Drug intelligence / Profile preview

SHR-1049

Development stage
Phase 1
Lead developer
Hengrui Pharmaceutical
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

SHR-1049 is an investigational antibody-drug conjugate (ADC) developed by HengRui Medicine, targeting Trophoblast cell-surface antigen 2 (TROP2). TROP2 is a transmembrane glycoprotein overexpressed in various epithelial cancers, including breast, lung, and gastric cancers, where it promotes tumor cell proliferation and survival. SHR-1049 consists of a humanized anti-TROP2 monoclonal antibody conjugated to a cytotoxic payload, typically a topoisomerase I inhibitor, via a linker. Upon binding to TROP2 on the tumor cell surface, the ADC is internalized via endocytosis, and the payload is released within the lysosomal compartment, leading to DNA damage and subsequent apoptosis. SHR-1049 is currently being evaluated in Phase 1 clinical trials for patients with advanced solid tumors.

02

Targets

TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)

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