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RAD-150 benefits include enhancing muscle mass and strength while maintaining bone quality, contributing to overall physical performance and stability. It also supports sexual function, improves urinary health, and may lower the risk of cancer, promoting long-term well-being.
RAD-150, also known as TLB-150 Benzoate, is a remarkable compound which stabilizes the levels of testosterone. It works by mimicking the role of natural testosterone in your body. Because of esterification, a chemical reaction that forms at least one type of compound called ester (byproduct of acid and alcohol reaction), RAD-150 can last much longer in your body than its parent compound RAD-140 (about twice as long). Due to its high absorption rate, stability, and half-life of 48 hours, it offers a broad range of health benefits with little to no side effects and is significantly more effective than other selective androgen receptor modulators (SARMs).
RAD-150, a modified version of RAD-140 with an ester attachment for longer-lasting effects, is believed to support bone strength and quality by promoting anabolic activity in both muscle and bone tissues. It binds selectively to androgen receptors, stimulating bone mineral density improvements while preventing bone loss — a crucial factor for athletes, bodybuilders, and aging individuals looking to maintain structural integrity. This enhanced bone support, combined with its muscle-building properties, makes RAD-150 an appealing option for those seeking comprehensive physical performance and durability.
RAD-150, a modified version of RAD-140 (Testolone), is gaining attention not only for its muscle-building and fat-loss properties but also for its potential to improve sexual function. Its chemical structure includes an ester chain, which extends its half-life, providing more stable and sustained effects on androgen receptors throughout the body. This prolonged activation may enhance libido, sexual performance, and overall vitality by supporting healthy testosterone levels and promoting androgenic activity in tissues linked to sexual health. Users often report increased desire, stamina, and confidence, making RAD-150 an intriguing option for those seeking both performance enhancement and improved sexual well-being.
RAD-150 has also been shown to address sexual dysfunction due to various causes:
RAD-150, an esterified version of RAD-140 (Testolone), is designed to promote significant increases in muscle mass and strength. Its extended half-life allows for a more sustained release, keeping androgen receptors activated longer, which supports continuous muscle protein synthesis and enhanced nitrogen retention — both crucial for muscle growth. This results in steady, lean muscle gains with improved muscle density and definition, while also helping to increase lean muscle mass and boost overall strength and power output. Athletes and bodybuilders using RAD-150 often report faster recovery times, reduced muscle fatigue, and the ability to push through more intense training sessions, making it a powerful option for those looking to break through plateaus and maximize performance.
RAD-150, while primarily known for its muscle-building benefits, may also contribute to improved urinary health by supporting muscle integrity and tissue function around the bladder and pelvic floor. Stronger pelvic muscles can enhance bladder control, reducing the risk of urinary incontinence — especially in those experiencing muscle weakening due to aging or hormonal imbalances. Additionally, RAD-150’s anabolic properties might aid in promoting better tissue repair and reducing inflammation, which can further support healthy urinary function.
The use of RAD-150 appears to reduce the prevalence of urinary tract infections and treat other urinary problems:
RAD-150, a newer generation selective androgen receptor modulator (SARM), has shown potential in lowering the risk of cancer by promoting lean muscle growth and reducing visceral fat — both factors linked to improved metabolic health and decreased cancer risk. Additionally, its anabolic properties may support cellular regeneration and reduce chronic inflammation, which are key contributors to cancer development. However, while early research is promising, more clinical studies are needed to fully understand RAD-150’s role in cancer prevention.
Evidence suggests that RAD-150 and other SARMs have anti-cancer properties:
RAD-150, like other selective androgen receptor modulators (SARMs), offers impressive muscle-building and performance-enhancing benefits, but it’s not without potential side effects. One of the most common issues reported is hormonal suppression — RAD-150 mimics testosterone in the body, which can lead to a decrease in natural testosterone production. This may result in fatigue, low libido, and mood swings, particularly after discontinuation. Post-cycle therapy (PCT) is often recommended to help restore hormone levels and minimize these effects.
