aspacytarabine

Aspacytarabine (BST-236) is a novel, proprietary prodrug of the antimetabolite cytarabine (Ara-C), developed by BioSight. It consists of cytarabine covalently linked to the amino acid L-asparagine. This chemical modification is designed to protect cytarabine from rapid inactivation by cytidine deaminase (CDA) in the blood and liver, thereby allowing for the delivery of high-dose cytarabine with significantly reduced systemic toxicity. Specifically, it aims to mitigate the severe gastrointestinal and neurological side effects typically associated with standard high-dose Ara-C therapy. Upon entering leukemic cells, the conjugate is cleaved to release active cytarabine, which then inhibits DNA synthesis by competing with cytidine for incorporation into DNA and inhibiting DNA polymerase. Aspacytarabine is primarily being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS), particularly in older patients or those unfit for intensive chemotherapy.

Brand names

Astarabine

Other names

aspacytarabineN4-aspartyl-cytarabineN-4-aspartyl-cytarabineN 4-aspartyl-cytarabineasparagine-cytarabine conjugateN4-L-aspartylcytarabineN-4-L-aspartylcytarabineN 4-L-aspartylcytarabine