Drug intelligence / Profile preview

cytarabine ocfosfate

Development stage
Unknown
Lead developer
Nippon Kayaku
Modality
Small Molecules
Administration
Oral
01

Overview

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.

Brand names
Starasid
Other names
Cytosine arabinoside 5'-stearylphosphateAra-C-stearylphosphate
02

Targets

POLB (DNA polymerase beta)POLL (DNA polymerase lambda)POLA1 (DNA polymerase alpha)DNA

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