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Chemical Compound Review

Sunitanib     N-(2-diethylaminoethyl)-5- [(Z)-(5-fluoro-2...

Synonyms: Sunitinib, Sutent, sunitinibum, CHEMBL535, QCR-67, ...
Nathalie Lassau, Serge Koscielny, Laurence Albiges, Linda Chami, Baya Benatsou, Mohamed Chebil, Alain Roche, Bernard J. Escudier,  Mendel,  Haznedar,  Ngai,  Shirazian,  Sun,  Blake,  McMahon,  Cherrington,  Chan,  Schreck,  Miller,  Louie,  Xin,  Murray,  Moss,  Tang,  Carver,  Christensen,  Li,  Laird,  Sukbuntherng,  Abrams,  Lee, Brian I. Rini, Tarek Mekhail, Ernest Borden, G. Thomas Budd, Matthew M. Cooney, Jorge A. Garcia, Allison Tyler, Pierre Triozzi, Afshin Dolwati, Kristi Beatty, Robert Dreicer, Joseph Bokar, Percy Ivy, Helen X. Chen, Paul Elson, R.M. Bukowski,  Fiedler,  Hossfeld,  Manning,  Louie,  Ottmann,  Bello,  Scigalla,  Berdel,  Massimini,  Brega,  Allred,  Hong,  Serve,  Döhner,  Schwittay,  Cherrington,  O'Farrell,  Takahashi,  Obata,  Tamaki,  Ciomei,  Croci,  Pesenti,  Ballinari,  Ciavolella, George D. Demetri, Annick D. Van den Abbeele, Darrel P. Cohen, Jeffrey A. Morgan, Michael C. Heinrich, Jonathan A. Fletcher, Charles M. Baum, Ming Hui Chen, Cristina R. Antonescu, Christopher D. M. Fletcher, Carlo L. Bello, Xin Huang, Robert G. Maki, Suzanne George, Christopher L. Corless,  Morimoto,  McArthur,  Tan,  Toner,  West,  Smolich,  Manning,  Cherrington, Pierre I. Karakiewicz, Claudio Jeldres, Paul Perrotte, Nazareno Suardi, Pascale Audet, Jean-Jacques Patard, Pierre Ghosn,  O'Farrell,  Town,  Ngai,  Wong,  Yee,  Yuen,  Heinrich,  Murray,  Cherrington,  Lee,  Manning,  Smolich,  Louie,  Hong,  Abrams,  Ikezoe,  Taguchi,  Nishioka,  Nakatani,  Yang,  Taguchi,  Bandobashi,  Koeffler,  Marzola,  Osculati,  Crescimanno,  Pesenti,  Nicolato,  Terron,  Calderan,  Degrassi,  Giusti,  Farace,  Sbarbati,  Sandri,  Sun,  Sistla,  Chu,  Shirazian,  Tang,  Nematalla,  Wei,  Zhou,  Wang,  Cui,  Liang,  Chen,  Miller,  Luu,  Tang,  Fukuda,  Pagel,  Rader,  Baldwin,  Kotyk,  Murray,  Olson,  Brassard,  Ngai,  Cherrington,  Pryer,  O'Farrell,  Abrams,  Keast,  Long,  Hong, Christian Eichelberg, Kristin Hinrichs, Mario Zacharias, Roman Heuer, Hans Heinzer, Felix K. Chun, Hartwig Huland,  Roskoski,  O'Farrell,  Yuen,  Cooper,  Louie,  Fiedler,  Cherrington,  Paquette,  Kim,  Jacobs,  Berdel,  Heinrich,  Manning,  Serve,  Nicholas,  Scigalla,  Bello,  Kelsey,  Foran, Glenn Liu, Robert Jeraj, Matt Vanderhoek, Scott Perlman, Jill Kolesar, Michael Harrison, Urban Simoncic, Jens Eickhoff, Lakeesha Carmichael, Bo Chao, Rebecca Marnocha, Percy Ivy, George Wilding,  
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Disease relevance of Sutent

