eng Oriental Scientific Publishing Company Biosciences Biotechnology Research Asia 0973-1245 2017-02-21 8 2 641 651 21233 article Acute lymphoblastic leukemia is more common in children, accounting for 85% of childhood leukemias. The incidence of this disease is highest in the three to four year old age group, falling off by ten years. L-asparaginase is an effective antineoplastic agent, used in the acute lymphoblastic leukemia chemotherapy. It has been an integral part of combination chemotherapy protocols of pediatric acute lymphoblastic leukemia for almost 3 decades. It is the first enzyme to be therapeutically effective in human malignant disease. Native or PEGylated L-asparaginase (ASNase or PEG-ASNase) are highly specific for the deamination of L-asparagine (Asn) to aspartic acid and ammonia. Depletion of Laspargine leads to a nutritional deprivation and inhibition of protein biosynthesis, resulting in apoptosis in T-lymphoblastic leukemia’s, which require L-aspargine from external sources. This review article comprises detailed information about L-asparaginase historical developments of therapy, its mechanism of action, Advantages of PEG-Lasparaginase versus native preparations, Pharmacokinetic and Pharmacodynamics models of the enzyme, Clinical potential ,its efficacy and host resistance to ASNase. https://www.biotech-asia.org/vol8no2/role-of-l-asparaginase-as-an-effective-chemotherapeutic-agent-for-acute-lymphoblastic-leukemia-in-childrens/ Acute lymphoblastic leukemia; Asparaginase; Enzymatic activity; PEGylation; Antibodies; Pharmacokinetics; Pharmacodynamics