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Description
Curator's Comment:: Description was created based on several sources, including

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. 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 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. Testosterone is 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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P10275
Gene ID: 367.0
Gene Symbol: AR
Target Organism: Homo sapiens (Human)
3.16 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TESTOSTERONE

Approved Use

Testosterone is an androgen indicated for replacement therapy in males for conditions associated with a deficiency or absence of endogenous testosterone: • Primary Hypogonadism (Congenital or Acquired) (1) • Hypogonadotropic Hypogonadism (Congenital or Acquired)

Launch Date

1.35950395E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
13.1 pg/mL
8.2 mg single, topical
dose: 8.2 mg
route of administration: Topical
experiment type: SINGLE
co-administered:
TESTOSTERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
214 ng/dL
30 mg single, topical
dose: 30 mg
route of administration: topical
experiment type: single
co-administered:
TESTOSTERONE unknown
Homo sapiens
population: healthy
age:
sex:
food status:
231 ng/dL
30 mg single, topical
dose: 30 mg
route of administration: topical
experiment type: single
co-administered:
TESTOSTERONE unknown
Homo sapiens
population: healthy
age:
sex:
food status:
930.1 ng/dL
5 g 1 times / day multiple, topical
dose: 5 g
route of administration: topical
experiment type: multiple
co-administered:
TESTOSTERONE unknown
Homo sapiens
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
948 pg × h/mL
8.2 mg single, topical
dose: 8.2 mg
route of administration: Topical
experiment type: SINGLE
co-administered:
TESTOSTERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
2120 ng*h/dL
30 mg single, topical
dose: 30 mg
route of administration: topical
experiment type: single
co-administered:
TESTOSTERONE unknown
Homo sapiens
population: healthy
age:
sex:
food status:
3110 ng*h/dL
30 mg single, topical
dose: 30 mg
route of administration: topical
experiment type: single
co-administered:
TESTOSTERONE unknown
Homo sapiens
population: healthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7 h
8.2 mg single, topical
dose: 8.2 mg
route of administration: Topical
experiment type: SINGLE
co-administered:
TESTOSTERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
13%
8.2 mg single, topical
dose: 8.2 mg
route of administration: Topical
experiment type: SINGLE
co-administered:
TESTOSTERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
75 mg 1 times / day steady, subcutaneous (median)
Recommended
Dose: 75 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, adult
n = 150
Health Status: unhealthy
Condition: hypogonadism
Age Group: adult
Sex: M
Population Size: 150
Sources:
Disc. AE: Hypertension...
AEs leading to
discontinuation/dose reduction:
Hypertension (5.6%)
Sources:
100 mg 1 times / day steady, topical
Recommended
Dose: 100 mg, 1 times / day
Route: topical
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean 74 years
n = 106
Health Status: unhealthy
Condition: with limitations in mobility
Age Group: mean 74 years
Sex: M
Population Size: 106
Sources:
Other AEs: Cardiac disorders, Atherosclerosis...
Other AEs:
Cardiac disorders (6.5%)
Atherosclerosis (6.4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Hypertension 5.6%
Disc. AE
75 mg 1 times / day steady, subcutaneous (median)
Recommended
Dose: 75 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, adult
n = 150
Health Status: unhealthy
Condition: hypogonadism
Age Group: adult
Sex: M
Population Size: 150
Sources:
Atherosclerosis 6.4%
100 mg 1 times / day steady, topical
Recommended
Dose: 100 mg, 1 times / day
Route: topical
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean 74 years
n = 106
Health Status: unhealthy
Condition: with limitations in mobility
Age Group: mean 74 years
Sex: M
Population Size: 106
Sources:
Cardiac disorders 6.5%
100 mg 1 times / day steady, topical
Recommended
Dose: 100 mg, 1 times / day
Route: topical
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean 74 years
n = 106
Health Status: unhealthy
Condition: with limitations in mobility
Age Group: mean 74 years
Sex: M
Population Size: 106
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major [Km 10 uM]
major [Km 38.7 uM]
minor
minor
minor
minor
minor
minor
minor
minor
no
no
no
no
no
no
no
no
yes
yes
yes
yes
PubMed

