Exelixis starts phase 2 program for XL784 in diabetes patients

By E. Janene Geiss

Philadelphia, March 27 - Exelixis, Inc. announced Monday the start of a phase 2 clinical development program for XL784 in patients with diabetes who have proteinuria, a marker for renal damage.

The primary endpoint is reduction in proteinuria and secondary endpoints will evaluate changes in renal function and cardiovascular effects, according to a company news release.

XL784 is a potent small molecule inhibitor of the ADAM-10 metalloprotease enzyme, which plays a role in blood vessel formation and cell proliferation that can cause renal fibrosis and impairment.

"We are making consistent progress in advancing compounds into phase 2 trials. In December of 2005, we initiated phase 2 trials of XL999. We expect to initiate phase 2 trials of XL647 by mid-year, and of XL880 and XL820 by year-end," George A. Scangos, president and chief executive officer of Exelixis, said in the release.

XL784 is the company's first product candidate to address an indication outside oncology. Data from preclinical studies indicated that XL784 has the potential to provide improvement in the treatment of renal disease, officials said.

In the United States alone, there are 3.7 million people living with diabetic nephropathy, and about 1.85 million patients are treated each year.

The company said it intends to pursue development of XL784 in this indication because it is an opportunity to provide patients with a potentially new treatment option.

Two phase 1 studies of XL784 have been completed in healthy volunteers and both studies demonstrated the compound is orally bioavailable, shows dose-proportional exposure and has an eight-hour half-life.

Results of single-dose, phase 1 clinical trials of XL784 administered orally to 96 healthy volunteers demonstrated that XL784 also has attractive safety and pharmacokinetic profiles.

The phase 2 trial is designed to enroll about 130 patients with diabetes who have clinically significant proteinuria. Participants will be randomly assigned to receive 200 mg of XL784 or a placebo daily for three months.

The primary endpoint of the trial is a reduction in proteinuria. Secondary endpoints include changes in renal function and cardiovascular events, officials said.

XL784 was the first small molecule compound developed from the company's proprietary drug discovery engine.

Exelixis is a South San Francisco biotechnology company dedicated to the discovery and development of novel therapeutics that will potentially enhance the care and lives of patients with cancer and other serious diseases.

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