Drug intelligence / Profile preview

sacituzumab govitecan + rezvilutamide

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

Overview

A1:SG + SHR3680 is a combination therapy being evaluated in the Future-Trop2 umbrella trial for the first-line treatment of locally advanced or metastatic triple-negative breast cancer (TNBC), specifically targeting the luminal androgen receptor (LAR) subtype. The combination consists of sacituzumab govitecan, a TROP-2-directed antibody-drug conjugate (ADC) carrying an SN-38 payload, and rezvilutamide (SHR3680), a second-generation small molecule androgen receptor (AR) antagonist. This precision medicine approach aims to leverage the high expression of TROP-2 in TNBC while simultaneously inhibiting the androgen signaling pathway that drives the LAR subtype. Sacituzumab govitecan provides targeted delivery of a cytotoxic topoisomerase I inhibitor, while rezvilutamide blocks the growth-promoting effects of androgens in AR-positive breast cancer cells.

Brand names
TrodelvyAiruijie
Other names
sacituzumab govitecan + SHR3680SG + SHR3680
02

Targets

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

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