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Masitinib mesylate is the orally bioavailable mesylate salt of masatinib, a multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK). As a consequence, tumor cell proliferation may be inhibited in cancer cell types that overexpress these receptor tyrosine kinases (RTKs). Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) .

Current developer: AB Science ( an emerging French biotechnology company )

Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity. Phase II clinical trials demonstrate that Masitinib appears to be effective as a first-line treatment of advanced GIST with comparable results to imatinib in terms of safety and response. PFS and in particular OS data show promise that masitinib may provide sustainable benefits. There is sufficient compelling evidence to warrant a phase III clinical trial. see http://www.ncbi.nlm.nih.gov/pubmed/20211560.

1. Le Cesne, Axel; Blay, Jean-Yves; Nguyen, Bui Binh; Bouche, Olivier; Adenis, Antoine; Domont, Julien; Cioffi, Angela; Ray-Coquard, Isabelle; Lassau, Nathalie; Bonvalot, Sylvie; Moussy, Alain; Kinet, Jean-Pierre; Hermine, Olivier. Phase II study of oral masitinib mesilate in imatinib-naive patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). European Journal of Cancer (2010), 46(8), 1344-1351. CODEN: EJCAEL ISSN:0959-8049. AN 2010:548092

2. Humbert, Martine; Casteran, Nathalie; Letard, Sebastien; Hanssens, Katia; Iovanna, Juan; Finetti, Pascal; Bertucci, Francois; Bader, Thomas; Mansfield, Colin D.; Moussy, Alain; Hermine, Olivier; Dubreuil, Patrice. Masitinib combined with standard gemcitabine chemotherapy: in vitro and in vivo studies in human pancreatic tumour cell lines and ectopic mouse model. PLoS One (2010), 5(3), No pp. given. CODEN: POLNCL ISSN:1932-6203. AN 2010:319241

3. Nechushtan, Hovav. The complexity of the complicity of mast cells in cancer. International Journal of Biochemistry & Cell Biology (2010), 42(5), 551-554. CODEN: IJBBFU ISSN:1357-2725. AN 2010:295880

4. Dubreuil, Patrice; Letard, Sebastien; Ciufolini, Marco; Gros, Laurent; Humbert, Martine; Casteran, Nathalie; Borge, Laurence; Hajem, Berengere; Lermet, Anne; Sippl, Wolfgang; Voisset, Edwige; Arock, Michel; Auclair, Christian; Leventhal, Phillip S.; Mansfield, Colin D.; Moussy, Alain; Hermine, Olivier. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS One (2009), 4(9), No pp. given. CODEN: POLNCL ISSN:1932-6203. CAN 151:373367 AN 2009:1226662

5. Soria, J. C.; Massard, C.; Magne, N.; Bader, Th.; Mansfield, C. D.; Blay, J. Y.; Bui, B. N.; Moussy, A.; Hermine, O.; Armand, J. P. Phase 1 dose-escalation study of oral tyrosine kinase inhibitor masitinib in advanced and/or metastatic solid cancers. European Journal of Cancer (2009), 45(13), 2333-2341. CODEN: EJCAEL ISSN:0959-8049. CAN 152:372918 AN 2009:1033103

6. Humbert, M.; de Blay, F.; Garcia, G.; Prud'homme, A.; Leroyer, C.; Magnan, A.; Tunon-de-Lara, J.-M.; Pison, C.; Aubier, M.; Charpin, D.; Vachier, I.; Purohit, A.; Gineste, P.; Bader, T.; Moussy, A.; Hermine, O.; Chanez, P. Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor, improves disease control in severe corticosteroid-dependent asthmatics. Allergy (Oxford, United Kingdom) (2009), 64(8), 1194-1201. CODEN: LLRGDY ISSN:0105-4538. CAN 152:254801 AN 2009:1010633

7. Walker, Ulrich A. More about masitinib. Arthritis Research & Therapy (2009), 11(4), No pp. given. CODEN: ARTRCV ISSN:1478-6362. CAN 152:205771 AN 2009:880814