Another significant concern is liver strain and toxicity, especially with prolonged or high-dose use. While RAD-150 is designed to be more stable and efficient than older SARMs, it still undergoes liver metabolism, which can elevate liver enzymes like alanine aminotransferase (ALT) and aspartate aminotransferase (AST) — markers of liver stress. Users should monitor liver health regularly and avoid combining RAD-150 with other hepatotoxic substances, like alcohol or certain medications, to reduce the risk of long-term damage.
Lastly, cardiovascular effects are worth noting. SARMs, including RAD-150, can negatively impact cholesterol levels by lowering HDL (good cholesterol) and raising LDL (bad cholesterol), potentially increasing the risk of heart disease over time. Some users also report elevated blood pressure, which can further strain the heart and arteries. To counteract these risks, a heart-healthy diet, regular cardio exercise, and periodic blood work are essential. While RAD-150 shows promise as a safer alternative to anabolic steroids, its long-term safety profile remains under-researched, making careful, informed use crucial.
RAD-150 and RAD-140 are both powerful selective androgen receptor modulators (SARMs) designed to promote muscle growth, strength, and performance. RAD-140, known as Testolone, has gained popularity for its potent anabolic effects, offering rapid increases in muscle mass and strength while minimizing fat gain. RAD-150, on the other hand, is a newer, esterified version of RAD-140, designed to have a longer half-life, meaning it stays active in the body for an extended period. This allows for more stable blood levels, potentially leading to smoother, more sustained muscle growth without the need for frequent dosing.
One of the standout differences between the two compounds is absorption and metabolism. RAD-140 works quickly, making it a favorite for those seeking fast, noticeable gains, but it requires daily dosing. RAD-150’s ester modification slows down its release, providing a more consistent anabolic effect with less frequent dosing — typically every other day or even less. This longer half-life may also contribute to fewer hormonal fluctuations, reducing the risk of side effects like mood swings or energy crashes. However, this also means that RAD-150 takes longer to clear from the body, which could be a concern for those who undergo drug testing.
When it comes to side effects and overall experience, both SARMs carry similar risks, including testosterone suppression, potential liver strain, and cholesterol imbalances. However, anecdotal reports suggest that RAD-150’s smoother release may cause slightly less hormonal suppression and fewer mood-related side effects compared to RAD-140. That said, research on RAD-150 is still limited compared to the more extensively studied RAD-140. Ultimately, the choice between the two depends on personal goals: RAD-140 is ideal for faster results and shorter cycles, while RAD-150 offers a more prolonged, steady approach with potentially reduced side effects over time.
RAD-150, an esterified version of RAD-140, is designed to offer longer-lasting effects and a more stable release in the body. While this modification enhances its anabolic benefits for muscle growth and strength, it also raises concerns about liver toxicity. Like most SARMs, RAD-150 is metabolized by the liver, which can lead to increased liver enzyme levels — specifically alanine aminotransferase (ALT) and aspartate aminotransferase (AST) — indicators of liver stress. Although RAD-150 may be less hepatotoxic than traditional anabolic steroids, prolonged use or high doses could still strain liver function, particularly without proper cycle support.
One factor contributing to RAD-150’s potential liver toxicity is its extended half-life, which means the compound stays active in the body longer than non-esterified SARMs. This prolonged exposure may increase the liver’s workload over time, especially if users run longer cycles. Additionally, since SARMs are still under investigation and lack long-term human studies, the full extent of RAD-150’s impact on liver health remains unclear. For this reason, users should approach RAD-150 cautiously, particularly if they have pre-existing liver conditions or are using other performance-enhancing compounds that may also tax the liver.
To minimize liver toxicity risks, users are encouraged to incorporate liver support supplements — such as N-acetylcysteine (NAC), TUDCA, or milk thistle — during their RAD-150 cycle. Regular bloodwork is essential to monitor liver enzyme levels and catch any signs of liver stress early. Additionally, cycling off RAD-150 for sufficient recovery time helps ensure the liver can repair and regenerate. While RAD-150 offers impressive muscle-building potential, prioritizing liver health is crucial to avoid long-term damage and ensure sustainable results.
The recommended dosage of RAD-150 typically ranges between 10 to 20 mg per day for most users, depending on their experience level and fitness goals. Beginners often start with 10 mg daily to assess tolerance and minimize potential side effects, while more advanced users may push closer to 20 mg daily for enhanced muscle growth and strength. Due to RAD-150’s extended half-life — lasting around 48 hours — some users prefer to take it every other day rather than daily, maintaining stable blood levels without frequent dosing.
