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]

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

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]