You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameMethyltestosterone
Accession NumberDB06710
TypeSmall Molecule
GroupsApproved
DescriptionA synthetic anabolic steroid used for treating men with testosterone deficiency or similar androgen replacement therapies. Also, has antineoplastic properties and so has been used secondarily in women with advanced breast cancer. Methyltestosterone is a schedule III drug in the US.
Structure
Thumb
Synonyms
17-beta-Hydroxy-17-methylandrost-4-en-3-one
17-methyltestosterone
17(alpha)-Methyl-delta(4)-androsten-17(beta)-ol-3-one
17alpha-Methyl-3-oxo-4-androsten-17beta-ol
17alpha-Methyl-delta(4)-androsten-17beta-ol-3-one
17alpha-Methyltestosterone
17beta-Hydroxy-17-methylandrost-4-en-3-one
17α-methyl-Δ4-androsten-17β-ol-3-one
17α-methyltestosterone
4-Androstene-17alpha-methyl-17beta-ol-3-one
Android
Methyltestosterone
Methyltestosteronum
Metiltestosterona
NSC-9701
Testred
Virilon
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Metandren 10mgtablet10 mgoralNovartis Pharmaceuticals Canada Inc1993-12-312001-04-05Canada
Metandren 25mgtablet25 mgoralNovartis Pharmaceuticals Canada Inc1992-12-312001-04-05Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Androidcapsule10 mg/1oralValeant Pharmaceuticals North America LLC1973-12-03Not applicableUs
Methitesttablet10 mg/1oralImpax Generics1974-10-17Not applicableUs
Methyltestosteronecapsule10 mg/1oralImpax Generics2015-09-21Not applicableUs
Testred C-IIIcapsule10 mg/1oralValeant Pharmaceuticals North America LLC1973-12-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TestredNot Available
VirilonNot Available
Brand mixtures
NameLabellerIngredients
CovaryxCentrix Pharmaceutical, Inc,
Covaryx HsCentrix Pharmaceutical, Inc,
EemtCreekwood Pharmaceutical, Inc,
Eemt HsCreekwood Pharmaceutical, Inc,
Esterified Estrogens and MethyltestosteroneSeton Pharmaceuticals
SaltsNot Available
Categories
UNIIV9EFU16ZIF
CAS number58-18-4
WeightAverage: 302.451
Monoisotopic: 302.224580204
Chemical FormulaC20H30O2
InChI KeyInChIKey=GCKMFJBGXUYNAG-HLXURNFRSA-N
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
IUPAC Name
(1S,2R,10R,11S,14S,15S)-14-hydroxy-2,14,15-trimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-5-one
SMILES
[H][C@@]12CC[C@](C)(O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassAndrostane steroids
Direct ParentAndrogens and derivatives
Alternative Parents
Substituents
  • Androgen-skeleton
  • 17-hydroxysteroid
  • Oxosteroid
  • Hydroxysteroid
  • 3-oxosteroid
  • 3-oxo-delta-4-steroid
  • Delta-4-steroid
  • Tertiary alcohol
  • Cyclic alcohol
  • Cyclic ketone
  • Ketone
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationMethyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency. It is also used in women to treat breast cancer, breast pain, swelling due to pregnancy, and with the addition of estrogen it can treat symptoms of menopause.
PharmacodynamicsTestosterone is a steroid hormone from the androgen group. Testosterone is primarily secreted from the testes of males. In females, it is produced in the ovaries, adrenal glands and by conversion of adrostenedione in the periphery. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does.
Mechanism of actionThe effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Related Articles
AbsorptionThe methyl group aids to increase oral bioavailability.
Volume of distributionNot Available
Protein binding40% of testosterone in plasma is bound to sex hormone-binding globulin and 2% remains unbound and the rest is bound to albumin and other proteins.
Metabolism

Hepatic. Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT).

