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Hormone · Profile

Testosterone

Testosterone Enanthate · Testosterone Cypionate · Testosterone Propionate · Testosterone Undecanoate

Sex Hormones & TRTPhase II
MW
288.4g/mol
Formula
C19H28O2

Testosterone is a steroid hormone classified as an androgen, primarily produced in the testes in males and in smaller amounts in the ovaries and adrenal glands in females. Researchers primarily study testosterone for its role in regulating muscle mass, strength, and various physiological processes. Key findings indicate that testosterone administration is associated with dose-dependent increases in muscle mass and strength, as well as changes in fat mass and certain biochemical markers. Additionally, studies suggest that different androgen-dependent processes exhibit varying testosterone dose-response relationships. Current research continues to explore the implications of testosterone levels in both clinical settings and the potential effects of testosterone replacement therapies on overall health.

Overview

Übersicht

Testosterone is a steroid hormone that is both endogenously produced and synthetically manufactured. It is primarily synthesized in the testes in males and in smaller amounts in the ovaries and adrenal glands in females. As a member of the androgen group, testosterone belongs to the chemical class of steroid hormones. Synthetic forms include testosterone enanthate, cypionate, and propionate, which are used in various therapeutic contexts. Researchers have observed that testosterone plays a crucial role in the development of male reproductive tissues, such as the testes and prostate, and in promoting secondary sexual characteristics like increased muscle and bone mass. It is also involved in regulating libido, energy levels, and immune function. Research areas include its effects on muscle mass, fat distribution, and cognitive functions. Testosterone exerts its effects by binding to androgen receptors, which then translocate to the cell nucleus and influence gene expression. This interaction initiates a cascade of biological processes that result in the development of male characteristics and various metabolic functions. The pharmacokinetic properties of testosterone vary by its form; for instance, testosterone enanthate and cypionate have longer half-lives due to their esterification, allowing for less frequent dosing. Testosterone is metabolized primarily in the liver and excreted in the urine. Clinically, testosterone and its esters are used in testosterone replacement therapy (TRT) for treating hypogonadism in males. Regulatory standing varies by country, with testosterone being a controlled substance due to its potential for abuse and performance enhancement.

Chemical profile

Chemische Struktur

Chemical structure of Testosterone
FormelC19H28O2
Molekulargewicht288.4g/mol
CAS-Nummer58-22-0
PubChem CID6013
Mechanism

Wirkmechanismus

Testosterone acts primarily on androgen receptors, which are part of the nuclear receptor family. Upon binding, these receptors influence the transcription of specific genes, leading to increased protein synthesis and muscle growth, among other effects.

Mechanism

Signalweg

Testosterone exerts its effects primarily through binding to androgen receptors (AR) in target tissues, initiating androgen receptor signaling pathways that regulate gene expression involved in muscle growth, protein synthesis, and fat metabolism. This interaction activates downstream signaling cascades, including the phosphoinositide 3-kinase (PI3K)/Akt pathway, which promotes muscle protein synthesis and increases fat-free mass, while also influencing hematopoiesis and lipid metabolism. Although the precise mechanisms are still being elucidated, the dose-dependent effects of testosterone on various androgen-dependent processes suggest a complex interplay of multiple signaling pathways.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~70 minutes

SCSubcutaneous

~8 days (enanthate ester)

IMIntramuscular

~14 days (cypionate ester)

TDTransdermal

Steady-state after 24-48h

POOral

Poor bioavailability due to first-pass

Testosterone enanthate and cypionate have longer half-lives due to esterification, allowing for extended release and less frequent dosing.

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Oil solution stable for 2+ years

Notes

Ensure vials are sealed properly to avoid contamination.

Solubility

Löslichkeit

Testosterone is soluble in oil, which is relevant for its formulation as injectable esters.

Legal Status

🇩🇪DE

Testosterone is a prescription-only medication (verschreibungspflichtig) and is listed under the Betäubungsmittelgesetz (BtMG) as a controlled substance.

🇺🇸US

Testosterone is FDA-approved for specific medical conditions and is classified as a Schedule III controlled substance by the DEA, requiring a prescription.

🇦🇺AU

In Australia, testosterone is classified as a Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

In the UK, testosterone is classified as a prescription-only medicine (POM) and is regulated by the MHRA.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Open Questions

Offene Forschungsfragen

Current evidence is limited regarding the specific dose-response relationships of testosterone across various androgen-dependent processes, particularly in diverse populations beyond healthy young men. Further research is needed to explore the long-term effects of different testosterone delivery methods on estradiol levels and hematocrit in hypogonadal men, as well as to assess the impact of supraphysiological doses on oral health and salivary gland function in both animal models and human subjects. Additionally, larger randomized controlled trials are necessary to clarify the effects of testosterone on cognitive function and mood, as current studies show inconsistent results.

