Innovive will develop the candidate NS-187 for the treatment of chronic myelogenous leukemia (CML) and anticipates commencing phase I trials this year.
NS-187 is a dual Bcr-Abl and Lyn kinase inhibitor. Bcr-Abl is commonly recognized as the primary molecular target in the treatment of CML. According to a study published in the journal Blood, NS-187 was shown to be 25 to 55 times more potent than Novartis’ Gleevec in vitro, and at least 10 times as effective as Gleevac in suppressing the growth of Bcr-Abl bearing tumors.
In addition to its Bcr-Abl inhibitory properties, NS-187 was designed to inhibit Lyn kinase. Lyn kinase activity is upregulated in some CML patients when resistance to Gleevec has developed. Lyn kinase activation has also been documented in a variety of solid tumors, including prostate cancer.
“CML is becoming a chronic condition in which patients will need several different treatment options. I am very excited about NS-187 because of its potent inhibition of Bcr-Abl and its specificity for Lyn which could contribute to a unique efficacy and toxicity profile,” said Dr Hagop Kantarjian, chairman of the Department of Leukemia at the MD Anderson Cancer Center.