Pralatrexate
Term · Oncology and biomedicine · MLC-T-ONC-006865
A drug used to treat peripheral T-cell lymphoma (a fast-growing form of non-Hodgkin lymphoma) that recurred (came back) or did not get better with other anticancer therapy. It is also being studied in the treatment of other types of cancer. Pralatrexate stops cells from using folic acid to make DNA. This may help keep cancer cells from growing and may kill them. Pralatrexate is a type of antimetabolite and a type of dihydrofolate reductase inhibitor. Also called Folotyn.
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.
| Identifier | MLC-T-ONC-006865 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | Folotyn |
| References | NCI Dictionary of Cancer Terms; National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-006865",
"term": "Pralatrexate",
"field": "Oncology and biomedicine",
"definitions": [
"A drug used to treat peripheral T-cell lymphoma (a fast-growing form of non-Hodgkin lymphoma) that recurred (came back) or did not get better with other anticancer therapy. It is also being studied in the treatment of other types of cancer. Pralatrexate stops cells from using folic acid to make DNA. This may help keep cancer cells from growing and may kill them. Pralatrexate is a type of antimetabolite and a type of dihydrofolate reductase inhibitor. Also called Folotyn.",
"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."
],
"synonyms": [
"Folotyn"
],
"references": [
"NCI Dictionary of Cancer Terms",
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/pralatrexate/"
}
Record 13,554 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.