General Information of Drug (ID: DMWLFGO)

Drug Name
Methyltestosterone
Synonyms Android (TN)
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Approved [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 302.5
Topological Polar Surface Area (xlogp) 3.4
Rotatable Bond Count (rotbonds) 0
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
Elimination
The elimination of drug is 90% via urine and 10% via feces [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 6 - 8 hours [4]
Metabolism
The drug is metabolized via the hepatic [5]
Chemical Identifiers
Formula
C20H30O2
IUPAC Name
(8R,9S,10R,13S,14S,17S)-17-hydroxy-10,13,17-trimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
Canonical SMILES
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(C)O)C
InChI
InChI=1S/C20H30O2/c1-18-9-6-14(21)12-13(18)4-5-15-16(18)7-10-19(2)17(15)8-11-20(19,3)22/h12,15-17,22H,4-11H2,1-3H3/t15-,16+,17+,18+,19+,20+/m1/s1
InChIKey
GCKMFJBGXUYNAG-HLXURNFRSA-N
Cross-matching ID
PubChem CID
6010
ChEBI ID
CHEBI:27436
CAS Number
58-18-4
DrugBank ID
DB06710
TTD ID
D0Z1XD
INTEDE ID
DR1064
ACDINA ID
D00421

Molecular Interaction Atlas of This Drug


Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [6]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [6]
UDP-glucuronosyltransferase 2A1 (UGT2A1) DEGKRXT UD2A1_HUMAN Substrate [7]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Methyltestosterone (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [27]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [28]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Methyltestosterone and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [29]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Cannabidiol. Epileptic encephalopathy [8A62] [30]
Brentuximab vedotin DMWLC57 Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Brentuximab vedotin. Hodgkin lymphoma [2B30] [31]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Methyltestosterone and Teriflunomide. Hyper-lipoproteinaemia [5C80] [32]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Methyltestosterone and BMS-201038. Hyper-lipoproteinaemia [5C80] [33]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [34]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Methyltestosterone and Idelalisib. Mature B-cell leukaemia [2A82] [35]
Carfilzomib DM48K0X Major Additive thrombogenic effects by the combination of Methyltestosterone and Carfilzomib. Multiple myeloma [2A83] [27]
Insulin degludec DMPL395 Moderate Increased risk of hypoglycemia by the combination of Methyltestosterone and Insulin degludec. Type-1/2 diabete [5A10-5A11] [36]
⏷ Show the Full List of 11 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Allura red AC dye E00338 33258 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Ferrosoferric oxide E00231 14789 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
⏷ Show the Full List of 10 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Methyltestosterone 10 mg capsule 10 mg Oral Capsule Oral
Methyltestosterone 10 mg tablet 10 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
4 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
6 Metabolism of anabolic steroids by recombinant human cytochrome P450 enzymes. Gas chromatographic-mass spectrometric determination of metabolites. J Chromatogr B Biomed Sci Appl. 1999 Nov 26;735(1):73-83.
7 Hepatic expression patterns of aryl hydrocarbon receptor, pregnane X receptor, two cytochrome P450s and five phase II metabolism genes responsive to 17alpha-methyltestosterone in rare minnow Gobiocypris rarus. Environ Toxicol Pharmacol. 2014 May;37(3):1157-68.
8 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.
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13 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.
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22 Drugs that may have potential CYP2B6 interactions.
23 Involvement of human cytochrome P450 2B6 in the omega- and 4-hydroxylation of the anesthetic agent propofol. Xenobiotica. 2007 Jul;37(7):717-24.
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30 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
31 Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
32 Canadian Pharmacists Association.
33 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
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35 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
36 Abad S, Moachon L, Blanche P, Bavoux F, Sicard D, Salmon-Ceron D "Possible interaction between glicazide, fluconazole and sulfamethoxazole resulting in severe hypoglycaemia." Br J Clin Pharmacol 52 (2001): 456-7. [PMID: 11678792]