Details of the Drug

General Information of Drug (ID: DMBSFFK)

Drug Name

Giredestrant

Synonyms

Giredestrant; 1953133-47-5; GDC-9545; RO7197597; Giredestrant [INN]; Giredestrant [USAN]; RO-7197597; 28P3DU6DB3; GDC9545; 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol; 3-((1R,3R)-1-(2,6-Difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido(3,4-b)indol-2-yl)-2,2-difluoropropan-1-ol; 3-((1R,3R)-1-(2,6-Difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol; 3-[(1R,3R)-1-(2,6-difluoro-4-{[1-(3-fluoropropyl)azetidin-3-yl]amino}phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol; Giredestrant [USAN:INN]; UNII-28P3DU6DB3; GIREDESTRANT [WHO-DD]; CHEMBL4650316; SCHEMBL17839430; GTPL12715; EX-A3541; BDBM50572808; NSC827275; RG6171; WHO 11226; AKOS040733254; AT22918; NSC-827275; RG-6171; compound 35 [PMID: 34251202]; AC-37111; MS-29682; HY-109176; CS-0116370; (1R,3R)-1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)-3-AZETIDINYL)AMINO)PHENYL)-.BETA.,.BETA.-DIFLUORO-1,3,4,9-TETRAHYDRO-3-METHYL-2H-PYRIDO(3,4-B)INDOLE-2-PROPANOL; 2H-PYRIDO(3,4-B)INDOLE-2-PROPANOL, 1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)-3-AZETIDINYL)AMINO)PHENYL)-.BETA.,.BETA.-DIFLUORO-1,3,4,9-TETRAHYDRO-3-METHYL-, (1R,3R)-; 2H-Pyrido(3,4-b)indole-2-propanol, 1-(2,6-difluoro-4-((1-(3-fluoropropyl)-3-azetidinyl)amino)phenyl)-beta,beta-difluoro-1,3,4,9-tetrahydro-3-methyl-, (1R,3R)-; 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-2,2-difluoropropan-1-ol; 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoro-propan-1-ol; ZNM

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 3	[1]
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Drug Type

Small molecule

Structure

3D MOL

2D MOL

Chemical Identifiers

Formula: C27H31F5N4O
Canonical SMILES: CC1CC2=C(C(N1CC(CO)(F)F)C3=C(C=C(C=C3F)NC4CN(C4)CCCF)F)NC5=CC=CC=C25
InChI: InChI=1S/C27H31F5N4O/c1-16-9-20-19-5-2-3-6-23(19)34-25(20)26(36(16)14-27(31,32)15-37)24-21(29)10-17(11-22(24)30)33-18-12-35(13-18)8-4-7-28/h2-3,5-6,10-11,16,18,26,33-34,37H,4,7-9,12-15H2,1H3/t16-,26-/m1/s1
InChIKey: GQCXHIKRWBIQMD-AKJBCIBTSA-N

Cross-matching ID

PubChem CID: 121410806
TTD ID: DGW9U7

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_HUMAN	Degrader	[2]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

References

1	ClinicalTrials.gov (NCT04961996) A Phase III, Randomized, Open-Label, Multicenter Study Evaluating the Efficacy and Safety of Adjuvant Giredestrant Compared With Physician's Choice of Adjuvant Endocrine Monotherapy in Patients With Estrogen Receptor-Positive, HER2-Negative Early Breast Cancer. U.S.National Institutes of Health.
2	GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer. J Med Chem. 2021 Aug 26;64(16):11841-11856.