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Chemical Compound Review

Pelitinib     (E)-N-[4-[(3-chloro-4-fluoro- phenyl)amino]...

Synonyms: WAY-EKB-569, WAY-EKB 569, cc-21, EKB-569, QCR-124, ...
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Disease relevance of EKB 569

  • Thus, EGFR blockade (using an irreversible EGFR kinase inhibitor designated EKB-569) prevents virus-induced increases in ciliated and goblet cells whereas IL-13 blockade (using s-IL-13Ralpha2-Fc) exacerbates ciliated cell hyperplasia but still inhibits goblet cell metaplasia [1].
  • RESULTS: Treatment of BPK mice with EKB-569 alone resulted in a marked reduction of kidney weight/body weight ratios, dramatically reduced collecting tubule cystic index, as well as BDE, and improved renal function [2].
  • The intraperitoneal administration of EKI-785 (90 mg/kg body weight every third day) or of EKB-569 (20 mg/kg body weight every third day) to cy/+ rats resulted in lower kidney weights, serum concentrations of blood urea nitrogen (BUN), cyst volumes, and fibrosis scores [3].
  • Consistent with these expression results, EKI-785 or EKB-569 administration had no effect or worsened PKD, and had no effect on the development of fibrocystic liver disease [4].
  • Dose-limiting toxicity was grade 3 diarrhea, and the MTD was 75 mg EKB-569 per day for both cohorts [5].

High impact information on EKB 569

  • These compounds demonstrated enhanced activities for inhibiting HER-2 kinase and the growth of HER-2 positive cells compared to our EGFR kinase inhibitor 86 (EKB-569) [6].
  • METHODS: To determine whether EGFR tyrosine kinase inhibition is protective in the PCK rat, male and female animals were treated with EKI-785 or EKB-569 or with vehicle alone between 3 and 10 weeks of age [4].
  • The administration of EKB-569 by gavage was less effective probably because of lower bioavailability [3].
  • The reduction in pEGF-R paralleled inhibition of phosphotyrosine-705 STAT3, while the inhibition of phosphorylated AKT and phosphorylated ERK1/2 occurred at higher concentrations of EKB-569 (75-500 nM) in both A431 and NHEK cells [7].

Biological context of EKB 569


Gene context of EKB 569

  • The RD of EKB-569 is 25 mg/day when combined with FOLFIRI and results in complete EGFR inhibition [9].

Analytical, diagnostic and therapeutic context of EKB 569


  1. Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals. Tyner, J.W., Kim, E.Y., Ide, K., Pelletier, M.R., Roswit, W.T., Morton, J.D., Battaile, J.T., Patel, A.C., Patterson, G.A., Castro, M., Spoor, M.S., You, Y., Brody, S.L., Holtzman, M.J. J. Clin. Invest. (2006) [Pubmed]
  2. Combination treatment of PKD utilizing dual inhibition of EGF-receptor activity and ligand bioavailability. Sweeney, W.E., Hamahira, K., Sweeney, J., Garcia-Gatrell, M., Frost, P., Avner, E.D. Kidney Int. (2003) [Pubmed]
  3. EGF receptor tyrosine kinase inhibition attenuates the development of PKD in Han:SPRD rats. Torres, V.E., Sweeney, W.E., Wang, X., Qian, Q., Harris, P.C., Frost, P., Avner, E.D. Kidney Int. (2003) [Pubmed]
  4. Epidermal growth factor receptor tyrosine kinase inhibition is not protective in PCK rats. Torres, V.E., Sweeney, W.E., Wang, X., Qian, Q., Harris, P.C., Frost, P., Avner, E.D. Kidney Int. (2004) [Pubmed]
  5. Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors. Erlichman, C., Hidalgo, M., Boni, J.P., Martins, P., Quinn, S.E., Zacharchuk, C., Amorusi, P., Adjei, A.A., Rowinsky, E.K. J. Clin. Oncol. (2006) [Pubmed]
  6. Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. Tsou, H.R., Overbeek-Klumpers, E.G., Hallett, W.A., Reich, M.F., Floyd, M.B., Johnson, B.D., Michalak, R.S., Nilakantan, R., Discafani, C., Golas, J., Rabindran, S.K., Shen, R., Shi, X., Wang, Y.F., Upeslacis, J., Wissner, A. J. Med. Chem. (2005) [Pubmed]
  7. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Nunes, M., Shi, C., Greenberger, L.M. Mol. Cancer Ther. (2004) [Pubmed]
  8. Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents. Wissner, A., Brawner Floyd, M.B., Rabindran, S.K., Nilakantan, R., Greenberger, L.M., Shen, R., Wang, Y.F., Tsou, H.R. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
  9. Phase I pharmacokinetic/pharmacodynamic study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor tyrosine kinase, in combination with irinotecan, 5-fluorouracil, and leucovorin (FOLFIRI) in first-line treatment of patients with metastatic colorectal cancer. Folprecht, G., Tabernero, J., Köhne, C.H., Zacharchuk, C., Paz-Ares, L., Rojo, F., Quinn, S., Casado, E., Salazar, R., Abbas, R., Lejeune, C., Marimón, I., Andreu, J., Ubbelohde, U., Cortes-Funes, H., Baselga, J. Clin. Cancer Res. (2008) [Pubmed]
  10. Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2). Wissner, A., Overbeek, E., Reich, M.F., Floyd, M.B., Johnson, B.D., Mamuya, N., Rosfjord, E.C., Discafani, C., Davis, R., Shi, X., Rabindran, S.K., Gruber, B.C., Ye, F., Hallett, W.A., Nilakantan, R., Shen, R., Wang, Y.F., Greenberger, L.M., Tsou, H.R. J. Med. Chem. (2003) [Pubmed]
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