Medicinal chemistry paper related to the discovery of CUDC-101 published

Curis, Inc. (NASDAQ: CRIS), a drug development company seeking to develop next generation targeted small molecule drug candidates for cancer treatment, today announced that a medicinal chemistry paper related to the discovery of CUDC-101, Curis’s HDAC, EGFR and Her2 inhibitor, was published online in the Journal of Medicinal Chemistry and also will be published in an upcoming print version of the journal. The paper describes the structure-based rational drug design, synthesis and structure-activity relationship (SAR) of a class of novel compounds that included CUDC-101 and the identification of CUDC-101 as a clinical candidate. Related in vitro and in vivo data associated with these compounds are also included.

“We look forward to providing data for the ongoing Phase I clinical development program and beginning the next stage of clinical testing for this molecule later this year.”

“This publication underscores both the quality of the research at Curis and the productivity of our research group. Remarkably, CUDC-101 was the subject of an IND filing only two years after the synthesis of the first set of compounds within this class of molecules, and since then, a U.S. patent covering CUDC-101 has been issued,” stated Dan Passeri, Curis’ President and Chief Executive Officer. “We look forward to providing data for the ongoing Phase I clinical development program and beginning the next stage of clinical testing for this molecule later this year.”

CUDC-101, a small organic molecule of the quinazoline class, inhibits several clinically and commercially validated cancer targets at the same time. The cancer targets were chosen for their potential of mechanistic synergy and include class I and II histone deacetylases, or HDACs, EGFR and Her2. The publication indicates that CUDC-101 is significantly more potent than first-in-class drugs targeting EGFR and HDAC or combinations thereof in a variety of in vitro studies. CUDC-101 promotes tumor regression or inhibition in vivo in various cancer xenograft models, including non-small cell lung, liver, breast, head and neck, colon and pancreatic cancers. The data presented suggest that a single compound that simultaneously inhibits HDAC, EGFR and HER2 may offer greater therapeutic benefits in cancer over single-acting agents and may address significant clinical needs in the treatment of patients who are unresponsive or resistant to EGFR-inhibitors.

CUDC-101 is currently in a dose escalation Phase I clinical trial, which is expected to conclude in the first half of 2010, with the establishment of a maximum tolerated dose and dose limiting toxicities.