Drug intelligence / Profile preview

etrumadenant + sacituzumab govitecan

Development stage
Unknown
Lead developer
Arcus Biosciences
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

**Etrumadenant + sacituzumab govitecan** is an investigational combination therapy for the treatment of cancers, particularly those expressing TROP-2, such as various solid tumors including breast cancer. Etrumadenant is an oral, small molecule dual antagonist of the adenosine A2A and A2B receptors, which functions to reverse adenosine-mediated immunosuppression in the tumor microenvironment. Sacituzumab govitecan is an antibody-drug conjugate (ADC) composed of a humanized anti-TROP-2 monoclonal antibody conjugated to the cytotoxic topoisomerase I inhibitor SN-38 via a hydrolyzable linker, targeting and killing TROP-2-expressing tumor cells through internalization and DNA damage-induced apoptosis. The combination is being studied to exploit both immunomodulatory and direct cytotoxic mechanisms for enhanced anticancer efficacy[1].

Other names
sacituzumab govitecan-hziyhRS 7SN38hRS7SN38hRS-7SN38hRS7-SN38hRS-7-SN38hRS 7-SN38IMMU132IMMU-132IMMU 132
02

Targets

ADORA2B (Adenosine A2B receptor)TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)ADORA2A (Adenosine A₂A Receptor)

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