Elacytarabine
Cytarabine is a cytosine derivative that is a common component of chemotherapy regimens for blood cancers such as acute myeloid leukaemia (AML), and because it can cross the blood–brain barrier, it is useful in the treatment of central nervous system lymphomas. However, the response is variable, and resistance commonly develops via multiple mechanisms. Its activity is dependent on the intracellular concentrations of the active phosphorylated form, and one of the main mechanisms of resistance involves the deficiency of the transporter molecule hENT1 that carries it into the cells. As a result, Clavis Pharma developed a lipophilic ester derivative, elacytarabine, whose cellular uptake is not hENT1-dependent.1
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