GW501516 was developed by GSK as a new drug to treat dyslipaemia. GW501516 is a selective activator or a receptor in the body called PPARbeta/delta. PPARb/d is related to the receptors that mediate the actions on a number of steroids. In the 2000's Prof Ron Evans group at the Salk Institute showed that overexpressing PPARb/d or activating PPARb/d with GW501516 increased endurance running in treadmill trained mice. It also decreased experimental diabetes and obesity.
Our interest in the field came from study the family of PPAR receptors in blood vessels. We were amongst the first to show they were present in blood vessels, and in particular activation of PPARb/d caused new blood vessel growth; which is potentially important in getting more oxygen in to training muscle.
As a therapeutic, PPARb/d activators looked very promising, and were given to volunteers and patients in short term phase 1 and phase 2 clinical trails, the development of the drug was halted when GSK themselves presented data that long term use of GW5015516 in rats and mice led to widespread tumours. The 2 year study in rats led to tumour formation with all doses of the drug tested and cancers (neoplasms) occurred in the liver, urinary bladder, thyroid gland, ,tongue, stomach, skin, testes, ovaries and uterus (Abstract by reported Geiger et al., in The Toxicologist 2009 vol 108(1)).
N.B. for a drug to get to phase 2 clinical trials takes a huge investment (millions) from the developing pharmaceutical company. Although there are as yet no reports of any cancers linked to GW501516 in the clinical trials, there was clearly sufficient concern that development be immediately halted for the treatment of dyslipidaemia.
Since they showed potential to enhance athletic endurance, GW501516 and PPARb/d activators are listed as substances banned by the World Anti-doping agency (WADA). WADA also released an unprecedented alert to highlight these cancer findings:
(https://www.wada-ama.org/en/media/news/2013-03/wada-issues-alert-on-gw501516)
A quick internet search alone will tell you that unlicensed black market GW501516 (also called GW-501,516, GW1516, GSK-516 and on the black market as Endurobol or Cardarine) is being sold and used by bodybuilders and athletes; with at least 5 athletes being caught with in in their system.
Although short term use in humans has not shown these signs - only very low numbers of subjects have ever been monitored. The long term consequences of taking GW501516 are not known, but the strength of the pre-clinical findings in rodents is a major cause for concern that the findings will be reproducible in time in the human population
Our interest in the field came from study the family of PPAR receptors in blood vessels. We were amongst the first to show they were present in blood vessels, and in particular activation of PPARb/d caused new blood vessel growth; which is potentially important in getting more oxygen in to training muscle.
As a therapeutic, PPARb/d activators looked very promising, and were given to volunteers and patients in short term phase 1 and phase 2 clinical trails, the development of the drug was halted when GSK themselves presented data that long term use of GW5015516 in rats and mice led to widespread tumours. The 2 year study in rats led to tumour formation with all doses of the drug tested and cancers (neoplasms) occurred in the liver, urinary bladder, thyroid gland, ,tongue, stomach, skin, testes, ovaries and uterus (Abstract by reported Geiger et al., in The Toxicologist 2009 vol 108(1)).
N.B. for a drug to get to phase 2 clinical trials takes a huge investment (millions) from the developing pharmaceutical company. Although there are as yet no reports of any cancers linked to GW501516 in the clinical trials, there was clearly sufficient concern that development be immediately halted for the treatment of dyslipidaemia.
Since they showed potential to enhance athletic endurance, GW501516 and PPARb/d activators are listed as substances banned by the World Anti-doping agency (WADA). WADA also released an unprecedented alert to highlight these cancer findings:
(https://www.wada-ama.org/en/media/news/2013-03/wada-issues-alert-on-gw501516)
A quick internet search alone will tell you that unlicensed black market GW501516 (also called GW-501,516, GW1516, GSK-516 and on the black market as Endurobol or Cardarine) is being sold and used by bodybuilders and athletes; with at least 5 athletes being caught with in in their system.
Although short term use in humans has not shown these signs - only very low numbers of subjects have ever been monitored. The long term consequences of taking GW501516 are not known, but the strength of the pre-clinical findings in rodents is a major cause for concern that the findings will be reproducible in time in the human population
RSS Feed