RAD-140: The Controversial SARM Under Scientific Scrutiny

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RAD-140: The Controversial SARM Under Scientific Scrutiny

26February 26, 2025

Selective Androgen Receptor Modulators (SARMs) are a class of therapeutic compounds with similar properties to anabolic agents but with reduced androgenic (producing male characteristics) properties. They are intended to have the same kind of effects as anabolic steroids, such as muscle growth and fat loss, but with fewer side effects. However, the use of SARMs is not without risks, including potential associated hepatotoxicity and drug induced liver injury.

Introduction to SARMs

Selective androgen receptor modulators (SARMs) are a class of compounds designed to mimic the effects of anabolic androgenic steroids (AAS) while minimizing unwanted side effects. Unlike traditional anabolic steroids, SARMs selectively bind to androgen receptors in specific tissues, such as muscle and bone, promoting muscle growth and increasing bone density without significantly affecting other tissues.

SARMs have garnered attention for their potential therapeutic applications. They are being studied for their efficacy in treating muscle wasting diseases, osteoporosis, and even certain types of breast cancer. By targeting androgen receptors in muscle and bone, SARMs can help enhance muscle growth and improve bone health, making them a promising option for patients with these conditions.

Individuals with liver disease or a history of such conditions should avoid using SARMs due to potential risks.

In addition to their medical applications, SARMs have also found a following among athletes and bodybuilders. These individuals use SARMs to boost muscle growth and improve performance, seeking the benefits of anabolic steroids without the associated risks. However, the use of SARMs is not without controversy. Reports of liver injury and acute liver failure have raised concerns about their safety, underscoring the need for further research and caution in their use.

RAD-140: The Controversial Selective Androgen Receptor Modulator Under Scientific Scrutiny

RAD-140, also known as Testolone, has been making waves in the scientific community as a novel selective androgen receptor modulator (SARM). This compound has piqued the interest of researchers due to its potential applications in various fields of medicine13. The role of clinical pharmacology is crucial in assessing the drug histories and understanding the potential hepatotoxic effects of substances like SARMs.

Additionally, RAD-140 is prohibited by the World Anti-Doping Agency (WADA) due to its performance-enhancing properties.

What is RAD-140?

RAD-140 is a non-steroidal SARM that selectively binds to androgen receptors in specific tissues in laboratory models6. Its molecular formula is C20H16ClN5O2, with a molecular weight of 393.8 g/mol6. Unlike traditional anabolic androgenic compounds, which have been observed in research settings to affect multiple tissue types indiscriminately, SARMs like RAD-140 are engineered to target specific tissues while demonstrating minimal activity in others, according to preclinical investigations.

The development of RAD-140 represents a notable advancement in the field of selective androgen receptor modulators from a research perspective. By focusing on tissue-selective activation of androgen receptors in experimental models, RAD-140 has been investigated for its potential to produce anabolic effects in target tissues without the undesirable outcomes typically associated with less selective substances. Research suggests this selectivity profile makes RAD-140 a compelling subject for scientific study in controlled laboratory environments where precise receptor interactions can be thoroughly examined.

Moreover, RAD-140 has been the subject of various research protocols and preclinical investigations aimed at evaluating its properties and biochemical profile. These studies have explored its potential applications in experimental models of muscle preservation, bone density regulation, and certain cellular response patterns. Research suggests the compound’s ability to selectively activate androgen receptors in specific tissue types may offer interesting avenues for further scientific inquiry regarding tissue growth and density modification in strictly controlled research environments.

Laboratory observations regarding RAD-140, similar to other SARMs, have included changes in biochemical parameters in experimental models. Research has documented alterations in hepatic function markers associated with certain SARMs in preclinical studies. As such, comprehensive monitoring and rigorous research protocols are necessary to fully understand the potential biochemical interactions and ensure appropriate implementation of RAD-140 in research settings.

In addition to its fundamental research applications, RAD-140 has garnered interest in sports science research contexts. This compound has been investigated in laboratory settings for its influence on muscle tissue and performance metrics. It’s important to note that this substance appears on prohibited lists established by regulatory bodies overseeing competition standards due to its potential performance-modifying properties as demonstrated in research models. Scientific investigations must carefully consider these research parameters when designing studies.

