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belzutifan + pembrolizumab
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
The combination of **belzutifan** (a small-molecule inhibitor of hypoxia-inducible factor 2 alpha, HIF-2α) and **pembrolizumab** (a monoclonal antibody against programmed cell death protein 1, PD-1) is under clinical investigation mainly as an adjuvant treatment after nephrectomy in patients with **clear cell renal cell carcinoma (ccRCC)** at increased risk of recurrence[1][3][7]. Belzutifan blocks HIF-2α dimerization, suppressing oncogenic transcriptional activity driven by VHL pathway alterations in ccRCC[6]. Pembrolizumab inhibits PD-1 to enhance T-cell mediated tumor immunity. This regimen is currently being tested in the randomized phase 3 LITESPARK-022 trial, assessing its efficacy and safety compared with pembrolizumab plus placebo in the adjuvant setting[1][3][7]. Both components are developed and manufactured by Merck.
- Brand names
- Welireg + Keytruda
- Other names
- pembrolizumabbelzutifan
02
Targets
EPAS1 (Hypoxia-inducible factor 2-alpha)PDCD1 (Programmed cell death protein 1 receptor)
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