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Hormone · Profile

Testosterone Topical

Androgel · Testogel · Fortesta · Axiron

Sex Hormones & TRTApproved
MW
288.4g/mol
Formula
C19H28O2

Testosterone topical refers to transdermal formulations of testosterone, primarily derived from the testes, that are applied to the skin to increase systemic testosterone levels. Researchers primarily study this hormone for its role in addressing testosterone deficiency, particularly in men with conditions such as hypogonadism and micropenis. Key findings from studies indicate that testosterone gel formulations, such as AndroGel and Testim, provide stable serum testosterone concentrations and improve quality of life metrics compared to intramuscular injections. Clinical evidence suggests that these topical preparations can enhance sexual desire, lean body mass, and overall well-being in hypogonadal men. Current research continues to explore the efficacy and safety of various testosterone gel formulations, highlighting their relevance in managing testosterone deficiency in clinical practice.

Overview

Übersicht

Testosterone topical, known commercially as Androgel, Testogel, and Fortesta, is a synthetic form of the endogenous androgen hormone testosterone. It is primarily produced in the testes in males and in smaller amounts in the ovaries and adrenal glands in females. As a member of the steroid hormone class, it is used in hormone replacement therapies, particularly for male hypogonadism. Researchers have focused on its ability to maintain stable serum testosterone levels when applied transdermally, offering an alternative to intramuscular injections. Testosterone plays a crucial role in the development and maintenance of male secondary sexual characteristics, muscle mass, and bone density. It is also involved in the regulation of libido and mood. Research has shown that testosterone topical is effective in treating conditions such as hypogonadism and micropenis by supplementing deficient testosterone levels. The mechanism of action involves binding to androgen receptors, which then translocate to the cell nucleus and influence gene expression. This interaction affects various physiological processes, including protein synthesis and muscle growth. Pharmacokinetically, testosterone topical provides a steady release of testosterone, achieving stable serum levels within 24 to 48 hours of application. It avoids the peaks and troughs associated with intramuscular injections, offering a more consistent therapeutic effect. Clinically, testosterone topical is approved for use in testosterone replacement therapy in men with hypogonadism. It is regulated by health authorities such as the FDA in the USA, and its use is subject to prescription requirements. Researchers have found it to be well-tolerated with fewer application site reactions compared to other forms like patches.

Chemical profile

Chemische Struktur

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

Wirkmechanismus

Testosterone topical acts by binding to androgen receptors, which are then translocated to the cell nucleus where they modulate gene expression. This cascade influences various biological processes, including the development of male secondary sexual characteristics and maintenance of muscle and bone mass.

Mechanism

Signalweg

Testosterone topical formulations, such as AndroGel, primarily exert their effects through binding to androgen receptors (AR) in target tissues, initiating androgen receptor signaling pathways that regulate gene expression involved in male sexual development and secondary sexual characteristics. This binding activates intracellular signaling cascades, including the MAPK pathway and PI3K/Akt pathway, leading to biological processes such as increased muscle mass, enhanced libido, and improved bone density. While the overall mechanism is well characterized, the precise details of all downstream effects and interactions with other signaling pathways remain incompletely understood.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~70 minutes

TDTransdermal

Steady-state after 24-48h

Topical formulations provide stable serum testosterone levels, avoiding peaks and troughs seen with other administration routes.

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Gel formulation stable for extended periods

Notes

Ensure cap is tightly closed to prevent evaporation.

Solubility

Löslichkeit

Testosterone is soluble in ethanol, which is used as a solvent in gel formulations.

Legal Status

🇩🇪DE

Prescription required (verschreibungspflichtig); not a controlled substance under BtMG.

🇺🇸US

FDA approved for testosterone replacement therapy; Schedule III controlled substance; prescription required.

🇦🇺AU

TGA Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

Prescription-only medicine (POM) under MHRA regulations.

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 long-term effects of topical testosterone therapy on adult penile length and function following treatment for micropenis in infancy and childhood, necessitating larger longitudinal studies to establish outcomes. Additionally, further research is needed to explore the pharmacokinetic differences between various testosterone gel formulations and their impact on quality of life across diverse populations, particularly in those with comorbid conditions such as HIV. There is also a need for randomized controlled trials comparing the efficacy and safety of topical testosterone versus alternative delivery methods, such as oral testosterone undecanoate, to clarify optimal treatment strategies for hypogonadal men.

