PT-2385 is a selective inhibitor of hypoxia-inducible factor-2 (HIF-2), a protein complex involved in the cellular response to low oxygen levels. It has gained attention for its potential in treating cancers where HIF-2 signaling is dysregulated, particularly clear cell renal cell carcinoma (ccRCC). In this type of kidney cancer, the von Hippel-Lindau (VHL) tumor suppressor pathway is often impaired, leading to abnormal accumulation of HIF-2 and activation of genes that promote tumor growth, angiogenesis, and metastasis. PT-2385 blocks the dimerization of HIF-2α with its partner ARNT, thereby suppressing the transcription of downstream oncogenic targets. Due to its targeted mechanism, PT-2385 has been used in preclinical studies to validate HIF-2 as a therapeutic target and to explore resistance mechanisms that may arise during treatment. It serves as a prototype for developing next-generation HIF-2 inhibitors with improved pharmacokinetic and safety profiles. While not currently approved for clinical use, PT-2385 has contributed significantly to the understanding of hypoxia signaling in cancer and has paved the way for related compounds now being evaluated in clinical trials.