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Chemical Compound Review

Lapatinib     N-[3-chloro-4-[(3- fluorophenyl)methoxy]phe...

Synonyms: Tycerb, Tykerb, Tyverb, CHEMBL554, QCR-63, ...
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Disease relevance of Lapatinib


Psychiatry related information on Lapatinib

  • Using gene interference, we confirm that acquired resistance to lapatinib is mediated by a switch in cell survival dependence and regulation of a key antiapoptotic mediator from ErbB2 alone to codependence upon ER and ErbB2 rather than loss of ErbB2 expression or insensitivity of ErbB2 signaling to lapatinib [11].

High impact information on Lapatinib


Chemical compound and disease context of Lapatinib


Biological context of Lapatinib


Anatomical context of Lapatinib


Associations of Lapatinib with other chemical compounds


Gene context of Lapatinib


Analytical, diagnostic and therapeutic context of Lapatinib


  1. Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers. Xia, W., Bisi, J., Strum, J., Liu, L., Carrick, K., Graham, K.M., Treece, A.L., Hardwicke, M.A., Dush, M., Liao, Q., Westlund, R.E., Zhao, S., Bacus, S., Spector, N.L. Cancer Res. (2006) [Pubmed]
  2. Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. Burris, H.A., Hurwitz, H.I., Dees, E.C., Dowlati, A., Blackwell, K.L., O'Neil, B., Marcom, P.K., Ellis, M.J., Overmoyer, B., Jones, S.F., Harris, J.L., Smith, D.A., Koch, K.M., Stead, A., Mangum, S., Spector, N.L. J. Clin. Oncol. (2005) [Pubmed]
  3. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Zhou, Y., Li, S., Hu, Y.P., Wang, J., Hauser, J., Conway, A.N., Vinci, M.A., Humphrey, L., Zborowska, E., Willson, J.K., Brattain, M.G. Cancer Res. (2006) [Pubmed]
  4. Old and new perspectives in the pharmacological treatment of advanced or recurrent endometrial cancer: Hormonal therapy, chemotherapy and molecularly targeted therapies. Gadducci, A., Cosio, S., Genazzani, A.R. Crit. Rev. Oncol. Hematol. (2006) [Pubmed]
  5. Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity. Montemurro, F., Valabrega, G., Aglietta, M. Expert opinion on biological therapy (2007) [Pubmed]
  6. Lapatinib antitumor activity is not dependent upon phosphatase and tensin homologue deleted on chromosome 10 in ErbB2-overexpressing breast cancers. Xia, W., Husain, I., Liu, L., Bacus, S., Saini, S., Spohn, J., Pry, K., Westlund, R., Stein, S.H., Spector, N.L. Cancer Res. (2007) [Pubmed]
  7. Multicenter phase II study of lapatinib in patients with brain metastases from HER2-positive breast cancer. Lin, N.U., Diéras, V., Paul, D., Lossignol, D., Christodoulou, C., Stemmler, H.J., Roché, H., Liu, M.C., Greil, R., Ciruelos, E., Loibl, S., Gori, S., Wardley, A., Yardley, D., Brufsky, A., Blum, J.L., Rubin, S.D., Dharan, B., Steplewski, K., Zembryki, D., Oliva, C., Roychowdhury, D., Paoletti, P., Winer, E.P. Clin. Cancer Res. (2009) [Pubmed]
  8. A phase I study of a 2-day lapatinib chemosensitization pulse preceding nanoparticle albumin-bound Paclitaxel for advanced solid malignancies. Chien, A.J., Illi, J.A., Ko, A.H., Korn, W.M., Fong, L., Chen, L.M., Kashani-Sabet, M., Ryan, C.J., Rosenberg, J.E., Dubey, S., Small, E.J., Jahan, T.M., Hylton, N.M., Yeh, B.M., Huang, Y., Koch, K.M., Moasser, M.M. Clin. Cancer Res. (2009) [Pubmed]
  9. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Wainberg, Z.A., Anghel, A., Desai, A.J., Ayala, R., Luo, T., Safran, B., Fejzo, M.S., Hecht, J.R., Slamon, D.J., Finn, R.S. Clin. Cancer Res. (2010) [Pubmed]
  10. Antiproliferative Effect of Lapatinib in HER2-Positive and HER2-Negative/HER3-High Breast Cancer: Results of the Presurgical Randomized MAPLE Trial (CRUK E/06/039). Leary, A., Evans, A., Johnston, S.R., A'Hern, R., Bliss, J.M., Sahoo, R., Detre, S., Haynes, B.P., Hills, M., Harper-Wynne, C., Bundred, N., Coombes, G., Smith, I., Dowsett, M. Clin. Cancer Res. (2015) [Pubmed]
