Category: Renal Carcinoma

PT2977 is an Orally Active and Selective HIF-2α Inhibitor for Solid Tumor Treatment

Previous studies have demonstrated that hypoxia-inducible factor 2α (HIF-2α) is a key oncogenic driver in clear cell renal cell carcinoma (ccRCC). PT2385 was the first reported HIF-2α inhibitor. However, PT2385 was restricted by variable and dose-limited pharmacokinetics. This results from extensive metabolism of PT2385 to its glucuronide metabolite. Herein,...

R916562, a Dual Axl/VEGF-R2 Inhibitor for Cancer Therapy

Axl tyrosine kinase is a putative driver of diverse cellular processes that are critical for the development, growth, and spread of tumors. It is a promising therapeutic target for cancer therapy. VEGFR2 is a primary responder to vascular endothelial growth factor signal, and thereby regulates endothelial migration and proliferation....