Cardarine (GW501516): Dosage, Benefits, and Side Effects

Cardarine, or GW501516, is a peroxisome proliferator-activated receptor delta (PPARD) agonist. However, it is often referred to as a SARM due to its similar anabolic and fat-burning effects.

Cardarine was recently formulated in 1992 and thus is classified as a research compound, similar to SARMs, with its effects not yet fully known and unapproved by the FDA.

However, early research has demonstrated cardarine’s positive effects on body composition and athletic performance, causing it to be banned in sports. The World Anti-Doping Agency (WADA) has added cardarine to its list of prohibited substances, placing it in the category of hormones and metabolic modulators.

Cardarine’s potent fat-burning effects provide initial promise for the medical community in the treatment of obesity. Increasing numbers of weightlifters are utilizing cardarine to retain muscle mass and enhance fat loss during cutting cycles.

Cardarine’s Legal Status

The FDA has yet to approve cardarine due to safety concerns. Thus, it is technically illegal for users to purchase cardarine in an attempt to improve their own body composition.

However, it is legal to purchase cardarine for research purposes. Such an instance would involve administering it to a group of rodents and observing its effects.

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Cardarine Benefits

Fat Loss

Cardarine enhances lipolysis by improving:

• Insulin sensitivity
• Lipid balance
• Glucose tolerance

Cardarine stimulates fatty acid oxidation by reducing the utilization of glucose, thus shifting energy metabolism. Consequently, the body will use fat stores as a primary energy source.

This causes a decrease in both subcutaneous and visceral fat mass in users, producing a leaner and more defined appearance. Decreases in visceral fat are desirable for users wanting to maintain a small waist, with high levels of visceral fat causing a protruding look to the stomach.

Dr. Anthony Hughes has cycled cardarine for over 15 years and describes it as a “miracle compound” after it increased his caloric burn by 30% per hour. He also reports that he has “never experienced any side effects.” Despite this being a very promising anecdotal report, researchers should use caution as each individual responds differently to PEDs.

Cardarine’s lipolytic effects are similar to SARMs used for cutting, such as ostarine. Anecdotally, we have found that cardarine’s fat-burning properties surpass its ability to build lean muscle tissue.

Cardarine’s positive effects on insulin and blood glucose may result in it being a potential treatment for type 2 diabetes in the future.

Muscle Hypertrophy

There is evidence of cardarine having mild anabolic effects, with a phase 2 study observing a 1.3 kg lean mass increase in users (1), following a dosage of 10 mg/day for 12 weeks. This modest increase in muscularity is similar to SARMs, although with less potency.

Muscle Endurance

We have seen Cardarine dramatically affect muscular endurance due to the remodeling of muscle tissue via mitochondrial biogenesis. Research indicates that cardarine facilitates the conversion of fast-twitch muscle fibers into slow-twitch fibers (2), thereby reducing a user’s susceptibility to fatigue during exercise.

Slow-twitch fibers are more efficient at utilizing oxygen due to the presence of mitochondria, enabling superior levels of adenosine triphosphate (ATP) production inside the muscle cells.

A study on mice found cardarine to increase endurance by 68% in just 3 weeks (3).

Consequently, if a person usually engages in 30 minutes of cardiovascular activity before tiring, a typical experience with cardarine would enable them to sustain 50 minutes of cardio before reaching the same degree of fatigue.

Cardarine’s effects on muscular endurance are quite remarkable. This effect may also indirectly aid fat burning when combined with regular cardiovascular training due to increased calorie burn.

In our experience, the majority of cardarine’s endurance-boosting results are temporary and will subside following cycle cessation. However, users may experience some permanent endurance improvements post-cycle due to cardiac muscle memory.

The level of endurance retained from a cardarine cycle will depend on whether the user continues cardiovascular training post-cycle.

Glycogen Storage

Cardarine increases intracellular glycogen storage, thus users can experience fuller muscles on-cycle.

This may be of use to bodybuilders or fitness models who require full muscle bellies onstage and are prone to glycogen depletion following calorie-restrictive diets. Increases in vascularity may also occur on cardarine due to decreased levels of extracellular fluid.

