Which medications in the drug class Antineoplastic Agents are used in the treatment of Pediatric Acute Lymphoblastic Leukemia?

Updated: Jan 02, 2019
  • Author: Vikramjit S Kanwar, MBBS, MBA, MRCP(UK), FAAP; Chief Editor: Jennifer Reikes Willert, MD  more...
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Antineoplastic Agents

Cancer chemotherapy is based on an understanding of tumor cell growth and how drugs affect this growth. After cells divide, they enter a period of growth (ie, phase G1), followed by DNA synthesis (ie, phase S). The next phase is a premitotic phase (ie, G2), then finally a mitotic cell division (ie, phase M).

Cell-division rates vary for different tumors. Most common cancers grow slowly compared with normal tissues, and the rate may be decreased in large tumors. This difference allows normal cells to recover from chemotherapy more quickly than malignant ones and is the rationale behind current cyclic dosage schedules.

Antineoplastic agents interfere with cell reproduction. Some agents act at specific phases of the cell cycle, whereas others (ie, alkylating agents, anthracyclines, cisplatin) are not phase-specific. Cellular apoptosis (ie, programmed cell death) is another potential mechanism of many antineoplastic agents.

Vincristine (Vincasar PFS)

Vincristine is a chemotherapeutic agent derived from the periwinkle plant. This agent acts by inhibiting microtubule formation in mitotic spindles, causing metaphase arrest.

Daunorubicin (Cerubidine)

Daunorubicin is an anthracycline that intercalates with DNA and interferes with DNA synthesis.

Methotrexate (Trexall)

Methotrexate is a folate analogue that competitively inhibits dihydrofolate reductase, thus inhibiting DNA, RNA, and protein synthesis.

Mercaptopurine (Purinethol)

Mercaptopurine is a synthetic purine analogue that kills cells by incorporating into DNA as a false base.


Cytarabine is a synthetic analogue of nucleoside deoxycytidine. This agent undergoes phosphorylation to arabinofuranosyl-cytarabine-triphosphate (ara-CTP), a competitive inhibitor of DNA polymerase.

Etoposide (Toposar)

Etoposide inhibits topoisomerase II and breaks DNA strands, causing cell proliferation to arrest in the late S or early G2 portion of the cell cycle.


Cyclophosphamide is chemically related to the nitrogen mustards. When this drug is used as an alkylating agent, the mechanism of action of its active metabolites may involve cross-linking of DNA, which may interfere with the growth of normal and neoplastic cells.

Nelarabine (Arranon)

Nelarabine is a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). This agent is converted to the active arabinofuranosyl-guanine-5'-triphosphate (ara-GTP), a T-cell–selective nucleoside analogue. Leukemic blast cells accumulate ara-GTP, which allows for incorporation into DNA, leading to inhibition of DNA synthesis and cell death.

Nelarabine was approved by the US Food and Drug Administration [FDA] as an orphan drug to treat T-cell lymphoblastic lymphoma (a type of non-Hodgkin lymphoma [NHL]) that does not respond or that relapses with at least 2 chemotherapy regimens.

Clofarabine (Clolar)

Clofarabine is a purine nucleoside antimetabolite that inhibits DNA synthesis and is indicated for relapsed or refractory acute lymphoblastic leukemia in pediatric patients. Pools of cellular deoxynucleotide triphosphate are decreased by inhibiting ribonucleotide reductase and terminating DNA chain elongation and repair. This agent also disrupts mitochondrial membrane integrity.

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