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Chemical Compound Review

Folotyn     (2S)-2-[[4-[1-(2,4- diaminopteridin-6...

Synonyms: Pralatrexate, pralatrexato, pralatrexatum, Folotyn (TN), S1497_Selleck, ...
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Disease relevance of Pralatrexate


High impact information on Pralatrexate


Chemical compound and disease context of Pralatrexate


Gene context of Pralatrexate

  • Compared with other 4-aminofolate analogues, 10-propargyl-10-deazaaminopterin (PDX) is the most efficient permeant for the RFC-1-mediated internalization and substrate for folylpolyglutamate synthetase [6].


  1. 10-propargyl-10-deazaaminopterin: an antifolate with activity in patients with previously treated non-small cell lung cancer. Krug, L.M., Azzoli, C.G., Kris, M.G., Miller, V.A., Khokhar, N.Z., Tong, W., Ginsberg, M.S., Venkatraman, E., Tyson, L., Pizzo, B., Baez, V., Ng, K.K., Sirotnak, F.M. Clin. Cancer Res. (2003) [Pubmed]
  2. Experimental therapeutics with a new 10-deazaaminopterin in human mesothelioma: further improving efficacy through structural design, pharmacologic modulation at the level of MRP ATPases, and combined therapy with platinums. Khokhar, N.Z., She, Y., Rusch, V.W., Sirotnak, F.M. Clin. Cancer Res. (2001) [Pubmed]
  3. Activity of a novel anti-folate (PDX, 10-propargyl 10-deazaaminopterin) against human lymphoma is superior to methotrexate and correlates with tumor RFC-1 gene expression. Wang, E.S., O'Connor, O., She, Y., Zelenetz, A.D., Sirotnak, F.M., Moore, M.A. Leuk. Lymphoma (2003) [Pubmed]
  4. A phase I clinical pharmacologic study of pralatrexate in combination with probenecid in adults with advanced solid tumors. Fury, M.G., Krug, L.M., Azzoli, C.G., Sharma, S., Kemeny, N., Wu, N., Kris, M.G., Rizvi, N.A. Cancer Chemother. Pharmacol. (2006) [Pubmed]
  5. Pralatrexate is synergistic with the proteasome inhibitor bortezomib in in vitro and in vivo models of T-cell lymphoid malignancies. Marchi, E., Paoluzzi, L., Scotto, L., Seshan, V.E., Zain, J.M., Zinzani, P.L., O'Connor, O.A. Clin. Cancer Res. (2010) [Pubmed]
  6. Phase I and pharmacokinetic study of 10-propargyl-10-deazaaminopterin, a new antifolate. Krug, L.M., Ng, K.K., Kris, M.G., Miller, V.A., Tong, W., Heelan, R.T., Leon, L., Leung, D., Kelly, J., Grant, S.C., Sirotnak, F.M. Clin. Cancer Res. (2000) [Pubmed]
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