A standard RAD-150 cycle lasts between 8 to 12 weeks, though shorter cycles of 6 to 8 weeks are recommended for first-time users to gauge how their body responds. Longer cycles may amplify muscle gains, but they also increase the risk of testosterone suppression and liver stress. Users often adjust their dosage mid-cycle based on their progress, though gradually increasing the dose — rather than making sudden jumps — is safer to avoid unwanted side effects like fatigue, headaches, or hormone imbalance.
Since RAD-150, like other SARMs, can suppress natural testosterone production, post-cycle therapy (PCT) is highly recommended after completing a cycle. Even at lower doses, RAD-150’s potency can affect hormone balance, so a 4-week PCT using compounds like clomiphene (Clomid) or tamoxifen (Nolvadex) helps restore natural testosterone levels. To further support recovery, users should prioritize proper nutrition, hydration, and rest. Monitoring overall health — including liver function and testosterone levels — ensures a safer, more effective experience with RAD-150, promoting not just muscle gains but also overall well being throughout the cycle and recovery process.
RAD-150, also known as TLB-150 Benzoate, is a modified version of RAD-140 (Testolone) designed for enhanced anabolic activity and longer-lasting effects. It binds directly to androgen receptors in muscle and bone tissues, promoting lean muscle growth, strength gains, and faster recovery. Its extended half-life allows for more stable blood concentrations, which may lead to more consistent results throughout a cycle. This makes RAD-150 particularly appealing to fitness enthusiasts and bodybuilders aiming to build muscle mass without the water retention commonly seen with anabolic steroids. Additionally, fitness enthusiasts appreciate RAD-150’s ability to support strength gains and muscle recovery, making it a versatile option for both bulking and cutting cycles.
Beyond muscle gains, RAD-150 is known to enhance endurance and boost metabolism, helping users push through intense workouts while promoting fat loss. It supports a more shredded, vascular appearance by encouraging the body to preserve lean muscle tissue while burning fat for energy. This makes RAD-150 an attractive option during cutting cycles or recomposition phases, where maintaining muscle while shedding excess body fat is key. Its anabolic-to-androgenic ratio suggests that it delivers powerful muscle-building benefits without the severe androgenic side effects associated with traditional steroids, such as hair loss or prostate enlargement.
In addition to physical performance improvements, RAD-150 is believed to support cognitive function and neurological health, similar to RAD-140. Some users report increased focus, motivation, and mental clarity during their cycles — a potential advantage for athletes looking to stay sharp in both training and competition. Furthermore, RAD-150 is thought to speed up muscle recovery by reducing inflammation and muscle soreness, allowing users to train harder and more frequently. It may also contribute to bone density improvements, promoting stronger, more resilient skeletal structures — a key benefit for athletes and weightlifters alike. This combination of physical and mental benefits, along with potential bone density support, positions RAD-150 as a well-rounded performance enhancer, ideal for those seeking strength, endurance, fat loss, and faster recovery — all in one compound.
RAD-150 is not a steroid — it’s a Selective Androgen Receptor Modulator (SARM), specifically a modified version of RAD-140 (Testolone). Unlike anabolic steroids, which flood the body with synthetic hormones like testosterone, RAD-150 selectively binds to androgen receptors in muscle and bone tissues, mimicking the anabolic effects of testosterone without the widespread androgenic side effects. This selective action promotes muscle growth, strength gains, and fat loss, while minimizing unwanted effects like hair loss, prostate enlargement, or gynecomastia (male breast tissue growth) that are common with traditional steroids.
While both RAD-150 and anabolic steroids enhance muscle mass and performance, they work in fundamentally different ways. Steroids raise systemic testosterone levels, affecting nearly every part of the body — including organs and glands — which leads to a higher risk of side effects like liver damage, hormonal imbalance, and cardiovascular strain. In contrast, RAD-150 targets only muscle and bone tissues, aiming to stimulate growth and recovery with less impact on other bodily systems. Additionally, RAD-150’s longer half-life means more stable blood levels, reducing the need for frequent dosing compared to traditional steroids.
