NCIt 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.;
Alternative definition : NCI-GLOSS: 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.;
UNII : A8Q8I19Q20;
InChIKey : OGSBUKJUDHAQEA-WMCAAGNKSA-N;
CAS number : 146464-95-1;
Drug name : Folotyn; Difolta;
Codes from synonyms : CDR0000657510; CDR0000657511; CDR0000044880; 414;