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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
AveedNot Available
AxironLilly
Bio-T-GelBioSante Pharmaceuticals, Inc. and Teva Pharmaceuticals USA, Inc.
DelatestrylEndo
Depo-TestosteroneNot Available
FORTESTANot Available
IntrinsaProcter & Gamble
LivensaProcter & Gamble
NebidoBayer
StriantActient
SustanonOrganon
Testamone 100Not Available
Testaqua IMNot Available
TestimAuxilium
TestodermNot Available
Testoderm TTSNot Available
TestogelBayer
TestolinNot Available
TestopatchPierre Fabre
TestopelNot Available
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 KeyMUMGGOZAMZWBJJ-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
Not Available
Testosterone sulfateDetails
Testosterone
DihydrotestosteroneDetails
Testosterone
Not Available
Testosterone glucuronideDetails
Testosterone
Not Available
5-alpha-Dihydrotestosterone glucuronideDetails
Testosterone
Not Available
5a-Dihydrotestosterone sulfateDetails
Testosterone
Not Available
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
SpectraGC-MSMS/MS1D NMR2D NMR
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

Targets

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

Enzymes

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

Carriers

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

Transporters

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

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