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MedKoo product information:

AEE-788

AEE-788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Current developer:   Novartis International AG。

 1: Evans AH, Pancholi S, Farmer I, Thornhill A, Evans DB, Johnston SR, Dowsett M, Martin LA. EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy. Br J Cancer. 2010 Apr 13;102(8):1235-43. PubMed PMID: 20386540; PubMed Central PMCID: PMC2856013.

2: Barbarroja N, Torres LA, Rodriguez-Ariza A, Valverde-Estepa A, Lopez-Sanchez LM, Ruiz-Limon P, Perez-Sanchez C, Carretero RM, Velasco F, López-Pedrera C. AEE788 is a vascular endothelial growth factor receptor tyrosine kinase inhibitor with antiproliferative and proapoptotic effects in acute myeloid leukemia. Exp Hematol. 2010 Apr 7. [Epub ahead of print] PubMed PMID: 20380868.

3: Deng M, Huang H, Jin H, Dirsch O, Dahmen U. The anti-proliferative side effects of AEE788, a tyrosine kinase inhibitor blocking both EGF- and VEGF-receptor, are liver-size-dependent after partial hepatectomy in rats. Invest New Drugs. 2010 Feb 12. [Epub ahead of print] PubMed PMID: 20148349.

4: Deng M, Huang H, Dirsch O, Dahmen U. Effect and risk of AEE788, a dual tyrosine kinase inhibitor, on regeneration in a rat liver resection model. Eur Surg Res. 2010;44(2):82-95. Epub 2010 Jan 19. PubMed PMID: 20090347.

5: Venkatesan P, Das S, Krishnan MM, Chakraborty C, Chaudhury K, Mandal M. Effect of AEE788 and/or Celecoxib on colon cancer cell morphology using advanced microscopic techniques. Micron. 2010 Apr;41(3):247-56. Epub 2009 Nov 10. PubMed PMID: 19945288.

6: Juengel E, Engler J, Mickuckyte A, Jones J, Hudak L, Jonas D, Blaheta RA. Effects of combined valproic acid and the epidermal growth factor/vascular endothelial growth factor receptor tyrosine kinase inhibitor AEE788 on renal cell carcinoma cell lines in vitro. BJU Int. 2010 Feb;105(4):549-57. Epub 2009 Jul 7. PubMed PMID: 19594733.

7: Juengel E, Engler J, Natsheh I, Jones J, Mickuckyte A, Hudak L, Jonas D, Blaheta RA. Combining the receptor tyrosine kinase inhibitor AEE788 and the mammalian target of rapamycin (mTOR) inhibitor RAD001 strongly inhibits adhesion and growth of renal cell carcinoma cells. BMC Cancer. 2009 May 27;9:161. PubMed PMID: 19473483; PubMed Central PMCID: PMC2693528.

8: Okamoto K, Neureiter D, Alinger B, Meissnitzer M, Sass G, Schmitz V, Di Fazio P, Wissniowski T, Gahr S, Hohenstein B, Kaufmann B, Schlösser A, Haus U, Hahn EG, Herold C, Ocker M. The dual EGF/VEGF receptor tyrosine kinase inhibitor AEE788 inhibits growth of human hepatocellular carcinoma xenografts in nude mice. Int J Oncol. 2008 Oct;33(4):733-42. PubMed PMID: 18813786.

9: Huamani J, Willey C, Thotala D, Niermann KJ, Reyzer M, Leavitt L, Jones C, Fleishcher A, Caprioli R, Hallahan DE, Kim DW. Differential efficacy of combined therapy with radiation and AEE788 in high and low EGFR-expressing androgen-independent prostate tumor models. Int J Radiat Oncol Biol Phys. 2008 May 1;71(1):237-46. Epub 2008 Mar 11. PubMed PMID: 18337021; PubMed Central PMCID: PMC2441843.

10: Oehler-Jänne C, Jochum W, Riesterer O, Broggini-Tenzer A, Caravatti G, Vuong V, Pruschy M. Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models. Mol Cancer Ther. 2007 Sep;6(9):2496-504. PubMed PMID: 17876047.

11: Yu C, Friday BB, Lai JP, McCollum A, Atadja P, Roberts LR, Adjei AA. Abrogation of MAPK and Akt signaling by AEE788 synergistically potentiates histone deacetylase inhibitor-induced apoptosis through reactive oxygen species generation. Clin Cancer Res. 2007 Feb 15;13(4):1140-8. PubMed PMID: 17317822.

12: Wiedmann M, Feisthammel J, Blüthner T, Tannapfel A, Kamenz T, Kluge A, Mössner J, Caca K. Novel targeted approaches to treating biliary tract cancer: the dual epidermal growth factor receptor and ErbB-2 tyrosine kinase inhibitor NVP-AEE788 is more efficient than the epidermal growth factor receptor inhibitors gefitinib and erlotinib. Anticancer Drugs. 2006 Aug;17(7):783-95. PubMed PMID: 16926628.

13: Younes MN, Yazici YD, Kim S, Jasser SA, El-Naggar AK, Myers JN. Dual epidermal growth factor receptor and vascular endothelial growth factor receptor inhibition with NVP-AEE788 for the treatment of aggressive follicular thyroid cancer. Clin Cancer Res. 2006 Jun 1;12(11 Pt 1):3425-34. PubMed PMID: 16740767.

14: Yokoi K, Thaker PH, Yazici S, Rebhun RR, Nam DH, He J, Kim SJ, Abbruzzese JL, Hamilton SR, Fidler IJ. Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model. Cancer Res. 2005 May 1;65(9):3716-25. PubMed PMID: 15867367.

15: Park YW, Younes MN, Jasser SA, Yigitbasi OG, Zhou G, Bucana CD, Bekele BN, Myers JN. AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005 Mar 1;11(5):1963-73. PubMed PMID: 15756022.

16: Kim S, Schiff BA, Yigitbasi OG, Doan D, Jasser SA, Bekele BN, Mandal M, Myers JN. Targeted molecular therapy of anaplastic thyroid carcinoma with AEE788. Mol Cancer Ther. 2005 Apr;4(4):632-40. PubMed PMID: 15827337.

17: Goudar RK, Shi Q, Hjelmeland MD, Keir ST, McLendon RE, Wikstrand CJ, Reese ED, Conrad CA, Traxler P, Lane HA, Reardon DA, Cavenee WK, Wang XF, Bigner DD, Friedman HS, Rich JN. Combination therapy of inhibitors of epidermal growth factor receptor/vascular endothelial growth factor receptor 2 (AEE788) and the mammalian target of rapamycin (RAD001) offers improved glioblastoma tumor growth inhibition. Mol Cancer Ther. 2005 Jan;4(1):101-12. PubMed PMID: 15657358.

18: Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J, Meyer T, Tang C, Wartmann M, Wood J, Caravatti G. AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2004 Jul 15;64(14):4931-41. PubMed PMID: 15256466.