The Real Deal Behind GW1516 and Cancer

John Biggs

April 11, 2016


Recently, a drug that was supposed to help obese people get thinner and hyperlipidemic people get healthier had been banned for use by World Anti-Doping Agency or WADA, which is an organization that aims to promote a doping-free sporting environment. The scientists call it GW1516 and the common people call it Endurobol.

A lot of controversies have reached the different parts of the world regarding GW1516. Debates have been done, researches have been made, opinions have been sought and questions have been raised but still, the truth about GW1516 has been kept in the dark for years. Many people are still curious as to what it can really do. Despite its prohibition, the distribution and selling of this drug is still rampant.

image1The pharmaceutical company GlaxoSmithKline (GSK) developed GW1516 in early 2000 and has reached Phase II clinical trials. This is a phase of clinical trial wherein a drug is tested for its efficacy and adverse reactions to at least a hundred people. It is a PPAR agonist, which means that it stimulates peroxisome proliferator-activated receptor (PPAR) to stimulate other cellular processes, one of which is the development of muscles that are able to endure exercises for longer periods of time. The development of GW1516 could have been an answer to obesity, dyslipidemia and diabetes mellitus. GW1516 has a lot of benefits to offer, but just like any other drug, it also has its adverse effects.

One of the most common adverse effects noted was the development of tumorigenic cells.

It has been linked with various forms of cancer in mice, particularly colorectal, hepatic and gastric cancers. How can this happen? PPAR, a receptor that is stimulated by this drug, is said to be over expressed among mice who developed colorectal malignancies. Researches revealed that GW1516, through activation of PPAR, increases incidences of intestinal adenoma or polyps among mice. Thus, the deletion of the PPAR gene is said to be a promising solution towards suppression of the development of intestinal adenoma among GW1516 users.

Cancer encompasses a number of complicated metabolic processes, including angiogenesis, proliferation and anti-apoptosis. Cellular proliferation is simply the increase in the number of cells as a result of stimulation of the cellular division. Apoptosis is the process of regulated cell death, wherein a worn-out cell “kills” itself after a certain period of time to give way to newer cells. Apoptosis is also expressed by some cells that are damaged or mutated. Normally, in a human DNA, a tumor suppressor gene is responsible for fixing cellular mutations. However, in the presence of an imbalance or alteration in their functions, cancer occurs. Angiogenesis, on the other hand, refers to the formation of new blood vessels to sustain the nutritional needs of the growing tumor. This is facilitated by various growth factors whose production is also stimulated by carcinogens.

Apoptosis, angiogenesis and cellular proliferation, in one way or another, are affected by GW1516. PPAR stimulates VEGF, vascular endothelial growth factor, to promote tumour progression and angiogenesis. This growth factor is also said to be responsible for distant metastases, a characteristic of cancer that allows it to break free from the original tumor and travel to different sites to produce another tumorigenic focus. With the development of new blood vessels, the nourishment of the growing tumour is facilitated, and thus, allowing the tumor to grow limitlessly. The new blood vessels also serve as the medium of metastasis of tumor cells. Researches made regarding PPAR and VEGF revealed that after 7 weeks of treatment of mice with GW1516, tumour number in the intestines increased by approximately 4-fold, an event that is most evident in the colon.

There are still a lot of things that has to be known about GW1516 and the consumers should be critical in taking this drug. GW1516 may enhance your performance and may help you lose weight, but these benefits would be meaningless in the presence of cancer.