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Identification
NameTestosterone
Accession NumberDB00624  (APRD00433)
Typesmall molecule
Groupsapproved, investigational
Description

Testosterone is a steroid sex hormone found in both men and women. In men, testosterone is produced primarily by the Leydig (interstitial) cells of the testes when stimulated by luteinizing hormone (LH). It functions to stimulate spermatogenesis, promote physical and functional maturation of spermatozoa, maintain accessory organs of the male reproductive tract, support development of secondary sexual characteristics, stimulate growth and metabolism throughout the body and influence brain development by stimulating sexual behaviors and sexual drive. In women, testosterone is produced by the ovaries (25%), adrenals (25%) and via peripheral conversion from androstenedione (50%). Testerone in women functions to maintain libido and general wellbeing. Testosterone exerts a negative feedback mechanism on pituitary release of LH and follicle-stimulating hormone (FSH). Testosterone may be further converted to dihydrotestosterone or estradiol depending on the tissue.

Structure
Thumb
Synonyms
SynonymLanguageCode
17beta-hydroxy-4-androsten-3-oneNot AvailableNot Available
17beta-Hydroxy-4-androsten-3-oneNot AvailableNot Available
4-androsten-17β-ol-3-oneNot AvailableNot Available
Depo-TestadiolNot AvailableIS
MertestateNot AvailableIS
Synandrol FNot AvailableIS
TestosteronGermanINN
TestosteronaSpanishINN
TestostéroneFrenchINN
TestosteronumLatinINN
TestoxylNot AvailableIS
TestrylNot AvailableIS
VirosteroneNot AvailableIS
Salts
Name/CAS Structure Properties
Testosterone Enanthate
Thumb Not applicable DBSALT001030
Testosterone Heptanoate
Thumb Not applicable DBSALT001031
Testosterone Propionate
Thumb Not applicable DBSALT001032
Testosterone Undecanoate
Thumb Not applicable DBSALT001033
Brand names
NameCompany
AndriolMerck
AndrodermHospira
AndrogelAbbott
Andronate 100Not Available
Andronate 200Not Available
AndropatchGlaxoSmithKline
Andropository 200Not Available
Andryl 200Not Available
AxironLilly
Bio-T-GelBioSante Pharmaceuticals, Inc. and Teva Pharmaceuticals USA, Inc.
DelatestrylEndo
IntrinsaProcter & Gamble
LivensaProcter & Gamble
NebidoBayer
StriantActient
SustanonOrganon
Testamone 100Not Available
Testaqua IMNot Available
TestimAuxilium
TestodermNot Available
Testoderm TTSNot Available
TestogelBayer
TestolinNot Available
TestopatchPierre Fabre
Testopel PelletsNot Available
Testrin-P.ANot Available
Testro AQNot Available
VirormoneNordic Pharma
Brand mixtures
Brand NameIngredients
ClimacteronEstradiol Benzoate + Estradiol Dienanthate + Testosterone Enanthate Benzilic Acid Hydrazone
Neo Pause InjectionEstradiol Valerate + Testosterone Enanthate
Categories
CAS number58-22-0
WeightAverage: 288.4244
Monoisotopic: 288.20893014
Chemical FormulaC19H28O2
InChI KeyInChIKey=MUMGGOZAMZWBJJ-DYKIIFRCSA-N
InChI
InChI=1S/C19H28O2/c1-18-9-7-13(20)11-12(18)3-4-14-15-5-6-17(21)19(15,2)10-8-16(14)18/h11,14-17,21H,3-10H2,1-2H3/t14-,15-,16-,17-,18-,19-/m0/s1
IUPAC Name
(1S,2R,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
SMILES
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Mass Specshow(13.5 KB)
Taxonomy
KingdomOrganic Compounds
SuperclassLipids
ClassSteroids and Steroid Derivatives
SubclassAndrogens and Derivatives
Direct parentAndrogens and Derivatives
Alternative parentsKetosteroids; Hydroxysteroids; Secondary Alcohols; Ketones; Cyclic Alcohols and Derivatives; Polyamines
Substituentscyclic alcohol; ketone; secondary alcohol; polyamine; alcohol; carbonyl group
Classification descriptionThis compound belongs to the androgens and derivatives. These are hydroxylated C19 steroid hormones. They are known to favour the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
Pharmacology
IndicationTo be used as hormone replacement or substitution of diminished or absent endogenous testosterone. Use in males: For management of congenital or acquired hypogonadism, hypogonadism associated with HIV infection, and male climacteric (andopause). Use in females: For palliative treatment of androgen-responsive, advanced, inoperable, metastatis (skeletal) carcinoma of the breast in women who are 1-5 years postmenopausal; testosterone esters may be used in combination with estrogens in the management of moderate to severe vasomotor symptoms associated with menopause in women who do not respond to adequately to estrogen therapy alone.
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.
AbsorptionApproximately 10% of the testosterone dose applied on the skin surface is absorbed into systemic circulation
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