Route of elimination90% urine / 10% feces
Half life6-8 hours
ClearanceNot Available
ToxicitySide effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9774
Caco-2 permeable+0.8737
P-glycoprotein substrateSubstrate0.6431
P-glycoprotein inhibitor IInhibitor0.5981
P-glycoprotein inhibitor IINon-inhibitor0.732
Renal organic cation transporterNon-inhibitor0.757
CYP450 2C9 substrateNon-substrate0.8075
CYP450 2D6 substrateNon-substrate0.8604
CYP450 3A4 substrateSubstrate0.7916
CYP450 1A2 substrateNon-inhibitor0.8619
CYP450 2C9 inhibitorNon-inhibitor0.8844
CYP450 2D6 inhibitorNon-inhibitor0.951
CYP450 2C19 inhibitorNon-inhibitor0.6629
CYP450 3A4 inhibitorNon-inhibitor0.8713
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8711
Ames testNon AMES toxic0.9429
CarcinogenicityNon-carcinogens0.9361
BiodegradationNot ready biodegradable0.9494
Rat acute toxicity2.0516 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.886
hERG inhibition (predictor II)Non-inhibitor0.7219
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, coatedoral
Tabletoral
Tablet, film coatedoral
Tabletoral10 mg
Tabletoral25 mg
Tabletoral10 mg/1
Capsuleoral10 mg/1
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point163 °CPhysProp
water solubility33.9 mg/L (at 25 °C)YALKOWSKY,SH & HE,Y (2003)
logP3.36HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0139 mg/mLALOGPS
logP3.61ALOGPS
logP3.65ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)19.09ChemAxon
pKa (Strongest Basic)-0.53ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area37.3 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity89.07 m3·mol-1ChemAxon
Polarizability35.65 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-006x-7921000000-0e8f2747a2f3c8166048View in MoNA
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesG03EA01G03EK01G03BA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
4-Androstenedione4-Androstenedione may increase the fluid retaining activities of Methyltestosterone.
AcarboseMethyltestosterone may increase the hypoglycemic activities of Acarbose.
AcenocoumarolMethyltestosterone may increase the anticoagulant activities of Acenocoumarol.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Methyltestosterone.
AlbiglutideMethyltestosterone may increase the hypoglycemic activities of Albiglutide.
AlclometasoneAlclometasone may increase the fluid retaining activities of Methyltestosterone.
AldosteroneAldosterone may increase the fluid retaining activities of Methyltestosterone.
AlogliptinMethyltestosterone may increase the hypoglycemic activities of Alogliptin.
AmcinonideAmcinonide may increase the fluid retaining activities of Methyltestosterone.
AmiodaroneThe metabolism of Methyltestosterone can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Methyltestosterone can be increased when it is combined with Aprepitant.
AtazanavirThe metabolism of Methyltestosterone can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Methyltestosterone can be decreased when combined with Atomoxetine.
Beclomethasone dipropionateBeclomethasone dipropionate may increase the fluid retaining activities of Methyltestosterone.
BetamethasoneBetamethasone may increase the fluid retaining activities of Methyltestosterone.
BevacizumabBevacizumab may increase the cardiotoxic activities of Methyltestosterone.
BexaroteneThe serum concentration of Methyltestosterone can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Methyltestosterone can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Methyltestosterone can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Methyltestosterone can be decreased when it is combined with Bosentan.
BromocriptineMethyltestosterone may increase the hypoglycemic activities of Bromocriptine.
BudesonideBudesonide may increase the fluid retaining activities of Methyltestosterone.
C1 Esterase Inhibitor (Human)Methyltestosterone may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).
C1 Esterase Inhibitor (Recombinant)Methyltestosterone may increase the thrombogenic activities of C1 Esterase Inhibitor (Recombinant).
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Methyltestosterone.
CanagliflozinMethyltestosterone may increase the hypoglycemic activities of Canagliflozin.
CarbamazepineThe metabolism of Methyltestosterone can be increased when combined with Carbamazepine.
