Chemical: Drug
testosterone

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.



PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for testosterone

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA UGT1A4 *1a N/A N/A N/A
No VIP available No VIP available VA UGT1A4 *2 N/A N/A N/A
No VIP available CA VA UGT1A4 *3a N/A N/A N/A
VIP No Clinical Annotations available No Variant Annotations available
rs776746 NC_000007.13:g.99270539C>T, NC_000007.14:g.99672916T>C, NG_007938.1:g.12083G=, NG_007938.1:g.12083G>A, NM_000777.4:c.219-237A>G, NM_000777.4:c.219-237G>A, NM_001190484.2:c.219-237A>G, NM_001190484.2:c.219-237G>A, NM_001291829.1:c.-253-1A>G, NM_001291829.1:c.-253-1G>A, NM_001291830.1:c.189-237A>G, NM_001291830.1:c.189-237G>A, NR_033807.2:n.717-1A>G, NR_033807.2:n.717-1G>A, NR_033808.1:n.689-1G>A, NR_033809.1:n.581-237G>A, NR_033810.1:n.689-1G>A, NR_033811.1:n.321-1G>A, NR_033812.1:n.321-1G>A, XM_005250169.1:c.189-237G>A, XM_005250170.1:c.-357-1G>A, XM_005250171.1:c.-253-1G>A, XM_005250172.1:c.-254G>A, XM_005250173.1:c.-331-237G>A, XM_005250198.1:c.806-4288C>T, XM_006715859.2:c.219-237A>G, XM_011515843.1:c.-254A>G, XM_011515844.1:c.-229-237A>G, XM_011515845.1:c.-463-1A>G, XM_011515846.1:c.-331-237A>G, XM_011515847.1:c.-571-1A>G, XR_927383.1:n.344-237A>G, XR_927402.1:n.1466+48736T>C, rs10361242, rs11266830, rs386613022, rs58244770
C > T
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Dea No. 4000
  • TES
  • Testosteron
  • Testosterona [INN-Spanish]
  • Testosterone Cypionate
  • Testosterone Enanthate
  • Testosterone Hydrate
  • Testosteronum [INN-Latin]
  • Testostosterone
  • Trans-Testosterone
  • testosterone
Trade Names
  • Andriol
  • Andro
  • Andro 100
  • Andro L.A. 200
  • Androderm
  • Androgel
  • Android 10
  • Android 25
  • Android 5
  • Androlin
  • Andronaq
  • Andronate 100
  • Andronate 200
  • Andropatch
  • Andropository 200
  • Androsorb
  • Andrusol
  • Andryl 200
  • Beta Testosterone
  • Bio-T-Gel
  • CDB 111C
  • Cristerona T
  • Cristerone T
  • Delatest
  • Delatestryl
  • Depo-Testosterone
  • Depo-Testosterone Cypionate
  • Depotest
  • Everone 200
  • Geno-Cristaux Gremy
  • Homosteron
  • Homosterone
  • Libigel
  • Malerone
  • Malestrone
  • Malogen in Oil
  • Malogen, Aquaspension Injection
  • Mertestate
  • Metandren
  • Methyltestosterone
  • Neo-Hombreol F
  • Neo-Testis
  • Neotestis
  • Oreton
  • Oreton F
  • Oreton Methyl
  • Oreton-F
  • Orquisteron
  • Perandren
  • Percutacrine Androgenique
  • Primotest
  • Primoteston
  • Relibra
  • Scheinpharm Testone-Cyp
  • Striant
  • Sustanon
  • Sustanone
  • Sustason 250
  • Synandrol F
  • T-Cypionate
  • Teslen
  • Testamone 100
  • Testandrone
  • Testaqua
  • Testiculosterone
  • Testim
  • Testobase
  • Testoderm
  • Testoderm Tts
  • Testogel
  • Testoject-50
  • Testolin
  • Testopel Pellets
  • Testopropon
  • Testosteroid
  • Testoviron
  • Testoviron Schering
  • Testoviron T
  • Testred
  • Testred Cypionate 200
  • Testrin-P.A
  • Testro Aq
  • Testrone
  • Testryl
  • Virilon
  • Virilon IM
  • Virormone
  • Virosterone
Brand Mixture Names
  • Anadiol Inj Liq (Estradiol Benzoate + Estradiol Enanthate + Testosterone Enanthate)
  • Climacteron Liq Im (Estradiol Benzoate + Estradiol Dienanthate + Testosterone Enanthate Benzilic Acid Hydrazone)
  • Component E-H Implants (Estradiol Benzoate + Testosterone Propionate)
  • Component E-H Implants with Tylan (Estradiol Benzoate + Testosterone Propionate + Tylosin Tartrate)
  • Neo Pause Injection (Estradiol Valerate + Testosterone Enanthate)
  • Synovex H (Heifer Implants) (Estradiol Benzoate + Testosterone Propionate)
  • Uni-Bol (Estradiol Benzoate + Estradiol Enanthate + Testosterone Enanthate)

PharmGKB Accession Id

PA451627

Type(s):

Drug

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.

Source: Drug Bank

Indication

To 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.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The 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 5alpha-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5alpha-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.

Source: Drug Bank

Pharmacology

Testosterone 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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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

Source: Drug Bank

Protein Binding

40% 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.

Source: Drug Bank

Absorption

Approximately 10% of the testosterone dose applied on the skin surface is absorbed into systemic circulation

Source: Drug Bank

Half-Life

10-100 minutes

Source: Drug Bank

Toxicity

Side effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation.

