Pralatrexate is an antineoplastic agent used for the treatment of relapsed or refractory peripheral T-cell lymphoma. Pralatrexate was developed in response due to the inferior responses of patients using the standard therapy for their B-cells counterparts.
- Mechanism
- Curator reviewed · 6 references
Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase (DHFR) selectively in cancer cells overexpressing the reduced folate carrier protein-1 (RFC-1). Folate is a water-soluble vitamin required for DNA synthesis and maintenance as well as DNA, RNA, and protein methylation. As cancer cells are rapidly replicating, they require a lot of folates to accommodate an accelerated cell division and DNA and protein modification for cellular transformation. Therefore, interruption with folate metabolism can inhibit tumor growth.
Additionally, pralatrexate also undergoes polyglutamylation catalyzed by folyopolyglutamate synthase (FPGS). This reaction both increases cellular retention of pralatrexate for extended drug action and impedes the uptake of folate, also a substrate of FPGS, to further inhibit folate metabolism in cancer cells.
- Primary indication
- Pralatrexate is indicated for the treatment of relapsed or refractory peripheral T-cell lymphoma.Curator reviewed · 3 structured indications
- Formula / weight
- C23H23N7O5 · 477.4726 g/mol (avg)
- First approval
- Canada, 2018 · United States, 2009
- Brand names
Resolves to
OGSBUKJUDHAQEA-WMCAAGNKSA-NSMILESNC1=NC2=NC=C(CC(CC#C)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)N=C2C(N)=N1What you can answer from here — as of January 29, 2025
Which drugs share a target with Pralatrexate, and which of those have an active Phase 3 trial?
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