8. Tebib, Jacques; Mariette, Xavier; Bourgeois, Pierre; Flipo, Rene-Marc; Gaudin, Philippe; Le Loet, Xavier; Gineste, Paul; Guy, Laurent; Mansfield, Colin D.; Moussy, Alain; Dubreuil, Patrice; Hermine, Olivier; Sibilia, Jean. Masitinib in the treatment of active rheumatoid arthritis: results of a multicentre, open-label, dose-ranging, phase 2a study. Arthritis Research & Therapy (2009), 11(3), No pp. given. CODEN: ARTRCV ISSN:1478-6362. CAN 151:564682 AN 2009:785488

9. Rickles, Richard; Lee, Margaret S. Use of adenosine A2A receptor agonists and phosphodiesterase (PDE) inhibitors for the treatment of B-cell proliferative disorders, and combinations with other agents. PCT Int. Appl. (2009), 70 pp. CODEN: PIXXD2 WO 2009011893 A2 20090122 CAN 150:160095 AN 2009:86451

10. Rickles, Richard; Pierce, Laura; Lee, Margaret S. Combinations for the treatment of B-cell proliferative disorders. PCT Int. Appl. (2009), 79pp. CODEN: PIXXD2 WO 2009011897 A1 20090122 CAN 150:160094 AN 2009:83374

11. Mao, Haiting; Wang, Minghua. Antitumor sustained-release gel for injection containing anti-angiogenic agents and copolymer. Faming Zhuanli Shenqing Gongkai Shuomingshu (2009), 29pp. CODEN: CNXXEV CN 101336890 A 20090107 CAN 150:129029 AN 2009:37599

12. Chen, Ying; Hou, Hongtao. Antitumor sustained-release gel injection containing neovascularization inhibitor and its preparation. Faming Zhuanli Shenqing Gongkai Shuomingshu (2008), 23pp. CODEN: CNXXEV CN 101283974 A 20081015 CAN 149:541541 AN 2008:1259968

13. Moussy, Alain; Kinet, Jean-Pierre. Combination treatment of solid cancers with antimetabolites and tyrosine kinase inhibitors. PCT Int. Appl. (2008), 49pp. CODEN: PIXXD2 WO 2008084103 A1 20080717 CAN 149:143942 AN 2008:857374

14. Kong, Qingzhong; Liu, Yuyan. Masitinib controlled-release implant for treating solid neoplasm. Faming Zhuanli Shenqing Gongkai Shuomingshu (2008), 19pp. CODEN: CNXXEV CN 101181232 A 20080521 CAN 148:593016 AN 2008:626104

15. Mitry Emmanuel; Hammel Pascal; Deplanque Gael; Mornex Francoise; Levy Philippe; Seitz Jean-Francois; Moussy Alain; Kinet Jean-Pierre; Hermine Olivier; Rougier Philippe; Raymond Eric Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer. Cancer chemotherapy and pharmacology (2010), 66(2), 395-403. Journal code: 7806519. E-ISSN:1432-0843. PubMed ID 20364428 AN 2010340333

16. Le Cesne Axel; Blay Jean-Yves; Bui Binh Nguyen; Bouche Olivier; Adenis Antoine; Domont Julien; Cioffi Angela; Ray-Coquard Isabelle; Lassau Nathalie; Bonvalot Sylvie; Moussy Alain; Kinet Jean-Pierre; Hermine Olivier Phase II study of oral masitinib mesilate in imatinib-naive patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). European journal of cancer (Oxford, England : 1990) (2010), 46(8), 1344-51. Journal code: 9005373. E-ISSN:1879-0852. PubMed ID 20211560 AN 2010302319

17. Gentilini F "Masitinib" is safe and effective for the treatment of canine mast cell tumors. Journal of veterinary internal medicine / American College of Veterinary Internal Medicine (2010), 24(1), 6; author reply 7. Journal code: 8708660. ISSN:0891-6640. PubMed ID 20391634 AN 2010261754

18. Nechushtan Hovav The complexity of the complicity of mast cells in cancer. The international journal of biochemistry & cell biology (2010), 42(5), 551-4. Journal code: 9508482. E-ISSN:1878-5875. PubMed ID 20026421 AN 2010186531

19. Humbert Martine; Casteran Nathalie; Letard Sebastien; Hanssens Katia; Iovanna Juan; Finetti Pascal; Bertucci Francois; Bader Thomas; Mansfield Colin D; Moussy Alain; Hermine Olivier; Dubreuil Patrice Masitinib combined with standard gemcitabine chemotherapy: in vitro and in vivo studies in human pancreatic tumour cell lines and ectopic mouse model. PloS one (2010), 5(3), e9430. Journal code: 101285081. E-ISSN:1932-6203. PubMed ID 20209107 AN 2010163477

20. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2009), 31(10), 661-700. Journal code: 7909595. ISSN:0379-0355. PubMed ID 20140276 AN 2010102238

21. Daigle Jenise; Moussy Alain; Mansfield Colin D; Hermine Olivier Masitinib for the treatment of canine atopic dermatitis: a pilot study. Veterinary research communications (2010), 34(1), 51-63. Journal code: 8100520. E-ISSN:1573-7446. PubMed ID 20033487 AN 2010042357

22. Dubreuil Patrice; Letard Sebastien; Ciufolini Marco; Gros Laurent; Humbert Martine; Casteran Nathalie; Borge Laurence; Hajem Berengere; Lermet Anne; Sippl Wolfgang; Voisset Edwige; Arock Michel; Auclair Christian; Leventhal Phillip S; Mansfield Colin D; Moussy Alain; Hermine Olivier Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PloS one (2009), 4(9), e7258. Journal code: 101285081. E-ISSN:1932-6203. PubMed ID 19789626 AN 2009656698

23. Walker Ulrich A More about masitinib. Arthritis research & therapy (2009), 11(4), 120. Journal code: 101154438. E-ISSN:1478-6362. PubMed ID 19664170 AN 2009630595

24. London Cheryl A Tyrosine kinase inhibitors in veterinary medicine. Topics in companion animal medicine (2009), 24(3), 106-12. Journal code: 101465592. ISSN:1938-9736. PubMed ID 19732728 AN 2009607716

25. Soria J C; Massard C; Magne N; Bader Th; Mansfield C D; Blay J Y; Bui B N; Moussy A; Hermine O; Armand J P Phase 1 dose-escalation study of oral tyrosine kinase inhibitor masitinib in advanced and/or metastatic solid cancers. European journal of cancer (Oxford, England : 1990) (2009), 45(13), 2333-41. Journal code: 9005373. E-ISSN:1879-0852. PubMed ID 19541476 AN 2009570599

26. Tebib Jacques; Mariette Xavier; Bourgeois Pierre; Flipo Rene-Marc; Gaudin Philippe; Le Loet Xavier; Gineste Paul; Guy Laurent; Mansfield Colin D; Moussy Alain; Dubreuil Patrice; Hermine Olivier; Sibilia Jean Masitinib in the treatment of active rheumatoid arthritis: results of a multicentre, open-label, dose-ranging, phase 2a study. Arthritis research & therapy (2009), 11(3), R95. Journal code: 101154438. E-ISSN:1478-6362. PubMed ID 19549290 AN 2009498621

27. Humbert M; de Blay F; Garcia G; Prud'homme A; Leroyer C; Magnan A; Tunon-de-Lara J-M; Pison C; Aubier M; Charpin D; Vachier I; Purohit A; Gineste P; Bader T; Moussy A; Hermine O; Chanez P Masitinib, a c-kit/PDGF receptor tyrosine kinase inhibitor, improves disease control in severe corticosteroid-dependent asthmatics. Allergy (2009), 64(8), 1194-201. Journal code: 7804028. E-ISSN:1398-9995. PubMed ID 19614621 AN 2009493857

28. Hahn K A; Ogilvie G; Oglivie G; Rusk T; Devauchelle P; Leblanc A; Legendre A; Powers B; Leventhal P S; Kinet J-P; Palmerini F; Dubreuil P; Moussy A; Hermine O Masitinib is safe and effective for the treatment of canine mast cell tumors. Journal of veterinary internal medicine / American College of Veterinary Internal Medicine (2008), 22(6), 1301-9. Journal code: 8708660. ISSN:0891-6640. PubMed ID 18823406 AN 2008729648

29. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(3), 231-51. Journal code: 7909595. ISSN:0379-0355. PubMed ID 18597009 AN 2008428084

30. Italiano Antoine; Bui Binh Gastrointestinal stromal tumors: molecular aspects and therapeutic implications. Bulletin du cancer (2008), 95(1), 107-16. Journal code: 0072416. E-ISSN:1769-6917. PubMed ID 18230576 AN 2008073940