Peloton Therapeutics, Inc. announced dosing of the first patient in a Phase 2 trial evaluating the efficacy and safety of lead investigational oncology agent, PT2977, to treat von Hippel-Lindau (VHL) disease-associated kidney cancer. PT2977 is a once-daily, oral inhibitor of HIF-2a, a transcription factor that has been implicated in the development and progression of renal cell carcinoma (RCC). The primary objective of the Phase 2 trial is to evaluate the efficacy of PT2977 for the treatment of VHL disease-associated renal tumors as measured by overall response rate. Secondary objectives include duration of response, time to response, progression free survival, and time to surgery for VHL disease-associated renal tumors. The trial will also evaluate the efficacy of PT2977 in other VHL disease-associated tumor types as well as the safety and pharmacokinetics of PT2977. Patients will be evaluated radiologically approximately every 12 weeks while continuing in the study. Peloton’s drug discovery and development efforts focus on identifying novel compounds capable of modulating complex protein-protein interactions that drive disease which have eluded conventional small molecule approaches. Peloton has the only clinical stage small-molecule inhibitors of HIF-2a, and PT2977 has demonstrated a favorable profile in a Phase 1 study in patients with advanced solid tumors including RCC. The study will enroll 50 patients at clinical trial centers across the United States and Europe.