Taragarestrant Explained

Cas Number:2118899-51-5
Pubchem:130330722
Chemspiderid:127404554
Unii:KD4HIM135V
Chembl:5087025
Synonyms:D-0502
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| C= 25| H= 25| Cl= 2| F= 1| N= 2| O= 2| molecular_weight = | 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| Jmol = | StdInChI = 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| StdInChI_comment = | StdInChIKey = PSJRZBBUWGIUPM-BBNFHIFMSA-N| density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }}

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. A phase III clinical trial has been initiated in China in patients with ER+/HER2- advanced or metastatic breast cancer.[2]

References

Notes and References

  1. Min J, Liu X, Peng R, Chen CC, Wang W, Guo RT . New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives . Acta Materia Medica . 3 . 1 . 57–71 . February 2024 . 39373009 . 11450757 . 10.15212/amm-2024-0006 .
  2. Web site: CTR20220511 . ((InventisBio, Co., Ltd.)) . chinadrugtrials.org.cn .