PubMed

TitleDatePubMed
Effects of hyperprolactinemia on testosterone production in rat Leydig cells.
2001
Psychophysiological responses to the Stroop Task after a maximal cycle ergometry in elite sportsmen and physically active subjects.
2001 Feb
Spz1, a novel bHLH-Zip protein, is specifically expressed in testis.
2001 Feb
Effects of the anti-androgen finasteride on the modulatory actions of oestradiol on androgen metabolism by human gingival fibroblasts.
2001 Feb
Androgens and the role of female "hyperaggressiveness" in spotted hyenas (Crocuta crocuta).
2001 Feb
Interactions among paternal behavior, steroid hormones, and parental experience in male marmosets (Callithrix kuhlii).
2001 Feb
Castration in Gambel's and Scaled Quail: ornate plumage and dominance persist, but courtship and threat behaviors do not.
2001 Feb
cDNA cloning and initial characterization of CYP3A43, a novel human cytochrome P450.
2001 Feb
Modulation of P450 CYP3A4-dependent metabolism by P-glycoprotein: implications for P450 phenotyping.
2001 Feb
Photoperiod-induced testicular apoptosis in European starlings (Sturnus vulgaris).
2001 Feb
Neuroendocrine regulation of sexually dimorphic brain structure and associated sexual behavior in male rats is genetically controlled.
2001 Feb
Influence of the degree of stimulation of the pituitary by gonadotropin-releasing hormone on the action of inhibin and testosterone to suppress the secretion of the gonadotropins in rams.
2001 Feb
Follicular-fluid factors and granulosa-cell gene expression associated with follicle deviation in cattle.
2001 Feb
Substitution mutation C268Y causes 17 beta-hydroxysteroid dehydrogenase 3 deficiency.
2001 Feb
Sex differences in androgen receptors of the human mamillary bodies are related to endocrine status rather than to sexual orientation or transsexuality.
2001 Feb
Plasma melatonin concentration before and during testosterone replacement in Klinefelter's syndrome: relation to hepatic indolamine metabolism and sympathoadrenal activity.
2001 Feb
Longitudinal effects of aging on serum total and free testosterone levels in healthy men. Baltimore Longitudinal Study of Aging.
2001 Feb
Evidence that cyproterone acetate improves psychological symptoms and enhances the activity of the dopaminergic system in postmenopause.
2001 Feb
Androgen deficiency in women with hypopituitarism.
2001 Feb
Muting of androgen negative feedback unveils impoverished gonadotropin-releasing hormone/luteinizing hormone secretory reactivity in healthy older men.
2001 Feb
Polycystic ovary syndrome is associated with obstructive sleep apnea and daytime sleepiness: role of insulin resistance.
2001 Feb
Disparate response of wild-type and variant forms of LH to GnRH stimulation in individuals heterozygous for the LHbeta variant allele.
2001 Feb
Testosterone concentrations in women aged 25-50 years: associations with lifestyle, body composition, and ovarian status.
2001 Feb 1
Neuronal size in the spinal nucleus of the bulbocavernosus: direct modulation by androgen in rats with mosaic androgen insensitivity.
2001 Feb 1
Luteinizing hormone-dependent activity and luteinizing hormone-independent differentiation of rat fetal Leydig cells.
2001 Feb 14
Changes in androgenic steroid profile due to urine contamination by microorganisms: a prospective study in the context of doping control.
2001 Feb 15
Progressive decrease in bone density over 10 years of androgen deprivation therapy in patients with prostate cancer.
2001 Jan
Long-term remission of ovarian hyperandrogenism after short-term treatment with a gonadotropin-releasing hormone agonist.
2001 Jan
Prevalence of polycystic ovary syndrome (PCOS) in first-degree relatives of patients with PCOS.
