{{Short description|Chemical compound}} {{cs1 config|name-list-style=vanc|display-authors=6}} {{Infobox drug | drug_name = | INN = | type = <!-- empty --> | image = Taragarestrant.svg | image_class = skin-invert-image | width = | alt = | caption = | image2 = | width2 = | alt2 = | caption2 = | imageL = | widthL = | altL = | imageR = | widthR = | altR = | captionLR =
<!-- Clinical data --> | pronounce = | tradename = | Drugs.com = | MedlinePlus = | licence_CA = <!-- Health Canada may use generic or brand name (generic name preferred) --> | licence_EU = <!-- EMA uses INN (or special INN_EMA) --> | DailyMedID = <!-- DailyMed may use generic or brand name (generic name preferred) --> | licence_US = <!-- FDA may use generic or brand name (generic name preferred) --> | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU_comment = | pregnancy_category= | dependency_liability = | addiction_liability = | routes_of_administration = | class = | ATCvet = | ATC_prefix = <!-- 'none' if uncategorised --> | ATC_suffix = | ATC_supplemental =
<!-- Legal status --> | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> | legal_AU_comment = | legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C5, D1, D2, E, F1, F2, F3, F4 --> | legal_BR_comment = | legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> | legal_CA_comment = | legal_DE = <!-- Anlage I, II, III or Unscheduled --> | legal_DE_comment = | legal_NZ = <!-- Class A, B, C --> | legal_NZ_comment = | legal_UK = <!-- GSL, P, POM, CD, CD Lic, CD POM, CD No Reg POM, CD (Benz) POM, CD (Anab) POM or CD Inv POM / Class A, B, C --> | legal_UK_comment = | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> | legal_US_comment = | legal_EU = | legal_EU_comment = | legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> | legal_UN_comment = | legal_status = <!-- For countries not listed above -->
<!-- Pharmacokinetic data --> | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action= | excretion =
<!-- Identifiers --> | CAS_number = 2118899-51-5 | CAS_supplemental = | PubChem = 130330722 | PubChemSubstance = | IUPHAR_ligand = | DrugBank = | ChemSpiderID = 127404554 | UNII = KD4HIM135V | KEGG = | ChEBI = | ChEMBL = 5087025 | NIAID_ChemDB = | PDB_ligand = | synonyms = D-0502
<!-- Chemical and physical data --> | IUPAC_name = <nowiki>(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</nowiki> | 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.<ref name="Min_2024">{{cite journal | vauthors = Min J, Liu X, Peng R, Chen CC, Wang W, Guo RT | title = New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives | journal = Acta Materia Medica | volume = 3 | issue = 1 | pages = 57–71 | date = February 2024 | pmid = 39373009 | pmc = 11450757 | doi = 10.15212/amm-2024-0006 }}</ref>
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.<ref>{{ClinicalTrialsGov|NCT03471663}}</ref> A phase III clinical trial has been initiated in China in patients with ER+/HER2- advanced or metastatic breast cancer.<ref>{{cite web | title = CTR20220511 |author=((InventisBio, Co., Ltd)) | work = chinadrugtrials.org.cn | url = http://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml?id=e3cb0588dc6242c99b99dad105dcfc06}}{{dead link|date=February 2026}}</ref>
== References == {{Reflist}}
{{Estrogen receptor modulators}} {{Tryptamines}}
Category:Antineoplastic drugs Category:Chlorobenzene derivatives Category:Enoic acids Category:Organofluorides Category:Selective estrogen receptor degraders Category:Tryptolines
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