Another key difference lies in their legal status and medical background. Anabolic steroids are controlled substances in most countries due to their high potential for misuse and severe side effects, whereas RAD-150, like other SARMs, falls into the category of research chemicals or investigational compounds — not yet approved for human consumption by regulatory bodies like the FDA. Despite this, RAD-150 is increasingly popular among bodybuilders and athletes for its muscle-building properties and perceived safety advantages over steroids. However, it’s important to remember that SARMs, including RAD-150, can still suppress natural testosterone production and may require post-cycle therapy (PCT) to help restore hormone balance after a cycle.
RAD-150 doesn’t directly increase testosterone production — in fact, like many other Selective Androgen Receptor Modulators (SARMs), it can actually suppress natural testosterone levels. RAD-150 binds to androgen receptors in muscle and bone tissues, mimicking the effects of testosterone by promoting muscle growth, strength gains, and fat loss. However, because the body senses this artificial stimulation, it may reduce or halt its own testosterone production, thinking it already has enough androgenic activity. This suppression can vary depending on dosage, cycle length, and individual response. For those on a fitness journey, understanding this balance is crucial — managing testosterone suppression with proper cycle planning and post-cycle therapy (PCT) can help maintain results and support long-term progress.
During a RAD-150 cycle, users may feel the benefits of increased strength, endurance, and muscle recovery, which can mimic the effects of higher testosterone. However, this isn’t due to a rise in natural testosterone — it’s the SARM’s targeted anabolic activity that creates the illusion of elevated testosterone levels. Over time, though, the body may slow down its endogenous testosterone production, which can lead to fatigue, low libido, mood swings, and muscle loss after the cycle if proper recovery steps aren’t taken. For bodybuilders aiming to maximize gains while minimizing side effects, post-cycle therapy (PCT) is essential to help restore natural hormone balance and maintain results.
Once the RAD-150 cycle ends, testosterone levels may remain suppressed for weeks or longer, depending on how much and how long it was used. To help the body restore natural testosterone production, many users turn to post-cycle therapy (PCT) — a regimen typically involving Selective Estrogen Receptor Modulators (SERMs) like Clomid or Nolvadex to stimulate the testes and kickstart hormone production again. Without PCT, testosterone levels may recover slowly, leading to prolonged low energy, poor recovery, and muscle loss. While RAD-150 offers anabolic benefits with fewer androgenic side effects than steroids, adverse effects like hormonal imbalance, fatigue, or muscle loss can still occur without proper cycle planning and recovery support.
When using RAD-150 in liquid form, it’s crucial to measure the dosage accurately. Most liquid SARMs, including RAD-150, come with a dropper or syringe for precise dosing. A typical daily dose ranges between 5-15 mg, depending on your experience level and goals — beginners should start at the lower end to assess their body’s response. RAD-150 has a long half-life, meaning you only need to take it once a day. Many users prefer taking it in the morning to maintain stable blood levels throughout the day, though some opt to take it before workouts to potentially enhance performance.
RAD-150 liquid should be taken orally, not injected. The most effective way is to squirt the liquid directly into your mouth, ideally under the tongue for faster absorption, and then swallow. Some users choose to mix it with water or juice to mask the taste, which can be quite bitter. It’s important to avoid mixing it with hot beverages or food, as heat might degrade the compound’s potency. Additionally, always shake the bottle well before use to ensure even distribution of the compound, especially if the liquid has settled. A typical cycle lasts 8 to 12 weeks, and consistent dosing is key to maintaining stable blood levels for optimal results.
Most RAD-150 cycles last between 8 to 12 weeks, followed by Post-Cycle Therapy (PCT) to help restore natural testosterone production. It’s essential to stay hydrated, maintain a clean, high-protein diet, and monitor your body’s response throughout the cycle duration. Regularly check for signs of testosterone suppression or side effects, such as fatigue, mood changes, or decreased libido. Since RAD-150, like other SARMs, may stress the liver, consider liver support supplements and avoid alcohol or other hepatotoxic substances during your cycle. Always consult a healthcare professional before starting, especially if you have pre-existing conditions or are on other medications.
