Enobosarm (Ostarine)
Enobosarm, also known as Ostarine or MK-2866, is a selective androgen receptor modulator (SARM) developed to treat conditions like muscle wasting and osteoporosis. Research shows it can selectively stimulate muscle and bone growth without the severe androgenic side effects on other tissues typically seen with anabolic steroids.
01Dosing reference
02Mechanism of action
Androgen Receptor (AR) Binding
Enobosarm binds selectively to androgen receptors in the body.
Tissue-Selective Activation
It activates ARs primarily in skeletal muscle and bone tissue, while having minimal effect on reproductive organs like the prostate or sebaceous glands.
Anabolic Effects without Androgenic Side Effects
This selective action promotes muscle hypertrophy and bone density increases, offering potential therapeutic benefits for muscle wasting diseases with a lower risk profile than traditional steroids.
03Human evidence
Increased lean body mass and improved physical function in healthy elderly men and postmenopausal women.
A 12-week double-blind, placebo-controlled Phase II clinical trial showed dose-dependent increases in total lean body mass and improvements in stair climb power.
Prevention of muscle wasting in cancer patients.
Phase II and Phase III trials in patients with cancer cachexia demonstrated improvements in lean body mass, though some Phase III endpoints for physical function were mixed.
04Preclinical evidence
Increased bone mineral density and bone strength.
Ovariectomized rat models (simulating postmenopausal osteoporosis) showed improved bone parameters after Enobosarm administration.
Muscle preservation in castrated animal models.
Rodent studies demonstrated that Enobosarm maintained muscle mass and strength equivalent to intact animals without stimulating prostate growth.
05What is known vs. unknown
- Highly selective for muscle and bone tissue over other androgen-responsive tissues.
- Has been extensively studied in human clinical trials for muscle wasting and stress urinary incontinence.
- Does not aromatize into estrogen, reducing the risk of estrogenic side effects like gynecomastia.
- Can suppress natural testosterone production, especially at higher doses or longer durations.
- Long-term safety profile in humans remains incompletely characterized, as it is not FDA-approved.
- The exact threshold at which testosterone suppression becomes clinically significant varies among individuals.
- Potential for liver toxicity with prolonged use is still a subject of investigation.
06Safety & regulatory context
07Compared with Ligandrol (LGD-4033)
08Glossary
09Knowledge check
10Sources
- PubMed The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial
- PubMed Enobosarm (GTx-024) for the prevention and treatment of muscle wasting in patients with cancer
- PubMed Selective androgen receptor modulators in preclinical and clinical development
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