In the last few years, there has been a significant surge in the acceptance of nonsteroidal Selective androgen receptor modulators (SARMs) as a promising alternative for testosterone replacement therapies.
A novel class of androgen receptor ligands, SARMs can be classified as synthetic drugs designed to have effects similar to those of Testosterone. They are believed to have the same kinds of effects as anabolic steroids but SARMs are much more selective in their action and this is exactly what differentiates them from steroids and other drugs. Some of the biggest advantages that help SARMs outscore over current therapies include androgen receptor specificity, tissue selectivity, oral bioavailability, flexibility of structural modification, and the lack of steroid-related side effects.
Here are excerpts from some pharmaceutical studies on SARMs that would be beneficial to understand their action mechanism and benefits.
- In a study conducted on one hundred twenty female Sprague-Dawley rats aged to twenty-three weeks, the rats were assigned to 12 treatment groups. Treatment with drugs was initiated on an immediate basis following ovariectomy and it continued for a period of 120 days. Dual energy x-ray absorptiometry measured body composition, whole body bone mineral density, and lumbar vertebrae BMD.
The study found that treatment with S4 (Andarine) was beneficial to maintain cortical content, and whole body and trabecular BMD. The S4 treatment also decreased body fat and increased body strength in these animals. It was further disclosed by this study that S4 had the ability to reduce the incidence of fracture via minimizing the incidence of falls through increased muscle strength and through direct effects in bone as compared to current therapies that are primarily antiresorptive in nature. The study also found that dosages of S4 were effective to increase lean mass and reduce body fat in intact and ovariectomized rats. It was also revealed that S4 provides the unique potential to prevent bone resorption, increase skeletal muscle mass/strength positions, and promote bone anabolism that makes it a possible new alternative for the treatment of osteoporosis.
Furthermore, the S4 treatment also had a positive effect on cortical bone and bone strength. In addition to this, S4 dose also proved effective to increase the differentiation of bone marrow cells towards the osteoblast lineage. This study also highlighted that S4 treatment resulted in a caused a significantly larger increase in total body bone mineral density than Dihydrotestosterone (DHT). Furthermore, the drug also significantly decreased plasma luteinizing hormone and follicle-stimulating hormone levels in castrated animals in a dose-dependent manner and demonstrated agonist activity in the pituitary.
- A different study revealed the clinical efficacy data for LGD-4033, MK-3984, MK-0773, and Enobosarm (GTx-024, Ostarine, and S-22) for the prevention and treatment of muscle wasting associated with cancer. A nonsteroidal SARM, Enobosarm was found to stimulate better physical function and increases in lean body mass across several populations along with a lower hazard ratio for survival in cancer patients. Results for the Phase III clinical trials entitled Prevention and treatment of muscle wasting in Patients with Cancer1 (POWER1) and POWER2 evaluating Enobosarm for the prevention and treatment of muscle wasting in patients with non-small cell lung cancer will likely establish Enobosarm as the first drug for the prevention and treatment of muscle wasting in cancer patients.
- A study on Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies disclosed that a number of nonsteroidal SARMs act as full agonists in muscle and bone and as partial agonists in prostate. This study reiterated the benefits of SARMs to improve bone health and physical function without affecting the prostate and cardiovascular outcomes.
The study highlighted that SARMs are extremely useful clinically to treat a wide range of health complications, including cancer cachexia, osteoporosis, aging and chronic disease, and frailty. This study also revealed that Selective Androgen Receptor Modulators have the ability to positively influence life of living beings that is prone to fractures, mobility limitation, physical disability, risk of falls, and poor quality of life.
- In another study, LGD-4033 (an oral selective androgen receptor modulator) was found to bind androgen receptor with high affinity and selectivity. During this study, 76 healthy men (21–50 years) were randomized to placebo or 0.1, 0.3, or 1.0 mg LGD-4033 daily for a period of 21 days as part of the placebo-controlled study. The researchers measured prostate-specific antigen, electrocardiogram, hormones, blood counts, chemistries, lipids, lean and fat mass, and muscle strength during and for 5 weeks after intervention.
It was found by the study that LGD-4033 (Anabolicum) was well tolerated. No drug-related serious adverse events were noticed during the study. This study disclosed that there was a long elimination half-life in the context of LGD. Furthermore, administration of LGD was associated with dose-dependent suppression of sex hormone–binding globulin, high density lipoprotein cholesterol, total testosterone, and triglyceride levels. The study also revealed that LGD had favorable pharmacokinetic profile, was safe, and increased lean body mass even during the short period without resulting in a change in prostate-specific antigen. The study also emphasized that LGD-4033 had the potential to increase periosteal bone formation, bone mineral density, and femur bending strength in preclinical models.
In short, it can be said that Selective androgen receptor modulators have been highly effective to treat health implicate and improve quality of life in more than just a way.