65 Research Publications

4,469

Total Citations

33

Human/RCT

5.4

Avg. Influence

2025

Latest

Sort
Filter
#01

The effects of supraphysiologic doses of testosterone on muscle size and strength in normal men.

Bhasin S, et al. · The New England journal of medicine · 1996

HumanInfluence52.0
1044
The study demonstrated that supraphysiologic doses of testosterone, particularly when combined with exercise, significantly increased fat-free mass, muscle size, and strength in normal men.

Key findings

  1. 01Testosterone increased muscle size in both arms and legs compared to placebo.
  2. 02Participants combining testosterone with exercise gained more fat-free mass and strength than those who did not exercise.
  3. 03Mood and behavior remained unchanged across all groups.
#02

Testosterone dose-response relationships in healthy young men.

Bhasin S, et al. · American journal of physiology. Endocrinology and metabolism · 2001

HumanInfluence26.0
908
The study demonstrated that testosterone administration in healthy young men resulted in dose-dependent increases in fat-free mass, muscle size, strength, and power, while different androgen-dependent processes exhibited varying testosterone dose-response relationships.

Key findings

  1. 01Higher testosterone doses resulted in greater increases in fat-free mass and muscle strength.
  2. 02Changes in muscle size and strength were closely linked to testosterone levels.
  3. 03Sexual function and cognitive abilities did not significantly change with varying testosterone doses.
#03

Effect of testosterone on muscle mass and muscle protein synthesis.

Griggs R C, et al. · Journal of applied physiology (Bethesda, Md. : 1985) · 1989

HumanInfluence11.0
483
Researchers observed a 20% increase in muscle mass and a 27% increase in muscle protein synthesis following administration of pharmacological doses of testosterone enanthate in normal male subjects.

Key findings

  1. 01Muscle mass increased by 20% on average.
  2. 02Muscle protein synthesis increased by 27%.
  3. 03Total body potassium also increased significantly.
#04

Outcomes of long-term testosterone replacement in older hypogonadal males: a retrospective analysis.

HumanInfluence11.0
321
The study demonstrated that long-term testosterone replacement therapy in older hypogonadal males was well tolerated, with significant improvements in libido and a notable increase in hematocrit levels.
#05

Effect of testosterone cypionate on postexercise ST segment depression.

HumanInfluence7.0
156
Researchers observed that testosterone cypionate treatment significantly reduced postexercise ST segment depression in men with baseline ST segment abnormalities.
#06

Effects of testosterone replacement on sexual behavior in hypogonadal men.

HumanInfluence3.0
154
The study demonstrated that testosterone replacement improved sexual behavior in hypogonadal men, with a critical testosterone threshold identified between 2.0 and 4.5 ng/ml.
#07

Testosterone treatment comes of age: new options for hypogonadal men.

ReviewInfluence7.0
138
The review highlighted advancements in testosterone replacement therapy options for hypogonadal men, emphasizing the development of long-acting formulations that improve patient adherence and outcomes.
#08

Comparison of the kinetics of injectable testosterone in eugonadal and hypogonadal men.

HumanInfluence2.0
136
The study demonstrated that testosterone enanthate injections maintained eugonadal hormone levels in hypogonadal men for up to 11 days, supporting a dosing regimen of 200 mg every 10 to 14 days.
#09

Hormonal therapy of male hypogonadism.

ReviewInfluence5.0
115
The review highlighted that parenteral testosterone esters are the most effective treatment for male hypogonadism, with various administration methods available depending on individual patient needs.
#10

Low dose of cyproterone acetate and testosterone enanthate for contraception in men.

HumanInfluence2.0
103
Researchers observed that a low dose of cyproterone acetate combined with testosterone enanthate achieved azoospermia in a majority of men, suggesting potential for male contraception.

