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

General Information of Drug (ID: DMDH9KX)

Drug Name
Megestrol Drug Info
Synonyms
Chronopil; Megestrolo; Megestrolo [DCIT]; Chronopil (TN); Megace (TN); Megestrol (INN); Megestrol [INN:BAN]; Megestrolum [INN-Latin]; (8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one; 17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
19090
CAS Number
CAS 3562-63-8
TTD Drug ID
DMDH9KX
INTEDE Drug ID
DR1017

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Download the Complete Related Drug List
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]
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [10]
Norgestimate DMYP4XC Acne vulgaris ED80 Approved [9]
Dydrogesterone DMAKIDV Menstrual disorder GA20.3 Approved [11]
Medroxyprogesterone DMBGWPH Solid tumour/cancer 2A00-2F9Z Approved [11]
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 Nuclear receptor subfamily 1 group I member 2 (NR1I2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Vidarabine DM0N85H Hepatosplenic T-cell lymphoma Approved [23]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [24]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [25]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [5]
Etidronic acid DM1XHYJ Bone Paget disease Approved [23]
Tiaprofenic acid DM23D7J Osteoarthritis FA00-FA05 Approved [23]
Bromperidol DM24XYQ Schizophrenia 6A20 Approved [23]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [26]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [27]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Metalloproteinase inhibitor 1 (TIMP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pentoxifylline DMU3DNC Alcoholic hepatitis DB94.1 Approved [28]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Selenium DM25CGV N. A. N. A. Approved [30]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [4]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [32]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [33]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [34]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [35]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Proto-oncogene tyrosine-protein kinase receptor Ret (RET)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [36]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [4]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Irbesartan DMTP1DC Diabetic kidney disease GB61.Z Approved [38]
Estrone DM5T6US Acne vulgaris ED80 Approved [36]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [4]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [39]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [40]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [41]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Clusterin (CLU)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Selenium DM25CGV N. A. N. A. Approved [42]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [4]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [43]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [44]
Panobinostat DM58WKG Chronic graft versus host disease Approved [45]
Levamisole DM5EN79 Parasitic infection 1D0Y-1G2Z Approved [46]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [47]
Testosterone DM7HUNW Hot flushes GA30 Approved [48]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [4]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Neuromodulin (GAP43)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [4]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [49]
Panobinostat DM58WKG Chronic graft versus host disease Approved [45]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [50]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [4]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [40]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [51]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [52]
Scopolamine DMOM8AL Addictive disorder 6C50-6C5Z Approved [53]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Galanin peptides (GAL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [4]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [54]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [4]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [55]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [56]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [57]
Testosterone DM7HUNW Hot flushes GA30 Approved [58]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [4]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [58]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [59]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Binder [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
Clusterin (CLU) OTQGG0JM CLUS_HUMAN Gene/Protein Processing [4]
Galanin peptides (GAL) OTB3VPTO GALA_HUMAN Gene/Protein Processing [4]
Metalloproteinase inhibitor 1 (TIMP1) OTOXC51H TIMP1_HUMAN Gene/Protein Processing [4]
Neuromodulin (GAP43) OT2OTGGV NEUM_HUMAN Gene/Protein Processing [4]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Gene/Protein Processing [5]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET) OTLU040A RET_HUMAN Gene/Protein Processing [4]

