belzutifan

11/16/2022 - "Belzutifan is a promising treatment for RH with the potential for both rapid and sustained tumor regression."
01/01/2021 - "Belzutifan was well tolerated and demonstrated preliminary anti-tumor activity in heavily pre-treated patients, suggesting that HIF-2α inhibition might offer an effective treatment for ccRCC."
01/01/2021 - "Maximum tolerated dose, safety, pharmacokinetics, pharmacodynamics and anti-tumor activity of belzutifan were evaluated in this first-in-human phase 1 study (NCT02974738). "
11/07/2023 - "This report demonstrates the use of belzutifan to safely and successfully reduce ocular tumor burden of complicated RHB with extrascleral extension, ultimately decreasing the need for enucleation."
01/01/2023 - "Indeed, one such agent (belzutifan) is already approved for VHL-associated RCC and other VHL-associated neoplasms. "

11/16/2022 - "She was treated for 2.5 years with belzutifan for renal cell carcinoma on the National Institutes of Health trial. "
07/01/2023 - "Currently, widespread in-vitro and in-vivo research is focusing on targeting HIF with drugs that have already been approved for use by the FDA, such as belzutifan, in renal cell carcinoma. "
01/01/2023 - "Belzutifan: enhancing the blockade of angiogenesis in renal cell carcinoma."
01/01/2023 - "The first-in-class, small molecule HIF-2α inhibitor, belzutifan, has demonstrated promising antitumor activity in previously treated patients with clear cell renal cell carcinoma (RCC). "
11/15/2023 - "Phase I LITESPARK-001 study of belzutifan for advanced solid tumors: Extended 41-month follow-up in the clear cell renal cell carcinoma cohort."

09/27/2022 - "Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan."
01/01/2022 - "Along the hypoxia inducible factor pathway, belzutifan has received FDA approval in von Hippel-Lindau-associated RCC. "
01/01/2022 - "Belzutifan inhibits the hypoxia-inducible factor by binding to the Per-ARNT -Sim-B binding pocket on the hypoxia-inducible factor -2α, inhibiting cellular proliferation and angiogenesis. "
11/01/2023 - "Belzutifan is a Hypoxia Inducible Factor 2-alpha inhibitor approved in 2021 by the FDA for the treatment of renal cell carcinoma (RCC) in patients with Von-Hippel Landau (VHL) disease. "
01/01/2023 - "Belzutifan is a second-generation small molecule hypoxia-inducible factor 2α (HIF-2α) inhibitor recently approved by US and UK regulators for the treatment of VHL (disease)-associated ccRCC, CNS-HB and pNET. "

11/01/2023 - "Belzutifan appears to be an effective and safe treatment for CNS hemangioblastoma in VHL patients. "
11/01/2023 - "The outcome of central nervous system hemangioblastomas in Von Hippel-Lindau (VHL) disease treated with belzutifan: a single-institution retrospective experience."
08/01/2023 - "We showed that belzutifan is safe and well-tolerated with strong disease response for CNS hemangioblastoma in adults with VHL, supporting continued use of belzutifan in this patient population. "
08/01/2023 - "Our objective was to report on our clinical experience with belzutifan in adult patients with VHL-associated CNS hemangioblastoma. "
08/01/2023 - "Belzutifan in adults with VHL-associated central nervous system hemangioblastoma: a single-center experience."

12/01/2022 - "Belzutifan in a Patient With VHL-Associated Metastatic Pancreatic Neuroendocrine Tumor."
01/01/2023 - "Belzutifan, a second-generation HIF-2α inhibitor, was shown to provide clinically meaningful benefit in the treatment of VHL-associated tumors (including ccRCC, pancreatic lesions as well as neuroendocrine tumor, and CNS hemangioblastomas). "
01/01/2023 - "Belzutifan, a highly specific and well-tolerated HIF2α inhibitor, recently received FDA approval for the treatment of nonmetastatic renal cell carcinomas, pancreatic neuroendocrine tumors, and central nervous system hemangioblastomas from patients with von Hippel-Lindau disease, who carry VHL germline mutations. "
01/01/2023 - "Lastly, we propose that the high efficacy of belzutifan observed in tumors with genetically driven hypoxia caused by VHL mutations suggests that a focus on other mutations that similarly lead to HIF2α stabilization, such as those occurring in neuroendocrine tumors with disruptions in the tricarboxylic acid cycle (SDHA/B/C/D, FH, MDH2, IDH2), HIF hydroxylases (EGLN/PHDs), and the HIF2α-encoding gene, EPAS1, are warranted."
05/01/2021 - "The small-molecule HIF 2 alpha inhibitor MK-6482 (belzutifan) has demonstrated significant efficacy in VHL disease related renal cell carcinomas, hemangioblastomas, and pancreatic neuroendocrine tumors while demonstrating an acceptable safety profile. "