Ostarine

CAS : CAS 841205-47-8

Supplied in : 10mg Pellet x 90

Specification : ≥ 99.36%

LGD-4033

CAS : CAS 841205-47-8

Supplied in : 10mg Pellet x 90

SARMS UK
Selective Androgen Receptor Modulators

Deep review of pharmacological properties, therapeutic potential, and challenges associated with SARMs in the UK.

The exact means by which this selectivity is achieved remain an area of focused research. Current evidence would imply that for each SARM, a specific conformational change in the AR that would expose a new surface for cofactor recruitment and have an impact on both the arrangement of an androgen-response element and AR binding in gene sequences. This differential gene activation could be tuned, therefore, theoretically so as to favor anabolic over androgenic pathways and provide most of the therapeutic benefits of androgens, while eliminating many of the side effects.

Clinical Applications of SARM Muscle-Wasting Disorders: The anabolic effects of SARMs on muscle tissue might have the potential to benefit people with conditions that involve the involuntary loss of muscles and the weakness that results from this loss, such as cachexia with cancer, chronic infection, and sarcopenia with renal failure.

Clinical trials with some SARMs demonstrated their ability to increase lean muscle mass and physical strength both in animal subjects and people who were carrying out the experiments, without the side effects usually induced by steroid-based drugs.

Osteoporosis: SARMs are also being studied for their potential use in treating osteoporosis as they allow new bone tissue to differentiate. This benefit becomes especially relevant compared to traditional treatments designed to prevent bone resorption, as it has the potential to increase bone density and thus lower the risk of suffering fractures.

Oncology Potential: New emerging research indicates that SARMs could be useful in the treatment of cancers that are hormone level-specific. For example, AR modulation has been promising in the management of types of breast cancers expressing the androgen receptors but responding poorly or not at all to traditional hormonal therapies. Challenges and Safety

But, with all the benefits that SARMs bring on board, they also come with their own baggage of problems. First, the long-term safety with these compounds has yet to be established. There are some concerns regarding the risk for cardiovascular events, liver toxicity, and hormonal disturbances.

Comparing AAS to SARMS

SARMs and anabolic steroids interact with androgen receptors, although there is a huge difference in the selectivity and the resulting effect, most often reflecting their different therapeutic and side effect profiles. Anabolic steroids, derivatives of testosterone, show characteristic effects not only on the growth of muscle tissue but also on the development of male secondary sexual characteristics, since they selectively activate androgen receptors found in muscular tissue.

This non-selective action underlies both its desired effects in muscle mass augmentation and its myriad adverse effects, including hepatotoxicity, changes in lipid profiles, and the promotion of masculinizing effects in females and children.

On the other hand, SARMs were designed to selectively target tissues in a bid to promote anabolic effects devoid of the far-reaching androgenic effects seen with steroids. Theoretical SARMs advantage: This compound can preferentially activate androgen receptors in muscles and bones and should not activate them in other tissues, like skin, liver, or the prostate.

It is in this activation that there are unwanted androgenic effects. This means a very favorable therapeutic profile for SARMs, since they increase muscle strength and health of the bone without these target cell nuclei’ normal side effects, unlike anabolic steroids.

Clinical Differences of SARMs and Testosterone

Clinically, whereas SARMs are still in the researching process and continuous studies are held to measure their clinical efficacy and safety profile more thoroughly, anabolic steroids have been used widely, and it reveals a strong efficacy with a well-known associated risk. Early clinical trials and anecdotal reports suggest potential for treating conditions such as muscle wasting and osteoporosis, but FDA approval and widespread clinical application remain pending.

Thus, both SARMs and anabolic steroids do their work by means of the androgen receptor-mediated mechanisms; however, the selectivity is dramatically different in between these two and therapeutic uses and their side-effect profiles are also drastically different.

Anabolic steroids elicit wide and potent anabolic effects but at the risk of great and often unacceptable side effects. In fact, the selectivity of SARMs may give them a safer profile with a more focused approach; however, comprehensive clinical evaluation is warranted for SARMs before being considered to be fully efficacious and safe. This fine balance between the effectiveness and side effects has remained at the core of pharmacological study and therapeutic development.

Further Reading : Systematic Review of Safety of Selective Androgen Receptor Modulators in Healthy Adults: Implications for Recreational Users

Anavar

Pharmacological differences between Oxandralone and SARMs

Anavar is a strong anabolic steroid derivative from dihydrotestosterone and synthetically produced with properties of powerful anabolic and minimal androgenic activity in the body.

It acts through its binding with the androgen receptors and enhances protein synthesis with an inhibition of proteolysis, thus producing increased lean body mass and decrease deposition of fats.

On the contrary, SARMs represent the distinct grouping of drugs purposed to realize anabolic benefits similar to androgenic steroids but with lessened androgenic impact.

These are the most selective agents for action on androgen receptors in specific tissues. While anabolic steroids such as Anavar, like SARMs, are promiscuous in activity and stimulate receptors all over the body, SARMs preferentially stimulate these receptors only in muscle and bone, with an eye towards decreasing the bigger overall number of side effects related to steroids.

