Drug intelligence / Profile preview

casdatifan + ipilimumab + zimberelimab

Development stage
Phase 1
Lead developer
Arcus Biosciences
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

Casdatifan + ipilimumab + zimberelimab is an investigational triplet combination regimen being developed for the treatment of advanced clear cell renal cell carcinoma (ccRCC). The combination consists of casdatifan (AB521), an oral small-molecule inhibitor of hypoxia-inducible factor 2-alpha (HIF-2α); ipilimumab, an anti-CTLA-4 monoclonal antibody; and zimberelimab, an anti-PD-1 monoclonal antibody. This regimen is designed to combine HIF-2α inhibition with dual immune checkpoint blockade (anti-PD-1 and anti-CTLA-4) without the use of a tyrosine kinase inhibitor. It is being evaluated in the Phase 1 ARC-20 platform study (NCT05536141) in the first-line setting for patients with advanced ccRCC.

Other names
casdatifan + ipilimumab + zimberelimab regimencasdatifan plus ipilimumab plus zimberelimab
02

Targets

CD28 (Cluster of Differentiation 28)CD80 (T-lymphocyte activation antigen CD80)CD86 (T-lymphocyte activation antigen CD86)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)HIF1A (Hypoxia-inducible factor 1-alpha)ICOS (Inducible T-cell costimulator)PDCD1 (Programmed cell death protein 1 receptor)CD274 (Programmed cell death protein 1 ligand 1)PDCD1LG2 (Programmed cell death 1 ligand 2)EPAS1 (Hypoxia-inducible factor 2-alpha)

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