MK-6482 (also known as PT2977) is an orally administered inhibitor of hypoxia-inducible factor (HIF)-2α that is being investigated in multiple advanced solid tumors in a phase 1 trial.
The first-in-class agent selectively inhibits HIF-2α, a master transcription factor involved in hypoxia-induced carcinogenic pathways, which was thought to be undruggable until recently.
In the advanced clear cell renal cell carcinoma cohort, results of which were reported at ASCO GU 2020, MK-6482 showed promise: