CUDC-101 (HDAC, EGFR, Her2 inhibitor)
CUDC-101 is a drug candidate that is designed to target EGFR/Her2 and HDAC. In preclinical studies, CUDC-101 demonstrated the potential to inhibit all three molecular targets resulting in the potent killing of a wide range of cancer cell lines that are representative of a variety of human cancer types, many of which have demonstrated resistance to various approved targeted agents.
We have completed three clinical trials withan intravenous formulation of CUDC-101, including a Phase I dose escalation clinical trial of CUDC-101 in 25 patients with advanced, refractory solid tumors and a Phase I expansion trial that tested CUDC-101 in 46 patients with specific tumor types, including breast, gastric, head and neck, NSCLC or liver cancers. The Phase I expansion trial was designed as an open-label study in which patients were treated with CUDC-101 at the maximum tolerated dose, which was determined in the Phase I dose escalation study to be 275 milligrams per meter squared of human body surface area (275mg/m2). The primary objectives of the expansion study were to assess the safety and tolerability of CUDC-101 in subjects with these specific advanced solid tumors when the drug was administered via one-hour intravenous infusion either on a five days per week schedule (one week on/one week off) or on a three days per week schedule (three weeks on/one week off).
We also recently concluded a Phase I clinical trial of CUDC-101 in locally advanced head and neck cancer patients. The primary objectives of this study were to evaluate the safety and tolerability of CUDC-101 when administered in combination with the current standard-of-care of cisplatin, a chemotherapeutic drug, and radiation. We have determined that we will not continue with the further development of intravenously administered CUDC-101 and are instead focusing on the development of an oral formulation of this molecule.
In 2012, we initiated a Phase I clinical trial of an oral formulation of CUDC-101. We subsequently terminated this study due to insufficient drug exposure observed in the first cohort of patients. We are currently assessing alternative formulations that may provide improved drug exposure for patients, as well as backup molecules whose chemical properties may be more amenable to the oral route of administration. We remain encouraged by the preclinical and clinical activity that we observed with the intravenous formulation of CUDC-101 and believe that this molecule can provide benefit to patients in the future if we are successful in our ongoing efforts to develop an oral form of CUDC-101.
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