Pralatrexate プララトレキサート

New Drug Approvals

10-Propargyl-10-deazaaminopterin.pngPralatrexate.pngChemSpider 2D Image | Pralatrexate | C23H23N7O5

Pralatrexate (JAN/USAN/INN);
10-Propargyl-10-deazaaminopterin;
Folotyn (TN)

Antineoplastic

Product
CAS:
FOLOTYN (Allos Therapeutics)
146464-95-1
Formula
C23H23N7O5
Exact mass
477.1761

Image result for Difolta

  • (2S)-2-((4-((1RS)-1-((2,4-diaminopteridin-6-yl)methyl)but-3-ynyl)benzoyl)amino)pentanedioic acid
  • (2S)-2-({4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl}amino)pentanedioic acid
  • 10-Propargyl-10-deazaaminopterin
  • N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
  • PDX
  • UNII:A8Q8I19Q20

Japan approved 2017

2017/7/3 PMDA JAPAN Pralatrexate Difolta Mundipharma NME

Image result for DifoltaImage result for Difolta

EMA 2012

http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002096/WC500129886.pdf

The molecule contains two asymmetric carbon centres (C10) and (C19). The C10 position exists in the RS-configuration (approx. 50:50 ratio) on the link between the two aryl groups. The C19 position is contained in the glutamic acid moiety and predominantly exists in the S-configuration. Pralatrexate is an off-white to yellow crystalline material, soluble in aqueous solutions at pH 6.5 or higher and practically insoluble in chloroform, and ethanol. It predominantly exists as a single polymorph (form A).

Pralatrexate, chemically known as “(2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl- ]-amino]pentanedioic acid”, also known as “10-Propargyl-10-deazaminopterin” or “PDX”, is a compound which has been tested and found useful in the treatment of cancer. In its racemic form, 2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]a- mino]-pentanedioic…

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