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Hormone · Profile

Testosterone Topical

Androgel · Testogel · Fortesta · Axiron

Sex Hormones & TRTApproved
MW
288.4g/mol
Formula
C19H28O2

Testosterone topical is a synthetic formulation of the male sex hormone testosterone, primarily produced in the testes, and is administered through the skin via gels or patches. Researchers primarily study it for its role in testosterone replacement therapy, particularly in individuals with hypogonadism or related conditions. Key findings from various studies indicate that testosterone topical can lead to significant increases in serum testosterone levels and may improve physical and emotional well-being compared to traditional intramuscular injections. Additionally, clinical evidence suggests that topical testosterone may be effective in addressing conditions such as micropenis and scrotal hypoplasia, showing promising results in enhancing penile and scrotal development. Current research continues to explore its pharmacokinetics, safety, and long-term efficacy, highlighting its clinical relevance in managing testosterone deficiency.

Overview

Übersicht

Testosterone topical, commonly known by brand names such as Androgel, Testogel, and Fortesta, is a synthetic form of the naturally occurring sex 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 androgen class of hormones, testosterone plays a crucial role in the development of male reproductive tissues and the maintenance of secondary sexual characteristics. Researchers have explored its use in testosterone replacement therapy (TRT) for conditions such as hypogonadism, where the body does not produce enough testosterone. Additionally, testosterone topical has been investigated for its potential benefits in treating conditions like micropenis and scrotal hypoplasia. Its mechanism of action involves binding to androgen receptors, which then modulate the expression of specific genes, leading to the development and maintenance of male characteristics. The pharmacokinetic profile of testosterone topical shows that it provides a steady release of testosterone, achieving stable serum levels after 24-48 hours of application. It is metabolized primarily in the liver and excreted in the urine. Clinically, testosterone topical is used for TRT in men with low testosterone levels. It is approved for use in several countries and is subject to regulatory controls due to its potential for misuse. Researchers have found that it offers a more stable serum testosterone level compared to intramuscular injections, with fewer fluctuations and improved patient quality of life.

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 widely distributed in various tissues. This binding initiates a cascade of biological events, including the modulation of gene expression, leading to the development and maintenance of male secondary sexual characteristics and other physiological functions.

Mechanism

Signalweg

Testosterone topical formulations, such as gels, exert their effects primarily through binding to androgen receptors (AR) in target tissues, initiating androgen receptor signaling pathways that regulate gene expression involved in male sexual development and function. This interaction activates downstream signaling cascades, including the modulation of the cAMP/PKA pathway, leading to biological processes such as spermatogenesis, libido enhancement, and the development of secondary sexual characteristics. While the precise mechanisms of action may not be fully elucidated for all effects, the activation of AR is central to the therapeutic efficacy of testosterone replacement therapy.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~70 minutes

TDTransdermal

Steady-state after 24-48h

POOral

Poor bioavailability due to first-pass

Transdermal application provides a more consistent serum testosterone level compared to other routes like intramuscular injections.

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Gel formulation stable for use as directed

Notes

Ensure the container is tightly closed to prevent evaporation and contamination.

Solubility

Löslichkeit

Testosterone is soluble in organic solvents like ethanol, which is often used in gel formulations.

Legal Status

🇩🇪DE

Prescription only (verschreibungspflichtig); not listed under BtMG.

🇺🇸US

FDA approved for TRT; classified as a Schedule III controlled substance by the DEA.

🇦🇺AU

Schedule 4 (S4) prescription-only medicine.

🇬🇧UK

Prescription only medicine (POM); 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 long-term efficacy and safety of topical testosterone treatments, particularly in pediatric populations with conditions like micropenis and scrotal hypoplasia, where follow-up studies are necessary to assess adult outcomes. Further research is needed to explore the pharmacokinetic differences between various topical formulations, such as Testim and AndroGel, in larger randomized controlled trials to establish bioequivalence and optimal dosing strategies. Additionally, the potential risks of adverse events, such as priapism, associated with topical testosterone therapies require more comprehensive studies to clarify their incidence and underlying mechanisms.

86 Research Publications

2,684

Total Citations

64

Human/RCT

2.7

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
631
The study demonstrated 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.

AnimalInfluence5.0
160
Researchers observed that a novel ethosomal formulation enhanced testosterone transdermal absorption, achieving plasma concentrations within the physiological range using a significantly smaller application area compared to traditional nonpatch delivery systems.
#03

Beneficial effects of testosterone replacement for the nonmotor symptoms of Parkinson disease.

Human
141
The study demonstrated that testosterone gel improved testosterone deficiency symptoms and showed trends toward enhancing nonmotor and motor symptoms in men with Parkinson's disease.
#04

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

Case ReportInfluence9.0
104
The study demonstrated that clomiphene citrate was as effective as testosterone gel replacement therapy in increasing serum testosterone levels while being more cost-effective.
#05

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
84
The study demonstrated that combination therapy with testosterone gel and sildenafil significantly improved potency in men with low-normal testosterone levels who were unresponsive to sildenafil alone.
#06

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

HumanInfluence1.0
74
The study demonstrated that oral enclomiphene citrate increased serum testosterone and maintained sperm counts in obese hypogonadal men, unlike topical testosterone gel which reduced sperm concentration.
#07

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

HumanInfluence2.0
74
Researchers observed that percutaneous testosterone treatment significantly improved sexual function and psychological well-being in postmenopausal women with low libido, despite high serum testosterone levels.
#08

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 testosterone gel provides significantly higher serum levels of total and free testosterone compared to AndroGel, indicating that 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.
#09

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

HumanInfluence3.0
72
Researchers observed significant improvement in negative symptoms of schizophrenia in male patients receiving testosterone augmentation alongside antipsychotic medication compared to those receiving a placebo.
#10

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
64
The study demonstrated that testosterone therapy is beneficial for men with age-related hypogonadism when clinical symptoms are present, emphasizing the need for individualized treatment.

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.

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 InjuryHypogonadismHormonal Contraception

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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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