62 Research Publications

2,082

Total Citations

47

Human/RCT

2.6

Avg. Influence

2025

Latest

Sort
Filter
#01

Long-term testosterone gel (AndroGel) treatment maintains beneficial effects on sexual function and mood, lean and fat mass, and bone mineral density in hypogonadal men.

HumanInfluence12.0
629
Researchers observed that long-term treatment with AndroGel maintained improvements in sexual function, mood, body composition, and bone mineral density in hypogonadal men.
#02

Testosterone ethosomes for enhanced transdermal delivery.

In VitroInfluence5.0
159
The study demonstrated that ethosomal formulations could enhance transdermal testosterone absorption in human skin, potentially addressing limitations of current testosterone therapies.
#03

Clomiphene citrate and testosterone gel replacement therapy for male hypogonadism: efficacy and treatment cost.

Case ReportInfluence9.0
103
The study demonstrated that clomiphene citrate (CC) provides comparable biochemical and clinical efficacy to testosterone gel replacement therapy (TGRT) for male hypogonadism at a significantly lower cost.
#04

Adjunctive use of AndroGel (testosterone gel) with sildenafil to treat erectile dysfunction in men with acquired androgen deficiency syndrome after failure using sildenafil alone.

HumanInfluence1.0
83
Researchers observed that combination therapy with testosterone gel and sildenafil significantly improved potency in human men with low-normal testosterone levels who previously failed sildenafil alone.
#05

Evaluation of the pharmacokinetic profiles of the new testosterone topical gel formulation, Testim, compared to AndroGel.

Marbury T, et al. · Biopharmaceutics & drug disposition · 2003

HumanInfluence9.0
73
The study demonstrated that Testim provided higher serum testosterone levels and greater bioavailability compared to AndroGel, indicating they are not bioequivalent.

Key findings

  1. 01Testim resulted in 30% higher total testosterone levels than AndroGel.
  2. 02Testim showed 19% higher dihydrotestosterone levels compared to AndroGel.
  3. 03Testim provided 38% higher free testosterone levels than AndroGel.
#06

Treatment with percutanous testosterone gel in postmenopausal women with decreased libido--effects on sexuality and psychological general well-being.

HumanInfluence2.0
73
The study demonstrated that percutaneous testosterone gel significantly improved sexual function and psychological well-being in postmenopausal women with low libido.
#07

Short-term testosterone augmentation in male schizophrenics: a randomized, double-blind, placebo-controlled trial.

HumanInfluence3.0
72
The study demonstrated that testosterone augmentation improved negative symptoms in human men with schizophrenia, suggesting a potential therapeutic strategy.
#08

Oral enclomiphene citrate raises testosterone and preserves sperm counts in obese hypogonadal men, unlike topical testosterone: restoration instead of replacement.

HumanInfluence1.0
72
The study demonstrated that enclomiphene citrate effectively raises testosterone levels and preserves sperm counts in obese hypogonadal men, unlike topical testosterone gel.
#09

Testosterone therapy--what, when and to whom?

Jockenhövel F · The aging male : the official journal of the International Society for the Study of the Aging Male · 2004

ReviewInfluence1.0
63
Researchers observed that testosterone therapy is necessary for men with low testosterone production due to primary or secondary hypogonadism, especially in those with clinical symptoms.

Key findings

  1. 0115-25% of men over 50 may have low testosterone levels.
  2. 02New testosterone gel shows high patient satisfaction and fewer side effects.
  3. 03Intramuscular testosterone undecanoate requires fewer injections and maintains stable hormone levels.
#10

Three-year follow-up of androgen treatment in hypogonadal men: preliminary report with testosterone gel.

Case ReportInfluence3.0
62
The study demonstrated that testosterone gel treatment maintained positive effects on muscle, bone, and mood over three years in hypogonadal men.

