OncoEthix, the Swiss-based specialist in oncology drug development, announces progress in its Phase I study of OTX015, a novel BET bromodomain inhibitor, with the first dosing of a patient. OTX015 is a synthetic orally administered small molecule which targets BET bromodomain proteins 2/3/4, which are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting and cell cycle regulators, especially c-MYC. Phase I trials of OTX015 in healthy volunteers have already been completed.
The design of the Phase I trial will seek to determine the optimum dosing regimen for OTX015, and to provide further safety, pharmacokinetic and pharmacodynamic data. The study will be conducted in two parts: dose escalation, followed by expansion cohorts. In the first part, dose escalation and determination of the recommended dose will be performed independently in two parallel subsets of patients: patients with acute leukemia and patients with other hematologic malignancies. Once the optimum dosing regimen has been determined, the second part of the study will further assess safety, pharmacokinetics, pharmacodynamics and clinical activity in disease specific cohorts of at least 12 patients treated at the recommended dose. Study centers are now open at five reference sites in Europe [France, Italy and Switzerland] selected for investigators having extensive hematology and clinical pharmacology expertise.
Bertrand Damour, CEO of OncoEthix, said "We believe that OTX015 has the potential to be an important new drug in the continuing battle to improve and extend the lives of patients with cancer."
Patrice Herait, CMO of OncoEthix, said: "This multi-center study is a critical step in determining an active dose of OTX15 and providing the necessary safety data, as well as detecting clues of clinical activity to support further progression through the development process."
Preclinical data have shown that OTX015 treatment of acute leukemia (both cell lines and patients' cells), various subtypes of lymphoma and multiple myeloma cell lines induces potent anti-proliferative effects associated with cell cycle arrest, cellular senescence or apoptosis.
Oncoethix in-licensed OTX015 from Mitsubishi Tanabe Pharma Corporation in March 2012 following completion of Phase I clinical studies in healthy volunteers.