Elacytarabine for treatment of acute myeloid leukaemia (AML)
Elacytarabine is a novel, patented LVT derivative of the anti-cancer drug cytarabine commonly used in the treatment of AML. Elacytarabine is a new chemical entity made by covalently binding elaidic acid to cytarabine.
Clavis Pharma’s ambition is to replace cytarabine with elacytarabine as the standard therapy for treatment of haematological malignancies.
Mechanism of action
Nucleoside analogues (such as cytarabine) has short plasma half-life, are rapidly metabolized and require transporter proteins (e.g. hENT1) to enter cancer cells. Low levels of hENT1 have been found in some cancers (e.g. AML and pancreatic cancer) and these cancers have been found to respond poorly to nucleoside analogues. This is thought to be the main form of resistance to these products. To learn more about mechanism of action for elacytarabine, click mechanism of action picture. Different from cytarabine, elacytarabine have longer plasma half-life, is metabolic stable and can access leukaemic cells independently of membrane transporters (Figure 1).
Figure 1. Cellular uptake and activation of elacytarabine.