GEMCITABINE (2',2'-difluorodeoxycytidine) is a fluorine- substituted deoxycytidine analog with a broad spectrum of antitumor activity. It is rapidly and extensively deaminated by cytidine deaminase to the inactive metabolite, 2',2'-difluorodeoxyuridine (dFdU). In order to enhance the bioavailability as well as the stability of gemcitabine via oral administration, INNOPHARMAX has applied OralPAS® technique on gemcitabine to prepare unique oral formulation. OralPAS® enhances the bioavailability of drugs through solubilization in the excipient matrix or interface and dispersion in the gastrointestinal tract. These characteristics result in faster drug release from nanoparticles in a reproducible manner, which can be designed further to make the release characteristics independent of the gastro-intestinal physiology and the fed/fasted state of the patient. Recently, several in-vitro and in-vivo studies (i.e. pilot tests in rats and dogs) have been done and study goals have been met.

Related Publications

• 2009 AAPS_Oral Administration of Gemcitabine (INNO-D07001) in Beagle Dogs_ Preliminary Pharmacokinetic Evaluation of Gemcitabine and Its metabolite
• 2010 AAPS_ In-vitro and in-vivo Evaluation of Oral SMEDDS (Self-Microemulsifying Drug Delivery System) Formulation
• 2011 AAPS_In vitro and in vivo Evaluation of a Novel Oral SMEDDS (Self-Microemulsifying Drug Delivery System) Formulation
• 2011 AAPS_The anti-proliferative efficacy of an OralPAS gemcitabine Formulation
• 2012 AAPS_Toxicokinetic Study of an OralPAS Gemcitabine
• 2013 AAPS_ Drug Distribution of [14C] Gemcitabine Using Quantitative Whole-Body Autoradiography after a Single Oral and Intravenous Bolus Doses Administration to Male Nu/Nu Mice
• 2014 ASCO_Phase I, Dose-escalation Study of the Investigational Drug D07001_F4, and Oral Formulation of Gemcitabine HCl, in Patients(pts) with Advanced Solid Tumors
• 2014 EORTC-NCI-AACR_ Phase I, Dose-escalation Study of the Investigational Drug D07001_F4, and Oral Formulation of Gemcitabine HCl, in Patients(pts) with Advanced Solid Tumors

C08001 is indicated for the treatment of hypertension, heart failure and left ventricular dysfunction following myocardial infarction. The active ingredient of C08001 is poor soluble, especially in aqueous media, which limits the release and absorption in the gastrointestinal tract. Its immediate release formulation is given twice daily. C08001 is designed to enhance the solubility and as an extended-release tablet intended for once-daily administration.