CeritinibThe serum concentration of Methyltestosterone can be increased when it is combined with Ceritinib.
ChlorpropamideMethyltestosterone may increase the hypoglycemic activities of Chlorpropamide.
CiclesonideCiclesonide may increase the fluid retaining activities of Methyltestosterone.
CitalopramThe metabolism of Methyltestosterone can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Methyltestosterone can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Methyltestosterone can be decreased when combined with Clemastine.
Clobetasol propionateClobetasol propionate may increase the fluid retaining activities of Methyltestosterone.
ClocortoloneClocortolone may increase the fluid retaining activities of Methyltestosterone.
ClopidogrelThe metabolism of Methyltestosterone can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Methyltestosterone can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Methyltestosterone can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Methyltestosterone can be increased when it is combined with Conivaptan.
Cortisone acetateCortisone acetate may increase the fluid retaining activities of Methyltestosterone.
CrizotinibThe metabolism of Methyltestosterone can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Methyltestosterone.
CyclosporineMethyltestosterone may increase the hepatotoxic activities of Cyclosporine.
CyclosporineThe metabolism of Methyltestosterone can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Methyltestosterone can be decreased when it is combined with Dabrafenib.
DapagliflozinMethyltestosterone may increase the hypoglycemic activities of Dapagliflozin.
DarunavirThe metabolism of Methyltestosterone can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Methyltestosterone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Methyltestosterone can be decreased when it is combined with Deferasirox.
DehydroepiandrosteroneDehydroepiandrosterone may increase the fluid retaining activities of Methyltestosterone.
dehydroepiandrosterone sulfatedehydroepiandrosterone sulfate may increase the fluid retaining activities of Methyltestosterone.
DelavirdineThe metabolism of Methyltestosterone can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Methyltestosterone can be decreased when combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Methyltestosterone.
DesoximetasoneDesoximetasone may increase the fluid retaining activities of Methyltestosterone.
Desoxycorticosterone acetateDesoxycorticosterone acetate may increase the fluid retaining activities of Methyltestosterone.
DexamethasoneDexamethasone may increase the fluid retaining activities of Methyltestosterone.
Dexamethasone isonicotinateDexamethasone isonicotinate may increase the fluid retaining activities of Methyltestosterone.
DicoumarolMethyltestosterone may increase the anticoagulant activities of Dicoumarol.
DiflorasoneDiflorasone may increase the fluid retaining activities of Methyltestosterone.
DifluocortoloneDifluocortolone may increase the fluid retaining activities of Methyltestosterone.
DifluprednateDifluprednate may increase the fluid retaining activities of Methyltestosterone.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Methyltestosterone.
DigoxinDigoxin may decrease the cardiotoxic activities of Methyltestosterone.
DihydroergotamineThe metabolism of Methyltestosterone can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Methyltestosterone can be decreased when combined with Diltiazem.
DisopyramideMethyltestosterone may increase the hypoglycemic activities of Disopyramide.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Methyltestosterone.
DoxorubicinThe metabolism of Methyltestosterone can be decreased when combined with Doxorubicin.
DoxycyclineThe metabolism of Methyltestosterone can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Methyltestosterone can be decreased when combined with Dronedarone.
DulaglutideMethyltestosterone may increase the hypoglycemic activities of Dulaglutide.
EfavirenzThe serum concentration of Methyltestosterone can be decreased when it is combined with Efavirenz.
EmpagliflozinMethyltestosterone may increase the hypoglycemic activities of Empagliflozin.
EnzalutamideThe serum concentration of Methyltestosterone can be decreased when it is combined with Enzalutamide.
EquileninEquilenin may increase the fluid retaining activities of Methyltestosterone.
EquilinEquilin may increase the fluid retaining activities of Methyltestosterone.
ErythromycinThe metabolism of Methyltestosterone can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Methyltestosterone can be decreased when it is combined with Eslicarbazepine acetate.
EstroneEstrone may increase the fluid retaining activities of Methyltestosterone.
