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Chemical Compound Review

Nolatrexed     2-amino-6-methyl-5-pyridin-4- ylsulfanyl-1H...

Synonyms: SureCN18489, CHEMBL320775, SureCN710461, CHEBI:283333, AG337, ...
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Disease relevance of Nolatrexed


High impact information on Nolatrexed

  • Preclinical and phase I clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors [1].
  • Bioavailability was close to 100% and, because inhibition of thymidylate synthase by nolatrexed is rapidly reversible, the slower absorption after a standard meal may result in a shorter duration of noninhibitory concentrations between doses [4].
  • Nolatrexed was rapidly absorbed with a median bioavailability of 89% (range 33-116%), with 88% of patients above 70% [4].
  • Average trough nolatrexed concentration, but not dose, was significantly related to the % decrease in both thrombocytes (r2 = 0.58; C50 = 6.0 microg/ml, where C50 is the plasma concentration associated with a 50% decrease in thrombocytes) and neutrophils (r2 = 0.63; C50 = 0.6 microg/ml) [4].
  • Plasma nolatrexed concentrations and systemic exposure, measured in 14 patients, were dose related, with mean AUC values of 36 mg(-1)ml(-1)min(-1), 50 mg ml(-1)min(-1)and 80 mg ml(-1)min(-1)at the 3 dose levels studied [5].

Biological context of Nolatrexed


Anatomical context of Nolatrexed


Associations of Nolatrexed with other chemical compounds


Gene context of Nolatrexed


Analytical, diagnostic and therapeutic context of Nolatrexed


  1. Preclinical and phase I clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors. Rafi, I., Boddy, A.V., Calvete, J.A., Taylor, G.A., Newell, D.R., Bailey, N.P., Lind, M.J., Green, M., Hines, J., Johnstone, A., Clendeninn, N., Calvert, A.H. J. Clin. Oncol. (1998) [Pubmed]
  2. Result of two randomized trials comparing nolatrexed (Thymitaq) versus methotrexate in patients with recurrent head and neck cancer. Pivot, X., Wadler, S., Kelly, C., Ruxer, R., Tortochaux, J., Stern, J., Belpomme, D., Humblet, Y., Domenge, C., Clendeninn, N., Johnston, A., Penning, C., Schneider, M. Ann. Oncol. (2001) [Pubmed]
  3. Phase II trial of nolatrexed dihydrochloride [Thymitaq, AG 337] in patients with advanced hepatocellular carcinoma. Jhawer, M., Rosen, L., Dancey, J., Hochster, H., Hamburg, S., Tempero, M., Clendeninn, N., Mani, S. Investigational new drugs (2007) [Pubmed]
  4. Phase I studies with the nonclassical antifolate nolatrexed dihydrochloride (AG337, THYMITAQ) administered orally for 5 days. Hughes, A.N., Rafi, I., Griffin, M.J., Calvert, A.H., Newell, D.R., Calvete, J.A., Johnston, A., Clendeninn, N., Boddy, A.V. Clin. Cancer Res. (1999) [Pubmed]
  5. A phase I study of nolatrexed dihydrochloride in children with advanced cancer. A United Kingdom Children's Cancer Study Group Investigation. Estlin, E.J., Pinkerton, C.R., Lewis, I.J., Lashford, L., McDowell, H., Morland, B., Kohler, J., Newell, D.R., Boddy, A.V., Taylor, G.A., Price, L., Ablett, S., Hobson, R., Pitsiladis, M., Brampton, M., Clendeninn, N., Johnston, A., Pearson, A.D. Br. J. Cancer (2001) [Pubmed]
  6. Clinical pharmacokinetic and in vitro combination studies of nolatrexed dihydrochloride (AG337, Thymitaq) and paclitaxel. Hughes, A.N., Griffin, M.J., Newell, D.R., Calvert, A.H., Johnston, A., Kerr, B., Lee, C., Liang, B., Boddy, A.V. Br. J. Cancer (2000) [Pubmed]
  7. A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration. Jodrell, D.I., Bowman, A., Rye, R., Byrne, B., Boddy, A., Rafi, I., Taylor, G.A., Johnston, A., Clendeninn, N.J. Br. J. Cancer (1999) [Pubmed]
  8. Serine/threonine protein phosphatase inhibition enhances the effect of thymidylate synthase inhibition. Sakoff, J.A., Howitt, I.J., Ackland, S.P., McCluskey, A. Cancer Chemother. Pharmacol. (2004) [Pubmed]
  9. Characterization and drug sensitivity of four newly established colon adenocarcinoma cell lines to antifolate inhibitors of thymidylate synthase. Longo, G.S., Izzo, J., Gorlick, R., Banerjee, D., Jhanwar, S.C., Bertino, J.R. Oncol. Res. (2000) [Pubmed]
  10. A multi-centre randomized phase II study of nolatrexed versus doxorubicin in treatment of Chinese patients with advanced hepatocellular carcinoma. Mok, T.S., Leung, T.W., Lee, S.D., Chao, Y., Chan, A.T., Huang, A., Lui, M.C., Yeo, W., Chak, K., Johnston, A., Johnson, P. Cancer Chemother. Pharmacol. (1999) [Pubmed]
  11. Elevation of radiolabelled thymidine uptake in RIF-1 fibrosarcoma and HT29 colon adenocarcinoma cells after treatment with thymidylate synthase inhibitors. Yau, K., Price, P., Pillai, R.G., Aboagye, E. Eur. J. Nucl. Med. Mol. Imaging (2006) [Pubmed]
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