Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMBSFFK)

• Drug Name: Giredestrant Drug Info
• 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]

• Cross-matching ID:
  PubChem CID: 121410806
  TTD Drug ID: DMBSFFK

Molecule-Related Drug Atlas

Drug(s) Targeting Estrogen receptor (ESR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[3]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[4]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[4]
Estradiol Valerate	DM8MC6O	Hormone replacement therapy	8E01	Approved	[5]
Estradiol Acetate	DM07U2A	Hormone replacement therapy	8E01	Approved	[5]
Estradiol Cypionate	DM27Z5T	Hormone replacement therapy	8E01	Approved	[5]
Ethinyl Estradiol	DMODJ40	Acne vulgaris	ED80	Approved	[6]
Raloxifene	DMDKF3M	Osteoporosis	FB83.0	Approved	[7]
Ospemifene	DMC4GEI	Dyspareunia	GA12	Approved	[8]
Toremifene	DMQYUWG	Breast cancer	2C60-2C65	Approved	[9]

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]

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.
• [3] Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause. Recent Pat Cardiovasc Drug Discov. 2008 Nov;3(3):165-86.
• [4] Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
• [7] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 620).
• [8] Clinical pipeline report, company report or official report of Shionogi (2011).
• [9] Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithe... Prostate Cancer Prostatic Dis. 2009;12(4):375-81.