Pralatrexate

Names

[ Name ]:
Pralatrexate

[Synonym ]:
pralatrexato
pralatrexatum
10-Propargyl-10-deazaaminopterin
N-{4-[1-(2,4-Diamino-6-pteridinyl)-4-pentyn-2-yl]benzoyl}-L-glutamic acid
Folotyn
N-{4-[1-(2,4-Diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl}-L-glutamic acid
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
(2S)-2-[[4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl]amino]pentanedioic acid
L-Glutamic acid, N-[4-[1-[(2,4-diamino-6-pteridinyl)methyl]-3-butyn-1-yl]benzoyl]-
Pralatrexate

Biological Activity

[Description]:

Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.IC50 Value: < 300 nMTarget: AntifolatePralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. Based on preclinical studies, researchers believe that Pralatrexate selectively enters cells expressing reduced folate carrier type 1 (RFC-1), a protein that is overexpressed on certain cancer cells compared to normal cells.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate

Research Areas >> Cancer

[References]

[1]. Foss F, Horwitz SM, Coiffier B, Bartlett N, Popplewell L, Pro B, Pinter-Brown LC, Shustov A, Furman RR, Haioun C, Koutsoukos T, O'Connor OA.,Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study,Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. Epub 2012 Apr 26.

[2]. Kelly K, Azzoli CG, Zatloukal P, Albert I, Jiang PY, Bodkin D, Pereira JR, Juhász E, Iannotti NO, Weems G, Koutsoukos T, Patel JD.,Randomized phase 2b study of pralatrexate versus erlotinib in patients with stage IIIB/IV non-small-cell lung cancer (NSCLC) after failure of prior platinum-based therapy.,J Thorac Oncol. 2012 Jun;7(6):1041-8.

[3]. Horwitz SM, Kim YH, Foss F, Zain JM, Myskowski PL, Lechowicz MJ, Fisher DC, Shustov AR, Bartlett NL, Delioukina ML, Koutsoukos T, Saunders ME, O'Connor OA, Duvic M.,Identification of an active, well-tolerated dose of pralatrexate in patients with relapsed or refractory cutaneous T-cell lymphoma.,Blood. 2012 May 3;119(18):4115-22. Epub 2012 Mar 6.

[4]. Casanova M, Medina-Pérez A, Moreno-Beltran M, Mata-Vazquez M, Rueda A.,Critical appraisal of pralatrexate in the management of difficult-to-treat peripheral T cell lymphoma.,Ther Clin Risk Manag. 2011;7:401-8. Epub 2011 Oct 7.

[5]. Hui J, Przespo E, Elefante A.,Pralatrexate: a novel synthetic antifolate for relapsed or refractory peripheral T-cell lymphoma and other potential uses.,J Oncol Pharm Pract. 2012 Jun;18(2):275-83. Epub 2011 Sep 26.

[Related Small Molecules]