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Cytarabine ocfosfate is an orally active prodrug of the antineoplastic antimetabolite cytarabine (Ara-C). Developed by Nippon Kayaku, it was designed to overcome the rapid deamination and short half-life of parenteral cytarabine by providing sustained plasma levels of the active metabolite. Upon oral administration, cytarabine ocfosfate is absorbed and subsequently converted into cytarabine, which is then phosphorylated by deoxycytidine kinase to its active form, cytarabine triphosphate (ara-CTP). Ara-CTP acts as a potent inhibitor of DNA polymerase and is incorporated into DNA, leading to the termination of DNA chain elongation and induction of apoptosis in rapidly dividing cells. It is primarily indicated for the treatment of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML), particularly in elderly patients or those requiring maintenance therapy.
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