  • In summary, monotherapy with SU11248 induced partial remissions of short duration in acute myeloid leukemia (AML) patients [1].
  • Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate [2].
  • The results suggest that edotecarin may serve as effective chemotherapy of colon cancer when used as a single agent, in combination with standard regimens and other topoisomerase inhibitors or with novel agents, such as the multitargeted tyrosine kinase inhibitor SU11248 [3].
  • This method has been used to assess the therapeutic efficacy of SU11248, a multi-targeted inhibitor with demonstrated anti-tumor activity and reduction of bone loss, in a murine model of metastasized breast tumor cells [4].
  • Patients on sunitinib should be strictly monitored for the appearance of hypothyroidism and promptly treated [5].
  • She was offered two cycles of sunitinib maleate (Sutent) induction therapy to down-stage the thrombus and to reduce the extent of the surgery [6].
  • There was one dose-limiting toxicity (grade 4 hypertension) at 37.5 mg sunitinib and 5 mg/kg bevacizumab [7].
  • The effect of sunitinib on the brain tumor distribution of TMZ was dose dependent and indicated that optimal tumor exposure was achieved at a lower dose and was associated with the VNI [8].
  • DCE-US is a useful tool for predicting the early efficacy of sunitinib in metastatic renal cell carcinoma patients [9].
  • The increase of cellular proliferation during sunitinib withdrawal in patients with renal cell carcinoma and other solid malignancies is consistent with a VEGF receptor (VEGFR) tyrosine kinase inhibitor (TKI) withdrawal flare [10].
  • Our results reveal that endothelial ATX acts through LPA signaling to promote renal tumorigenesis and is functionally involved in the acquired resistance of RCC to sunitinib [11].

High impact information on Sutent

  • These data suggest that the addition of potent FLT3 inhibitors such as SU11248 to AML chemotherapy regimens could result in improved treatment results [12].
  • The synergistic interaction of SU11248 and the traditional antileukemic agents was more pronounced for induction of apoptosis [12].
  • SU11248 inhibited the proliferation of primary AML myeloblasts expressing mutant FLT3 ITD but not WT FLT3 protein [12].
  • SU11248 is a recently described selective inhibitor with selectivity for split kinase domain RTKs, including platelet-derived growth factor receptors, vascular endothelial growth factor receptors, and KIT [13].
  • We show that SU11248 also has potent activity against wild-type FLT3 (FLT3-WT), FLT3-ITD, and FLT3 activation loop (FLT3-Asp835) mutants in phosphorylation assays [13].

Chemical compound and disease context of Sutent


Biological context of Sutent


Anatomical context of Sutent


Associations of Sutent with other chemical compounds

  • Combining SU11248 and cytarabine synergistically inhibited the proliferation of primary AML myeloblasts expressing FLT3 ITD but not WT FLT3 protein [12].
  • SU11248 is an oral, selective multitargeted tyrosine kinase inhibitor currently in Phase II oncology clinical trials [15].
  • EXPERIMENTAL DESIGN: Primary imatinib-resistant tumor cells and cell lines expressing clinically identified imatinib-resistant KIT-V654A, KIT-T670I, or PDGFRA-D842V mutant isoforms were evaluated for sensitivity to SU11248 by Western immunoblotting and proliferation assays [2].
  • Design: SU11248, SU5416, and SU6668 were synthesized, and their inhibitory potencies were evaluated using an in vitro RET/PTC kinase assay [22].
  • To our knowledge, this is the second largest study reporting results of sequential therapy from sorafenib followed by sunitinib [23].
  • Cellular and molecular analyses showed that sunitinib clinical activity is associated with inhibition of KIT in GIST following imatinib failure, illustrating the rational approach used to develop a therapy aimed at the underlying oncogenic signaling pathway aberrancy [24].
  • Sunitinib resistance in GIST shares similar pathogenetic mechanisms identified in imatinib failure, with acquisition of secondary mutations in the activation domain after an extended initial response to the drug [25].