  11. A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer. Xia, W., Bacus, S., Hegde, P., Husain, I., Strum, J., Liu, L., Paulazzo, G., Lyass, L., Trusk, P., Hill, J., Harris, J., Spector, N.L. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  12. Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Konecny, G.E., Pegram, M.D., Venkatesan, N., Finn, R., Yang, G., Rahmeh, M., Untch, M., Rusnak, D.W., Spehar, G., Mullin, R.J., Keith, B.R., Gilmer, T.M., Berger, M., Podratz, K.C., Slamon, D.J. Cancer Res. (2006) [Pubmed]
  13. The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Chu, I., Blackwell, K., Chen, S., Slingerland, J. Cancer Res. (2005) [Pubmed]
  14. Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Xia, W., Gerard, C.M., Liu, L., Baudson, N.M., Ory, T.L., Spector, N.L. Oncogene (2005) [Pubmed]
  15. Lapatinib plus capecitabine for HER2-positive advanced breast cancer. Geyer, C.E., Forster, J., Lindquist, D., Chan, S., Romieu, C.G., Pienkowski, T., Jagiello-Gruszfeld, A., Crown, J., Chan, A., Kaufman, B., Skarlos, D., Campone, M., Davidson, N., Berger, M., Oliva, C., Rubin, S.D., Stein, S., Cameron, D. N. Engl. J. Med. (2006) [Pubmed]
  16. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Wood, E.R., Truesdale, A.T., McDonald, O.B., Yuan, D., Hassell, A., Dickerson, S.H., Ellis, B., Pennisi, C., Horne, E., Lackey, K., Alligood, K.J., Rusnak, D.W., Gilmer, T.M., Shewchuk, L. Cancer Res. (2004) [Pubmed]
  17. Epidermal growth factor receptor autocrine signaling in RIE-1 cells transformed by the Ras oncogene enhances radiation resistance. Grana, T.M., Sartor, C.I., Cox, A.D. Cancer Res. (2003) [Pubmed]
  18. Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Xia, W., Mullin, R.J., Keith, B.R., Liu, L.H., Ma, H., Rusnak, D.W., Owens, G., Alligood, K.J., Spector, N.L. Oncogene (2002) [Pubmed]
  19. Epidermal growth factor receptor inhibitors in development for the treatment of non-small cell lung cancer. Heymach, J.V., Nilsson, M., Blumenschein, G., Papadimitrakopoulou, V., Herbst, R. Clin. Cancer Res. (2006) [Pubmed]
  20. Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC. Langer, C.J. Int. J. Radiat. Oncol. Biol. Phys. (2004) [Pubmed]
  21. Prospective Study of Positron Emission Tomography for Evaluation of the Activity of Lapatinib, a Dual Inhibitor of the ErbB1 and ErbB2 Tyrosine Kinases, in Patients with Advanced Tumors. Kawada, K., Murakami, K., Sato, T., Kojima, Y., Ebi, H., Mukai, H., Tahara, M., Shimokata, K., Minami, H. Jpn. J. Clin. Oncol. (2007) [Pubmed]
  22. Inhibition of HER-2/neu kinase impairs androgen receptor recruitment to the androgen responsive enhancer. Liu, Y., Majumder, S., McCall, W., Sartor, C.I., Mohler, J.L., Gregory, C.W., Earp, H.S., Whang, Y.E. Cancer Res. (2005) [Pubmed]
  23. Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Xia, W., Liu, L.H., Ho, P., Spector, N.L. Oncogene (2004) [Pubmed]
  24. HER-2 gene amplification, HER-2 and epidermal growth factor receptor mRNA and protein expression, and lapatinib efficacy in women with metastatic breast cancer. Press, M.F., Finn, R.S., Cameron, D., Di Leo, A., Geyer, C.E., Villalobos, I.E., Santiago, A., Guzman, R., Gasparyan, A., Ma, Y., Danenberg, K., Martin, A.M., Williams, L., Oliva, C., Stein, S., Gagnon, R., Arbushites, M., Koehler, M.T. Clin. Cancer Res. (2008) [Pubmed]
  25. The 17q12-q21 amplicon: Her2 and topoisomerase-IIalpha and their importance to the biology of solid tumours. Mano, M.S., Rosa, D.D., De Azambuja, E., Ismael, G.F., Durbecq, V. Cancer Treat. Rev. (2007) [Pubmed]
  26. Synergistic inhibition of breast cancer cell lines with a dual inhibitor of EGFR-HER-2/neu and a Bcl-2 inhibitor. Witters, L.M., Witkoski, A., Planas-Silva, M.D., Berger, M., Viallet, J., Lipton, A. Oncol. Rep. (2007) [Pubmed]
  27. Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Nelson, M.H., Dolder, C.R. The Annals of pharmacotherapy. (2006) [Pubmed]
  28. Determination of lapatinib (GW572016) in human plasma by liquid chromatography electrospray tandem mass spectrometry (LC-ESI-MS/MS). Bai, F., Freeman, B.B., Fraga, C.H., Fouladi, M., Stewart, C.F. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. (2006) [Pubmed]
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