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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 a transdermal formulation of testosterone, a steroid hormone primarily produced in the testes in males and in smaller amounts in the ovaries and adrenal glands in females. Researchers primarily study testosterone topical for its role in addressing conditions related to testosterone deficiency, such as hypogonadism and developmental disorders like micropenis and scrotal hypoplasia. Key findings from recent studies indicate that testosterone gel formulations can lead to significant increases in serum testosterone levels and improvements in quality of life compared to traditional intramuscular injections. Clinical evidence suggests that topical testosterone may also enhance physical and emotional well-being while demonstrating efficacy in promoting penile and scrotal development in certain pediatric cases. Current research continues to explore the pharmacokinetics, safety, and long-term outcomes of testosterone topical applications, highlighting its growing relevance in hormone replacement therapy.

Overview

Übersicht

Testosterone topical, commonly known under brand names such as Androgel, Testogel, and Fortesta, is a synthetic form of the endogenous hormone testosterone. It is primarily produced in the testes in males and in smaller amounts in the ovaries and adrenal glands in females. Chemically, testosterone belongs to the class of steroid hormones known as androgens. It is used in testosterone replacement therapy (TRT) to treat conditions associated with low testosterone levels, such as hypogonadism.

The primary physiological role of testosterone includes the development and maintenance of male secondary sexual characteristics, such as increased muscle and bone mass, and the growth of body hair. Research has focused on its application in treating conditions like micropenis, hypogonadism, and scrotal hypoplasia. Researchers have also explored its efficacy in improving quality of life in testosterone-deficient individuals, including those with HIV.

Testosterone acts by binding to androgen receptors, which are distributed throughout various tissues in the body. This binding initiates a cascade of biological events that result in the modulation of gene expression, leading to the development of male characteristics and other physiological effects.

Pharmacokinetically, testosterone gel formulations like Androgel and Testim provide a more stable serum testosterone concentration compared to intramuscular injections, which can cause fluctuations. Testim has been found to offer higher bioavailability than Androgel, with greater serum levels of testosterone. Steady-state concentrations are typically achieved after 24-48 hours of application.

Clinically, testosterone topical is used for testosterone replacement therapy in men with conditions associated with a deficiency or absence of endogenous testosterone. It is approved by regulatory agencies like the FDA for this purpose, though its use must be monitored due to potential side effects and the risk of transference to others through skin contact.

Chemical profile

Chemische Struktur

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

Wirkmechanismus

Testosterone topical acts on androgen receptors, which are part of the nuclear receptor family of intracellular receptors. Upon binding, the testosterone-receptor complex translocates to the cell nucleus, where it influences the transcription of specific genes, leading to the development of male secondary sexual characteristics and other androgenic effects.

Mechanism

Signalweg

Testosterone topical formulations, such as AndroGel and Testim, 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 function. This activation leads to biological processes such as increased protein synthesis, muscle growth, and enhancement of libido, as well as the development of secondary sexual characteristics. While the precise mechanisms and downstream signaling pathways involved are not fully elucidated, the overall action of testosterone is recognized to influence various physiological functions, including spermatogenesis and maintenance of bone density.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~70 minutes

TDTransdermal

Steady-state after 24-48h

Testosterone gel formulations provide more stable serum levels compared to intramuscular injections, which have more pronounced peak-trough fluctuations.

Storage

Temperature

Store at room temperature (15-30C)

Light

Protect from light

Form

Gel formulation stable for use as directed

Notes

Avoid exposure to open flame or smoking until the gel has dried completely on the skin.

Solubility

Löslichkeit

Testosterone is soluble in organic solvents such as ethanol and oils, which are used in gel formulations.

Legal Status

🇩🇪DE

Prescription only (verschreibungspflichtig); not listed under BtMG.

🇺🇸US

FDA approved for testosterone replacement therapy; classified as a Schedule III controlled substance under the DEA.

🇦🇺AU

Schedule 4 (S4) prescription-only medicine under the TGA.

🇬🇧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 efficacy and safety of topical testosterone treatments, particularly in pediatric populations with conditions like micropenis and scrotal hypoplasia. Further research is needed to conduct larger randomized controlled trials (RCTs) to assess the long-term outcomes of testosterone therapy in these populations, including the impact on adult penile and scrotal development. Additionally, studies should focus on understanding the pharmacokinetic differences between various topical formulations and their effects on quality of life across diverse demographic groups, including those with underlying conditions such as HIV.

57 Research Publications

1,915

Total Citations

46

Human/RCT

2.4

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
626
Researchers observed that long-term treatment with AndroGel resulted in sustained improvements in sexual function, mood, body composition, and bone mineral density in hypogonadal men.
#02

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

HumanInfluence9.0
103
Researchers observed that clomiphene citrate showed comparable biochemical efficacy to testosterone gel replacement therapy in men with hypogonadism, while also being significantly less expensive.
#03

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
82
The study demonstrated that combining testosterone gel with sildenafil improved potency in men with low-normal testosterone levels who previously did not respond to sildenafil alone.
#04

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 the new testosterone gel formulation, Testim, resulted in significantly higher serum testosterone levels compared to AndroGel in hypogonadal subjects.

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.
#05

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.
#06

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

HumanInfluence3.0
73
The study demonstrated that testosterone augmentation improved negative symptoms in male patients with schizophrenia who had previously failed sildenafil treatment.
#07

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.
#08

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.
#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
60
The review indicated that testosterone therapy is beneficial for men with hypogonadism, particularly when clinical symptoms are present, and highlighted the advantages of newer delivery methods like gels.

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

Testosterone and erectile function in hypogonadal men unresponsive to tadalafil: results from an open-label uncontrolled study.

Case ReportInfluence2.0
59
Researchers observed that combination therapy with transdermal testosterone and tadalafil improved erectile function in hypogonadal men who were unresponsive to tadalafil alone.

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 Pharmaceuticals

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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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