Gene context of Sutent


Analytical, diagnostic and therapeutic context of Sutent


  1. A phase 1 study of SU11248 in the treatment of patients with refractory or resistant acute myeloid leukemia (AML) or not amenable to conventional therapy for the disease. Fiedler, W., Serve, H., Döhner, H., Schwittay, M., Ottmann, O.G., O'Farrell, A.M., Bello, C.L., Allred, R., Manning, W.C., Cherrington, J.M., Louie, S.G., Hong, W., Brega, N.M., Massimini, G., Scigalla, P., Berdel, W.E., Hossfeld, D.K. Blood (2005) [Pubmed]
  2. Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Prenen, H., Cools, J., Mentens, N., Folens, C., Sciot, R., Schöffski, P., Van Oosterom, A., Marynen, P., Debiec-Rychter, M. Clin. Cancer Res. (2006) [Pubmed]
  3. Antitumor efficacy of edotecarin as a single agent and in combination with chemotherapy agents in a xenograft model. Ciomei, M., Croci, V., Ciavolella, A., Ballinari, D., Pesenti, E. Clin. Cancer Res. (2006) [Pubmed]
  4. Assessment of anti-metastatic drug efficacy via localization and quantification of ex vivo murine bone tumor load using high-throughput MRI T1 parametric analysis. Pagel, M.D., Baldwin, S.J., Rader, R.K., Kotyk, J.J. NMR in biomedicine. (2006) [Pubmed]
  5. A novel tyrosine-kinase selective inhibitor, sunitinib, induces transient hypothyroidism by blocking iodine uptake. Mannavola, D., Coco, P., Vannucchi, G., Bertuelli, R., Carletto, M., Casali, P.G., Beck-Peccoz, P., Fugazzola, L. J. Clin. Endocrinol. Metab. (2007) [Pubmed]
  6. Neoadjuvant sutent induction therapy may effectively down-stage renal cell carcinoma atrial thrombi. Karakiewicz, P.I., Suardi, N., Jeldres, C., Audet, P., Ghosn, P., Patard, J.J., Perrotte, P. Eur. Urol. (2008) [Pubmed]
  7. A phase I study of sunitinib plus bevacizumab in advanced solid tumors. Rini, B.I., Garcia, J.A., Cooney, M.M., Elson, P., Tyler, A., Beatty, K., Bokar, J., Mekhail, T., Bukowski, R.M., Budd, G.T., Triozzi, P., Borden, E., Ivy, P., Chen, H.X., Dolwati, A., Dreicer, R. Clin. Cancer Res. (2009) [Pubmed]
  8. Differential effect of sunitinib on the distribution of temozolomide in an orthotopic glioma model. Zhou, Q., Gallo, J.M. Neuro-oncology (2009) [Pubmed]
  9. Metastatic renal cell carcinoma treated with sunitinib: early evaluation of treatment response using dynamic contrast-enhanced ultrasonography. Lassau, N., Koscielny, S., Albiges, L., Chami, L., Benatsou, B., Chebil, M., Roche, A., Escudier, B.J. Clin. Cancer Res. (2010) [Pubmed]
  10. Pharmacodynamic study using FLT PET/CT in patients with renal cell cancer and other solid malignancies treated with sunitinib malate. Liu, G., Jeraj, R., Vanderhoek, M., Perlman, S., Kolesar, J., Harrison, M., Simoncic, U., Eickhoff, J., Carmichael, L., Chao, B., Marnocha, R., Ivy, P., Wilding, G. Clin. Cancer Res. (2011) [Pubmed]
  11. Autotaxin-lysophosphatidic acid signaling axis mediates tumorigenesis and development of acquired resistance to sunitinib in renal cell carcinoma. Su, S.C., Hu, X., Kenney, P.A., Merrill, M.M., Babaian, K.N., Zhang, X.Y., Maity, T., Yang, S.F., Lin, X., Wood, C.G. Clin. Cancer Res. (2013) [Pubmed]
  12. Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells. Yee, K.W., Schittenhelm, M., O'Farrell, A.M., Town, A.R., McGreevey, L., Bainbridge, T., Cherrington, J.M., Heinrich, M.C. Blood (2004) [Pubmed]
  13. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. O'Farrell, A.M., Abrams, T.J., Yuen, H.A., Ngai, T.J., Louie, S.G., Yee, K.W., Wong, L.M., Hong, W., Lee, L.B., Town, A., Smolich, B.D., Manning, W.C., Murray, L.J., Heinrich, M.C., Cherrington, J.M. Blood (2003) [Pubmed]
  14. Sunitinib inhibits tumor growth and synergizes with cisplatin in orthotopic models of cisplatin-sensitive and cisplatin-resistant human testicular germ cell tumors. Castillo-Avila, W., Piulats, J.M., Garcia Del Muro, X., Vidal, A., Condom, E., Casanovas, O., Mora, J., Germà, J.R., Capellà, G., Villanueva, A., Viñals, F. Clin. Cancer Res. (2009) [Pubmed]
  15. Gene expression profiling of human colon xenograft tumors following treatment with SU11248, a multitargeted tyrosine kinase inhibitor. Morimoto, A.M., Tan, N., West, K., McArthur, G., Toner, G.C., Manning, W.C., Smolich, B.D., Cherrington, J.M. Oncogene (2004) [Pubmed]
