Chemistry:Taragarestrant
Taragarestrant is an orally bioavailable selective estrogen receptor degrader (SERD) developed by Inventis Bio for the treatment of estrogen receptor-positive (ER+) breast cancer. Structurally similar to AZD9496, taragarestrant has demonstrated potent efficacy across multiple breast cancer cell lines expressing ER and related xenograft models. In preclinical studies, taragarestrant exhibited anti-tumor activity, warranting further clinical investigation.[1]
A phase I study (NCT03471663) evaluated taragarestrant in females with ER+/HER2- advanced or metastatic breast cancer, both as monotherapy and in combination with the CDK4/6 inhibitor palbociclib.[2] A phase III clinical trial has been initiated in China in patients with ER+/HER2- advanced or metastatic breast cancer.[3]
References
- ↑ "New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives". Acta Materia Medica 3 (1): 57–71. February 2024. doi:10.15212/amm-2024-0006. PMID 39373009.
- ↑ Clinical trial number NCT03471663 at ClinicalTrials.gov
- ↑ "CTR20220511". chinadrugtrials.org.cn. http://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml?id=e3cb0588dc6242c99b99dad105dcfc06.
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