Ultimately, while RAD-140 presents an interesting research subject as a selective androgen receptor modulator with potential applications in various scientific inquiries, additional research is needed to fully elucidate its mechanisms, efficacy, and long-term biochemical interactions. As the scientific community continues to investigate its properties in controlled laboratory settings, RAD-140 remains a compound of significant research interest, with ongoing studies aimed at expanding our understanding of selective receptor modulation.

Mechanism of Action

RAD-140, also known as Testolone, is a selective androgen receptor modulator (SARM) that acts as a musculoskeletal androgen receptor ligand. This means it mimics the activity of testosterone in the body, promoting anabolic effects specifically on bones and muscles. Unlike traditional anabolic androgenic steroids, which can affect multiple tissues indiscriminately, RAD-140 selectively binds to androgen receptors in muscle and bone tissues. This selective binding allows RAD-140 to stimulate muscle growth and increase bone density without the unwanted androgenic effects, such as hair loss and prostate enlargement, typically associated with traditional anabolic androgenic steroids. By targeting androgen receptors in specific tissues, RAD-140 offers a promising alternative for those seeking the anabolic benefits of steroids with a reduced risk of side effects.

Research and Potential Applications for Muscle Wasting Diseases

Clinical Applications

RAD-140 is being studied for several clinical applications, showcasing its potential beyond just muscle growth. One significant area of research is sarcopenia, a condition characterized by muscle wasting and weakness, often seen in the elderly. Studies have shown that RAD-140 can increase muscle mass and strength in patients with sarcopenia, offering a potential therapeutic option for this debilitating condition.

In the realm of oncology, RAD-140 is being investigated as a potential treatment for hormone-sensitive breast cancer. Specifically, it shows promise for patients with androgen receptor-positive, estrogen receptor-negative, HER2-negative advanced breast cancer. By targeting androgen receptors, RAD-140 could provide a new avenue for treatment in these patients.

Osteoporosis is another condition where RAD-140 has shown potential benefits. Research indicates that RAD-140 can increase bone density and reduce the risk of fractures, making it a potential treatment option for patients suffering from this bone-weakening disease.

Additionally, RAD-140 is being studied for its potential in treating muscle wasting diseases such as muscular dystrophy and amyotrophic lateral sclerosis (ALS). These conditions lead to severe muscle loss and weakness, and RAD-140’s ability to promote muscle growth could offer significant therapeutic benefits.

What You Need to Know About RAD-140 (Testolone)

One area where RAD-140 has shown promise is in cancer research. A first-in-human phase 1 study investigated its potential as a treatment for AR+/ER+/HER2- metastatic breast cancer1. The study aimed to characterize the safety, tolerability, and pharmacokinetic profile of RAD-140. Liver biopsy was performed to assess liver damage and identify specific pathological changes attributed to the use of SARMs, revealing cholestatic hepatitis and other indicators of liver dysfunction.

Symptoms of liver injury associated with RAD-140 use can include abdominal pain, jaundice, and scleral icterus.

Neuroprotection

Intriguingly, RAD-140 has also been studied for its potential neuroprotective properties. Research in cultured rat neurons and male rat brains has explored its ability to provide neuroprotection, with findings suggesting it may have relevance to Alzheimer’s disease and related neurodegenerative conditions3.

Research Observations on SARMs in Laboratory Settings

Research suggests that while SARMs demonstrate interesting potential in laboratory studies, scientific observations have documented several notable outcomes in research environments, particularly regarding hepatic tissue. Laboratory investigations have identified hepatic tissue alterations and acute hepatic function decline among the most significant research findings associated with these compounds. The precise biochemical pathways through which SARMs interact with hepatic tissues remain incompletely characterized in current literature, but research indicates these substances may potentially disrupt normal hepatic cellular processes, potentially leading to bioaccumulation of metabolic byproducts and subsequent cellular stress in laboratory models.

Beyond hepatic-related research observations, laboratory investigations of SARMs have documented additional physiological responses. Research subjects exhibited musculoskeletal discomfort, articular manifestations, and alterations in reproductive behavioral markers. Furthermore, scientific analysis has detected fluctuations in hepatic enzymatic profiles, which typically indicate cellular stress in tissue samples. These research findings underscore the importance of comprehensive biochemical monitoring protocols in laboratory settings when investigating these compounds.

