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Bafetinib

Description of Bafetinib: Bafetinib is an orally bioavailable 2-phenylaminopyrimidine derivative with potential antineoplastic activity. Bafetinib specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML). This agent also inhibits the Src-family member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety of solid cancer cell types. The inhibitory effect of bafetinib on these specific tyrosine kinases may decrease cellular proliferation and induce apoptosis in tumor cells that overexpress these kinases. CML patients may be refractory to imatinib, which sometimes results from point mutations occurring in the kinase domain of the Bcr/Abl fusion product. Due to its dual inhibitory activity, the use of bafetinib has been shown to overcome this particular drug resistance. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Current developer:   CytRx Corporation

1. Moll, Juergen; Ballinari, Dario; Pesenti, Enrico. Therapeutic combination comprising an aurora kinase inhibitor and imatinib. U.S. Pat. Appl. Publ. (2010), 5pp. CODEN: USXXCO US 2010022553 A1 20100128 CAN 152:200065 AN 2010:112369

2. Kimura, Shinya. Bafetinib (INNO-406), a novel tyrosine kinase inhibitor for imatinib-resistant CML. Ketsueki, Shuyoka (2009), 59(4), 381-387. CODEN: KETSBI ISSN:0915-8529. AN 2010:55942

3. Rix, U.; Remsing Rix, L. L.; Terker, A. S.; Fernbach, N. V.; Hantschel, O.; Planyavsky, M.; Breitwieser, F. P.; Herrmann, H.; Colinge, J.; Bennett, K. L.; Augustin, M.; Till, J. H.; Heinrich, M. C.; Valent, P.; Superti-Furga, G. A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells. Leukemia (2010), 24(1), 44-50. CODEN: LEUKED ISSN:0887-6924. AN 2010:53301

4. Ramchandren, Radhakrishnan; Schiffer, Charles A. Dasatinib in the treatment of imatinib refractory chronic myeloid leukemia. Biologics: Targets & Therapy (2009), 3 205-214. CODEN: BTTICT ISSN:1177-5491. CAN 152:292 AN 2009:1487323

5. Takeuchi, M.; Kimura, S.; Ashihara, E.; Maekawa, T. BAFETINIB: dual BCR/ABL and Lyn tyrosine kinase inhibitor treatment of chronic myeloid leukemia. Drugs of the Future (2009), 34(4), 261-269. CODEN: DRFUD4 ISSN:0377-8282. CAN 152:491593 AN 2009:1293435

6. Aguilera, Dolly G.; Tsimberidou, Apostolia M. Dasatinib in chronic myeloid leukemia: a review. Therapeutics and Clinical Risk Management (2009), 5 281-289. CODEN: TCRMA6 ISSN:1178-203X. CAN 151:235303 AN 2009:928660

7. Adrian, Francisco; Dierks, Christine; Gray, Nathanael S.; Warmuth, Markus. Compositions and methods for treating antitumor resistant cancers using a combination of a ATP-competitive BCR-ABL inhibitor and a non-ATP BCR-ABL inhibitor. PCT Int. Appl. (2009), 56pp. CODEN: PIXXD2 WO 2009091476 A1 20090723 CAN 151:189956 AN 2009:885621

8. Pytel, Dariusz; Sliwinski, Tomasz; Poplawski, Tomasz; Ferriola, Deborah; Majsterek, Ireneusz. Tyrosine kinase blockers: new hope for successful cancer therapy. Anti-Cancer Agents in Medicinal Chemistry (2009), 9(1), 66-76. CODEN: AAMCE4 ISSN:1871-5206. CAN 150:463172 AN 2009:387485

9. Dierks, Christine; Warmuth, Markus. Methods and compositions of a hedgehog signaling antagonist and a BCR-ABL inhibitor for treating cancers. PCT Int. Appl. (2009), 49pp. CODEN: PIXXD2 WO 2009026075 A1 20090226 CAN 150:252611 AN 2009:237899

10. Gora-Tybor, Joanna; Robak, Tadeusz. Targeted drugs in chronic myeloid leukemia. Current Medicinal Chemistry (2008), 15(29), 3036-3051. CODEN: CMCHE7 ISSN:0929-8673. CAN 150:89605 AN 2009:90926

