Taragarestrant

Taragarestrant
Clinical data
Other names	D-0502
Identifiers
	IUPAC name (E)-3-[3,5-dichloro-4-[(1R,3R)-2-(2-fluoro-2-methyl-propyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid;
CAS Number	2118899-51-5;
PubChem CID	130330722;
ChemSpider	127404554;
UNII	KD4HIM135V;
ChEMBL	ChEMBL5087025;
Chemical and physical data
Formula	C25H25Cl2FN2O2
Molar mass	475.39 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H]1CC2=C([C@H](N1CC(C)(C)F)C3=C(C=C(C=C3Cl)/C=C/C(=O)O)Cl)NC4=CC=CC=C24;
	InChI InChI=InChI=1S/C25H25Cl2FN2O2/c1-14-10-17-16-6-4-5-7-20(16)29-23(17)24(30(14)13-25(2,3)28)22-18(26)11-15(12-19(22)27)8-9-21(31)32/h4-9,11-12,14,24,29H,10,13H2,1-3H3,(H,31,32)/b9-8+/t14-,24-/m1/s1; Key:PSJRZBBUWGIUPM-BBNFHIFMSA-N;

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

^ Min J, Liu X, Peng R, Chen CC, Wang W, Guo RT (February 2024). "New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives". Acta Materia Medica. 3 (1): 57–71. doi:10.15212/amm-2024-0006. PMC 11450757. PMID 39373009.
^ Clinical trial number NCT03471663 at ClinicalTrials.gov
^ InventisBio, Co., Ltd. "CTR20220511". chinadrugtrials.org.cn.

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[Min_2024-1] Min J, Liu X, Peng R, Chen CC, Wang W, Guo RT (February 2024). "New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives". Acta Materia Medica. 3 (1): 57–71. doi:10.15212/amm-2024-0006. PMC 11450757. PMID 39373009.

[2] Clinical trial number NCT03471663 at ClinicalTrials.gov

[3] InventisBio, Co., Ltd. "CTR20220511". chinadrugtrials.org.cn.

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