Ethyl biscoumacetateMethyltestosterone may increase the anticoagulant activities of Ethyl biscoumacetate.
EtravirineThe serum concentration of Methyltestosterone can be decreased when it is combined with Etravirine.
ExenatideMethyltestosterone may increase the hypoglycemic activities of Exenatide.
FluconazoleThe metabolism of Methyltestosterone can be decreased when combined with Fluconazole.
FludrocortisoneFludrocortisone may increase the fluid retaining activities of Methyltestosterone.
FlumethasoneFlumethasone may increase the fluid retaining activities of Methyltestosterone.
FlunisolideFlunisolide may increase the fluid retaining activities of Methyltestosterone.
Fluocinolone AcetonideFluocinolone Acetonide may increase the fluid retaining activities of Methyltestosterone.
FluocinonideFluocinonide may increase the fluid retaining activities of Methyltestosterone.
FluocortoloneFluocortolone may increase the fluid retaining activities of Methyltestosterone.
FluorometholoneFluorometholone may increase the fluid retaining activities of Methyltestosterone.
FluprednideneFluprednidene may increase the fluid retaining activities of Methyltestosterone.
FluprednisoloneFluprednisolone may increase the fluid retaining activities of Methyltestosterone.
FlurandrenolideFlurandrenolide may increase the fluid retaining activities of Methyltestosterone.
Fluticasone furoateFluticasone furoate may increase the fluid retaining activities of Methyltestosterone.
Fluticasone PropionateFluticasone Propionate may increase the fluid retaining activities of Methyltestosterone.
FluvoxamineThe metabolism of Methyltestosterone can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Methyltestosterone can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Methyltestosterone can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Methyltestosterone can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Methyltestosterone can be increased when it is combined with Fusidic Acid.
GliclazideMethyltestosterone may increase the hypoglycemic activities of Gliclazide.
GlimepirideMethyltestosterone may increase the hypoglycemic activities of Glimepiride.
GlipizideMethyltestosterone may increase the hypoglycemic activities of Glipizide.
GlyburideMethyltestosterone may increase the hypoglycemic activities of Glyburide.
HydrocortisoneHydrocortisone may increase the fluid retaining activities of Methyltestosterone.
IdelalisibThe serum concentration of Methyltestosterone can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Methyltestosterone can be decreased when combined with Imatinib.
IndinavirThe metabolism of Methyltestosterone can be decreased when combined with Indinavir.
Insulin AspartMethyltestosterone may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirMethyltestosterone may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineMethyltestosterone may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineMethyltestosterone may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanMethyltestosterone may increase the hypoglycemic activities of Insulin Human.
Insulin LisproMethyltestosterone may increase the hypoglycemic activities of Insulin Lispro.
IsavuconazoniumThe metabolism of Methyltestosterone can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Methyltestosterone can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Methyltestosterone can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Methyltestosterone can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Methyltestosterone can be decreased when combined with Ketoconazole.
LanreotideMethyltestosterone may increase the hypoglycemic activities of Lanreotide.
LiraglutideMethyltestosterone may increase the hypoglycemic activities of Liraglutide.
LopinavirThe metabolism of Methyltestosterone can be decreased when combined with Lopinavir.
LovastatinThe metabolism of Methyltestosterone can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Methyltestosterone can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Methyltestosterone can be decreased when it is combined with Lumacaftor.
MecaserminMethyltestosterone may increase the hypoglycemic activities of Mecasermin.
MedrysoneMedrysone may increase the fluid retaining activities of Methyltestosterone.
MelengestrolMelengestrol may increase the fluid retaining activities of Methyltestosterone.
MetforminMethyltestosterone may increase the hypoglycemic activities of Metformin.
MethylprednisoloneMethylprednisolone may increase the fluid retaining activities of Methyltestosterone.
MifepristoneMethyltestosterone may increase the hypoglycemic activities of Mifepristone.
MifepristoneThe metabolism of Methyltestosterone can be decreased when combined with Mifepristone.
