San Diego, June, 06, 2012: CalAsia Pharmaceuticals today announced that it has successfully demonstrated CNS Pharmacodynamic effects of its “first in class” brain-permeable heat shock protein-90 (HSP90) inhibitor for CNS oncology.
HSP90 is both a validated and druggable cancer target. Numerous HSP90 inhibitors have been discovered since 1950 and approximately 20 HSP90 inhibitors are currently in clinical development with marketed drugs expected within the next 2 years. Importantly, clinical liabilities (liver and ocular toxicity) commonly associated with HSP90 inhibitors have been elucidated and all current HSP90 inhibitors in clinical development including those that cross the blood brain barrier have been evaluated in both pre-clinical and clinical studies to avoid these liabilities.
These findings establish HSP90 as a clinically accessible target with a safety profile that is well suited for CNS oncology. Using fragment-based screening combined with X-ray crystallography, CalAsia Pharmaceuticals has discovered novel proprietary HSP90 inhibitors that target the ATP binding site with nanomolar biochemical potency. In addition, our HSP90 inhibitors achieved micromolar CNS concentrations after parenteral administration into rats, and pharmacodynamics studies demonstrated a significant reduction in CNS Akt1 levels.
Although, there are numerous HSP90 inhibitors in clinical trials, the HSP90 lead candidates discovered by CalAsia are unique “drug candidates” designed to treat CNS cancers, due to their selective partitioning into the CNS, said Dr. Sridhar Prasad, Vice President of Research.
We are actively seeking corporate partners to advance our HSP90 inhibitors for further preclinical development and IND enabling studies, added Dr. Jeffrey Stebbins, Head of Biology.
About CalAsia’s Drug-discovery:
CalAsia Pharmaceuticals, Inc. is an employee owned early stage pharmaceutical company focused on the rapid discovery of drug-like small molecules by utilizing its core technologies. In detail, CalAsia core technologies combine functional fragment screening with X-ray crystallography co-crystallization to rationally design and synthesize New Chemical Entities (NCEs) with drug-like properties. By differential fragment screening of closely related isotypes, CalAsia also develops selective NCEs early in the drug discovery process thereby increasing the quality of potential drug candidates. Currently, CalAsia has 6 internal drug-discovery programs for the treatment of unmet medical needs for Parkinson Disease, Type II Diabetes, Inflammation, Prostate Cancer and Malaria. Of note, the CalAsia team has decades of drug-discovery experience and has been involved in numerous drug discovery programs that have resulted in multiple clinical candidates as well as one marketed drug.
About CalAsia’s Services:
The CalAsia team provides its expertise, which includes cloning, recombinant protein expression (E. coli, baculovirus, and yeast), recombinant protein purification, biochemical assays, cellular assays, fragment screening, and X-ray crystallography co-crystallization to the drug discovery community through contract research.
