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. 2019 Jun 13;11(6):824. doi: 10.3390/cancers11060824

Table 2.

Chemical structures, relevant properties and clinical use of antineoplastic agents indicated for IT use in pediatric oncology.

Name of Drug and Structure Chemical Formula Properties Indications for IT Use in Pediatric Oncology
Methotrexate (MTX) graphic file with name cancers-11-00824-i001.jpg C20H22N8O5
Molecular weight: 454.45 g/mol		 MTX does not penetrate the BBB in therapeutic amounts when given orally or parenterally. High CSF concentrations of the drug may be achieved by IT administration. Acute lymphoblastic leukemia (ALL)
Advanced non-Hodgkin lymphomas (NHL)
CNS leukemia and lymphoma (prophylaxis)
Cytosine Arabinoside (Ara-C)
graphic file with name cancers-11-00824-i002.jpg 		C9H13N3O5
Molecular weight: 243.22 g/mol		 Only the use of high IV doses of Ara-C (>1 g/mq) produces significant CSF level of Ara-C above 1 micromol/L, with increased risk of neurotoxicity Acute myeloid leukemia
Acute lymphoblastic leukemia (ALL)
CNS leukemia and lymphoma (prophylaxis)
Hydrocortisone
graphic file with name cancers-11-00824-i003.jpg 		C21H30O5
Molecular weight: 362.47 g/mol		 Good penetration into the CSF compartment after IV infusion CNS leukemia and lymphoma (prophylaxis)
Thiotepa
graphic file with name cancers-11-00824-i004.jpg 		C6H12N3PS
Molecular Weight: 189.217 g/mol		 Good penetration into the CSF compartment after IV infusion Hematopoietic stem cell transplant (HSCT) for CNS malignancy
Busulfan
graphic file with name cancers-11-00824-i005.jpg 		C6H14O6S2
Molecular Weight: 246.30 g/mol		 Good penetration into the CSF compartment after IV infusion Leptomeningeal disease from recurrent or progressive primary brain tumors
Topotecan
graphic file with name cancers-11-00824-i006.jpg 		C23H23N3O5
Molecular Weight: 421.453 g/mol		 Moderate penetration into the CSF (about 30%) after IV infusion CNS leukemia or lymphoma, relapsed or refractory
6-Mercaptopurine (6-MP)
graphic file with name cancers-11-00824-i007.jpg 		C5H4N4S
Molecular Weight: 152.175 g/mol		 Poor penetration into the CSF compartment after IV infusion Acute lymphoblastic leukemia
Lymphoblastic lymphoma
Mafosfamide
graphic file with name cancers-11-00824-i008.jpg 		C9H19Cl2N2O5PS2
Molecular Weight: 401.269 g/mol		 Phase I trials showed that IV administration is unacceptable due to severe local pain at the injection site, thus mafosfamide is used through IT route Leptomeningeal disease from recurrent or progressive primary brain tumors
Rituximab * C6416H9874N1688O1987S44
Molecular Weight: 143859.7 g/mol		 Poor penetration into the CSF compartment after IV infusion Recurrent lymphomatous meningitis

* Rituximab is a monoclonal antibody (macromolecule) and not a small molecule like the others.