"Since 2007, we have focused ArQule's efforts in drug discovery to leverage our learnings in the parallel chemistry business together with our structural analysis of inactive kinases," ArQule's vp of chemistry Mark Ashwell, Ph.D., explained to GEN.
lead drug candidate is tivantinib, a c-MET kinase inhibitor currently in clinical trials for non-small-cell lung cancer (NSCLC).
The company expects that it will enter Phase III trials to test its efficacy in liver cancer in late 2012/early 2013.
"The story of tivantinib's discovery is unusual," Dr. Ashwell
"We found it while screening a small molecule kinase library in a cellular assay, looking for a cell signature that we felt would lead to an anticancer agent.
"We found the profile we were looking for, and discovered that the activity came from only one of a pair of enantiomers, leading us to conclude that the active small molecule had a highly specific target with a strict molecular recognition requirement."
noted that he
colleagues screened the compound against a group of kinases and found it was a c-MET inhibitor.
Since then, he
said, "We have been able to look at the activation states of kinases in very specific ways, and we found tivantinib prevents cMET from assuming an activated form.