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

SubstrateEnzymesProduct
Testosterone
6-beta-hydroxytestosteroneDetails
Testosterone
EstradiolDetails
Testosterone
    Testosterone sulfateDetails
    Testosterone
    DihydrotestosteroneDetails
    Testosterone
      Testosterone glucuronideDetails
      Testosterone
        5-alpha-Dihydrotestosterone glucuronideDetails
        Testosterone
          5a-Dihydrotestosterone sulfateDetails
          Testosterone
            17-Hydroxyandrostane-3-glucuronideDetails
            Route of eliminationAbout 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form.
            Half life10-100 minutes
            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 organisms
            • Humans and other mammals
            Pathways
            PathwayCategorySMPDB ID
            17-Beta Hydroxysteroid Dehydrogenase III DeficiencyDiseaseSMP00356
            Androgen and Estrogen MetabolismMetabolicSMP00068
            Aromatase deficiencyDiseaseSMP00565
            SNP Mediated EffectsNot Available
            SNP Mediated Adverse Drug ReactionsNot Available
            ADMET
            Predicted ADMET features
            Property Value Probability
            Human Intestinal Absorption + 1.0
            Blood Brain Barrier + 0.973
            Caco-2 permeable + 0.8984
            P-glycoprotein substrate Substrate 0.6498
            P-glycoprotein inhibitor I Inhibitor 0.5489
            P-glycoprotein inhibitor II Non-inhibitor 0.8923
            Renal organic cation transporter Non-inhibitor 0.7324
            CYP450 2C9 substrate Non-substrate 0.8167
            CYP450 2D6 substrate Non-substrate 0.9116
            CYP450 3A4 substrate Substrate 0.7739
            CYP450 1A2 substrate Non-inhibitor 0.9005
            CYP450 2C9 substrate Non-inhibitor 0.95
            CYP450 2D6 substrate Non-inhibitor 0.9452
            CYP450 2C19 substrate Non-inhibitor 0.6668
            CYP450 3A4 substrate Non-inhibitor 0.8812
            CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8683
            Ames test Non AMES toxic 0.9382
            Carcinogenicity Non-carcinogens 0.9483
            Biodegradation Not ready biodegradable 0.9174
            Rat acute toxicity 1.6259 LD50, mol/kg Not applicable
            hERG inhibition (predictor I) Weak inhibitor 0.8938
            hERG inhibition (predictor II) Non-inhibitor 0.7163
            Pharmacoeconomics
            Manufacturers
            • Heather drug co inc
            • Valeant pharmaceuticals international
            • Schering corp sub schering plough corp
            • Novartis pharmaceuticals corp
            • Impax laboratories inc
            • Eli lilly and co
            • Purepac pharmaceutical co
            • Private formulations inc
            • Tablicaps inc
            • Usl pharma inc
            • Inwood laboratories inc sub forest laboratories inc
            • Kv pharmaceutical co
            • Lannett co inc
            • Parke davis div warner lambert co
            • Watson laboratories inc
            • West ward pharmaceutical corp
            • Alza corp
            • Unimed pharmaceuticals inc
            • Auxilium pharmaceuticals
            • Par pharmaceutical
            • Watson laboratories
            • Slate pharmaceuticals inc
            • Columbia laboratories inc
            • Pharmacia and upjohn co
            • Bedford laboratories div ben venue laboratories inc
            • Paddock laboratories inc
            • Sandoz canada inc
            • Synerx pharma llc
            • Endo pharmaceutical solutions inc
            • Solvay Pharmaceuticals, Inc.
            Packagers
            Dosage forms
            FormRouteStrength
            CapsuleOral
            GelTopical
            LiquidIntramuscular
            PatchTransdermal
            SolutionIntramuscular