11. Fabarius, Alice; Giehl, Michelle; Rebacz, Blanka; Kraemer, Alwin; Frank, Oliver; Haferlach, Claudia; Duesberg, Peter; Hehlmann, Ruediger; Seifarth, Wolfgang; Hochhaus, Andreas. Centrosome aberrations and G1 phase arrest after in vitro and in vivo treatment with the SRC/ABL inhibitor dasatinib. Haematologica (2008), 93(8), 1145-1154. CODEN: HAEMAX ISSN:0390-6078. CAN 151:236548 AN 2008:1416814

12. Kufareva, Irina; Abagyan, Ruben. Type-II Kinase Inhibitor Docking, Screening, and Profiling Using Modified Structures of Active Kinase States. Journal of Medicinal Chemistry (2008), 51(24), 7921-7932. CODEN: JMCMAR ISSN:0022-2623. CAN 150:49894 AN 2008:1411316

13. Grupe, Andrew; Li, Yonghong. Genetic polymorphisms associated with an increased risk of neurodegenerative disease and their detection and diagnostic and prophylactic use. PCT Int. Appl. (2008), 137pp. CODEN: PIXXD2 WO 2008137110 A1 20081113 CAN 149:553338 AN 2008:1360637

14. Kamitsuji, Y.; Kuroda, J.; Kimura, S.; Toyokuni, S.; Watanabe, K.; Ashihara, E.; Tanaka, H.; Yui, Y.; Watanabe, M.; Matsubara, H.; Mizushima, Y.; Hiraumi, Y.; Kawata, E.; Yoshikawa, T.; Maekawa, T.; Nakahata, T.; Adachi, S. The Bcr-Abl kinase inhibitor INNO-406 induces autophagy and different modes of cell death execution in Bcr-Abl-positive leukemias. Cell Death and Differentiation (2008), 15(11), 1712-1722. CODEN: CDDIEK ISSN:1350-9047. CAN 150:344480 AN 2008:1228922

15. Tanaka, Ruriko; Kimura, Shinya. Abl tyrosine kinase inhibitors for overriding Bcr-Abl/T315I: from the second to third generation. Expert Review of Anticancer Therapy (2008), 8(9), 1387-1398. CODEN: ERATBJ ISSN:1473-7140. CAN 150:274692 AN 2008:1072042

16. Mauro, Michael J.; Heinrich, Michael C. Treatment of chronic myeloid leukemia with Bcr-Abl kinase inhibitors. Basic and Clinical Oncology (2008), 35(Innovative Leukemia and Lymphoma Therapy), 411-428. CODEN: BCLOEQ ISSN:1073-0028. CAN 151:48225 AN 2008:981408

17. Cortes, Jorge; Kantarjian, Hagop. Beyond dose escalation: clinical options for relapse or resistance in chronic myelogenous leukemia. Journal of the National Comprehensive Cancer Network (2008), 6(Suppl. 2), S22-S30. CODEN: JNCCA4 ISSN:1540-1405. CAN 149:369439 AN 2008:883874

18. Jabbour, Elias; Kantarjian, Hagop; Jones, Dan; Breeden, Megan; Garcia-Manero, Guillermo; O'Brien, Susan; Ravandi, Farhad; Borthakur, Gautam; Cortes, Jorge. Characteristics and outcomes of patients with chronic myeloid leukemia and T315I mutation following failure of imatinib mesylate therapy. Blood (2008), 112(1), 53-55. CODEN: BLOOAW ISSN:0006-4971. CAN 149:191322 AN 2008:838599

19. Morinaga, Koji; Yamauchi, Takahiro; Kimura, Shinya; Maekawa, Taira; Ueda, Takanori. Overcoming imatinib resistance using Src inhibitor CGP76030, Abl inhibitor nilotinib and Abl/Lyn inhibitor INNO-406 in newly established K562 variants with BCR-ABL gene amplification. International Journal of Cancer (2008), 122(11), 2621-2627. CODEN: IJCNAW ISSN:0020-7136. CAN 148:462717 AN 2008:532204