2001 Jan
Concentrations of steroid hormones in layers and biopsies of chelonian egg yolks.
2001 Jan
Insulin action and insulin secretion in polycystic ovary syndrome treated with ethinyl oestradiol/cyproterone acetate.
2001 Jan
Testosterone-induced inhibition of spermatogenesis is more closely related to suppression of FSH than to testicular androgen levels in the cynomolgus monkey model (Macaca fascicularis).
2001 Jan
Side of ovulation, hormones and sex ratios.
2001 Jan
The female-to-male transsexual patient: a source of human ovarian cortical tissue for experimental use.
2001 Jan
Short-term 17beta-estradiol decreases glucose R(a) but not whole body metabolism during endurance exercise.
2001 Jan
Effects of testosterone on production of perivitelline membrane glycoprotein ZPC by granulosa cells of Japanese quail (Coturnix japonica).
2001 Jan
Lysyl oxidase and MMP-2 expression in dehydroepiandrosterone-induced polycystic ovary in rats.
2001 Jan
Identification of twelve O-glycosylation sites in equine chorionic gonadotropin beta and equine luteinizing hormone ss by solid-phase Edman degradation.
2001 Jan
Androgen-dependent regulation of human angiotensinogen expression in KAP-hAGT transgenic mice.
2001 Jan
17beta-oestradiol acutely regulates Cl- secretion in rat distal colonic epithelium.
2001 Jan 1
Induction of nuclear transcription factors, cytochrome P450 monooxygenases, and glutathione S-transferase alpha gene expression in Aroclor 1254-treated rat hepatocyte cultures.
2001 Jan 15
Cross-talk between steroid-receptor-mediated and cell-membrane-receptor-mediated signalling pathways results in the in vivo modulation of c-Met and ornithine decarboxylase gene expression in mouse kidney.
2001 Jan 15
Expression of the 17beta-hydroxysteroid dehydrogenase type 5 mRNA in the human brain.
2001 Jan 22
Distribution of 17beta-hydroxysteroid dehydrogenases in human osteoblast-like cells.
2001 Jan 22
Phytoestrogens inhibit human 17beta-hydroxysteroid dehydrogenase type 5.
2001 Jan 22
Structure-function aspects and inhibitor design of type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3).
2001 Jan 22
Inhibitors of type II 17beta-hydroxysteroid dehydrogenase.
2001 Jan 22
Reproductive effects of valproate, carbamazepine, and oxcarbazepine in men with epilepsy.
2001 Jan 9
Effects of low-frequency magnetic fields on implantation in rats.
2001 Jan-Feb
Testosterone influences libido and well being in women.
2001 Jan-Feb
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment:: can also be injected https://www.drugs.com/pro/testosterone.html
Starting dose of testosterone gel is 50 mg of testosterone (4 pump actuations, two 25 mg packets, or one 50 mg packet), applied once daily in the morning.
Route of Administration: Topical
10 nM Testosterone significantly reduced secretion of BDNF in in human airway smooth muscle
Substance Class
Concept
Record UNII
UV7U6AQ9KP
Record Status Validated (UNII)
Record Version
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Name Type Language
TESTOSTERONE PALMITATE
Common Name English
Code System Code Type Description
WIKIPEDIA
Testosterone_palmitate
Created by admin on Sat Jun 26 06:37:48 UTC 2021 , Edited by admin on Sat Jun 26 06:37:48 UTC 2021
PRIMARY
FDA UNII
UV7U6AQ9KP
Created by admin on Sat Jun 26 06:37:48 UTC 2021 , Edited by admin on Sat Jun 26 06:37:48 UTC 2021
PRIMARY
PUBCHEM
164765
Created by admin on Sat Jun 26 06:37:48 UTC 2021 , Edited by admin on Sat Jun 26 06:37:48 UTC 2021
PRIMARY
This is a non-substance concept
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METABOLITE ACTIVE -> PRODRUG
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ACTIVE MOIETY
This is a non-substance concept