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PT2399 is a small molecule that inhibits Hif2-alpha, resulting in decreased downstream signaling and potentially leading to reduced growth of tumors with defective VHL (PMID: 27595393, PMID: 30523118).
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|PT2399||HIF2A Inhibitor 6||PT2399 is a small molecule that inhibits Hif2-alpha, resulting in decreased downstream signaling and potentially leading to reduced growth of tumors with defective VHL (PMID: 27595393, PMID: 30523118).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|VHL inact mut||clear cell renal cell carcinoma||conflicting||PT2399||Preclinical - Pdx||Actionable||In a preclinical study, PT2399 had variable impact on tumor growth in clear cell renal cell carcinoma (ccRCC) cell line and patient-derived xenograft (PDX) models with defective VHL, with decreased tumor growth in a VHL-defective ccRCC PDX model and some VHL-defective ccRCC cell line xenograft models, and no tumor suppression in other cell line xenograft models (PMID: 27595393).||27595393|
|TP53 R248W VHL inact mut||clear cell renal cell carcinoma||resistant||PT2399||Preclinical - Cell culture||Actionable||In a preclinical study, TP53 R248W was associated with resistance to PT2399 in VHL-defective clear cell renal cell carcinoma cell lines in culture (PMID: 27595393).||27595393|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|