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OSTARINE

MODULATORS OF ANDROGEN RECEPTORS:
Androgenic compounds are famous for their uses in banned drugs for sportsmen but very few people have knowledge to link these compounds for therapeutic purposes. Although androgen receptor modulators have restricted legitimate uses compared to anabolic steroids, many of these are undergoing clinical trials, these Selective androgen receptor modulators (SARMs) proved to be far more specific in their activities as well. The increases in knowledge about these modulators lead to the assessment in preclinical and clinical studies against different diseases [1]. The structural diversity has been increased dramatically due to more application of SARMs for various modifying levels of androgen [2]. The ability of SARMs as therapeutics is reported to enhance by anabolic dissociation and androgenic activities [3]. In elder age the muscle wasting is being cured by using SARMs [4] therefore their uses at a larger scale lead to the better drug design [5]. Receptors of androgen are altered in a pleiotropic way [6] in order to produce promising drugs against ageing, andropause, hypogonadism, muscle wasting, sarcopenia and osteoporosis [7]. Keeping in mind this potential, these SARMs are becoming famous as potent and novel therapeutics [8].
 

OSTARINE:
Ostarine androgen receptor inhibitor
is manufactured by Merck and company it is also known by name Ostarine mk-2866 or GTx-024 that is based on the GTX company, this company is generating this molecule for treatment of muscle wasting, NSCLC having osteoporosis as well. Almost 70% of NSCLC cases linked with devastating muscle wasting and currently there is not any approved drug available for it, a new hope for many patients is SARM Ostarine. One can purchase Ostarine from any of the Ostarine suppliers for use in research and laboratory. Ostarine price is about $350 for a 10mg vial. IC50 for this inhibitor is present in form of ED50 that is 0.44 mg per day. The structure of Ostarine contains three fluorine molecules having anabolic action, however the cycle of this compound should be managed under careful and proper medical supervision. This drug is soluble in DMSO.
Ostarine is now considered as potential candidate for the treatment of Sarcopenia, this disease refers to the progressive loss of skeletal muscles which leads to the loss of strength and mobility [9]. For treatment in elder patients of frailty Ostarine is a hope [10], this drug was also made for the cachexia treatment [11] [12] as there are many other therapeutics are available for this disease [13].


CLINICAL TRIALS OF OSTARINE:
During preclinical studies Ostarine has also been used as contraceptive alternative for males [14] and went through preclinical studies [15] however more thorough studies are needed to support its use for this function. More than 5 clinical trials have been carried out by the parent GTX, Inc. company, in about 600 subjects three studies were done for the assessment of its safe dose and efficacy. During clinical trial phase II-B its action was noted against colorectal, breast, NSCLC, chronic lymphocytic lymphoma and non-Hodgkin’s lymphoma, where significant increase in muscle mass was seen, although with few side effects. All of these reports were re-confirmed by a research group working in phase II of clinical trials [16].
Treatment with Ostarine was noted effective in Cachexia cancer [17] therefore it was applied in phase 1 and 2 to cachexia patients [18]. Not only these phases but it also worked efficiently in phase III trials against cachexia [19] due to these results various researchers recommended the use of Ostarine [20] and all these findings forcing its candidature to be approved. Like other previous phases Ostarine also showed remarkable results for NSCLC patient’s treatment [19].
 
REFERENCES:
1. Narayanan, R.e.a., Selective androgen receptor modulators in preclinical and clinical development. Nucl Recept Signal., 2008. 6.
2. Zhang, X.e.a., Recent advances in the development of selective androgen receptor modulators. Expert Opin Ther Pat., 2009. 19(9): p. 1239-58.
3. Mohler, M.L.e.a., Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem, 2009. 52(12): p. 3597-617.
4. Lynch, G.S., New Emerging Drugs for Muscle Wasting. Expert Opinion on Emerging Drugs, 2008. 13(4): p. 655-673.
5. Zhang, X.e.a., Recent advances in the development of selective androgen receptor modulators. Expert Opinion on Therapeutic Patents, 2009. 19(9): p. 1239-1258.
6. Mohler, M.L.e.a., Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit. J Med Chem, 2009. 52(12): p. 3597-3617.
7. Mohler, M.L.e.a., Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates. Expert Opinion on Therapeutic Patents, 2005. 15(11): p. 1565-1585.
8. Segal, S.e.a., Therapeutic potential of the SARMs: revisiting the androgen receptor for drug discovery. Expert Opinion on Investigational Drugs, 2006. 15(4): p. 377-387.
9. Morley, J.E., Sarcopenia: Diagnosis and treatment. The Journal of Nutrition, Health & Aging, 2005. 12(7): p. 452-456.
10. Morley, J.E., Developing Novel Therapeutic Approaches to Frailty. Current Pharmaceutical Design, 2009. 15(29): p. 3384-3395.
11. Murphy, K.T.e.a., New emerging drugs for cancer cachexia. Expert Opinion on Emerging Drugs, 2009. 14(4): p. 619-632.
12. Dodson, S.e.a., Muscle Wasting in Cancer Cachexia: Clinical Implications, Diagnosis, and Emerging Treatment Strategies. Annual Review of Medicine, 2011. 62: p. 265-279.
13. Argilés, J.M.e.a., Novel approaches to the treatment of cachexia. Drug Discovery Today, 2008. 13(1-2): p. 73-78.
14. Jones, A.e.a., Preclinical characterization of a (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide: a selective androgen receptor modulator for hormonal male contraception. Endocrinology, 2009. 150(1): p. 385-95.
15. Jones, J.O.e.a., Improving selective androgen receptor modulator discovery and preclinical evaluation. Expert Opinion on Drug Discovery, 2009. 4(9): p. 981-993.
16. Cilotti, A.a.F., A., Male osteoporosis and androgenic therapy: from testosterone to SARMs. Clin Cases Miner Bone Metab, 2009. 6(3): p. 229-233.
17. Madeddu, C.a.M., G., An update on promising agents for the treatment of cancer cachexia. Curr Opin Support Palliat Care, 2009. 3(4): p. 258-62.
18. Zilbermint, M.F.a.D., A.S., Nonsteroidal selective androgen receptor modulator Ostarine in cancer cachexia. Future Oncol, 2009. 5(8): p. 1211-20.
19. Mantovani, G.e.a., Randomized Phase III Clinical Trial of Five Different Arms of Treatment in 332 Patients with Cancer Cachexia. The Oncologist, 2010. 15(2): p. 200-211.
20. Zilbermint, M.F.a.D., A.S., Nonsteroidal selective androgen receptor modulator Ostarine in cancer cachexia. Future Oncol., 2009. 5(8): p. 1211-20.

 

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Cat.No. Product Name Information Publications Customer Product Validation
S1174 Ostarine (GTx-024) Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3. (5)

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