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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.
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