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Chemical Compound Review

Amsalog     9-[[2-methoxy-4- (methylsulfonylamino)pheny...

Synonyms: Asulacrine, CHEMBL48880, CCRIS 1030, Ci-921, NSC-343499, ...
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Disease relevance of Ci-921


High impact information on Ci-921


Chemical compound and disease context of Ci-921

  • Pharmacokinetic and toxicity scaling of the antitumor agents amsacrine and CI-921, a new analogue, in mice, rats, rabbits, dogs, and humans [1].

Biological context of Ci-921

  • Pharmacokinetics were evaluated following 65 infusions on Days 1 and 3 with plasma concentrations of CI-921 measured by high performance liquid chromatography [9].
  • Pulse exposure of cells to CI-921 resulted in transient accumulations of cells in S and/or G2 phase depending upon dose [10].
  • It was concluded that allometric equations may be developed for CI-921 and amsacrine from animal pharmacokinetic data which allow a reasonable prediction of Cl and Vss in patients, despite these agents being eliminated mainly by biotransformation [1].
  • Cell viability was unaffected in Friend erythroleukemic cell cultures at concentrations up to 50 nM, although growth was inhibited by 50% following 24 h of continuous exposure to 9.5 nM or a 1 h pulse of 67.5 nM CI-921 [10].
  • A study of amsalog (CI-921) administered orally on a 5-day schedule, with bioavailability and pharmacokinetically guided dose escalation [11].

Anatomical context of Ci-921

  • The selectivity of CI-921 for L1210 versus bone marrow, and for LLAK versus L1210 or P388, was greater than that of amsacrine, again in keeping with its in vivo properties [12].
  • Both amsacrine and its analogue, N-5-dimethyl-9-[(2-methoxy-4- methylsulphonylamino)phenylamino]-4-acridinecarboxamide (CI-921) are absorbed from the gastrointestinal tract in rabbits [13].

Associations of Ci-921 with other chemical compounds


Gene context of Ci-921

  • For CI-921 the allometric equations for the kinetic parameters calculated from plasma "free" concentrations were: Vssfu (liters) = 247W0.93 (r = 0.984, P = 0.002) and Clu (liters/h) = 186W0.76 (r = 0.961, P = 0.009) [1].
  • The activity of DACA was comparable with that of 5-fluorouracil and superior to that of doxorubicin, cyclophosphamide and the experimental amsacrine analogue CI-921 [16].
  • RESULTS: Patients who had a high TP level in normal liver tissue had significantly earlier recurrence (median disease-free survival, 819 days; 95% confidence interval [95% CI], 478-1044 days) compared with patients who had a low TP level (median disease-free survival, 1376 days; lower limit of 95% CI, 921 days; P = 0.0171) [17].

