Drug intelligence / Profile preview

belrestotug + inupadenant

Development stage
Unknown
Lead developer
iTeos Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous (belrestotug), Oral (inupadenant)
01

Overview

**belrestotug + inupadenant** is a combination of two investigational immunotherapy drugs developed for oncology. Belrestotug (formerly EOS-448, GSK4428859A) is a fully human IgG1 monoclonal antibody that antagonizes TIGIT, a checkpoint receptor implicated in tumor immune evasion, and exerts both checkpoint inhibition and antibody-dependent cell cytotoxicity (ADCC) to enhance anti-tumor immune responses. Inupadenant (EOS-850) is a selective, small molecule antagonist of the adenosine A2A receptor (A2AR), aiming to counteract the immunosuppressive tumor microenvironment driven by extracellular adenosine. The combination targets both inhibitory immune checkpoint pathways (TIGIT) and adenosine-mediated immune suppression (A2A receptor), aiming to synergistically promote T cell activation and antitumor immunity in patients with advanced solid tumors and hematological malignancies. Both agents were primarily explored as a combination in phase I and II clinical trials, but further development was deprioritized or discontinued due to insufficient efficacy results in recent studies.

Brand names
belrestotug + inupadenant
Other names
EOS-448 + EOS-850EOS-448 + inupadenantGSK4428859A + inupadenant
02

Targets

ADORA2A (Adenosine A₂A Receptor)TIGIT (T cell immunoreceptor with Ig and ITIM domains)

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