SARM Profiles

Ostarine SARM

Detail	Link
PubChem CID (11326715)	PubChem
DrugBank (DB12078)	DrugBank
ChemSpider (9501667)	ChemSpider
UNII (O3571H3R8N)	UNII
KEGG (D10221)	KEGG
ChEMBL (ChEMBL1738889)	ChEMBL
PDB ligand (RLJ)	PDBe, RCSB PDB
CompTox Dashboard (DTXSID30233006)	EPA CompTox

Ostarine, also known by its developmental code MK-2866, represents a prototypical member of the selective androgen receptor modulators (SARMs) class of compounds.

Engineered to selectively target androgen receptors in skeletal muscle and bone, ostarine stands at the forefront of an emerging class of molecules designed with the intention of achieving the beneficial effects of androgens, such as testosterone, while minimizing untoward effects on other tissues.

The molecular design of ostarine allows it to preferentially induce anabolic activity in muscle and bone. This specific activity profile is derived from its ability to bind to the androgen receptors in these tissues more effectively than in others, such as the prostate, liver, and brain.

Consequently, ostarine has been the subject of considerable interest for its potential applications in treating a range of musculoskeletal conditions, including muscle wasting diseases associated with cancer, age, and other chronic conditions, as well as osteoporosis, where its ability to stimulate bone formation could prove beneficial.

Known side effects

Ostarine Clinical Studies

A Phase 2b clinical trial by Veru Inc. explores the use of enobosarm (ostarine) in combination with GLP-1 receptor agonists for the treatment of muscle loss in sarcopenic obese or overweight elderly patients. This study aims to validate enobosarm’s ability to preserve muscle and physical function while enhancing fat loss (globenewswire).
Another study presented by GTx at the Endocrine Society Annual Meeting evaluated the effects of ostarine in patients with cancer cachexia. The trial demonstrated significant improvements in lean body mass and muscle performance in the patients treated with ostarine compared to baseline (fiercebiotech).
GTx also conducted a Phase II clinical trial that was discussed in a press release from Business Wire. This study focused on cancer cachexia in patients suffering from various types of cancer, and found that ostarine treatment led to significant increases in lean body mass (businesswire).
The results from multiple clinical trials involving ostarine were summarized in a GlobeNewswire press release, indicating dose-dependent increases in muscle mass and reductions in fat mass across different patient groups, including elderly and cancer patients (globenewswire).
A further Phase 2b clinical trial by Veru Inc., as described on Finance Yahoo, aims to start in April 2024. This trial will investigate the effectiveness of enobosarm in preventing muscle loss and augmenting fat loss in elderly patients on GLP-1 RA therapy (finance.yahoo).

SARMs Clinical Safety

General Warning

Cardiovascular Risks: Notably, the reduction in high-density lipoprotein (HDL) cholesterol, potentially increasing the risk of cardiovascular diseases.
Hepatotoxicity: Manifestations include elevated liver enzymes, indicating liver stress or damage, which may be reversible upon discontinuation.
Endocrine Disruption: Suppression of natural testosterone production leading to symptoms such as fatigue, reduced libido, and mood changes, particularly in men.

Side Effect Profile

- Mild Liver Enzyme Elevations: Transient increases in liver enzymes that typically resolve after cessation of therapy.
- Headaches and Nausea: Occasional, non-severe headaches and gastrointestinal discomfort such as nausea.
- Hair Thinning: A less common side effect which may manifest as a reduction in hair density.
- Acne: Minor skin eruptions occasionally reported, reflecting subtle androgenic activity.

SARM Side Effect Profile

Cardiovascular Risks: Reduction in high-density lipoprotein (HDL) cholesterol, potentially elevating cardiovascular risk.
- Reference: Dalton, J. T., et al. “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.” Journal of Cachexia, Sarcopenia and Muscle 2.3 (2011): 153-161.
Hepatotoxicity: Increases in liver enzymes indicating potential liver stress or damage, which may be reversible with cessation of usage.
- Reference: Basaria, S., et al. “The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men.” Journals of Gerontology Series A: Biological Sciences and Medical Sciences 68.1 (2013): 87-95.
Endocrine Effects: Suppression of endogenous testosterone production leading to symptoms such as fatigue, mood disturbances, and decreased libido.
- Reference: Narayanan, R., et al. “Selective androgen receptor modulators in preclinical and clinical development.” Nuclear Receptor Signaling 6 (2008): e010.
Masculinizing Effects in Women: Potential masculinizing effects such as increased body hair and vocal changes, though less pronounced than with anabolic steroids.
- Reference: Jones, A., & Chen, J. “New therapeutic strategies for combating sarcopenia and frailty: emerging treatment options including SARMs.” Clinical Geriatrics 17.4 (2009): 26-33.
Psychological Impact: Mood swings and other changes in mental health.
- Reference: Cunningham, G. R., et al. “Testosterone replacement therapy and cardiovascular risk factors modification.” Aging Male 14.2 (2011): 83-90.