Clinical Trials (15)

Preclinical
Phase I
Phase II
Phase III
Approved

15

Total Trials

648

Total Enrolled

The Role of Follicle Stimulating Hormone in Advanced Prostate Cancer

NCT04134130COMPLETED
Sponsor

Lund University

Enrollment

33

Started

2019

Primary outcome

PSA-concentration

Prostate Cancer Recurrent

Perioperative Testosterone Replacement Therapy in Sarcopenic Male Colorectal Cancer Patients

Sponsor

London North West Healthcare NHS Trust

Enrollment

30

Started

2022

Primary outcome

Number of days required for a patient to be recruited on the study and how many patients are recruited

Colorectal CancerSarcopeniaHypogonadism, MalePerioperative CareTestosterone Replacement Therapy

Purification of Testis-Stimulating Factor in Precocious Puberty

NCT00004344COMPLETED
Sponsor

National Center for Research Resources (NCRR)

Enrollment

4

Started

1997

Precocious Puberty

A Study of Ejaculatory Dysfunction in Men With Low Testosterone Levels

NCT01419236Phase 2COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

76

Started

2011

Primary outcome

Change From Baseline in the Male Sexual Health Questionnaire-Ejaculatory Dysfunction-Short Form (MSHQ-EjD-SF) Ejaculatory Function Score at 16 Weeks

Ejaculatory DysfunctionHypogonadism

Effectiveness of Testosterone Undecanoate to Improve Sexual Function in Postmenopausal Women

NCT01724658Phase 2COMPLETED
Sponsor

Chulalongkorn University

Enrollment

70

Started

2012

Primary outcome

female sexual function index score

Female Sexual Dysfunction

Randomized Phase II Trial of Targeted Radiation With no Castration for Mcrpc

NCT06084338Phase 2RECRUITING
Sponsor

VA Office of Research and Development

Enrollment

60

Started

2023

Primary outcome

6-month radiographic progression-free survival (rPFS)

Prostate Cancer

Bipolar Androgen Therapy + Carboplatin in mCRPC

NCT03522064Phase 2RECRUITING
Sponsor

St Vincent's Hospital, Sydney

Enrollment

30

Started

2018

Primary outcome

PSA Response Rate

Castration-resistant Prostate CancerHomologous Recombination Deficiency

Study to Determine the Effect of Food on the Absorption of an Oral Testosterone Undecanoate Formulation

NCT00924612Phase 2COMPLETED
Sponsor

Clarus Therapeutics, Inc.

Enrollment

16

Started

2009

Primary outcome

Mean T Cavg25 Following Meals Containing Various Amounts of Dietary Fat Compared to Normal Fat Diet

Male Hypogonadism

Effect of Testosterone Treatment on Embryo Quality

NCT01662466Phase 1/2UNKNOWN
Sponsor

Center for Human Reproduction

Enrollment

180

Started

2012

Primary outcome

Clinical and Ongoing Pregnancy

Primary Ovarian InsufficiencyFemale Infertility Due to Diminished Ovarian Reserve

Testosterone Pellets Plus Vitamin D and E Versus Vitamin D and E Alone for the Treatment of Peyronie's Disease

NCT01578473Phase 1COMPLETED
Sponsor

Men's Health Boston

Enrollment

75

Started

2013

Primary outcome

penile curvature

Peyronie's Disease

A Study of Effect of Deodorant and Axillary Hair on Testosterone Absorption in Healthy Participants

NCT01725451Phase 1COMPLETED
Sponsor

Eli Lilly and Company

Enrollment

30

Started

2012

Primary outcome

Pharmacokinetics: Area Under the Concentration Curve (AUC) of Testosterone

Healthy Participants

A Pharmacokinetic (PK) Study to Compare the Absorption of Two Formulations of Transdermal Testosterone Spray and Intrinsa®

NCT01096329Phase 1TERMINATED
Sponsor

VIVUS LLC

Enrollment

16

Started

2010

Primary outcome

To measure the amount of testosterone in the blood after dosing

Hypoactive Sexual Desire Disorder

Bipolar Androgen Therapy to Restore Sensitivity to Androgen Deprivation Therapy for Patients With Metastatic Castration Resistant Prostate Cancer

NCT06305598Phase 1RECRUITING
Sponsor

Roswell Park Cancer Institute

Enrollment

14

Started

2024

Primary outcome

Androgen receptor (AR) activity

Castration-Resistant Prostate CarcinomaMetastatic Prostate CarcinomaStage IVB Prostate Cancer AJCC v8

Testosterone MD-Lotion Residual Washing Study

NCT00996151Phase 1COMPLETED
Sponsor

Acrux DDS Pty Ltd

Enrollment

10

Started

2009

Primary outcome

The amount of Testerone MD-Lotion 2% remaining on the axilla after a single dose application in healthy males who undergo a post dose washing procedure.

Hypergonadism

Steroid Profile: Differentiating Testosterone Administration From (Simultaneous) Ethanol Consumption

NCT04166786Phase 1COMPLETED
Sponsor

Parc de Salut Mar

Enrollment

4

Started

2019

Primary outcome

Change in steroid profile in urine

Healthy Volunteers

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This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer