belzutifan

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). "
05/01/2024 - "Adults with VHL diagnosis based on germline VHL alteration, ≥1 measurable RCC tumor, no renal tumor >3 cm or other VHL neoplasm requiring immediate surgery, Eastern Cooperative Oncology Group performance status of 0 or 1, and no prior systemic anticancer treatment received belzutifan 120 mg once daily. "
04/19/2024 - "This review summarizes the history, mechanism of action and research evidence to date supporting the use of belzutifan in VHL disease and cancer treatment. "
04/19/2024 - "The novel drug belzutifan was developed after years of research in identifying the VHL gene and how genetic abnormalities in VHL may result in tumor growth. "

04/19/2024 - "Belzutifan is a novel small-molecule inhibitor of hypoxia-inducible factor 2α which has demonstrated efficacy in treating von Hippel-Lindau (VHL) disease, earning regulatory approvals for this indication. "
09/19/2023 - "A concise linear synthesis of hypoxia inducible factor-2α (HIF-2α) inhibitor, belzutifan was achieved by reproducing key components of previous synthetic approaches to this molecule as described in several publications and patents. "
09/27/2022 - "Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan."
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. "
01/01/2022 - "Along the hypoxia inducible factor pathway, belzutifan has received FDA approval in von Hippel-Lindau-associated RCC. "

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."

05/01/2024 - "She was treated for 2.5 years with belzutifan for renal cell carcinoma on the National Institutes of Health trial. "
01/01/2024 - "Belzutifan, HIF-2α Inhibitor, and Clear Cell Renal Cell Carcinoma With Somatic Von-Hippel-Lindau Loss-of-Function Mutation."
09/19/2023 - "Belzutifan is an orally bioavailable small-molecule (HIF-2α) inhibitor for the treatment of von Hippel-Lindau (VHL) disease-associated renal cell carcinoma (RCC) that received FDA approval in 2021. "
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 - "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). "

04/19/2024 - "Belzutifan: a novel therapeutic for the management of von Hippel-Lindau disease and beyond."
05/01/2024 - "Belzutifan for von Hippel-Lindau Disease: Pancreatic Lesion Population of the Phase 2 LITESPARK-004 Study."
01/01/2023 - "Belzutifan, a second-generation HIF2a inhibitor, was the first to receive FDA approval for the treatment of unresectable ccRCC in VHL syndrome. "
01/01/2023 - "Neurological applications of belzutifan in von Hippel-Lindau disease."
10/01/2022 - "Belzutifan (Welireg™) for von Hippel Lindau disease."