Next Generation NSAID Targets Specific Tissues

The 4th Annual Pain Therapeutics Summit, October 4-5,2010, will feature a presentation on the CG100649, the first-in-class NSAID drug candidate with a new “tissue selective” mechanism of action.

Dr. William Schmidt, vice president of Clinical Development at CrystalGenomics, Inc., will present a talk on "Development of CG100649, Tissue-selective Dual Inhibitor of COX-2 and Carbonic Anhydrase for Treatment of Osteoarthritis."

CrystalGenomics is a structural chemoproteiomics-based drug discovery and development company headquartered in Seoul, Korea. CG100649 is the company’s lead development candidate, a possible next generation NSAID, according to the website. The tissue specific anti-inflammatory agent potentially improves cardiovascular, gastrointestinal, and renal safety profiles. It has recently completed a Phase IIa clinical trial in Europe.

The “tissue-seleactive” mechanism of action is designed to deliver sustained levels of drug to inflamed tissues, while maintaining low systemic exposure. It maintains low systemic exposure by binding in a protected-inactive state. It then is released into inflamed tissues that have little or no CA binding activity. The unique dual-COX-2 and CA binding properties are designed to provide potentially superior safety to cardiovascular, renal, and gastrointestinal tissues than other approved NSAIDS or COX-2 inhibitor drugs.

A Phase IIa osteoarthritis trial was successfully completed in Europe with 248 patients. The efficacy and safety results data showed that CG100649's efficacy profile is at least as favorable as other COX-2 drugs.

CrystalGenomics then conducted a supra-threshold Phase I Multiple Ascending Dose (MAD) study to explore higher doses of CG100649 in pharmacokinetic and pharmacodynamic tests prior to initiating a Phase IIb efficacy study. Based on clinical data collected so far, it is anticipated that CG100649 should achieve significant safety as well as even higher levels of efficacy at higher doses.

The Phase I MAD study evaluated doses up to 6.7 times higher than the established efficacious dose from the Phase IIa OA study and, successfully enrolled and dosed all subjects in three cohorts without any Serious Adverse Events related to the study medication.

“We are very pleased with the preliminary results and this will enable us to begin the Phase IIb study with a high level of confidence about our drug's safety even at much higher doses,” Joong Myung Cho, President & CEO of CrystalGenomics, in a press release.

CrystalGenomics also manufactures the novel HDAC inhibitor CG200745 for cancer. This experimental drug is Phase I ready. The company also manufactures the novel antibiotic candidate CG400549 for MRSA and VRSA, which is currently in Phase I stage in Europe.