Chemistry:Rintodestrant
From HandWiki
Rintodestrant (G1T48) is an orally bioavailable selective estrogen receptor degrader (SERD) discovered in Greg Thatcher's lab at UIC[1] and developed by G1 Therapeutics for the treatment of estrogen receptor-positive (ER+) breast cancer[2]. Structurally inspired by the 6-OH-benzothiophene scaffold used in arzoxifene and raloxifene, rintodestrant selectively binds to the estrogen receptor and inhibits ER signaling, demonstrating efficacy in endocrine-resistant tumors.[3]
A phase I clinical trial evaluated rintodestrant as monotherapy and in combination with the CDK4/6 inhibitor palbociclib in patients with ER+/HER2- advanced breast cancer.[4]
References
- ↑ "Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer". Journal of Medicinal Chemistry 60 (4): 1325–1342. February 2017. doi:10.1021/acs.jmedchem.6b01355. PMID 28117994.
- ↑ "G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer". Breast Cancer Research and Treatment 180 (3): 635–646. April 2020. doi:10.1007/s10549-020-05575-9. PMID 32130619.
- ↑ "Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review". Cancer Treatment Reviews 130. November 2024. doi:10.1016/j.ctrv.2024.102825. PMID 39293125.
- ↑ Clinical trial number NCT03455270 for "G1T48, an Oral SERD, Alone and in Combination With Palbociclib in ER-Positive, HER2-Negative Advanced Breast Cancer" at ClinicalTrials.gov
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