MK-2866
Selective Androgen Receptor Modulator | Muscle Wasting Research
MK-2866 (Ostarine, Enobosarm) is a non-steroidal selective androgen receptor modulator (SARM) originally developed by GTx, Inc. (now Oncternal Therapeutics) for the prevention and treatment of muscle wasting and sarcopenia. It is the most extensively studied SARM in clinical trials, having progressed through Phase I, II, and III trials for cancer-related cachexia, stress urinary incontinence, and age-related muscle loss. MK-2866 selectively binds to androgen receptors in muscle and bone tissue with high affinity while exhibiting minimal activity in prostate and sebaceous glands, which differentiates it from traditional anabolic-androgenic steroids. Despite promising clinical data demonstrating significant lean body mass gains in cancer patients and elderly subjects, the FDA has not granted approval, and GTx's New Drug Application for stress urinary incontinence was not approved in 2018. MK-2866 remains classified as an investigational compound and is prohibited by WADA in competitive sports.
Moleküler Gösterim
M.W.: 389.33 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
MK-2866 binds to the androgen receptor (AR) with high affinity and selectivity, functioning as a partial agonist in muscle and bone tissue. Upon binding, the MK-2866-AR complex undergoes a conformational change that promotes nuclear translocation and interaction with androgen response elements (AREs) on DNA, activating transcription of genes involved in protein synthesis, nitrogen retention, and myogenic differentiation. The tissue selectivity of MK-2866 arises from its non-steroidal structure, which produces a distinct AR conformational change compared to testosterone or DHT. This results in differential coactivator and corepressor recruitment across tissues. In skeletal muscle, MK-2866 robustly activates anabolic signaling pathways including PI3K/Akt/mTOR, increasing muscle protein synthesis and reducing protein degradation via suppression of ubiquitin-proteasome and myostatin pathways. In bone, it stimulates osteoblast differentiation and mineralization. Critically, MK-2866 demonstrates reduced androgenic activity in prostate tissue and does not undergo 5-alpha reduction to a more potent metabolite (unlike testosterone), nor does it aromatize to estrogen, which accounts for its lower incidence of androgenic and estrogenic side effects.
MK-2866 (Ostarine, Enobosarm) is a non-steroidal selective androgen receptor modulator (SARM) originally developed by GTx, Inc. (now Oncternal Therapeutics) for the prevention and treatment of muscle wasting and sarcopenia. It is the most extensively studied SARM in clinical trials, having progressed through Phase I, II, and III trials for cancer-related cachexia, stress urinary incontinence, and age-related muscle loss. MK-2866 selectively binds to androgen receptors in muscle and bone tissue with high affinity while exhibiting minimal activity in prostate and sebaceous glands, which differentiates it from traditional anabolic-androgenic steroids. Despite promising clinical data demonstrating significant lean body mass gains in cancer patients and elderly subjects, the FDA has not granted approval, and GTx’s New Drug Application for stress urinary incontinence was not approved in 2018. MK-2866 remains classified as an investigational compound and is prohibited by WADA in competitive sports.
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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RAD-140
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Kaynaklar
- The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men (Dalton et al. - Ostarine Phase II) — Dalton, J.T., Barnette, K.G., Bohl, C.E., et al.
- Effects of Enobosarm on Muscle Wasting and Physical Function in Patients with Cancer: A Double-Blind, Randomised Controlled Phase 2 Trial — Dobs, A.S., Boccia, R.V., Croot, C.C., et al.
- Enobosarm (GTx-024) Phase III Clinical Trials for Cancer Cachexia: POWER 1 and POWER 2 — Crawford, J., Prado, C.M., Johnston, M.A., et al.
- Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies — Narayanan, R., Coss, C.C., Dalton, J.T.
- Pharmacology of Selective Androgen Receptor Modulators — Mohler, M.L., Bohl, C.E., Jones, A., et al.