  16. Early antiangiogenic activity of SU11248 evaluated in vivo by dynamic contrast-enhanced magnetic resonance imaging in an experimental model of colon carcinoma. Marzola, P., Degrassi, A., Calderan, L., Farace, P., Nicolato, E., Crescimanno, C., Sandri, M., Giusti, A., Pesenti, E., Terron, A., Sbarbati, A., Osculati, F. Clin. Cancer Res. (2005) [Pubmed]
  17. An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. O'Farrell, A.M., Foran, J.M., Fiedler, W., Serve, H., Paquette, R.L., Cooper, M.A., Yuen, H.A., Louie, S.G., Kim, H., Nicholas, S., Heinrich, M.C., Berdel, W.E., Bello, C., Jacobs, M., Scigalla, P., Manning, W.C., Kelsey, S., Cherrington, J.M. Clin. Cancer Res. (2003) [Pubmed]
  18. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. Sun, L., Liang, C., Shirazian, S., Zhou, Y., Miller, T., Cui, J., Fukuda, J.Y., Chu, J.Y., Nematalla, A., Wang, X., Chen, H., Sistla, A., Luu, T.C., Tang, F., Wei, J., Tang, C. J. Med. Chem. (2003) [Pubmed]
  19. SU11248 inhibits tumor growth and CSF-1R-dependent osteolysis in an experimental breast cancer bone metastasis model. Murray, L.J., Abrams, T.J., Long, K.R., Ngai, T.J., Olson, L.M., Hong, W., Keast, P.K., Brassard, J.A., O'Farrell, A.M., Cherrington, J.M., Pryer, N.K. Clin. Exp. Metastasis (2003) [Pubmed]
  20. SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Schueneman, A.J., Himmelfarb, E., Geng, L., Tan, J., Donnelly, E., Mendel, D., McMahon, G., Hallahan, D.E. Cancer Res. (2003) [Pubmed]
  21. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Mendel, D.B., Laird, A.D., Xin, X., Louie, S.G., Christensen, J.G., Li, G., Schreck, R.E., Abrams, T.J., Ngai, T.J., Lee, L.B., Murray, L.J., Carver, J., Chan, E., Moss, K.G., Haznedar, J.O., Sukbuntherng, J., Blake, R.A., Sun, L., Tang, C., Miller, T., Shirazian, S., McMahon, G., Cherrington, J.M. Clin. Cancer Res. (2003) [Pubmed]
  22. An Orally Administered Multitarget Tyrosine Kinase Inhibitor, SU11248, Is a Novel Potent Inhibitor of Thyroid Oncogenic RET/Papillary Thyroid Cancer Kinases. Kim, D.W., Jo, Y.S., Jung, H.S., Chung, H.K., Song, J.H., Park, K.C., Park, S.H., Hwang, J.H., Rha, S.Y., Kweon, G.R., Lee, S.J., Jo, K.W., Shong, M. J. Clin. Endocrinol. Metab. (2006) [Pubmed]
  23. Sequential use of the tyrosine kinase inhibitors sorafenib and sunitinib in metastatic renal cell carcinoma: a retrospective outcome analysis. Eichelberg, C., Heuer, R., Chun, F.K., Hinrichs, K., Zacharias, M., Huland, H., Heinzer, H. Eur. Urol. (2008) [Pubmed]
  24. Molecular target modulation, imaging, and clinical evaluation of gastrointestinal stromal tumor patients treated with sunitinib malate after imatinib failure. Demetri, G.D., Heinrich, M.C., Fletcher, J.A., Fletcher, C.D., Van den Abbeele, A.D., Corless, C.L., Antonescu, C.R., George, S., Morgan, J.A., Chen, M.H., Bello, C.L., Huang, X., Cohen, D.P., Baum, C.M., Maki, R.G. Clin. Cancer Res. (2009) [Pubmed]
  25. Mechanisms of sunitinib resistance in gastrointestinal stromal tumors harboring KITAY502-3ins mutation: an in vitro mutagenesis screen for drug resistance. Guo, T., Hajdu, M., Agaram, N.P., Shinoda, H., Veach, D., Clarkson, B.D., Maki, R.G., Singer, S., Dematteo, R.P., Besmer, P., Antonescu, C.R. Clin. Cancer Res. (2009) [Pubmed]
  26. Sunitinib: A VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Roskoski, R. Biochem. Biophys. Res. Commun. (2007) [Pubmed]
  27. The receptor tyrosine kinase inhibitor SU11248 impedes endothelial cell migration, tubule formation, and blood vessel formation in vivo, but has little effect on existing tumor vessels. Osusky, K.L., Hallahan, D.E., Fu, A., Ye, F., Shyr, Y., Geng, L. Angiogenesis (2004) [Pubmed]
  28. Hair depigmentation is a biological readout for pharmacological inhibition of KIT in mice and humans. Moss, K.G., Toner, G.C., Cherrington, J.M., Mendel, D.B., Laird, A.D. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  29. A novel vascular endothelial growth factor receptor 2 inhibitor, SU11248, suppresses choroidal neovascularization in vivo. Takahashi, H., Obata, R., Tamaki, Y. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. (2006) [Pubmed]
  30. Effect of SU11248 on gastrointestinal stromal tumor-T1 cells: enhancement of growth inhibition via inhibition of 3-kinase/Akt/mammalian target of rapamycin signaling. Ikezoe, T., Yang, Y., Nishioka, C., Bandobashi, K., Nakatani, H., Taguchi, T., Koeffler, H.P., Taguchi, H. Cancer Sci. (2006) [Pubmed]
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