Improved Cholesterol

Based on our lipid profile tests, cardarine has cardioprotective properties, significantly increasing HDL cholesterol. This is a unique benefit compared to SARMs and anabolic steroids, which often cause negative cholesterol fluctuations.

• In the previous phase 2-cited study, HDL levels increased by 17%, with LDL cholesterol decreasing by 7% from a 10 mg/day dosage.
• Thus, stacking cardarine with SARMs or anabolic steroids may not only enhance body composition and performance but also reduce cardiac risk.

Cardarine’s ability to improve cholesterol may result in the PPARD agonist being a potential treatment for dyslipidemia in the future.

No Testosterone Suppression

Anabolic steroids and SARMs decrease endogenous testosterone levels, which is caused by overstimulation of the androgen receptor. However, PPARD agonists do not affect the hypothalamic-pituitary-testicular axis (HPTA), thus testosterone levels will remain stable on cardarine with no post-cycle therapy (PCT) required.

No Virilization in Women

Cardarine does not cause masculinization in women. Thus, if females are interested in losing subcutaneous fat, cardarine may be more optimal than anabolic steroids or SARMs for retaining feminine characteristics.

This is due to cardarine not affecting hormones, specifically testosterone, and thus preventing:

1. Hair loss
2. Clitoral enlargement
3. Breast reduction
4. Deepened voice box

Although cardarine does not cause masculinization effects in women, it does not mean it is safe for females to take, with it remaining a research chemical. In contrast, Anavar, for example, is well-tolerated among women and children in clinical trials. Thus, users are more informed regarding its effects.

We have observed incidents of virilization in women supplementing with Anavar to be rare when taken in conservative dosages and cycles. Thus, we consider Anavar to be a safer compound for promoting significant fat loss in comparison to cardarine, due to Anavar’s effects being well-known and studied over an extensive period of time.

Cardarine Side Effects

Cancer

In 2009, cardarine was withdrawn from further development after it produced cancer in all tested dosages, following long-term preclinical safety trials (4). Such tests are standard for safety evaluations, with approved medications passing such requirements.

Tumors were found in the following:

1. Thyroid
2. Liver
3. Bladder
4. Stomach
5. Skin
6. Tongue
7. Uterus
8. Eyes
9. Testes

Such trials have been criticized in the fitness community due to excessive dosages and the duration of use. The lowest dosage given to rodents was 5 mg/kg per day, which translates as 500 mg/day for a 100 kg human.

A 2-year cardarine cycle, as conducted in the research, is excessive compared to weightlifters’ cycles, who typically administer cardarine for 8 weeks.

Dr. Rand McClain is “skeptical” of this study, labeling the dosages as “extreme,” while pointing out that rodent genomics are different from humans. Dr. McClain also asserts that the rodents in these studies frequently endure unnatural living conditions, including overeating and sedentary behavior.

Liver Toxicity

In phase 1 and phase 2 human studies, cardarine demonstrated insignificant fluctuations in alanine transaminase (ALT) and aspartate transferase (AST) liver enzymes at dosages up to 10 mg/day.

However, Dr. Thomas O’Connor has treated patients who have used cardarine and consequently has likened its hepatotoxicity to the equivalent of taking “50 mg/day of Anavar.”

The reason for conflicting hepatic results in research and anecdotal data may be attributed to cardarine causing cellular proliferation. By stimulating cell growth and division, cardarine increases the overall cell count. This is an acceptable chemical process in a healthy person, but in the case of someone with an existing hepatic injury, cardarine may accelerate the death of liver cells (5).

We find cardarine is often taken by individuals who have also taken SARMs or anabolic steroids. This may explain such hepatic complications, as users are often combining cardarine with other hepatotoxic compounds.

Note: Anti-depressants and alcohol consumption may also be a lethal combination in conjunction with cardarine.

Thus, users should monitor their liver enzymes to be aware of the condition of this organ before any potential cellular proliferation occurs.

Insomnia

Some cardarine users report insomnia, indicating a stimulating effect on the central nervous system (CNS) and an increase in adrenaline output.