Analytical, diagnostic and therapeutic context of Ci-921


  1. Pharmacokinetic and toxicity scaling of the antitumor agents amsacrine and CI-921, a new analogue, in mice, rats, rabbits, dogs, and humans. Paxton, J.W., Kim, S.N., Whitfield, L.R. Cancer Res. (1990) [Pubmed]
  2. CI-921: an analog of amsacrine with experimental activity against solid tumors. Grove, W.R., DeLap, L.W., Grillo-López, A.J. Investigational new drugs. (1986) [Pubmed]
  3. Potentiation by phenylbisbenzimidazoles of cytotoxicity of anticancer drugs directed against topoisomerase II. Finlay, G.J., Baguley, B.C. Eur. J. Cancer (1990) [Pubmed]
  4. Phase II study of the amsacrine analogue CI-921 (NSC 343499) in non-small cell lung cancer. Harvey, V.J., Hardy, J.R., Smith, S., Grove, W., Baguley, B.C. Eur. J. Cancer (1991) [Pubmed]
  5. Comparison of the mutagenicity of amsacrine with that of a new clinical analogue, CI-921. Ferguson, L.R., van Zijl, P., Baguley, B.C. Mutat. Res. (1988) [Pubmed]
  6. Design of DNA intercalators to overcome topoisomerase II-mediated multidrug resistance. Baguley, B.C., Holdaway, K.M., Fray, L.M. J. Natl. Cancer Inst. (1990) [Pubmed]
  7. Experimental antitumor activity of the amsacrine analogue CI-921. Leopold, W.R., Corbett, T.H., Griswold, D.P., Plowman, J., Baguley, B.C. J. Natl. Cancer Inst. (1987) [Pubmed]
  8. Disposition of amsacrine and its analogue 9-([2-methoxy-4-[(methylsulfonyl)amino]phenyl]amino)-N,5-dimethyl-4- acridinecarboxamide (CI-921) in plasma, liver, and Lewis lung tumors in mice. Kestell, P., Paxton, J.W., Evans, P.C., Young, D., Jurlina, J.L., Robertson, I.G., Baguley, B.C. Cancer Res. (1990) [Pubmed]
  9. Phase I trial of the amsacrine analogue 9-[( 2-methoxy-4-[(methylsulfonyl)amino]-phenyl]amino)-N,5-dimethyl-4- acridinecarboxamide (CI-921). Hardy, J.R., Harvey, V.J., Paxton, J.W., Evans, P., Smith, S., Grove, W., Grillo-Lopez, A.J., Baguley, B.C. Cancer Res. (1988) [Pubmed]
  10. Effects of a new amsacrine derivative, N-5-dimethyl-9-(2-methoxy-4-methylsulfonylamino)phenylamino-4- acridinecarboxamide, on cultured mammalian cells. Traganos, F., Bueti, C., Darzynkiewicz, Z., Melamed, M.R. Cancer Res. (1987) [Pubmed]
  11. A study of amsalog (CI-921) administered orally on a 5-day schedule, with bioavailability and pharmacokinetically guided dose escalation. Fyfe, D., Raynaud, F., Langley, R.E., Newell, D.R., Halbert, G., Gardner, C., Clayton, K., Woll, P.J., Judson, I., Carmichael, J. Cancer Chemother. Pharmacol. (2002) [Pubmed]
  12. Comparison of the cytotoxicity of amsacrine and its analogue CI-921 against cultured human and mouse bone marrow tumour cells. Ching, L.M., Finlay, G.J., Joseph, W.R., Baguley, B.C. Eur. J. Cancer (1990) [Pubmed]
  13. The effect of food on the bioavailability and kinetics of the anticancer drug amsacrine and a new analogue, N-5-dimethyl-9-[(2-methoxy-4-methylsulphonylamino)phenylamino]-4 acridinecarboxamide in rabbits. Paxton, J.W. J. Pharm. Pharmacol. (1986) [Pubmed]
  14. Oxidative metabolism of amsacrine by the neutrophil enzyme myeloperoxidase. Kettle, A.J., Robertson, I.G., Palmer, B.D., Anderson, R.F., Patel, K.B., Winterbourn, C.C. Biochem. Pharmacol. (1992) [Pubmed]
  15. Dose-dependent pharmacokinetics of N-5-dimethyl-9-[(2-methoxy-4-methylsulphonylamino)phenylamino]- 4-acridinecarboxamide (CI-921) in rabbits. Paxton, J.W., Evans, P.C., Singh, R.M. Cancer Chemother. Pharmacol. (1987) [Pubmed]
  16. Experimental solid tumour activity of N-[2-(dimethylamino)ethyl]-acridine-4-carboxamide. Baguley, B.C., Zhuang, L., Marshall, E. Cancer Chemother. Pharmacol. (1995) [Pubmed]
  17. Prognostic value of thymidine phosphorylase activity in liver tissue adjacent to hepatocellular carcinoma. Ezaki, T., Ikegami, T., Maeda, T., Yamada, T., Ishida, T., Hashizume, M., Maehara, Y. Int. J. Clin. Oncol. (2005) [Pubmed]
  18. The clinical pharmacokinetics of N-5-dimethyl-9-[(2-methoxy-4-methyl-sulfonylamino)phenylamino]-4 -acridinecarboxamide (CI-921) in a phase 1 trial. Paxton, J.W., Hardy, J.R., Evans, P.C., Harvey, V.J., Baguley, B.C. Cancer Chemother. Pharmacol. (1988) [Pubmed]
  19. A phase I trial of amsalog (CI-921) administered by intravenous infusion using a 5-day schedule. Fyfe, D., Price, C., Langley, R.E., Pagonis, C., Houghton, J., Osborne, L., Woll, P.J., Gardner, C., Baguley, B.C., Carmichael, J. Cancer Chemother. Pharmacol. (2001) [Pubmed]
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