SR16388

SR16388 is a novel, orally active amino steroid developed by SRI International that functions as a multi-target antagonist of estrogen receptors (ER-α and ER-β) and the orphan nuclear receptor ERR-α. Preclinical studies have demonstrated its potent anti-proliferative and anti-angiogenic properties across various malignancies, including multiple myeloma, lung, prostate, and breast cancers. The drug's mechanism involves inducing cell cycle arrest at the G1 or G2 phase, promoting apoptosis, and triggering persistent macroautophagy. Additionally, SR16388 has been shown to inhibit the IL-6/STAT3 signaling pathway and reduce microvessel density in tumor xenografts. It reached Phase 1 clinical evaluation for advanced solid tumors, where its safety and pharmacokinetics were investigated.