abstract |
The present invention relates to prodrugs of monophosphate nucleotides of the known tumor drug gemcitabine. In particular, when present as a single phosphate diastereomer, it relates to gemcitabine-[phenyl-benzoyloxy-L-alanyl)]-phosphate, and in particular relative to (R) -Diastereomer provides a significant and unexpectedly increased solubility of the (S)-phosphate diastereomer. The (S)-phosphate epimer was also preferentially absorbed into the cyclodextrin solution relative to the (R)-diastereomer. |