Yes, RAD140 suppresses natural testosterone production and may carry a risk of drug-induced liver injury, which is a concern with many oral selective androgen receptor modulators (SARMs). While it shows promise in inhibiting AR/ER+ breast cancer growth and enhancing efficacy with treatments like palbociclib, further clinical evaluation is needed to assess both its therapeutic potential and safety profile.
There’s no strong evidence of kidney damage from RAD140, but more research is needed. It’s known for promoting rapid muscle growth, which makes it popular among athletes and bodybuilders, though its safety and long-term effects, especially on hormone suppression and liver health, remain under investigation.
RAD140 promotes muscle growth, fat loss, and increased strength, making it a popular option for those looking to gain muscle mass quickly. However, its long-term effects and safety are still under investigation.
RAD140 may support neuroprotection and brain health in some studies, unlike traditional anabolic steroids, which are primarily focused on muscle growth and often come with more severe side effects.
It’s not known to cause direct kidney damage, but long-term effects are unclear, and acute liver failure remains a potential risk with prolonged or high-dose use.
It may cause mild liver strain, especially with prolonged use or high doses, but it’s also associated with muscle hypertrophy, promoting increased muscle size and strength.
It doesn’t aromatize, but hormone imbalances can still lead to gyno, which may affect athletic performance over time.
No, it suppresses natural testosterone rather than increasing it, though some users take it to improve athletic performance.
It can cause mild liver stress, so liver health should be monitored to avoid adverse reactions.
Some SARMs, including RAD140, can be mildly hepatotoxic, so it’s important to consult healthcare professionals before use.
Acetaminophen (Tylenol) is one of the most liver-toxic common drugs, so it’s essential to minimize risks by following dosage guidelines carefully.
No, enclomiphene is generally considered safe for liver health and may help the body recover natural testosterone production after SARM use.
Yes, it can trigger a positive test for performance-enhancing substances, often linked to enhanced strength and muscle growth.
It may promote neuroprotection and improve cognitive resilience, potentially supporting significant gains in brain health and function.
Yes, most SARMs suppress natural testosterone production, which is why they’re often paired with dietary supplements to support hormone recovery.
No, it suppresses testosterone like other SARMs, but a notable benefit is its potential to promote lean muscle growth with fewer androgenic side effects.
They typically stay detectable for 3 to 6 weeks, depending on the compound, with improved stability in longer-acting formulations.
A typical dose is 10-25 mg, so the milliliters depend on the concentration, but it’s important to monitor for adverse events.
Keep SARMs in a cool, dark place away from sunlight and heat, as preliminary research suggests this helps maintain their stability.
Solomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW. Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications. Sex Med Rev. 2019;7(1):84-94. doi:10.1016/j.sxmr.2018.09.006.
Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications
Selective androgen receptor modulators (SARMs) selectively bind to androgen receptors, promoting anabolic activity while minimizing the side effects of traditional anabolic steroids. They show promise in treating conditions like cachexia, hypogonadism, benign prostatic hyperplasia (BPH), and breast cancer, with early clinical studies reporting positive results — though no SARMs are yet FDA-approved. Researchers continue to explore their pharmacokinetics, safety, and potential therapeutic applications.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC6326857/.
Komrakova M, Nagel J, Hoffmann DB, Lehmann W, Schilling AF, Sehmisch S. Effect of Selective Androgen Receptor Modulator Enobosarm on Bone Healing in a Rat Model for Aged Male Osteoporosis. Calcif Tissue Int. 2020;107(6):593-602. doi:10.1007/s00223-020-00751-x.
Effect of Selective Androgen Receptor Modulator Enobosarm on Bone Healing in a Rat Model for Aged Male Osteoporosis
Enobosarm (ostarine, MK-2866) was tested in an orchiectomized rat model for aged male osteoporosis, comparing its effects on bone healing to testosterone. While both testosterone and enobosarm increased callus formation and muscle weight, testosterone showed stronger overall bone healing benefits without affecting prostate size, whereas enobosarm increased prostate weight and, when used as a therapy after fracture, actually impaired healing. Prophylactic enobosarm showed some positive effects on bone but needs further research due to potential hormonal side effects.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC7593387/.
