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Peloton Therapeutics, Inc.
Drug Names(s): PT-2977, PT 2977
PT2977 is an antagonist of HIF-2a, a transcription factor that drives the expression of multiple gene products impacting metabolism, angiogenesis, cell proliferation, metastasis, inflammation, and evasion of anti-tumor immune responses. HIF-2a plays a key role in driving disease progression in many pathological disorders affected and propagated by hypoxia and is implicated in the development and progression of several types of cancer.
The role of HIF-2a is particularly important in clear cell renal cell carcinoma (ccRCC). In the majority of patients with ccRCC, the tumor suppressor von Hippel-Lindau protein (pVHL) that targets HIF-2a for degradation is inactivated, leading to the accumulation of HIF-2a and the transcription of genes that drive kidney cancer tumorigenesis.
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