Source: Drug Bank

Route of Elimination

About 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.

Source: Drug Bank

Chemical Properties

Chemical Formula

C19H28O2

Source: Drug Bank

Isomeric SMILES

C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=O)CC[C@]34C

Source: OpenEye

Canonical SMILES

C[C@]12CC[C@H]

Source: Drug Bank

Average Molecular Weight

288.4244

Source: Drug Bank

Monoisotopic Molecular Weight

288.20893014

Source: Drug Bank

SMILES

[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

Source: Drug Bank

InChI String

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

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ALB (source: Drug Bank)
AR (source: Drug Bank)
NPPB (source: Drug Bank)
SHBG (source: Drug Bank)

Drug Interactions

Interaction Description
docetaxel - testosterone The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
docetaxel - testosterone Testosterone propionate may increase the serum levels and toxicity of docetaxel. (source: Drug Bank)
testosterone - acenocoumarol The androgen increases the anticoagulant effect (source: Drug Bank)
testosterone - acenocoumarol The 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. (source: Drug Bank)
testosterone - anisindione The androgen may increase the anticoagulant effect of anisindione. (source: Drug Bank)
testosterone - cyclosporine The 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. (source: Drug Bank)
testosterone - dicumarol The androgen increases the anticoagulant effect (source: Drug Bank)
testosterone - dicumarol The androgen may increase the anticoagulant effect of dicumarol. (source: Drug Bank)
testosterone - docetaxel The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
testosterone - docetaxel Testosterone may increase the serum levels and toxicity of docetaxel. (source: Drug Bank)
testosterone - warfarin The androgen increases the anticoagulant effect (source: Drug Bank)
testosterone - warfarin The androgen, Testosterone, may incrase the anticoagulant effect of the Vitamin K antagonist, Warfarin. Monitor for changes in the therapeutic effect of Warfarin if Testosterone is initiated, discontinued or dose changed. (source: Drug Bank)
warfarin - testosterone Testosterone 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. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to testosterone: 19

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic Factors Affecting Gene Transcription and Catalytic Activity of UDP-Glucuronosyltransferases in Human Liver. Human molecular genetics. 2014. Liu Wanqing, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of CYP3A5 Expression on the Inhibition of CYP3A-Catalyzed Drug Metabolism: Impact on CYP3A-Mediated Drug-Drug Interactions. Drug metabolism and disposition: the biological fate of chemicals. 2013. Shirasaka Yoshiyuki, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Functional analysis of UGT1A4(P24T) and UGT1A4(L48V) variant enzymes. Pharmacogenomics. 2011. Zhou Jin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Tamoxifen metabolites as active inhibitors of aromatase in the treatment of breast cancer. Breast cancer research and treatment. 2011. Lu Wenjie Jessie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Substrate-specific modulation of CYP3A4 activity by genetic variants of cytochrome P450 oxidoreductase. Pharmacogenetics and genomics. 2010. Agrawal Vishal, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Methadone: a substrate and mechanism-based inhibitor of CYP19 (aromatase). Drug metabolism and disposition: the biological fate of chemicals. 2010. Lu Wenjie Jessie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Variation in anastrozole metabolism and pharmacodynamics in women with early breast cancer. Cancer research. 2010. Ingle James N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genome-wide copy-number-variation study identified a susceptibility gene, UGT2B17, for osteoporosis. American journal of human genetics. 2008. Yang Tie-Lin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A genomic "roadmap" to "better" drugs. Drug metabolism reviews. 2008. Liao Guochun, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In silico and in vitro pharmacogenetic analysis in mice. Proceedings of the National Academy of Sciences of the United States of America. 2007. Guo Yingying, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
X-chromosome inactivation patterns and androgen receptor functionality influence phenotype and social characteristics as well as pharmacogenetics of testosterone therapy in Klinefelter patients. The Journal of clinical endocrinology and metabolism. 2004. Zitzmann Michael, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug metabolism and disposition: the biological fate of chemicals. 2003. Patki Kiran C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Human extrahepatic cytochromes P450: function in xenobiotic metabolism and tissue-selective chemical toxicity in the respiratory and gastrointestinal tracts. Annual review of pharmacology and toxicology. 2003. Ding Xinxin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Gene-drug interaction: additive influence of mutant APOA1 and testosterone on plasma HDL-cholesterol. Clinical biochemistry. 2002. Keyhan Golyar, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vivo and in vitro induction of human cytochrome P4503A4 by dexamethasone. Clinical pharmacology and therapeutics. 2000. McCune J S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4. Journal of the National Cancer Institute. 1998. Rebbeck T R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The glucuronidation of opioids, other xenobiotics, and androgens by human UGT2B7Y(268) and UGT2B7H(268). Drug metabolism and disposition: the biological fate of chemicals. 1998. Coffman B L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. The Journal of pharmacology and experimental therapeutics. 1994. Shimada T, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0051-8488-88
DrugBank:
DB00624
PDB:
DHT
ChEBI:
17347
KEGG Compound:
C00535
KEGG Drug:
D00075
PubChem Compound:
6013
PubChem Substance:
46505691
7847143
Drugs Product Database (DPD):
2246063
ChemSpider:
5791
HET:
DHT
Therapeutic Targets Database:
DAP000841
FDA Drug Label at DailyMed:
c506aaa3-04f8-4eb1-8dc4-e964cdd08e7f

Clinical Trials

These are trials that mention testosterone and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.