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belzutifan

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Overview

NCI Definition [1]:
An orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha (HIF-2a), with potential antineoplastic activity. Upon oral administration, HIF-2alpha inhibitor PT2977 binds to and blocks the function of HIF-2alpha, thereby preventing HIF-2alpha heterodimerization and its subsequent binding to DNA. This results in decreased transcription and expression of HIF-2alpha downstream target genes, many of which regulate hypoxic signaling. This inhibits cell growth and survival of HIF-2alpha-expressing tumor cells. HIF-2alpha, the alpha subunit for the heterodimeric transcription factor HIF-2, is overexpressed in many cancers and promotes tumorigenesis.

Clinical Trials

View Clinical Trials for belzutifan

Belzutifan has been investigated in 11 clinical trials, of which 11 are open and 0 are closed. Of the trials investigating belzutifan, 3 are phase 1 (3 open), 2 are phase 1/phase 2 (2 open), 3 are phase 2 (3 open), and 3 are phase 3 (3 open).

VHL Loss (germline) and VHL Mutation (germline) are the most frequent biomarker inclusion criteria for belzutifan clinical trials.

Clear cell renal cell carcinoma, malignant solid tumor, and renal cell carcinoma are the most common diseases being investigated in belzutifan clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Belzutifan
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating belzutifan and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
belzutifan, mk-6482, pt 2977, pt2977, hif-2alpha inhibitor pt2977, pt2977
Drug Categories [2]:
Angiogenesis inhibitors
Drug Target(s) [2]:
EPAS1
NCIT ID [1]:
C135627

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.