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

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Progesterone receptor (PGR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [6]
Desogestrel DM27U4Y Contraception QA21 Approved [7]
Ulipristal DMBNI20 Contraception QA21 Approved [8]
Etonogestrel DMKA8J4 Contraception QA21 Approved [9]
Megestrol DMDH9KX Breast cancer 2C60-2C65 Approved [10]
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [11]
Norgestimate DMYP4XC Acne vulgaris ED80 Approved [9]
Dydrogesterone DMAKIDV Menstrual disorder GA20.3 Approved [2]
Ethynodiol Diacetate DMZM84R Contraception QA21 Approved [12]
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [14]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [17]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [18]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [19]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [20]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [21]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [15]
Verapamil DMA7PEW Angina pectoris BA40 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [4]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [23]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [4]
Ifosfamide DMCT3I8 Adult central nervous system germ cell tumor Approved [23]
Sulfinpyrazone DMEV954 Gout FA25 Approved [24]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [4]
Zafirlukast DMHNQOG Asthma CA23 Approved [4]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [4]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [25]
Dabrafenib DMX6OE3 Melanoma 2C30 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Estrogen receptor (ESR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [28]
Gefitinib DM15F0X Colon adenocarcinoma Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [31]
Liraglutide DM3FXPS Non-insulin dependent diabetes 5A11 Approved [32]
Quercetin DM3NC4M Obesity 5B81 Approved [33]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [34]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [30]
Estrone DM5T6US Acne vulgaris ED80 Approved [35]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 2C8 (CYP2C8) OTHCWT42 CP2C8_HUMAN Gene/Protein Processing [4]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Drug Response [5]
Membrane progestin receptor alpha (mpra) OTEUBPKL MPRA_CYNNE Drug Response [5]

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 Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78.
5 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
6 Clinical pipeline report, company report or official report of lipocine.
7 Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40.
8 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
9 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
10 Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
11 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
12 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.
13 Met909 plays a key role in the activation of the progesterone receptor and also in the high potency of 13-ethyl progestins. Mol Pharmacol. 2009 Jun;75(6):1317-24.
14 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.
15 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
16 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.
17 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
18 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.
19 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.
20 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
21 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.
22 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.
23 Identification of the polymorphically expressed CYP2C19 and the wild-type CYP2C9-ILE359 allele as low-Km catalysts of cyclophosphamide and ifosfamide activation. Pharmacogenetics. 1997 Jun;7(3):211-21.
24 Essential requirements for substrate binding affinity and selectivity toward human CYP2 family enzymes. Arch Biochem Biophys. 2003 Jan 1;409(1):32-44.
25 Differential inhibition of human CYP2C8 and molecular docking interactions elicited by sorafenib and its major N-oxide metabolite. Chem Biol Interact. 2021 Apr 1;338:109401. doi: 10.1016/j.cbi.2021.109401. Epub 2021 Feb 5.
26 Dabrafenib inhibits ABCG2 and cytochrome P450 isoenzymes; potential implications for combination anticancer therapy. Toxicol Appl Pharmacol. 2022 Jan 1;434:115797. doi: 10.1016/j.taap.2021.115797. Epub 2021 Nov 13.
27 Estrogen-like activity of metals in MCF-7 breast cancer cells. Endocrinology. 2003 Jun;144(6):2425-36. doi: 10.1210/en.2002-221054.
28 Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens. Toxicol Appl Pharmacol. 2010 Jun 1;245(2):160-70. doi: 10.1016/j.taap.2010.02.015. Epub 2010 Mar 4.
29 Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth. Breast Cancer Res Treat. 2006 Mar;96(2):131-46. doi: 10.1007/s10549-005-9070-2. Epub 2005 Oct 27.
30 Sensitivity of human dental pulp cells to eighteen chemical agents used for endodontic treatments in dentistry. Odontology. 2013 Jan;101(1):43-51.
31 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
32 Antitumoral activity of liraglutide, a new DNMT inhibitor in breast cancer cells in vitro and in vivo. Chem Biol Interact. 2021 Nov 1;349:109641. doi: 10.1016/j.cbi.2021.109641. Epub 2021 Sep 14.
33 Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on human breast cancer cells. Mol Pharmacol. 2001 Sep;60(3):595-602.
34 Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth. Br J Cancer. 2007 Apr 23;96(8):1204-15. doi: 10.1038/sj.bjc.6603705. Epub 2007 Mar 27.
35 Prediction of the combined effects of multiple estrogenic chemicals on MCF-7 human breast cancer cells and a preliminary molecular exploration of the estrogenic proliferative effects and related gene expression. Ecotoxicol Environ Saf. 2018 Sep 30;160:1-9. doi: 10.1016/j.ecoenv.2018.05.025. Epub 2018 May 21.