20. Deguchi, Yasuyuki; Kimura, Shinya; Ashihara, Eishi; Niwa, Tomoko; Hodohara, Keiko; Fujiyama, Yoshihide; Maekawa, Taira. Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines. Leukemia Research (2008), 32(6), 980-983. CODEN: LEREDD ISSN:0145-2126. CAN 149:416994 AN 2008:360658

21. Kimrua, Shinya. Novel ABL tyrosine kinase inhibitors. Farumashia (2008), 44(3), 213-217. CODEN: FARUAW ISSN:0014-8601. CAN 148:417132 AN 2008:347333

22. Jin, Linhua; Tabe, Yoko; Konoplev, Sergej; Xu, Yuanyuan; Leysath, Clinton E.; Lu, Hongbo; Kimura, Shinya; Ohsaka, Akimichi; Rios, Mary-Beth; Calvert, Leslie; Kantarjian, Hagop; Andreeff, Michael; Konopleva, Marina. CXCR4 up-regulation by imatinib induces chronic myelogenous leukemia (CML) cell migration to bone marrow stroma and promotes survival of quiescent CML cells. Molecular Cancer Therapeutics (2008), 7(1), 48-58. CODEN: MCTOCF ISSN:1535-7163. CAN 148:299217 AN 2008:64838

23. Jabbour, Elias; Cortes, Jorge E.; Ghanem, Hady; O'Brien, Susan; Kantarjian, Hagop M. Targeted therapy in chronic myeloid leukemia. Expert Review of Anticancer Therapy (2008), 8(1), 99-110. CODEN: ERATBJ ISSN:1473-7140. CAN 149:43803 AN 2007:1450929

24. Manley, Paul W.; Martiny-Baron, Georg; Mestan, Juergen. Pyrimidylaminobenzamide compound Ephrin receptor kinase inhibitors, and their therapeutic use. PCT Int. Appl. (2007), 23pp. CODEN: PIXXD2 WO 2007137981 A1 20071206 CAN 148:24408 AN 2007:1395968

25. Maekawa, Taira; Ashihara, Eishi; Kimura, Shinya. The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias. International Journal of Clinical Oncology (2007), 12(5), 327-340. CODEN: IJCOF6 ISSN:1341-9625. CAN 148:298631 AN 2007:1153309

26. Kamitsuji, Yuri; Kimura, Shinya. A novel dual BCR-ABL/LYN kinase inhibitor, INNO-406. Biotherapy (Tokyo, Japan) (2007), 21(4), 256-263. CODEN: BITPE9 ISSN:0914-2223. CAN 147:533854 AN 2007:1007486

27. Kuroda, J.; Kimura, S.; Strasser, A.; Andreeff, M.; O'Reilly, L. A.; Ashihara, E.; Kamitsuji, Y.; Yokota, A.; Kawata, E.; Takeuchi, M.; Tanaka, R.; Tabe, Y.; Taniwaki, M.; Maekawa, T. Apoptosis-based dual molecular targeting by INNO-406, a second-generation Bcr-Abl inhibitor, and ABT-737, an inhibitor of antiapoptotic Bcl-2 proteins, against Bcr-Abl-positive leukemia. Cell Death and Differentiation (2007), 14(9), 1667-1677. CODEN: CDDIEK ISSN:1350-9047. CAN 148:23856 AN 2007:918575

28. Pan, Jingxuan; Quintas-Cardama, Alfonso; Manshouri, Taghi; Cortes, Jorge; Kantarjian, Hagop; Verstovsek, Srdan. Sensitivity of human cells bearing oncogenic mutant kit isoforms to the novel tyrosine kinase inhibitor INNO-406. Cancer Science (2007), 98(8), 1223-1225. CODEN: CSACCM ISSN:1347-9032. CAN 147:157589 AN 2007:849671

29. Jabbour, Elias; Cortes, Jorge E.; Giles, Francis J.; O'Brien, Susan; Kantarjian, Hagop M. Current and emerging treatment options in chronic myeloid leukemia. Cancer (Hoboken, NJ, United States) (2007), 109(11), 2171-2181. CODEN: CANCAR ISSN:0008-543X. CAN 147:226039 AN 2007:686023