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Discovery and therapeutic promise of selective androgen receptor modulators
Nonsteroidal selective androgen receptor modulators (SARMs) offer a promising alternative to traditional steroidal androgens for testosterone replacement therapy, providing better oral bioavailability, tissue selectivity, androgen receptor specificity, and fewer steroid-related side effects, making them more effective for maintaining muscle mass, bone mass, and male characteristics.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC2072877/.
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Novel, non-steroidal, selective androgen receptor modulators (SARMs) with anabolic activity in bone and muscle and improved safety profile
Non-steroidal, orally-active selective androgen receptor modulators (SARMs) like LGD2226 show promise as a novel treatment for osteoporosis by preventing bone loss, stimulating new bone formation, and improving bone strength in androgen-deficient models, while avoiding prostate enlargement and other steroid-related side effects — making them a potential alternative to traditional anti-resorptive therapies for both men and women.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/15758439/.
Gao W, Reiser PJ, Coss CC, et al. Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats. Endocrinology. 2005;146(11):4887-4897. doi:10.1210/en.2005-0572.
Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats
S-4, a selective androgen receptor modulator (SARM), demonstrated strong anabolic effects by restoring muscle mass, strength, lean body mass, and bone mineral density in castrated male rats, while minimizing androgenic effects on the prostate — highlighting its potential as a safer, tissue-selective alternative to traditional steroidal androgen therapies.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC2039881/.
Christiansen AR, Lipshultz LI, Hotaling JM, Pastuszak AW. Selective androgen receptor modulators: the future of androgen therapy?. Transl Androl Urol. 2020;9(Suppl 2):S135-S148. doi:10.21037/tau.2019.11.02.
Selective androgen receptor modulators: the future of androgen therapy?
Selective androgen receptor modulators (SARMs) are versatile small molecule drugs that act as androgen receptor agonists or antagonists, offering anabolic benefits with fewer side effects and good oral and transdermal bioavailability — showing promise as potential treatments for conditions like osteoporosis, Alzheimer’s, cancer, muscle wasting, and hypogonadism, though none are yet FDA-approved.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC7108998/.
Morimoto, M., Amano, Y., Oka, M., Harada, A., Fujita, H., Hikichi, Y., Tozawa, R., Yamaoka, M., & Hara, T. (2017). Amelioration of sexual behavior and motor activity deficits in a castrated rodent model with a selective androgen receptor modulator SARM-2f. PloS one, 12(12), e0189480. https://doi.org/10.1371/journal.pone.0189480.
Amelioration of sexual behavior and motor activity deficits in a castrated rodent model with a selective androgen receptor modulator SARM-2f
SARM-2f, a novel selective androgen receptor modulator, shows promise as a treatment for sarcopenia and cachexia by promoting muscle growth and improving physical function — including increased locomotor activity and restored sexual behavior — while minimizing prostate stimulation, thanks to its tissue-specific androgen receptor activity rather than tissue concentration.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC5720794/.
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Nonsteroidal selective androgen receptor modulators enhance female sexual motivation
Selective androgen receptor modulators (SARMs) show promise as a treatment for osteoporosis, muscle wasting, and hypoactive sexual desire disorder in postmenopausal women by promoting muscle growth and increasing sexual motivation, with certain B-ring modifications enhancing tissue selectivity and minimizing androgenic effects on the prostate.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC2913771/.
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Selective androgen receptor modulators as function promoting therapies
Selective androgen receptor modulators (SARMs) have evolved from steroidal to nonsteroidal compounds that selectively promote muscle and bone growth while minimizing effects on the prostate, showing promise as anabolic therapies for aging-related frailty, cancer cachexia, osteoporosis, and other conditions.
You can read the abstract of the article at https://pmc.ncbi.nlm.nih.gov/articles/PMC2907129/.
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Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer
Selective androgen receptor modulators (SARMs), particularly enobosarm (GTx-024), show promise as orally active, tissue-selective therapies for preventing and treating cancer-related muscle wasting, improving lean body mass and physical function without androgenic side effects; Phase III trials (POWER1 and POWER2) may soon establish enobosarm as the first approved drug for this indication.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/24189892/.
Bhasin S, Jasuja R. Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies. Current opinion in clinical nutrition and metabolic care. 2009;12(3):232-240. doi:10.1097/MCO.0b013e32832a3d79. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2907129/.