            SolutionIntramuscular
            Prices
            Unit descriptionCostUnit
            AndroGel Pump 1% Gel (1 Box Contains Two 75 gm Bottles)290.63USDbox
            Androderm 60 2.5 mg/24hr Patches 1 Box = 60 Patches278.56USDbox
            Androderm 30 5 mg/24hr Patches 1 Box = 30 Patches277.53USDbox
            AndroGel (each Box Contains Thirty - 50 mg/5 gm Packets) 150 gm Box274.58USDbox
            AndroGel (each Box Contains Thirty - 25 mg/2.5 gm Packets) 75 gm Box270.61USDbox
            Delatestryl 200 mg/ml Oil 5ml Vial93.98USDvial
            Testosterone Cypionate 200 mg/ml Oil 10ml Vial88.99USDvial
            Testosterone Cypionate 100 mg/ml Oil 10ml Vial57.99USDvial
            Depo-Testosterone 200 mg/ml Oil 1ml Vial34.99USDvial
            Testosterone cypionate powd32.74USDg
            Testosterone Cypionate 200 mg/ml Oil 1ml Vial28.99USDvial
            Depo-testosterone 200 mg/ml28.63USDml
            Testopel 75 mg pellets27.5USDpellet
            Testosterone cyp 200 mg/ml23.18USDml
            Delatestryl 200 mg/ml vial19.86USDml
            Testred 10 mg capsule17.6USDcapsule
            Testosterone enan 200 mg/ml16.99USDml
            Testosterone Enanthate 200 mg/ml Oil16.66USDml
            Depo-Testosterone 200 mg/ml Oil13.23USDml
            Android 10 mg capsule11.91USDcapsule
            Delatestryl 200 mg/ml10.75USDml
            Testim 1% Gel 5 gm Tube10.08USDtube
            Androderm 5 mg/24hr patch10.06USDpatch
            Methyltestosterone powder8.54USDg
            Depo-Testosterone 100 mg/ml Oil7.87USDml
            Depo-testosterone 100 mg/ml vial7.67USDml
            Testosterone powder6.25USDg
            Testosterone propionate powder6.25USDg
            Testosterone cyp 100 mg/ml5.91USDml
            Androderm 2.5 mg/24hr patch5.03USDpatch
            Methitest 10 mg tablet4.84USDtablet
            Striant 30 mg Miscellaneous4.32USDea
            Striant 30 mg mucoadhesive4.31USDeach
            Depo-Testosterone Cypionate 100 mg/ml2.98USDml
            Testim 1%(50 mg) gel2.47USDg
            Testosterone Cypionate 100 mg/ml2.23USDml
            Androgel 1% gel pump1.92USDg
            First-testosterone mc 2% cr0.91USDg
            First 2% testosterone oint0.88USDg
            First-Testosterone 2% Ointment0.86USDgm
            DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
            Patents
            CountryPatent NumberApprovedExpires (estimated)
            United States73209682005-01-182025-01-18
            United States51529971993-12-112010-12-11
            Canada23668562006-05-162020-03-27
            Canada13325701994-10-182011-10-18
            Properties
            Statesolid
            Experimental Properties
            PropertyValueSource
            melting point155 °CPhysProp
            water solubility23.4 mg/L (at 25 °C)YALKOWSKY,SH & HE,Y (2003)
            logP3.32HANSCH,C ET AL. (1995)
            Caco2 permeability-4.34ADME Research, USCD
            Predicted Properties
            PropertyValueSource
            water solubility3.33e-02 g/lALOGPS
            logP2.99ALOGPS
            logP3.37ChemAxon
            logS-3.9ALOGPS
            pKa (strongest acidic)19.09ChemAxon
            pKa (strongest basic)-0.88ChemAxon
            physiological charge0ChemAxon
            hydrogen acceptor count2ChemAxon
            hydrogen donor count1ChemAxon
            polar surface area37.3ChemAxon
            rotatable bond count0ChemAxon
            refractivity84.43ChemAxon
            polarizability34.02ChemAxon
            number of rings4ChemAxon
            bioavailability1ChemAxon
            rule of fiveYesChemAxon
            Ghose filterYesChemAxon
            Veber's ruleYesChemAxon
            MDDR-like ruleNoChemAxon
            Spectra
            Spectra
            References
            Synthesis Reference