MiglitolMethyltestosterone may increase the hypoglycemic activities of Miglitol.
MitotaneThe serum concentration of Methyltestosterone can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Methyltestosterone can be decreased when it is combined with Modafinil.
MometasoneMometasone may increase the fluid retaining activities of Methyltestosterone.
NafcillinThe serum concentration of Methyltestosterone can be decreased when it is combined with Nafcillin.
NateglinideMethyltestosterone may increase the hypoglycemic activities of Nateglinide.
NefazodoneThe metabolism of Methyltestosterone can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Methyltestosterone can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Methyltestosterone can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Methyltestosterone can be decreased when combined with Nevirapine.
NilotinibThe metabolism of Methyltestosterone can be decreased when combined with Nilotinib.
OctreotideMethyltestosterone may increase the hypoglycemic activities of Octreotide.
OlaparibThe metabolism of Methyltestosterone can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Methyltestosterone can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Methyltestosterone.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Methyltestosterone.
PalbociclibThe serum concentration of Methyltestosterone can be increased when it is combined with Palbociclib.
ParamethasoneParamethasone may increase the fluid retaining activities of Methyltestosterone.
ParoxetineThe metabolism of Methyltestosterone can be decreased when combined with Paroxetine.
PasireotideMethyltestosterone may increase the hypoglycemic activities of Pasireotide.
PentamidineMethyltestosterone may increase the hypoglycemic activities of Pentamidine.
PentobarbitalThe metabolism of Methyltestosterone can be increased when combined with Pentobarbital.
PhenindioneMethyltestosterone may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Methyltestosterone can be increased when combined with Phenobarbital.
PhenprocoumonMethyltestosterone may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Methyltestosterone can be increased when combined with Phenytoin.
PioglitazoneMethyltestosterone may increase the hypoglycemic activities of Pioglitazone.
PosaconazoleThe metabolism of Methyltestosterone can be decreased when combined with Posaconazole.
PramlintideMethyltestosterone may increase the hypoglycemic activities of Pramlintide.
PrednicarbatePrednicarbate may increase the fluid retaining activities of Methyltestosterone.
PrednisolonePrednisolone may increase the fluid retaining activities of Methyltestosterone.
PrednisonePrednisone may increase the fluid retaining activities of Methyltestosterone.
PregnenolonePregnenolone may increase the fluid retaining activities of Methyltestosterone.
PrimidoneThe metabolism of Methyltestosterone can be increased when combined with Primidone.
QuazepamThe serum concentration of Methyltestosterone can be increased when it is combined with Quazepam.
QuinineMethyltestosterone may increase the hypoglycemic activities of Quinine.
RanolazineThe metabolism of Methyltestosterone can be decreased when combined with Ranolazine.
RepaglinideMethyltestosterone may increase the hypoglycemic activities of Repaglinide.
RifabutinThe metabolism of Methyltestosterone can be increased when combined with Rifabutin.
RifampicinThe metabolism of Methyltestosterone can be increased when combined with Rifampicin.
RifapentineThe metabolism of Methyltestosterone can be increased when combined with Rifapentine.
RimexoloneRimexolone may increase the fluid retaining activities of Methyltestosterone.
RitonavirThe metabolism of Methyltestosterone can be decreased when combined with Ritonavir.
RosiglitazoneMethyltestosterone may increase the hypoglycemic activities of Rosiglitazone.
SaquinavirThe metabolism of Methyltestosterone can be decreased when combined with Saquinavir.
SaxagliptinMethyltestosterone may increase the hypoglycemic activities of Saxagliptin.
SertralineThe metabolism of Methyltestosterone can be decreased when combined with Sertraline.
SildenafilThe metabolism of Methyltestosterone can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Methyltestosterone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Methyltestosterone can be increased when it is combined with Simeprevir.
SitagliptinMethyltestosterone may increase the hypoglycemic activities of Sitagliptin.