Clinical Trials (12)

Preclinical
Phase I
Phase II
Phase III
Approved

12

Total Trials

8,617

Total Enrolled

ESPRIT Study in Hypogonadal Men

NCT01143818COMPLETED
Sponsor

Abbott

Enrollment

1,053

Started

2007

Primary outcome

Percent Change From Baseline to Month 6 in Aging Male Symptoms (AMS) in Mean Total Score

Hypogonadism

A Study to Evaluate the Effect of Testosterone Replacement Therapy (TRT) on the Incidence of Major Adverse Cardiovascular Events (MACE) and Efficacy Measures in Hypogonadal Men

NCT03518034Phase 4COMPLETED
Sponsor

AbbVie

Enrollment

5,246

Started

2018

Primary outcome

Time From Randomization to the First Component Event of Major Adverse Cardiac Event (MACE): Number and Percentage of Participants With an Event

HypogonadismCardiovascular Diseases

A Study of the Effect of Testosterone Replacement Therapy on Blood Pressure in Adult Male Participants With Hypogonadism

NCT04456296Phase 4COMPLETED
Sponsor

Endo USA Inc., a Keenova Therapeutics Company

Enrollment

673

Started

2020

Primary outcome

Change From Baseline in 24-Hour Average Systolic Ambulatory Blood Pressure to End of Study (EOS)

HypogonadismHypogonadism, MaleHypogonadotropic Hypogonadism

A Study of the Effect of Topical Testosterone Replacement Therapy on Blood Pressure in Adult Male Participants With Hypogonadism

NCT04274894Phase 4COMPLETED
Sponsor

AbbVie

Enrollment

246

Started

2020

Primary outcome

Change From Baseline to End of Treatment (EOT) in 24-hour Average Systolic Blood Pressure (SBP)

Hypogonadism

Adaptions and Resiliency to Multi-Stressor OpeRations

NCT06455969Phase 4RECRUITING
Sponsor

Bradley Nindl

Enrollment

120

Started

2024

Primary outcome

Biomechanical: Tendon Cross-Sectional Area, change from baseline and throughout training, mean

Musculoskeletal InjuryHypogonadism

Efficacy and Safety of Oral Testosterone Undecanoate in Hypogonadal Men

NCT03198728Phase 3COMPLETED
Sponsor

Marius Pharmaceuticals

Enrollment

314

Started

2017

Primary outcome

Percentage of Male Hypogonadal Subjects With Average NaF/EDTA Plasma Total Testosterone (T Cavg) Within the Normal Range Using Oral SOV2012-F1.

Hypogonadism, Male

A Study of Oral Testosterone Undecanoate (TU) in Hypogonadal Men

NCT02722278Phase 3COMPLETED
Sponsor

Clarus Therapeutics, Inc.

Enrollment

222

Started

2016

Primary outcome

Number of Oral TU Treated Subjects Who Have a Total T Cavg in the Eugonadal Range of 252 to 907 ng/dL at Visit 7

Hypogonadism

Bioequivalence Study of Test and Reference Testosterone Topical Gel, 1.62% Metered Pump in Testosterone Deficient Adult Male Subjects Under Fasting Conditions

NCT02110368Phase 3COMPLETED
Sponsor

Amneal Pharmaceuticals, LLC

Enrollment

32

Started

2014

Primary outcome

AUC0-t

Primary HypogonadismHypogonadotropic Hypogonadism

Effects of Early Testosterone Gel Administration on Physical Performance in the Critically Ill

NCT05825092Phase 2RECRUITING
Sponsor

University Hospital, Clermont-Ferrand

Enrollment

600

Started

2023

Primary outcome

the 6-minute-walk distance test (6MWD)

Critical Illness

A One Year Open Label Study for the Treatment of Hypogonadism (Low Testosterone) in Men Who Have Completed ZA-203

NCT01386567Phase 2COMPLETED
Sponsor

Repros Therapeutics Inc.

Enrollment

48

Started

2011

Primary outcome

Change in testosterone comparing Androxal to Testim

HypogonadismLow Testosterone

To Evaluate Sperm Parameters in Men With Secondary Hypogonadism Previously Treated With Topical Testosterone

NCT00706719Phase 2COMPLETED
Sponsor

Repros Therapeutics Inc.

Enrollment

17

Started

2008

Primary outcome

Sperm Concentration

Secondary Hypogonadism

Pharmacokinetics of a Novel Vaginal Delivery System for Testosterone and Dehydroepiandrosterone (DHEA)

NCT03967964Phase 1COMPLETED
Sponsor

Laboratorios Andromaco S.A.

Enrollment

46

Started

2015

Primary outcome

Testosterone: Area under the serum concentration time curve (AUC0-72)

PharmacokineticsHormone Deficiency

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Legal Disclaimer

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