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

General Information of Drug (ID: DMQZ9GF)

• Drug Name: Trilostane Drug Info
• Synonyms: Desopan; Desopan (TN); Modrenal (TN); Vetoryl (TN); Vetoryl, Trilostane; Win-24540; Trilostane (JAN/USAN); (4alpha,5alpha,17beta)-3,17-dihydroxy-4,5-epoxyandrost-2-ene-2-carbonitrile; 3,17beta-dihydroxy-4alpha,5-epoxy-5alpha-androst-2-ene-2-carbonitrile

Indication

Disease Entry	ICD 11	Status	REF
Cushing disease	5A70	Approved	[1] , [2]

• Cross-matching ID:
  PubChem CID: 656583
  ChEBI ID: CHEBI:32260
  CAS Number: CAS 13647-35-3
  TTD Drug ID: DMQZ9GF
  INTEDE Drug ID: DR1645

Molecule-Related Drug Atlas

Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Solid tumour/cancer	2A00-2F9Z	Approved	[5]
Progesterone	DMUY35B	Premature labour	JB00	Approved	[6]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[7]
Estradiol	DMUNTE3	Breast cancer	2C60-2C65	Approved	[8]
Acetaminophen	DMUIE76	Pain	MG30-MG3Z	Approved	[9]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[10]
Etoposide	DMNH3PG	Solid tumour/cancer	2A00-2F9Z	Approved	[11]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[12]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[6]
Verapamil	DMA7PEW	Hypertension	BA00-BA04	Approved	[13]

Drug(s) Targeting Estrogen receptor beta (ESR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Conjugated estrogens	DMLT0E1	Menopause symptom	GA30.0	Approved	[14]
ARZOXIFENE	DMOKCVI	Breast cancer	2C60-2C65	Approved	[15]
Estrogen	DMGY0UT	Menopause symptom	GA30.0	Approved	[16]
Premarin/Pravachol	DMLSOB7	Hyperlipidaemia	5C80	Phase 3	[17]
MF-101	DM8Z0I3	Hepatitis virus infection	1E50-1E51	Phase 3	[18]
Genistein	DM0JETC	Menopause symptom	GA30.0	Phase 2/3	[19]
AUS-131	DMZMSQJ	Hot flushes	GA30	Phase 2	[20]
ERB-041	DMCEPUA	Inflammatory bowel disease	DD72	Phase 2	[21]
Erteberel	DMU1XZD	Prostate hyperplasia	GA90	Phase 2	[22]
VG-101	DMAN21O	Menopause symptom	GA30.0	Phase 1/2	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor beta (ESR2)	TTOM3J0	ESR2_HUMAN	Modulator	[3]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[4]

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: 6850).
• [2] FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018719.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Long-term low-dose ketoconazole treatment in bilateral macronodular adrenal hyperplasia. Endocrinol Diabetes Metab Case Rep. 2014;2014:140083.
• [5] Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
• [6] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [7] Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
• [8] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [9] Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
• [10] Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
• [11] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [12] The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
• [13] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
• [14] Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
• [15] Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007 May 31;50(11):2682-92.
• [16] Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6.
• [17] Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.
• [18] MF101, a selective estrogen receptor beta modulator for the treatment of menopausal hot flushes: a phase II clinical trial. Menopause. 2009 May-Jun;16(3):458-65.
• [19] Company report (Axcentua)
• [20] S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
• [21] Erb-041, an estrogen receptor-beta agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
• [22] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
• [23] Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.