MK-2866 (Ostarine), also known as Enobosarm and GTx-024, is an investigational selective androgen receptor modulator (SARM). It is currently under evaluation in two pivotal phase III clinical trials for preventing and treating muscle wasting in animals with non-small cell lung cancer.

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WHAT IS MK-2866 (OSTARINE)?

MK-2866 (Ostarine) is a SARM with an aryl-propionamide structure. It is a non-steroidal compound not subjected to transformations typical of steroids: aromatization and reduction by aromatase and 5-α reductase.

MK-2866 (Ostarine), unlike other naturally occurring androgens, such as testosterone, is a compound that selectively activates the AR and belongs to the group of compounds whose development makes it possible to avoid adverse effects on receptors located in androgenic tissues, e.g., prostate.

In many preclinical animal models, MK-2866 (Ostarine) showed promising effects on lean body mass.

STRUCTURE OF MK-2866 (OSTARINE)

Molecular Formula: C₁₉H₁₄F₃N₃O₃

Molecular weight: 389.3 g/mol

CAS number: 841205-47-8

IUPAC name: (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide

MECHANISM OF ACTION

Based on clinical research in rats, MK-2866 (Ostarine) stimulates muscle tissue proliferation and differentiation via the androgen receptor.

During muscle development and growth, inactive satellite cells activate to proliferate myoblasts; then, myoblasts multiply and begin the differentiation process to allow for regenerating muscle tissue. Thus, new muscle fibers are formed by fusing mononuclear cells that form multinucleated myotubes, which mature into muscle fibers with hundreds of cell nuclei.

MK-2866 (OSTARINE) EFFECTS

Clinical studies with MK-2866 (Ostarine) show its potential for the following:

• Improving bone healing
• Modulating the functions of the uterus
• Regulating the metabolism of isolated rat adipocytes
• Treating muscle wasting and osteoporosis

MK-2866 (OSTARINE) SIDE EFFECTS

Some reported adverse effects from the use of MK-2866 (Ostarine) are:

• Heart attack
• Stroke
• Liver damage
• Mood swings
• Decreased testicular size
• Acne
• Headache
• Nausea
• Fatigue
• Back pain

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References:

1. Jones A, Coss CC, Steiner MS, Dalton JT (2013) An overview on selective androgen receptor modulators: focus on Enobosarm. Drugs Future 38(5):309–316

2. Komrakova M, Nagel J, Hoffmann DB, Lehmann W, Schilling AF, Sehmisch S. Effect of Selective Androgen Receptor Modulator Enobosarm on Bone Healing in a Rat Model for Aged Male Osteoporosis. Calcif Tissue Int. 2020 Dec;107(6):593-602. doi: 10.1007/s00223-020-00751-x. Epub 2020 Sep 2. PMID: 32876707; PMCID: PMC7593387.

3. Dobs AS, Boccia RV, Croot CC, Gabrail NY, Dalton JT, Hancock ML, et al. (2013) Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomized controlled phase 2 trial. Lancet Oncol 14(4):335–345

1. Dalton JT, Barnette KG, Bohl CE, Hancock ML, Rodriguez D, Dodson ST, et al. (2011) 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. J Cachexia Sarcopenia Muscle