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

General Information of Drug (ID: DMBGWPH)

• Drug Name: Medroxyprogesterone Drug Info
• Synonyms: Asconale; Colirest; Hematrol; Hydroxymethylprogesterone; Lunelle; Medrossiprogesterone; Medroxiprogesterona; Medroxiprogesteronum; Medroxyprogesteron; Medroxyprogesteronum; Methylhydroxyprogesterone; Adgyn Medro; Farlutal inyectable; Medroprogesterone Acetate; Medrossiprogesterone [DCIT]; Medroxyprogesteron acetate; Medroxyprogesterone Strakan Brand; Sodelut G; Strakan Brand of Medroxyprogesterone; MPA Gyn 5; U 8840; CBP-1011; Farlutal inyectable (TN); G-Farlutal; Medroxiprogesterona [INN-Spanish]; Medroxyprogesterone (INN); Medroxyprogesterone [INN:BAN]; Medroxyprogesteronum [INN-Latin]; Novo-Medrone; Pregn-4-ene-3,20-dione, 17-hydroxy-6-methyl-, (6alpha)-(9CI); Pregn-4-ene-3,20-dione, 17-hydroxy-6-methyl-, (6-alpha)-(9CI); (6S,8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one; (6alpha)-17-hydroxy-6-methylpregn-4-ene-3,20-dione; 17 alpha Hydroxy 6 alpha Methylprogesterone; 17 alpha-Hydroxy-6 alpha-Methylprogesterone; 17-Hydroxy-6.alpha.-methylprogesterone; 17-Hydroxy-6alpha-methyl-pregn-4-ene-3,20-dione; 17-Hydroxy-6alpha-methylprogesterone; 17.alpha.-Hydroxy-6.alpha.-methylprogesterone; 17alpha-Hydroxy-6alpha-methyl-4-pregnene-3,20-dione; 17alpha-Hydroxy-6alpha-methylprogesterone; 6-Dihydromegestrol; 6-alpha-Methyl-17-alpha-hydroxyprogesterone; 6.alpha.-Methyl-17.alpha.-hydroxyprogesterone; 6alpha-Methyl-17alpha-hydroxyprogesterone; 6alpha-Methyl-4-pregnen-17alpha-ol-3,20-dione; 6alpha-Methyl-5-pregnen-17alpha-ol-3,20-dione

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Approved	[1]

• Therapeutic Class: Contraceptive Agents
• Cross-matching ID:
  PubChem CID: 10631
  ChEBI ID: CHEBI:6715
  CAS Number: CAS 520-85-4
  TTD Drug ID: DMBGWPH
  INTEDE Drug ID: DR1012

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	[4]
Progesterone	DMUY35B	Premature labour	JB00	Approved	[5]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[6]
Estradiol	DMUNTE3	Breast cancer	2C60-2C65	Approved	[7]
Acetaminophen	DMUIE76	Pain	MG30-MG3Z	Approved	[8]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[9]
Etoposide	DMNH3PG	Solid tumour/cancer	2A00-2F9Z	Approved	[10]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[11]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[5]
Verapamil	DMA7PEW	Hypertension	BA00-BA04	Approved	[12]

Drug(s) Targeting Progesterone receptor (PGR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Progesterone	DMUY35B	Premature labour	JB00	Approved	[13]
Desogestrel	DM27U4Y	Contraception	QA21	Approved	[14]
Ulipristal	DMBNI20	Contraception	QA21	Approved	[15]
Etonogestrel	DMKA8J4	Contraception	QA21	Approved	[16]
Megestrol	DMDH9KX	Breast cancer	2C60-2C65	Approved	[17]
Segesterone acetate; ethinyl estradiol	DMFEGB0	Contraception	QA21	Approved	[18]
Norgestimate	DMYP4XC	Contraception	QA21	Approved	[16]
Dydrogesterone	DMAKIDV	Menstrual disorder	GA20.3	Approved	[2]
Ethynodiol diacetate	DMZM84R	Contraception	QA21	Approved	[19]
Estradiol valerate/dienogest	DMLNMEA	Discovery agent	N.A.	Approved	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Progesterone receptor (PGR)	TTUV8G9	PRGR_HUMAN	Agonist	[2]

Drug-Metabolizing Enzyme (DME)

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

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [2] Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharm... Steroids. 2008 Feb;73(2):222-31.
• [3] Metabolic profiling and cytochrome P450 reaction phenotyping of medroxyprogesterone acetate. Drug Metab Dispos. 2008 Nov;36(11):2292-8.
• [4] 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.
• [5] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [6] 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.
• [7] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [8] 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.
• [9] 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.
• [10] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [11] 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.
• [12] 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.
• [13] Clinical pipeline report, company report or official report of lipocine.
• [14] Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40.
• [15] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [16] Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
• [17] Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
• [18] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [19] Contribution of functional groups of 19-nor-progestogens to binding to progesterone and estradiol-17beta receptors in rabbit uterus. Endocrinology. 1977 Jun;100(6):1579-84.