MLN8054, an orally administered small molecule, was discovered and is being developed by Millennium scientists. This first clinical study will assess safety, determine the maximum tolerated dose, and evaluate preliminary activity against the malignancies.
“MLN8054 selectively inhibits the cancer-promoting Aurora kinase,” said Dr Joseph Bolen, senior vice president of research and drug discovery at Millennium. “Preclinical studies indicated significant therapeutic potential and showed that MLN8054 distributes widely throughout the body and has activity across a range of tumors.”
The phase I study is expected to enroll approximately 30 patients with advanced solid tumors, including lymphomas. MLN8054 will be given orally and the dose will be escalated in cohorts of patients as tolerability is demonstrated at the given dose level.
The primary endpoint is to determine dose-limiting toxicities and maximum tolerated dose. Secondary endpoints of the study will include pharmacokinetics, pharmacodynamics, and preliminary assessment of anti-tumor activity. Exploratory analysis will also include the evaluation of specific molecular biomarkers.