Merck's Belzutifan, the World's First HIF-2α Inhibitor, Approved in China for VHL-Associated Tumors

Nov 21, 2024 16:00 CST Updated 16:00

MSD

Pharmaceutical R&D and Manufacturer

On November 21, the NMPA website showed that MSD's HIF-2α inhibitor Bezufigo（Belzutifan）Approved in China,Used forVHL（von Hippel-Lindau）Disease-related renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastoma, or pancreatic neuroendocrine tumor (pNET)。

Screenshot source: NMPA database

Bezuclifan was initially developed by Peloton Therapeutics. In May 2019, Merck & Co., Inc. (MSD) acquired Peloton Therapeutics for an upfront payment of $1.05 billion and milestone payments totaling $1.15 billion, thereby obtaining Bezuclifan.

HIF, or hypoxia-inducible factor, is a key oncogenic driver in renal cell carcinoma. As an HIF-2α inhibitor, belzutifan blocks the heterodimerization of HIF-2α and HIF-1β, thereby inhibiting cell growth, proliferation, and preventing abnormal blood vessel formation to achieve anti-cancer efficacy.

On August 14, 2021, Belzutifan was approved by the FDA, becoming the world's first and currently the only approved HIF-2α inhibitor.(Oral Hypoxia-Inducible Factor 2α)Inhibitor.

A previous open-label Phase II clinical study（NCT03401788）The results showed that VHL-related RCC patientsORR was 49%（95% CI：36, 62）All responsive VHL-RCC patients were followed up for at least 18 months from the start of treatment, without reaching the median DoR; 56% of responders had a DoR ≥ 12 months, with a median TTR of 8 months.

Among patients with other VHL-related non-RCC tumors, 24 patients had measurable CNS hemangioblastomas.ORR was 63%, 12 patients with measurable pNETORR was 83%The median DoR has not been reached, and 73% and 50% of patients with CNS hemangioblastoma and pNET, respectively, have a response duration ≥12 months.

In terms of safety, ≥ 20% acceptanceBezutifanThe most common adverse reactions reported by treated patients, including laboratory abnormalities, were decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, and nausea. Anemia occurred in 90% of patients, with 7% experiencing Grade 3 anemia and 1.6% developing hypoxia.

Screenshot source: Insight database

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