Selective Androgen Receptor Modulators (SARMs) as Function Promoting Therapies
Selective androgen receptor modulators (SARMs), especially nonsteroidal ones, are emerging as promising anabolic therapies that selectively promote muscle and bone growth while minimizing effects on the prostate and cardiovascular system, making them potential treatments for aging-related decline, chronic disease, frailty, cancer cachexia, and osteoporosis.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC2907129/.
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Anabolic agents: recent strategies for their detection and protection from inadvertent doping
The World Anti-Doping Agency (WADA) classifies anabolic agents — including anabolic androgenic steroids (AAS), clenbuterol, and selective androgen receptor modulators (SARMs) — as prohibited substances, with detection strategies evolving to catch doping and protect clean athletes. These methods include extending detection windows, using isotope ratio mass spectrometry, athlete biological passports, and identifying designer steroids. Efforts also focus on preventing inadvertent doping from contaminated supplements, meat, or natural products, alongside athlete education and improved testing methods to distinguish intentional from unintentional violations.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC4033149/.
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Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140
This report details the discovery and characterization of RAD140, a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM), demonstrating its anabolic effects in various preclinical models.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC4018048/.
Kadekawa, K., Kawamorita, N., Shimizu, T., Kurobe, M., Turnbull, P. S., Chandra, S., Kambara, T., Barton, J. C., Russell, A. J., & Yoshimura, N. (2020). Effects of a selective androgen receptor modulator (SARM), GSK2849466A, on stress urinary incontinence and bladder activity in rats with ovariectomy-induced oestrogen deficiency. BJU international, 125(6), 911–919. https://doi.org/10.1111/bju.15022.
Effects of a selective androgen receptor modulator (SARM), GSK2849466A, on stress urinary incontinence and bladder activity in rats with ovariectomy-induced oestrogen deficiency
In a rat model of stress urinary incontinence (SUI) induced by ovariectomy (OVX), selective androgen receptor modulators (SARMs) improved urethral continence by restoring baseline urethral pressure and enhancing urethral muscle function without affecting bladder function — effects that were more effective than dihydrotestosterone (DHT) treatment, suggesting SARMs as a promising therapy for SUI.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC7261644/.
Ponnusamy, S., Sullivan, R. D., Thiyagarajan, T., Tillmann, H., Getzenberg, R. H., & Narayanan, R. (2017). Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice. Journal of cellular biochemistry, 118(3), 640–646. https://doi.org/10.1002/jcb.25751.
Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice
Stress urinary incontinence (SUI), caused by weakened pelvic floor muscles, has limited treatment options and no oral therapies. This study tested two selective androgen receptor modulators (SARMs), GTx-024 and GTx-027, in a post-menopausal mouse model, showing that SARM treatment restored pelvic muscle weight to normal levels and suppressed muscle catabolism-related genes, suggesting potential for improving SUI symptoms and supporting their clinical evaluation.
You can read the full article at https://onlinelibrary.wiley.com/doi/10.1002/jcb.25751.
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Selective androgen receptor modulators: in pursuit of tissue-selective androgens
Selective androgen receptor modulators (SARMs) are designed to selectively activate androgen receptors in muscle and bone, promoting anabolic effects while minimizing androgenic effects on the prostate. Leveraging insights into androgen receptor structure and ligand interactions, SARMs show potential for treating conditions like male hypogonadism, osteoporosis, muscle wasting, frailty, burns, anemia, mood disorders, and prostate-related diseases.
You can read the abstract of the article at https://pubmed.ncbi.nlm.nih.gov/17086931/.
Nejishima H, Yamamoto N, Suzuki M, Furuya K, Nagata N, Yamada S. Anti-androgenic effects of S-40542, a novel non-steroidal selective androgen receptor modulator (SARM) for the treatment of benign prostatic hyperplasia. The Prostate. 2012; 72(14):1580-7. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/22430536.
Anti-androgenic effects of S-40542, a novel non-steroidal selective androgen receptor modulator (SARM) for the treatment of benign prostatic hyperplasia
S-40542, a tetrahydroquinoline (THQ) derivative, is a novel selective androgen receptor modulator (SARM) antagonist that binds to androgen receptors with high affinity and exhibits prostate-selective effects. It reduces prostate weight in both normal and benign prostatic hyperplasia (BPH) rat models while sparing muscle mass, unlike traditional antiandrogens like flutamide. S-40542 shows potential as a safer, more targeted treatment for BPH without affecting testosterone or luteinizing hormone levels, making THQ compounds valuable for future SARM research and development.
