Abstract: The present invention provides an oral formulation of a cytidine analog, including, 5-azacytidine, for delivery to the lower gastrointestinal tract, including, the large intestine; methods to treat diseases associated with abnormal cell proliferation by treatment with the oral formulations of the present invention; and methods to increase the bioavailability of a cytidine analog upon administration to a patient by providing an oral formulation of the present invention.

Abstract: The invention provides methods for stabilizing 5-azacytidine against hydrolysis in plasma. By extracting the 5-azacytidine into acetonitrile and zinc sulfate, the 5-azacytidine can be stored for at least about 3 hours at about room temperature, and for at least about 4 days at about ?70° C. If the acetonitrile is removed and evaporated to dryness, the 5-azacytidine in the resulting residue is stable for at least about 14 months at about ?70° C. The invention also provides methods for determining the 5-azacytidine in acetonitrile, or in the acetonitrile residue, using, for example, high-performance liquid chromatography. The methods of the invention permit a significant time interval between the initial processing of the whole blood sample and the time of 5-azacytidine determination.

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.

Abstract: The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure also includes pharmaceutical compositions comprising said forms.

Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

Abstract: The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

Abstract: The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure also includes pharmaceutical compositions comprising said forms.

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.