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Therapy Name | Belzutifan + PRT1419 |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Belzutifan | Welireg | PT2977|MK-6482|PT-2977 | HIF2A Inhibitor 6 | Welireg (belzutifan) is a hypoxia inducible factor-2alpha (EPAS1, HIF2A) inhibitor that suppresses expression of HIF2A target genes, resulting in tumor regression (Mol Cancer Ther 2018,17(1 Suppl):Abstract nr B140, PMID: 31282155). Welireg (belzutifan) is FDA-approved for use in patients with von Hippel-Lindau (VHL) disease-associated renal cell carcinoma, central nervous system hemangioblastomas, or pancreatic neuroendocrine tumors that require therapy, and in patients with advanced renal cell carcinoma who have received anti-PD-1 or PD-L1 therapy and VEGF inhibitor (FDA.gov). |
PRT1419 | PRT 1419|PRT-1419 | MCL1 Inhibitor 18 | PRT1419 is an inhibitor of myeloid cell leukemia 1 (MCL1) that blocks inactivation of pro-apoptotic proteins by Mcl1, which may lead to apoptosis of tumor cells overexpressing Mcl1 (NCI Drug Dictionary). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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PBRM1 inact mut VHL loss | clear cell renal cell carcinoma | sensitive | Belzutifan + PRT1419 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PRT1419 and Welireg (belzutifan) inhibited tumor growth of a clear cell renal cell carcinoma cell line xenograft model harboring an inactivating PBRM1 mutation and with loss of VHL (PMID: 38371625). | 38371625 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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