SorafenibThe metabolism of Methyltestosterone can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Methyltestosterone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Methyltestosterone can be increased when it is combined with Stiripentol.
SulfadiazineMethyltestosterone may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleMethyltestosterone may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleMethyltestosterone may increase the hypoglycemic activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Methyltestosterone can be decreased when combined with Sulfisoxazole.
SunitinibMethyltestosterone may increase the hypoglycemic activities of Sunitinib.
TelaprevirThe metabolism of Methyltestosterone can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Methyltestosterone can be decreased when combined with Telithromycin.
ThiotepaThe metabolism of Methyltestosterone can be decreased when combined with Thiotepa.
TiclopidineThe metabolism of Methyltestosterone can be decreased when combined with Ticlopidine.
TixocortolTixocortol may increase the fluid retaining activities of Methyltestosterone.
TocilizumabThe serum concentration of Methyltestosterone can be decreased when it is combined with Tocilizumab.
TolazamideMethyltestosterone may increase the hypoglycemic activities of Tolazamide.
TolbutamideMethyltestosterone may increase the hypoglycemic activities of Tolbutamide.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Methyltestosterone.
TriamcinoloneTriamcinolone may increase the fluid retaining activities of Methyltestosterone.
VenlafaxineThe metabolism of Methyltestosterone can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Methyltestosterone can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Methyltestosterone can be decreased when combined with Voriconazole.
WarfarinMethyltestosterone may increase the anticoagulant activities of Warfarin.
ZiprasidoneThe metabolism of Methyltestosterone can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
Gene Name:
AR
Uniprot ID:
P10275
Molecular Weight:
98987.9 Da
References
  1. Small EJ, Ryan CJ: The case for secondary hormonal therapies in the chemotherapy age. J Urol. 2006 Dec;176(6 Pt 2):S66-71. [PubMed:17084172 ]
  2. Omwancha J, Brown TR: Selective androgen receptor modulators: in pursuit of tissue-selective androgens. Curr Opin Investig Drugs. 2006 Oct;7(10):873-81. [PubMed:17086931 ]
  3. Petraki CD, Sfikas CP: Histopathological changes induced by therapies in the benign prostate and prostate adenocarcinoma. Histol Histopathol. 2007 Jan;22(1):107-18. [PubMed:17128417 ]
  4. Maudsley S, Davidson L, Pawson AJ, Freestone SH, Lopez de Maturana R, Thomson AA, Millar RP: Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5. Neuroendocrinology. 2006;84(5):285-300. Epub 2007 Jan 4. [PubMed:17202804 ]
  5. Lapauw B, Goemaere S, Crabbe P, Kaufman JM, Ruige JB: Is the effect of testosterone on body composition modulated by the androgen receptor gene CAG repeat polymorphism in elderly men? Eur J Endocrinol. 2007 Mar;156(3):395-401. [PubMed:17322500 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [PubMed:3521955 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Androgen binding
Specific Function:
Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone, and 17-beta-estradiol. Regulates the plasma metabolic clearance rate of steroid hormones by controlling their plasma concentration.
Gene Name:
SHBG
Uniprot ID:
P04278
Molecular Weight:
43778.755 Da
References
  1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [PubMed:3521955 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Lu R, Kanai N, Bao Y, Wolkoff AW, Schuster VL: Regulation of renal oatp mRNA expression by testosterone. Am J Physiol. 1996 Feb;270(2 Pt 2):F332-7. [PubMed:8779895 ]
  2. Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [PubMed:8779894 ]
  3. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. Kobayashi Y, Hirokawa N, Ohshiro N, Sekine T, Sasaki T, Tokuyama S, Endou H, Yamamoto T: Differential gene expression of organic anion transporters in male and female rats. Biochem Biophys Res Commun. 2002 Jan 11;290(1):482-7. [PubMed:11779196 ]
Comments
comments powered by Disqus
Drug created on May 16, 2010 09:41 / Updated on August 17, 2016 12:24