lung cancer,” Brian Stuglik, CEO of Verastem, said in a press release. “The start of our registration-directed trial in recurrent LGSOC is a significant milestone in our work to develop the backbone of therapy for RAS driven tumors, an area of minimal therapeutic results, significant toxicity and limited treatment options,” he added. VS-6766 is an orally available small molecule that inhibits the activity of MEK and RAF, two proteins belonging to a pathway involved in several cancer processes, including cell proliferation, survival, and migration. Mutations in KRAS, which are present in about 30% of all cancers, appear to result in the abnormal activation of this signaling pathway, and blocking this signaling has long been seen as an attractive treatment for these cancers. Defactinib (VS-6063) is an oral small molecule inhibitor of FAK and PYK2 that targets cancer cells both directly and through modulation of the tumor microenvironment. It has already received orphan drug designation in the U.S., the European Union, and Australia for the treatment of ovarian cancers. Preclinical and clini
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