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

General Information of Drug (ID: DM3C5GZ)

• Drug Name: FADROZOLE Drug Info
• Synonyms: 102676-47-1; CGS-16949A; Fadrozole [INN]; Fadrozolum [INN-Latin]; Fadrozol [INN-Spanish]; CHEMBL9298; Fadrozole (INN); 5-p-cyanophenyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine; Benzonitrile, 4-(5,6,7,8-tetrahydroimidazo(1,5-a)pyridin-5-yl)-; Fadrozolum; Fadrozol; 4-{5H,6H,7H,8H-imidazo[1,5-a]pyridin-5-yl}benzonitrile; Benzonitrile, 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[1] , [2] , [3]

• Cross-matching ID:
  PubChem CID: 59693
  ChEBI ID: CHEBI:94355
  CAS Number: CAS 102676-47-1
  TTD Drug ID: DM3C5GZ

Molecule-Related Drug Atlas

Drug(s) Targeting Aromatase (CYP19A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Anastrozole	DMNP60F	Breast cancer	2C60-2C65	Approved	[6]
Letrozole	DMH07Y3	Hormonally-responsive breast cancer	2C60-2C65	Approved	[7]
Exemestane	DM9HPW3	Hormonally-responsive breast cancer	2C60-2C65	Approved	[7]
Aminoglutethimide	DMWFHMZ	Cushing disease	5A70	Approved	[8]
Testolactone	DMVY4GN	Breast cancer	2C60-2C65	Approved	[9]
Atamestane + Toremifene	DM3QLK2	Breast cancer	2C60-2C65	Phase 3	[10]
LIAROZOLE	DM4OYXE	Dermatological disease	DA24.Y	Phase 2/3	[11]
Coumate	DMVKW0N	Breast cancer	2C60-2C65	Phase 2	[12]
Dextromethorphan+quinidine	DMFI5J4	Diabetic neuropathy	8C0Z	Phase 2	[13]
BGS-649	DMO4MNQ	Endometriosis	GA10	Phase 2	[14]

Drug(s) Targeting Steroid 11-beta-hydroxylase (CYP11B1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Osilodrostat	DMIJC9X	Cushing disease	5A70	Approved	[15]
Metyrapone	DMI7FVQ	Cushing disease	5A70	Approved	[16]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol	DM6Z5EK	Discovery agent	N.A.	Investigative	[17]
4-Indan-(1Z)-ylidenemethyl-pyridine	DM25DR7	Discovery agent	N.A.	Investigative	[18]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine	DMIEMWA	Discovery agent	N.A.	Investigative	[17]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine	DMY08FE	Discovery agent	N.A.	Investigative	[18]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine	DM2RIHT	Discovery agent	N.A.	Investigative	[18]
4-((1H-imidazol-1-yl)methyl)benzonitrile	DMFUBRC	Discovery agent	N.A.	Investigative	[5]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine	DMHDZUO	Discovery agent	N.A.	Investigative	[18]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine	DMQKHXN	Discovery agent	N.A.	Investigative	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aromatase (CYP19A1)	TTSZLWK	CP19A_HUMAN	Inhibitor	[4]
Steroid 11-beta-hydroxylase (CYP11B1)	TTIQUX7	C11B1_HUMAN	Inhibitor	[5]

References

• [1] 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. (Ligand id: 8311).
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [3] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000824)
• [4] Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach. J Med Chem. 2005 Nov 17;48(23):7282-9.
• [5] Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2). J Med Chem. 2010 Feb 25;53(4):1712-25.
• [6] Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. J Pediatr Endocrinol Metab. 2002;15 Suppl 3:945-8.
• [7] Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51.
• [8] Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chem Res Toxicol. 2007 Jul;20(7):1038-45.
• [9] Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9.
• [10] Toremifene-atamestane; alone or in combination: predictions from the preclinical intratumoral aromatase model. J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):1-7.
• [11] Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64.
• [12] Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. J Med Chem. 2010 Mar 11;53(5):2155-70.
• [13] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [14] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032111)
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [16] Effects of 3-MeSO2-DDE and some CYP inhibitors on glucocorticoid steroidogenesis in the H295R human adrenocortical carcinoma cell line. Toxicol In Vitro. 2002 Apr;16(2):113-21.
• [17] Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prosta... J Med Chem. 2010 Aug 12;53(15):5749-58.
• [18] Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitor... J Med Chem. 2005 Mar 10;48(5):1563-75.