RIGEL ANNOUNCES LAUNCH OF AURORA KINASE INHIBITOR TRIAL

Rigel Pharmaceuticals announced that its partner Merck Serono has begun enrolling patients in a Phase I study evaluating the safety and tolerability of R763, a highly potent, orally available, multi-Aurora kinase inhibitor, for the treatment of patients with hematological malignancies. This is the second of several Phase I studies being conducted to evaluate the safety and initial efficacy of R763 in different types of cancers, including solid tumors and hematological malignancies.

The open-label, dose-escalation study is designed to evaluate safety and tolerability at two different dosing regimens of the Aurora kinase inhibitor R763. Up to 54 subjects with acute or chronic myeloid leukemia or myelodysplastic syndrome will be enrolled in each regimen and dosed orally with R763.

R763 has shown encouraging results in in vitro and in vivo models of hematological malignancies where Aurora kinase is thought to play a role. The over-expression of Aurora kinase can cause cells to rapidly develop an abnormal number of chromosomes, according to the company. Elevated levels of Aurora kinase are frequently associated with various human cancers, and inhibition of this enzyme disrupts cell division and promotes programmed cell death.