OSTARINE SARMs MK-2866

Ostarine SARMs (Selective Androgen Receptor Modulator). Investigational names: (MK-2866) GTx-024

Ostarine profile:

Androgens like testosterone regulate diverse physiological process involving both reproductive and non-reproductive functions.¹ Most of the signalling effects of androgens are mediated through the androgen receptor (AR), which has been a target for drug development focused on the treatment of pathological conditions resulting from abnormal androgen levels or altered target tissue responsiveness, the improvement of physical performance and the regulation of male fertility.¹

The primary focus for drug design has been the synthesis of chemicals to regulate the transcriptional activity of AR based on the structural and functional properties of the ligands, with a recent preference for selectively anabolic non-steroidals.¹ Nonsteroidal selective androgen receptor modulators (SARMs) are a new class of anabolic agents that bind the AR and exhibit tissue selectivity.² Ostarine is an orally bioavailable nonsteroidal SARM that elicits muscle-anabolic effects while only sparingly affecting reproductive tissues.³

The role of muscle androgen receptor (AR) in the anabolic effect of Ostarine has been previously investigated.⁴ For example, in mice subjected to orchidectomy and also lacking AR in the satellite cell lineage, Ostarine was effective in restoring androgen-sensitive levator ani muscle weights to sham levels. In control group, Ostarine was able to restore muscle-specific androgen-responsive gene expression reduced by orchidectomy (unaffected by androgen status in AR-lacking mice).⁴ Studies in rats demonstrated that Ostarine is completely absorbed, widely distributed, biotransformed through several metabolic pathways, and eliminated primarily as an unchanged compound.⁵

Ostarine has been also tested in Phase I, II and III trials with promising results in terms of improving lean body mass and measurements of physical function and power.² It was the first SARM to undergo phase III clinical trials to assess a SARM for muscle wasting in patients with cancer, and demonstrated a potential therapeutic application in the prevention and treatment of muscle wasting in patients with non-small-cell lung cancer.^2,3,6

The overall potential of Ostarine for clinical utility is demonstrated by its selective activity in anabolic tissues at low doses.In a phase II, double-blind, placebo-controlled study in healthy postmenopausal women and elderly men, use of Ostarine yielded significant improvements in LBM, physical function, and quality in life.³ Plasma pharmacokinetics of Ostarine has been characterized in detail; this SARM is well tolerated and poses very little risk of generating clinically relevant drug-drug interactions.⁶ Androgenic adverse events, including negative effects on the prostate, virilization and hirsutism, have not been reported.³

Description:

Formula : C19H14F3N3O3
Mol. Mass: 389.33 g/mol
Molecular Structure:

 Synonyms:

Ostarine, SARMs, Selective Androgen Receptor Modulator, MK-2866, GTx-024.

Physical Appearance:

White tablets.

Specificity:

Ostarine is capable to selectively interact with androgen receptors in certain tissues.

Purity:

>99.8% (HPLC analyzed).

Stability:

Store at at 20 °C in dry place until the expiration date.

Source:

Chemical Synthesis

Usage:

Product is prepared for LABORATORY RESEARCH USE ONLY. The product may not be used for other purposes.

References:

1. Zhang, et al. “Recent advances in the development of selective androgen receptor modulators.” Expert Opin Ther Pat. 2009 Sep;19(9):1239-58. doi: 10.1517/13543770902994397.  

2. Srinath, et al. “Enobosarm (GTx-024, S-22): a potential treatment for cachexia.” Future Oncol. 2014 Feb;10(2):187-94. doi: 10.2217/fon.13.273. 

3. Crawford, et al. “Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials).” Curr Oncol Rep. 2016 Jun;18(6):37. doi: 10.1007/s11912-016-0522-0. 

4. Dubois, et al. “Enobosarm (GTx-024) Modulates Adult Skeletal Muscle Mass Independently of the Androgen Receptor in the Satellite Cell Lineage.” Endocrinology. 2015 Dec;156(12):4522-33. doi: 10.1210/en.2015-1479. 

5. Kim, et al. “Absorption, distribution, metabolism and excretion of the novel SARM GTx-024 [(S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide] in rats.” Xenobiotica. 2013 Nov;43(11):993-1009. doi: 10.3109/00498254.2013.788233

6. Coss, et al. “Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin.” Invest New Drugs. 2016 Aug;34(4):458-67. doi: 10.1007/s10637-016-0353-8. 

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