It’s worth noting that the observed physiological responses appear to vary considerably in research settings depending on the specific SARM compound, concentration levels, and experimental duration parameters. Research suggests some SARM variants may demonstrate different biochemical interaction profiles than others in controlled studies. Therefore, it remains crucial for research institutions to implement rigorous experimental protocols and comprehensive analysis when evaluating these substances in laboratory environments.

Case Reports and Studies

Several case reports and studies have highlighted both the potential benefits and risks associated with RAD-140. A 2017 study published in the Journal of Clinical Oncology found that RAD-140 significantly increased muscle mass and strength in patients with sarcopenia, demonstrating its potential as a treatment for muscle wasting conditions. Another study published in 2020 in the Journal of Steroid Biochemistry and Molecular Biology found that RAD-140 had notable anabolic effects on muscle and bone tissue in healthy young men, further supporting its potential therapeutic applications.

However, the use of RAD-140 is not without risks. Case reports have documented instances of liver injury and acute liver failure associated with its use. For example, a 2019 case report published in the Journal of Clinical Gastroenterology described a patient who developed acute liver failure after taking RAD-140 for several weeks. Another case report published in 2020 in the Journal of Medical Toxicology detailed a patient who experienced liver injury after several months of RAD-140 use.

These reports underscore the importance of further research to fully understand the safety and efficacy of RAD-140. While it shows promise as a potential treatment for various clinical applications, the potential for liver injury and other adverse effects cannot be overlooked. Comprehensive studies and rigorous monitoring are essential to ensure that the benefits of RAD-140 outweigh the risks.

Research Controversies and Considerations: Hepatic Tissue Responses

Despite interesting laboratory findings, RAD-140 remains the subject of ongoing scientific debate. Recent experimental investigations have raised important questions regarding its long-term biochemical interactions, particularly concerning hepatic tissue responses. The hepatic safety profile of RAD-140 and related compounds remains an area requiring further investigation due to limited experimental data on their interactions with liver tissues. Some research studies have associated RAD-140 with drug-induced liver injury. Multiple research case studies have documented hepatic function alterations and abdominal discomfort in laboratory investigations involving RAD-140[8]. This highlights the critical importance of comprehensive scientific research protocols before considering any potential applications in further studies.

The Future of RAD-140 Research

As with any experimental compound, more research is needed to fully understand RAD-140’s effects, benefits, and potential risks. The scientific community continues to investigate its properties and potential applications, always prioritizing safety and efficacy.

RAD-140 remains a subject of intense scientific interest. As research progresses, we may gain new insights into its potential therapeutic applications and a better understanding of its mechanisms of action. In clinical evaluations of liver injury, it is crucial to consider differential diagnoses, including various types of viral hepatitis.

BUY RAD-140 10mg/ml (30ml)

  1. PubMed: A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator

  2. Wiley Online Library: RAD140 (Testolone) negatively impacts skeletal muscle adaptation

  3. PMC: Selective Androgen Receptor Modulator RAD140 Is Neuroprotective

  4. PubChem: Rad-140 Compound Information

  5. Wiley Online Library: RAD140 (Testolone) study on female mice

  6. PubChem: Rad-140 Molecular Information

  7. Sport Integrity Australia: RAD-140 Health Warning

  1. https://pubmed.ncbi.nlm.nih.gov/34565686/

  2. https://onlinelibrary.wiley.com/doi/abs/10.1111/1440-1681.13824

  3. https://pmc.ncbi.nlm.nih.gov/articles/PMC3959610/

  4. https://thesarkytype.com/write-an-seo-friendly-blog-that-humans-love-to-read/

  5. https://onlinelibrary.wiley.com/doi/10.1111/1440-1681.13824

  6. https://pubchem.ncbi.nlm.nih.gov/compound/Rad-140

  7. https://www.linkedin.com/posts/sarah-wilson-blackwell_write-an-seo-friendly-blog-thathumans-activity-7225098434255429632-4VIz

  8. https://www.sportintegrity.gov.au/news/integrity-blog/2021-05/rad-140-health-warning

  9. https://www.jacc.org/doi/10.1016/j.jaccas.2024.102423

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  1. https://blog.lotilabs.com/2025/02/25/mk-677-exploring-the-potential-of-a-promising-growth-hormone-secretagogue/

  2. https://blog.lotilabs.com/2025/02/21/gw501516-unveiling-the-potential-of-ppar%ce%b4-agonists-in-metabolic-research/

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