References

1 Hormonal therapy in epithelial ovarian cancer. Expert Rev Anticancer Ther. 2006 Jan;6(1):43-7.
2 Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
3 Metabolism of megestrol acetate in vitro and the role of oxidative metabolites. Xenobiotica. 2018 Oct;48(10):973-983.
4 Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arrays. Physiol Genomics. 2002 Oct 29;11(2):45-52. doi: 10.1152/physiolgenomics.00064.2002.
5 Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening. Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10.
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 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
11 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.
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 Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. Toxicol Lett. 2015 Jan 5;232(1):193-202. doi: 10.1016/j.toxlet.2014.10.009. Epub 2014 Oct 16.
24 Induction of PXR-mediated metabolism by beta-carotene. Biochim Biophys Acta. 2005 May 30;1740(2):162-9. doi: 10.1016/j.bbadis.2004.11.013. Epub 2004 Dec 8.
25 Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR). Toxicol Appl Pharmacol. 2005 Dec 1;209(2):123-33. doi: 10.1016/j.taap.2005.03.015.
26 Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
27 Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor. Toxicol Lett. 2017 Jan 4;265:86-96.
28 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.
29 Cannabidiol inhibits lung cancer cell invasion and metastasis via intercellular adhesion molecule-1. FASEB J. 2012 Apr;26(4):1535-48. doi: 10.1096/fj.11-198184. Epub 2011 Dec 23.
30 Inhibition of invasion and induction of apoptosis by selenium in human malignant brain tumour cells in vitro. Int J Oncol. 2007 May;30(5):1263-71.
31 Dietary supplementation with the anti-tumour promoter quercetin: its effects on matrix metalloproteinase gene regulation. Mutat Res. 2001 Sep 1;480-481:269-76. doi: 10.1016/s0027-5107(01)00184-1.
32 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
33 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
34 Arsenic trioxide (As2O3) inhibits invasion of HT1080 human fibrosarcoma cells: role of nuclear factor-kappaB and reactive oxygen species. J Cell Biochem. 2005 Aug 1;95(5):955-69. doi: 10.1002/jcb.20452.
35 Aspirin inhibits MMP-2 and MMP-9 expressions and activities through upregulation of PPARalpha/gamma and TIMP gene expressions in ox-LDL-stimulated macrophages derived from human monocytes. Pharmacology. 2009;83(1):18-25. doi: 10.1159/000166183. Epub 2008 Oct 30.
36 Moving toward integrating gene expression profiling into high-throughput testing: a gene expression biomarker accurately predicts estrogen receptor alpha modulation in a microarray compendium. Toxicol Sci. 2016 May;151(1):88-103.
37 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
38 Hypotensive shock and angio-oedema from angiotensin II receptor blocker: a class effect in spite of tripled tryptase values. J Intern Med. 2005 Oct;258(4):385-7. doi: 10.1111/j.1365-2796.2005.01547.x.
39 Dual inhibition of RET and FGFR4 restrains medullary thyroid cancer cell growth. Clin Cancer Res. 2005 Feb 1;11(3):1336-41.
40 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
41 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
42 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
43 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
44 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
45 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
46 Levamisole induced apoptosis in cultured vascular endothelial cells. Br J Pharmacol. 2000 Dec;131(8):1577-83.
47 Chronic occupational exposure to arsenic induces carcinogenic gene signaling networks and neoplastic transformation in human lung epithelial cells. Toxicol Appl Pharmacol. 2012 Jun 1;261(2):204-16.
48 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
49 Arsenic trioxide inhibits neuroblastoma growth in vivo and promotes apoptotic cell death in vitro. Biochem Biophys Res Commun. 2000 Oct 14;277(1):179-85. doi: 10.1006/bbrc.2000.3651.
50 Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
51 Lovastatin induces neuronal differentiation and apoptosis of embryonal carcinoma and neuroblastoma cells: enhanced differentiation and apoptosis in combination with dbcAMP. Mol Cell Biochem. 2010 Dec;345(1-2):1-11. doi: 10.1007/s11010-010-0553-z. Epub 2010 Aug 9.
52 The neuroprotective action of the mood stabilizing drugs lithium chloride and sodium valproate is mediated through the up-regulation of the homeodomain protein Six1. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):124-34.
53 Protective role of Ashwagandha leaf extract and its component withanone on scopolamine-induced changes in the brain and brain-derived cells. PLoS One. 2011;6(11):e27265. doi: 10.1371/journal.pone.0027265. Epub 2011 Nov 11.
54 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
55 Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
56 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
57 JunD is involved in the antiproliferative effect of Delta9-tetrahydrocannabinol on human breast cancer cells. Oncogene. 2008 Aug 28;27(37):5033-44.
58 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
59 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.