You can read the abstract of the article at https://onlinelibrary.wiley.com/doi/10.1002/pros.22511.
Christiansen AR, Lipshultz LI, Hotaling JM, Pastuszak AW. Selective androgen receptor modulators: the future of androgen therapy?. Transl Androl Urol. 2020;9(Suppl 2):S135-S148. doi:10.21037/tau.2019.11.02.
Selective androgen receptor modulators: the future of androgen therapy?
Selective androgen receptor modulators (SARMs) are small molecule drugs that act as tissue-specific androgen receptor agonists or antagonists, providing anabolic benefits while minimizing side effects seen with traditional androgen therapies. With strong oral and transdermal bioavailability, SARMs are being explored as potential treatments for various conditions, including osteoporosis, Alzheimer’s disease, cancer, stress urinary incontinence, hypogonadism, muscular dystrophy, and muscle wasting. Though no SARMs are currently FDA-approved, ongoing research shows promising therapeutic potential across multiple indications.
You can read the full article at https://pmc.ncbi.nlm.nih.gov/articles/PMC7108998/.
Yu Z, He S, Wang D. Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action. Clinical cancer research : an official journal of the American Association for Cancer Research. 2017; 23(24):7608-7620. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/28974548.
Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action
RAD140, an oral selective androgen receptor modulator (SARM), binds AR with high affinity and selectively activates AR in AR/ER+ breast cancer cells while sparing prostate cells. It suppresses the estrogen receptor (ER) pathway, including ESR1 gene expression, and inhibits tumor growth in AR/ER+ breast cancer xenograft models. When combined with palbociclib, RAD140 shows enhanced efficacy, suggesting its potential as a novel therapy for AR/ER+ breast cancer patients.
You can read the full article at https://aacrjournals.org/clincancerres/article/23/24/7608/79963/Selective-Androgen-Receptor-Modulator-RAD140.
Ziyang Yu, Suqin He, Jeffrey Brown, Chris Miller, Jamal Saeh, Gary Hattersley. RAD140, an orally available selective androgen receptor modulator, inhibits the growth of AR/ER positive breast cancer cell line- and patient-derived xenograft models [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 3608. doi:10.1158/1538-7445.AM2017-3608. Retrieved from http://cancerres.aacrjournals.org/content/77/13_Supplement/3608.
RAD140, an orally available selective androgen receptor modulator, inhibits the growth of AR/ER positive breast cancer cell line- and patient-derived xenograft models
RAD140, an oral nonsteroidal selective androgen receptor modulator (SARM), acts as a potent AR agonist in AR/ER+ breast cancer cells while avoiding activity in prostate cells. In preclinical studies using AR/ER+ breast cancer xenograft models, RAD140 significantly inhibited tumor growth, outperforming fulvestrant, and showed enhanced anti-tumor efficacy when combined with the CDK4/6 inhibitor palbociclib or the mTOR inhibitor everolimus. These findings highlight RAD140’s potential as a promising targeted therapy for AR/ER+ breast cancer.
You can read the abstract of the article at https://aacrjournals.org/cancerres/article/77/13_Supplement/3608/619400/Abstract-3608-RAD140-an-orally-available-selective.
Yu Z, He S, Wang D. Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action. Clinical cancer research : an official journal of the American Association for Cancer Research. 2017; 23(24):7608-7620. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/28974548.
Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action
RAD140, an oral selective androgen receptor modulator (SARM), binds to androgen receptors with high specificity, activating AR in AR/ER+ breast cancer cells while sparing prostate cells. In preclinical models, RAD140 inhibited tumor growth, suppressed the estrogen receptor pathway (including ESR1), and showed enhanced efficacy when combined with the CDK4/6 inhibitor palbociclib. These findings support further clinical evaluation of RAD140 as a promising treatment for AR/ER+ breast cancer.
You can read the abstract of the article at https://www.ncbi.nlm.nih.gov/pubmed/28974548.
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