Phase I, dose-escalation study of the investigational drug D07001-F4, an oral formulation of gemcitabine HCl, in patients (pts) with advanced solid tumors.

TPS2631^ Background: Gemcitabine HCl is a nucleoside analogue that exhibits antitumor activity and is approved for IV use in the world. Oral dosing of gemcitabine HCl would simplify administration and extend the systemic exposure time after a dose relative to an intravenous exposure profile, which has been correlated with increased activity of gemcitabine in both pre-clinical and clinical studies. Nonetheless, in a reported clinical study, the systemic exposure to oral gemcitabine was low due to extensive first-pass metabolism to dFdU. D07001-F4 is a unique oral formulation of gemcitabine HCl that is expected to enhance the systemic exposure to difluorodeoxycytidine (dFdC) and ultimately dFdCTP, intracellularly. Methods: D07001-F4 is being evaluated of in an open-label, dose escalation study in patients with advanced solid tumors or lymphoma. Eligibility: pts with evaluable tumors, age ³a 20 yrs, PS 0–2 and with adequate oral therapy absorption. Primary objects includes determination of maximum tolerated ...