Intellikine, Inc., a company focused on the discovery and development of innovative, small molecule drugs targeting the PI3K/mTOR pathway, announced today that the first patient has been treated in a Phase I dose escalation study of INK1117 in patients with advanced solid malignancies. INK1117, a selective, orally available, small molecule inhibitor of the PI3Kalpha isoform has demonstrated impressive efficacy in several PI3Kalpha mutant-specific preclinical tumor models.
“PI3Kalpha is among the most frequently mutated oncogenes in many cancers, and preclinical studies have revealed important features, which differentiate INK1117 from less selective inhibitors that target the PI3K/Akt/mTOR pathway” said Dr. Josep Tabernero, head of the Medical Oncology Department at Vall d’Hebron University Hospital in Barcelona and a study investigator. “We look forward to exploring INK1117 in cancer patients, particularly those patients whose tumors have a mutation of the PIK3CA gene.”
The Phase I study of INK1117 will consist of a dose escalation phase in patients with advanced solid malignancies, followed by expansion cohorts in breast cancer patients as well as patients with other cancers whose tumors are characterized with a mutation of the gene. The PIK3CA gene represents one of the most highly mutated oncogenes in human cancers and is frequently mutated in a broad spectrum of tumors including breast, colon, brain, bladder and lung.
“We are delighted to announce another significant milestone for Intellikine as we advance INK1117 into human clinical testing,” said Troy Wilson, Ph.D., J.D., President and CEO of Intellikine. “INK1117 is among the first isoform selective inhibitors of PI3Kalpha, potentially one of the most important drug targets for the treatment of solid tumors. We are encouraged by the support and enthusiasm of our collaborators in the United States and Europe, and we look forward to bringing this new personalized medicine to patients as quickly as possible.”
The INK1117 Phase I trial is a multi-center trial enrolling patients in the United States, United Kingdom and Spain. For more information, please visit http://clinicaltrials.gov.
INK1117 is an orally available, small molecule inhibitor of the PI3Kalpha-isoform for the treatment of solid tumor malignancies. The PI3K/Akt/mTOR pathway is frequently upregulated and/or dysregulated in human tumors, and PI3Ks are important regulators of cancer-related pathways involved in cell proliferation, adhesion, survival and motility. INK1117 has demonstrated significant efficacy in several PIK3CA mutant-specific preclinical mouse xenograft tumor models. Moreover, daily oral administration of INK1117 inhibited tumor growth in a dose-dependent manner with a predict PK/PD relationship, was well tolerated at a range of efficacious doses, and exhibited both efficacy and tolerability which distinguish it from less selective inhibitors that target the PI3K/Akt/mTOR pathway.
About Intellikine, Inc.
Intellikine is a leading private company focused on the development of innovative, small molecule drugs targeting the PI3K/mTOR pathway for the treatment of cancer and other serious diseases. Intellikine’s most advanced drug candidate, INK128, a novel TORC1/2 inhibitor, has generated encouraging data in multiple Phase 1 studies and is expected to enter Phase II studies in early 2012. INK1117, a novel and selective inhibitor of the PI3Kalpha isoform, entered human clinical testing in October 2011. Intellikine owns all rights to INK128 and INK1117. In addition, an IND as well as a corresponding clinical trial application with a national regulatory authority in Europe has been filed for IPI-145, a PI3Kdelta/gamma inhibitor partnered with Infinity Pharmaceuticals, to enable clinical development of IPI-145. Intellikine has raised $41 million from a group of leading including Abingworth, BiogenIdec, CMEA Capital, Fintech Global Capital, Novartis Venture Funds, Sofinnova Ventures and U.S. Venture Partners and has attracted significant support from leading foundations such as the Multiple Myeloma Research Foundation and the Polycystic Kidney Disease Foundation.