Phase I clinical trial for Intellikine's INK128 inhibitor initiated

Intellikine, Inc. has initiated a Phase I clinical trial for its targeted anticancer drug INK128, a novel orally-available small molecule inhibitor of both the TORC1 and TORC2 complexes, key components of the PI3K/mTOR signaling pathway.

"Advancing INK128 to this point is a significant achievement for Intellikine," said Troy Wilson, Ph.D., J.D., President and CEO of Intellikine. "INK128 is the first drug resulting from our internal discovery pipeline to enter human clinical trials and furthers our goal of building the industry's leading pipeline of small molecule drugs against this important class of drug targets."

The mTOR kinase represents a central node in human cancer biology and has become an important target for oncology drug development. Unlike other drugs targeting the pathway, INK128 directly inhibits the activity associated with both the TORC1 and TORC2 complexes of the mTOR kinase. This direct inhibition and dual activity differentiates INK128 from rapamycin and related analogs, or rapalogs, which predominately modulate TORC1 activity. By inhibiting both TORC1 and TORC2, INK128 more potently inhibits mTOR kinase and may provide for greater efficacy.

"Preclinical studies have demonstrated that INK128 has the potential for efficacy in a broad range of human cancers," added Pamela Klein, M.D., Chief Medical Officer at Intellikine. "In addition, the selectivity and novel mechanism of INK128 may allow for combination with other targeted agents and standard of care therapies."

The Phase I trial is a dose escalation study to evaluate the safety, tolerability and pharmacokinetics of single-agent INK128 in patients with advanced tumors. The study is evaluating pharmacodynamic correlation between INK128 exposure and biomarkers of the mTOR pathway as well as candidate predictive markers and is being conducted initially at three sites: Premiere Oncology in Scottsdale, Arizona; Sarah Cannon Research Institute in Nashville, Tennessee; and the Vall d'Hebron University Hospital in Barcelona, Spain.