Ipilimumab

drugbox-mab


source = Human
target = CTLA-4
CAS_number = 477202-00-9
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C=6742 | H= 9972 | N=1732 | O=2004 | S=40
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Ipilimumab (also known as MDX-010 or MDX-101) is a human monoclonal antibody being developed by Bristol-Myers Squibb and Medarex. It is intended to be used as a drug to activate the immune system. Ipilimumab is undergoing clinical trials for the treatment of melanoma. [ClinicalTrialsGov|NCT00094653]

Ipilimumab is a fully human antibody that binds to CTLA-4 (cytotoxic T lymphocyte-associated antigen 4), a molecule on T-cells that is believed to play a critical role in regulating natural immune responses. The absence or presence of CTLA-4 can augment or suppress the immune system's T-cell response in fighting disease. Ipilimumab is designed to block the activity of CTLA-4, thereby sustaining an active immune response in its attack on cancer cells.

As of October 2007 there are two fully human anti CTLA-4 [http://www.healthvalue.net/ctlaigenglish.html] monoclonal antibodies in advanced clinical trials. Ipilimumab, which is an IgG1 isotype, and Tremelimumab (from Pfizer) which is an IgG2 isotype.

On December 10, 2007, Bristol-Myers Squibb and Medarex released the results of three studies on ipilimumab. One of the three studies failed to meet its primary goal of shrinking tumors in at least 10.0% of the study's 155 patients. The three studies tested 487 patients with advanced skin cancer. Side effects are often considered acceptable risks for cancer drugs given the severity of the disease, and ipilimumab is no exception. The medication caused rashes, diarrhea and hepatitis in a number of the patients being tested. Despite the weaker-than-anticipated results, the companies are still planning to meet with regulatory agencies to discuss moving ahead with the medication. They hope to submit a filing to the U.S. Food and Drug Administration seeking approval in the first half of 2008. Since patients suffering from extremely serious diseases like melanoma have so few treatment options, the companies believe that even the marginal success rate will be appealing to some.

As of September 2008, Medarex is performing a Phase I/II dose escalation clinical trial of ipilimumab in metastatic hormone-refractory prostate cancer (HRPC).

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