30. Horio, Tatsuya; Hamasaki, Tomohiro; Inoue, Toshihiko; Wakayama, Tatsushi; Itou, Shinsaku; Naito, Haruna; Asaki, Tetsuo; Hayase, Hiroki; Niwa, Tomoko. Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. Bioorganic & Medicinal Chemistry Letters (2007), 17(10), 2712-2717. CODEN: BMCLE8 ISSN:0960-894X. CAN 147:132881 AN 2007:477977

31. Jabbour, Elias; Cortes, Jorge; O'Brien, Susan; Giles, Francis; Kantarjian, Hagop. New targeted therapies for chronic myelogenous leukemia: opportunities to overcome imatinib resistance. Seminars in Hematology (2007), 44(1, Suppl. 1), S25-S31. CODEN: SEHEA3 ISSN:0037-1963. CAN 146:474578 AN 2007:387711

32. Yokota, Asumi; Kimura, Shinya; Masuda, Satohiro; Ashihara, Eishi; Kuroda, Junya; Sato, Kiyoshi; Kamitsuji, Yuri; Kawata, Eri; Deguchi, Yasuyuki; Urasaki, Yoshimasa; Terui, Yasuhito; Ruthardt, Martin; Ueda, Takanori; Hatake, Kiyohiko; Inui, Ken-ichi; Maekawa, Taira. INNO-406, a novel BCR-ABL/Lyn dual tyrosine kinase inhibitor, suppresses the growth of Ph+ leukemia cells in the central nervous system, and cyclosporine A augments its in vivo activity. Blood (2007), 109(1), 306-314. CODEN: BLOOAW ISSN:0006-4971. CAN 146:287913 AN 2007:288892

33. Kimura, Shinya. Second generation Abl kinase inhibitors and novel compounds to eliminate the Bcr-Abl/T315I clone. Recent Patents on Anti-Cancer Drug Discovery (2006), 1(3), 347-355. CODEN: RPADDY ISSN:1574-8928. CAN 146:242988 AN 2006:1292915

34. Kimura, Shinya; Ashihara, Eishi; Maekawa, Taira. Molecular targeting therapy for chronic myeloid leukemia: a novel dual Bcr-Abl/Lyn kinase inhibitor, INNO-406. Kyoto-furitsu Ika Daigaku Zasshi (2006), 115(10), 749-760. CODEN: KFIZAO ISSN:0023-6012. CAN 146:434360 AN 2006:1277336

35. Kimura, Shinya; Ashihara, Eishi; Maekawa, Taira. New tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia. Current Pharmaceutical Biotechnology (2006), 7(5), 371-379. CODEN: CPBUBP ISSN:1389-2010. CAN 146:19110 AN 2006:1025243

36. Kantarjian Hagop; Coutre Phillipp le; Cortes Jorge; Pinilla-Ibarz Javier; Nagler Arnon; Hochhaus Andreas; Kimura Shinya; Ottmann Oliver Phase 1 study of INNO-406, a dual Abl/Lyn kinase inhibitor, in Philadelphia chromosome-positive leukemias after imatinib resistance or intolerance. Cancer (2010), 116(11), 2665-72. Journal code: 0374236. ISSN:0008-543X. PubMed ID 20310049 AN 2010357422 In-process for

37. Niwa Tomoko; Asaki Tetsuo; Kimura Shinya NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor. Analytical chemistry insights (2007), 2 93-106. Journal code: 101463741. E-ISSN:1177-3901. PubMed ID 19662183 AN 2009541042

38. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(7), 543-88. Journal code: 7909595. ISSN:0379-0355. PubMed ID 18985183 AN 2008718978

39. Maekawa Taira Innovation of clinical trials for anti-cancer drugs in Japan--proposals from academia with special reference to the development of novel Bcr-Abl/Lyn tyrosine kinase inhibitor INNO-406 (NS-187) for imatinib-resistant chronic myelogenous leukemia. Gan to kagaku ryoho. Cancer & chemotherapy (2007), 34(2), 301-4. Journal code: 7810034. ISSN:0385-0684. PubMed ID 17301549 AN 2007102221