One methodology our patients implement to avoid this side effect is to consume doses earlier in the day, preferably in the morning, giving ample time for the CNS to regulate before sleep.

Although the CNS may become more aroused on cardarine, this effect is not believed to be excessive. Thus, cardarine does not replicate the jittery effects of more notorious thermogenic fat burners, such as clenbuterol. Instead, energy levels on cardarine remain stable while maintaining overall well-being in users.

Cardarine Dosage

As cardarine, or GW501516, has not been approved by the FDA for medicinal purposes, therefore no dosage guidelines have been established. However, in studies, researchers have administered up to 10 mg/day to participants.

Users utilizing cardarine for cosmetic purposes typically consume 10-20 mg/day (6). This is taken once per day and approximately 30 minutes before workouts to encourage fat oxidation during exercise.

Suitability of Stacking Cardarine

Due to cardarine’s cellular proliferation ability, it may not be suitable to stack it with hepatotoxic compounds, such as SARMs or oral anabolic steroids. Doing so may exacerbate their adverse effects on the liver, further elevating ALT and AST enzymes and increasing the risk of cholestatic hepatitis.

Short, one-off cycles of cardarine stacked with other hepatotoxic compounds may present low risk. However, due to a lack of medical research concerning such stacking protocols with cardarine, it may be wise to avoid such.

How to Take Cardarine

• Like SARMs, cardarine often comes as a liquid solution (20 mg/mL) or in tablet form (10 mg).
• Users can use a syringe to measure liquid cardarine before placing it in the mouth to swallow.

We have found that taking cardarine sublingually notably increases absorption (7) by letting it sit underneath the tongue for 10-15 seconds before swallowing. This method allows it to come into contact with the mucus membrane, allowing a more direct route into the bloodstream and thus greater biological availability.

Organizing workouts earlier in the day may be effective in reducing cardarine’s stimulating nature. Thus, consuming dosages prior to working out, preferably in the morning, will allow the central nervous system sufficient time to regulate before bedtime.

Cardarine Half-Life

The half-life of cardarine, or GW501516, is approximately 12–24 hours.

Cardarine on an Empty Stomach

Consuming cardarine on an empty stomach does not alter its biological availability. Thus, users may take it with or without food.

Cardarine Reviews

The following cardarine reviews were posted in our Facebook group and have been republished below.

I lost 40 pounds after a 3-month cycle of cardarine. I was losing 3 to 4 pounds per week! You want to be eating clean during supplementation. Also do cardio. You’ll cut weight like you’ve never seen. I didn’t notice any adverse effects. If muscle mass is important to you, stack it alongside Ostarine. Amazing compound.

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My extremely limited experience with Cardarine is pretty amazing. Jumped on the bike and rode hard for 60 minutes. Felt better the last 15 minutes than I did in the first 15 minutes. The weirdest thing is I’m not even breathing hard during the whole session. This is a 10ml dose.

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The endurance from GW is crazy however it gives no buzz so to speak or crash. It works straight away after the 1st dose but I’ve found the effects wear off over time so you have to increase the dosage however I’ve never gone over 30mg per day.

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I was massively suppressed on ostarine and cardarine. I think I went too low on my calories to boot. Looking forward to redoing bloods in a week or two.

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Summary

Cardarine, or GW501516, is a potent fat-burning compound. However, its effects on muscular strength and hypertrophy are minimal in our experience.

Cardarine’s ability to enhance muscular endurance is extraordinary (8). However, it is a prohibited substance by the World Anti-Doping Agency (WADA); therefore, Olympic athletes supplementing with cardarine are at risk of failing a drug test.

Cardarine remains a research chemical and is unlikely to receive FDA approval due to various dosages causing cancer.

The main reason weightlifters purchase cardarine is to burn fat and improve their body composition. However, these two objectives can be achieved naturally with a diligent exercise and diet plan. Thus, potentially increasing the risk of various cancers as a result of taking cardarine may be deemed unnecessary.

Eating in a small calorie deficit can produce similar fat-burning and muscle-retaining effects to cardarine. However, it may take longer to achieve identical results to cardarine when attempting to do so by natural means.

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