Oral Gallium Compound (G4544)    

The initial clinical trial of G4544, currently pending review, will examine safety and pharmacokinetics of a range of G4544 doses in normal volunteers.

High IV doses of gallium nitrate (Ganite®) are extremely effective for treatment of patients (pts) with cancer-related hypercalcemia, and preliminary studies have shown consistent anticancer activity in pts with relapsed non-Hodgkin’s lymphoma (NHL).  In preclinical studies, low concentrations of gallium nitrate act as a potent inhibitor of osteoclast-mediated bone resorption, and the agent may also have anabolic effects on bone formation.

Clinical studies have shown that low doses of gallium nitrate administered by subcutaneous injection significantly reduced metabolic markers of disordered bone turnover in patients with advanced Paget’s disease.  Moreover, a multi-year longitudinal study in pts with advanced multiple myeloma showed that similarly low doses administered by intermittent subcutaneous injection significantly reduced bone loss in pts receiving chemotherapy.  Since gallium nitrate has low oral bioavailability, and in order to improve dosing convenience over extended periods, we have developed a novel formulation of gallium nitrate, known as G4544, which has now advanced into initial clinical studies.

An IND has been filed in the U.S. and initial clinical trials with G4544 are planned for the third quarter of 2007.  These trials will seek to establish the bioequivalence of G45644 to Ganite® and to eventually secure regulatory approval for this new drug in patients with cancer-related hypercalcemia.  The drug may also be developed for other oncology indications by Genta, and the Company will seek a partner to develop G4544 in other diseases, such as osteoporosis and Paget’s disease.