            Merle G. Wovcha, Frederick J. Antosz, John M. Beaton, Alfred B. Garcia, Leo A. Kominek, “Process for preparing 9.alpha.-OH testosterone.” U.S. Patent US4221868, issued November, 1977.

            US4221868
            General Reference
            1. Freeman ER, Bloom DA, McGuire EJ: A brief history of testosterone. J Urol. 2001 Feb;165(2):371-3. Pubmed
            2. Hoberman JM, Yesalis CE: The history of synthetic testosterone. Sci Am. 1995 Feb;272(2):76-81. Pubmed
            3. Contraceptive efficacy of testosterone-induced azoospermia in normal men. World Health Organization Task Force on methods for the regulation of male fertility. Lancet. 1990 Oct 20;336(8721):955-9. Pubmed
            4. Dean JD, Carnegie C, Rodzvilla J, Smith T: Long-term effects of testim® 1% testosterone gel in hypogonadal men. Rev Urol. 2004;6 Suppl 6:S22-9. Pubmed
            External Links
            ResourceLink
            KEGG DrugD00075
            KEGG CompoundC00535
            PubChem Compound6013
            PubChem Substance46505691
            ChemSpider5791
            ChEBI17347
            ChEMBLCHEMBL386630
            Therapeutic Targets DatabaseDAP000841
            PharmGKBPA451627
            IUPHAR2858
            Guide to Pharmacology2858
            HETDHT
            Drug Product Database2246063
            RxListhttp://www.rxlist.com/cgi/generic2/androgel.htm
            PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tes1438.shtml
            WikipediaTestosterone
            ATC CodesG03BA02G03BA03G03EK01
            AHFS Codes
            • 68:08.00
            PDB EntriesNot Available
            FDA labelshow(738 KB)
            MSDSshow(49.6 KB)
            Interactions
            Drug Interactions
            Drug
            AcenocoumarolThe androgen, Testosterone, may incrase the anticoagulant effect of the Vitamin K antagonist, Acenocoumarol. Monitor for changes in the therapeutic effect of Acenocoumarol if Testosterone is initiated, discontinued or dose changed.
            AnisindioneThe androgen may increase the anticoagulant effect of anisindione.
            CyclosporineThe androgen, Testosterone, may increase the hepatotoxicity of Cyclosporine. Testosterone may also elevate serum concentrations of Cyclosporine. Consider alternate therapy or monitor for signs of renal and hepatic toxicity.
            DicoumarolThe androgen may increase the anticoagulant effect of dicumarol.
            DocetaxelTestosterone may increase the serum levels and toxicity of docetaxel.
            WarfarinTestosterone may increase the serum concentration and anticoagulant effect of warfarin. Monitor for changes in prothrombin time and therapeutic effects of warfarin if testosterone is initiated, discontinued or dose changed.
            Food InteractionsNot Available

            1. Androgen receptor

            Kind: protein

            Organism: Human

            Pharmacological action: yes

            Actions: agonist

            Components

            Name UniProt ID Details
            Androgen receptor P10275 Details

            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
            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
            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
            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
            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
            6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

            1. Cytochrome P450 3A5

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 3A5 P20815 Details

            References:

            1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
            2. 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. Epub 2009 Nov 24. Pubmed

            2. Cytochrome P450 19A1

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 19A1 P11511 Details

            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. Epub 2009 Nov 24. Pubmed

            3. Cholesterol side-chain cleavage enzyme, mitochondrial

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inhibitor

            Components

            Name UniProt ID Details
            Cholesterol side-chain cleavage enzyme, mitochondrial P05108 Details

            References:

            1. Kostic TS, Stojkov NJ, Bjelic MM, Mihajlovic AI, Janjic MM, Andric SA: Pharmacological doses of testosterone upregulated androgen receptor and 3-Beta-hydroxysteroid dehydrogenase/delta-5-delta-4 isomerase and impaired leydig cells steroidogenesis in adult rats. Toxicol Sci. 2011 Jun;121(2):397-407. Epub 2011 Apr 6. Pubmed

            4. Amine oxidase [flavin-containing] A

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inducer

            Components

            Name UniProt ID Details
            Amine oxidase [flavin-containing] A P21397 Details

            References:

            1. Sjoberg RL, Ducci F, Barr CS, Newman TK, Dell’osso L, Virkkunen M, Goldman D: A non-additive interaction of a functional MAO-A VNTR and testosterone predicts antisocial behavior. Neuropsychopharmacology. 2008 Jan;33(2):425-30. Epub 2007 Apr 11. Pubmed
            2. Hoff KM: Interaction of testosterone with monoamineoxidase in mouse brain maturation. Gen Pharmacol. 1977;8(1):55-7. Pubmed

            5. Cytochrome P450 3A7

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 3A7 P24462 Details

            References:

            1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
            2. 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. Epub 2009 Nov 24. Pubmed

            6. Cytochrome P450 3A4

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate inhibitor inducer

            Components

            Name UniProt ID Details
            Cytochrome P450 3A4 P08684 Details

            References:

            1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
            2. © Tianyi Zhang, Yongxin Zhu, and Chandrani Gunaratna. Simultaneous Determination of Metabolites from Multiple Cytochrome P450 Probe Substrates by Gradient Liquid Chromatography with UV Detection. Source
            3. 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. Epub 2009 Nov 24. Pubmed
            4. Zhang T, Zhu Y, Gunaratna C: Rapid and quantitative determination of metabolites from multiple cytochrome P450 probe substrates by gradient liquid chromatography-electrospray ionization-ion trap mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2002 Nov 25;780(2):371-9. Pubmed

            7. Cytochrome P450 1A1

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 1A1 P04798 Details

            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. Epub 2009 Nov 24. Pubmed

            8. Cytochrome P450 1B1

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 1B1 Q16678 Details

            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. Epub 2009 Nov 24. Pubmed

            9. Cytochrome P450 2A13

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 2A13 Q16696 Details

            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. Epub 2009 Nov 24. Pubmed

            10. Cytochrome P450 2B6

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate inducer

            Components

            Name UniProt ID Details
            Cytochrome P450 2B6 P20813 Details

            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. Epub 2009 Nov 24. Pubmed

            11. Cytochrome P450 2C19

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 2C19 P33261 Details

            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. Epub 2009 Nov 24. Pubmed

            12. Cytochrome P450 2C8

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 2C8 P10632 Details

            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. Epub 2009 Nov 24. Pubmed

            13. Cytochrome P450 2C9

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 2C9 P11712 Details

            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. Epub 2009 Nov 24. Pubmed

            14. Cytochrome P450 3A43

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Cytochrome P450 3A43 Q9HB55 Details

            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. Epub 2009 Nov 24. Pubmed

            1. Serum albumin

            Kind: protein

            Organism: Human

            Pharmacological action: no

            Actions: other/unknown

            Components

            Name UniProt ID Details
            Serum albumin P02768 Details

            References:

            1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. Pubmed

            2. Sex hormone-binding globulin

            Kind: protein

            Organism: Human

            Pharmacological action: no

            Actions: other/unknown

            Components

            Name UniProt ID Details
            Sex hormone-binding globulin P04278 Details

            References:

            1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. Pubmed

            1. Solute carrier organic anion transporter family member 1A2

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inhibitor inducer

            Components

            Name UniProt ID Details
            Solute carrier organic anion transporter family member 1A2 P46721 Details

            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
            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
            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

            2. Solute carrier family 22 member 8

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inducer

            Components

            Name UniProt ID Details
            Solute carrier family 22 member 8 Q8TCC7 Details

            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

            3. Solute carrier family 22 member 7

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inducer

            Components

            Name UniProt ID Details
            Solute carrier family 22 member 7 Q9Y694 Details

            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

            4. Solute carrier family 22 member 1

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inhibitor

            Components

            Name UniProt ID Details
            Solute carrier family 22 member 1 O15245 Details

            References:

            1. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. Pubmed

            5. Multidrug resistance protein 1

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inhibitor

            Components

            Name UniProt ID Details
            Multidrug resistance protein 1 P08183 Details

            References:

            1. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. Pubmed
            2. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. Pubmed

            6. Sodium/bile acid cotransporter

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: inhibitor

            Components

            Name UniProt ID Details
            Sodium/bile acid cotransporter Q14973 Details

            References:

            1. Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. Pubmed

            7. Solute carrier family 22 member 3

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Solute carrier family 22 member 3 O75751 Details

            References:

            1. Tzvetkov MV, Vormfelde SV, Balen D, Meineke I, Schmidt T, Sehrt D, Sabolic I, Koepsell H, Brockmoller J: The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009 Sep;86(3):299-306. Epub 2009 Jun 17. Pubmed

            8. Solute carrier family 22 member 4

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            Solute carrier family 22 member 4 Q9H015 Details

            References:

            1. Tzvetkov MV, Vormfelde SV, Balen D, Meineke I, Schmidt T, Sehrt D, Sabolic I, Koepsell H, Brockmoller J: The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009 Sep;86(3):299-306. Epub 2009 Jun 17. Pubmed

            9. ATP-binding cassette sub-family G member 2

            Kind: protein

            Organism: Human

            Pharmacological action: unknown

            Actions: substrate

            Components

            Name UniProt ID Details
            ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

            References:

            1. Janvilisri T, Venter H, Shahi S, Reuter G, Balakrishnan L, van Veen HW: Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51. Epub 2003 Mar 28. Pubmed

            Comments
            Drug created on June 13, 2005 07:24 / Updated on February 11, 2014 11:24