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Version: 17.12d (Release date: 2017-12-26)
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Pralatrexate (Code C2250)

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Terms & Properties

Preferred Name: Pralatrexate

Definition: A folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intracellularly, this agent is highly polyglutamylated and competes for the folate binding site of DHFR, blocking tetrahydrofolate synthesis, which may result in depletion of nucleotide precursors; inhibition of DNA, RNA and protein synthesis; and apoptotic tumor cell death. Efficient intracellular polyglutamylation of pralatrexate results in higher intracellular concentrations compared to non-polyglutamylated pralatrexate, which is more readily effuxed by the MRP (multidrug resistance protein) drug efflux pump. RFC-1, an oncofetal protein expressed at highest levels during embryonic development, may be over-expressed on the cell surfaces of various cancer cell types.

NCI-GLOSS Definition: A drug used in the treatment of peripheral T-cell lymphoma (a fast-growing form of non-Hodgkin lymphoma). It is also being studied in the treatment of other types of cancer. Pralatrexate may block the growth of cancer cells and cause them to die. It is a type of dihydrofolate reductase (DHFR) inhibitor.

Display Name: Pralatrexate

Label: Pralatrexate

NCI Thesaurus Code: C2250 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C0879404  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
(2S)-2-[[4-[(1RS)-1-[(2, 4-Diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic Acid
N-(4-{1-[(2,4-Diaminopteridin-6-yl)methyl]but-3-yn-1-yl}benzoyl)-L-glutamic Acid

External Source Codes: 
CAS Registry Number 146464-95-1 (see NLM ChemIDplus info)
FDA UNII Code A8Q8I19Q20
PDQ Closed Trial Search ID 37828
PDQ Open Trial Search ID 37828 (check for NCI PDQ open clinical trial info)
UMLS CUI C0879404

Other Properties:
     Name Value (qualifiers indented underneath)
code C2250
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name _10-Propargyl-10-Deazaaminopterin
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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