Cardarine Key Points
- Enhances Fat Oxidation
- Remodels Muscle Fiber Type
- Improves Endurance
- Improves Lipids
- Failed Safety Study. Possible Carcinogen.
Cardarine was developed by the U.S. biotechnologies firm Ligand Pharmaceuticals. This drug came about as part of an agreement the company signed with GlaxoSmithKline (GSK) in 1992, which focused on developing drugs jointly for the treatment of cardiovascular diseases. As subject to this agreement, GSK would obtain worldwide exclusive rights to cardarine. GSK would fund further development, and Ligand would receive substantial royalties and milestone payments as the drug progressed through investigatory stages.
The first appearance of cardarine in the medical literature came in 2001, when its effect on reverse cholesterol transport was investigated. For several years, there appeared to be a flurry of research activity around this agent. The drug appeared in numerous animal studies, and then entered Phase I human trials. Ligand announced the receipt of a $1 million milestone payment in 2004, when GSK then announced the decision to progress to Phase II trials. The drug seemed to be on a strong development track. However, it was discontinued in 2009, when long-term animal studies revealed a carcinogenic effect (see: Description).
In 2013, the World Anti Doping Agency (WADA) issued a press release warning the public about the "serious toxicities" that were discovered during pre-clinical testing of cardarine. This statement came as a result of an emerging cooperation between GSK and WADA, which involved the sharing of information. GSK had apparently learned of the black market availability of cardarine. WADA learned of the drug's potential carcinogenicity. As expected, cardarine appears on the WADA banned substances list. Its use can now be detected during a doping test.
How is Cardarine Supplied
Cardarine is not available as a pharmaceutical product. Standard dosage information is unavailable. When used in clinical studies, cardarine was prepared in 2.5, 5, and 10 mg tablets.
As a research compound, it is found in both encapsulated powder form, and as a liquid suspension. It is typically supplied at a dosage of 10 mg when in capsules, and 20 mg/mL for liquid oral suspensions.
Structural Characteristics of Cardarine
Cardarine is a thiazolyl derived compound. It has the chemical name 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-acetic acid.
Cardarine is an unapproved new drug. A thorough understanding of its safety and propensity for side effects in humans is lacking at this time. Further, the discontinuation of human studies, combined with striking animal carcinogenicity data, leaves us with serious concerns about its safety. More research would be needed before this could be considered safe for human use, and that does not appear likely at this time.
Cardarine Side Effects
During Phase I and II human studies, cardarine was well tolerated. There were no significant side effects reported. Further, an examination of liver enzymes (AST and ALT), hematology (blood cell counts), and renal function (creatinine) tests found no changes with the daily administration of 10 mg. Again, the potential side effects of this drug have not been fully characterized.
Cardarine is taken orally. This drug has not been approved for use in humans. Prescribing guidelines are unavailable. During clinical studies, the maximum daily human therapeutic dosage tested was 10 mg.
When used for physique- or performance-enhancing purposes, cardarine is most commonly taken at a dosage of 10-20 mg per day. This is administered in one episode, often before exercise on training days. Cycles of cardarine usually last 6 to 12 weeks.
There are no commercial preparations containing cardarine known to exist. This drug is currently available as a research compound only.
Wlliam Llewellyn (2017) - Anabolics