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belrestotug + inupadenant + dostarlimab

Development stage: Discontinued
Lead developer: GSK
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Intravenous (for Belrestotug And Dostarlimab), Oral (for Inupadenant)

Overview

A combination immunotherapy regimen consisting of belrestotug (an anti-TIGIT monoclonal antibody), inupadenant (an adenosine A2A receptor antagonist), and dostarlimab (an anti–PD-1 monoclonal antibody). Belrestotug blocks TIGIT, a checkpoint inhibitor, to increase T cell–mediated immune responses against tumor cells. Dostarlimab blocks PD-1, another checkpoint protein, to reactivate T cell activity. Inupadenant blocks the adenosine A2A receptor to further relieve immunosuppression in the tumor microenvironment. The regimen was developed for use in advanced solid tumors, especially non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC), but all ongoing trials and development were terminated in 2025 after mixed Phase 2 results and no benefit in progression-free survival[1][3][4][9].

Brand names: Jemperli (for dostarlimab only)
Other names: TIGIT antagonist monoclonal antibody (for belrestotug)anti-TIGIT antibody (for belrestotug)anti–PD-1 antibody (for dostarlimab)

Targets

PDCD1 (Programmed cell death protein 1 receptor)ADORA2A (Adenosine A₂A Receptor)TIGIT (T cell immunoreceptor with Ig and ITIM domains)

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