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Saracatinib
Saracatinib (AZD-0530) is an experimental drug being developed by AstraZeneca. It acts as a dual kinase inhibitor, with selective actions as a Src inhibitor and a Bcr-Abl tyrosine-kinase inhibitor.〔Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A, Otterbein L, Plé PA, Warin N, Costello G. N-(5-chloro-1,3-benzodioxol-4-yl)-7-()-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. ''J Med Chem''. 2006 Nov 2;49(22):6465-88. PMID 17064066〕〔Schenone S, Brullo C, Musumeci F, Botta M. Novel dual Src/Abl inhibitors for hematologic and solid malignancies. ''Expert Opin Investig Drugs''. 2010 Aug;19(8):931-45. doi: 10.1517/13543784.2010.499898 PMID 20557276〕 It was originally under development for the treatment of cancer, but while it appeared promising in animal studies and was well tolerated in humans, it failed to show sufficient efficacy in cancer patients and was ultimately not developed further for this application.〔Gubens MA, Burns M, Perkins SM, Pedro-Salcedo MS, Althouse SK, Loehrer PJ, Wakelee HA. A phase II study of saracatinib (AZD0530), a Src inhibitor, administered orally daily to patients with advanced thymic malignancies. ''Lung Cancer''. 2015 Jul;89(1):57-60. doi: 10.1016/j.lungcan.2015.04.008 PMID 26009269〕〔Reddy SM, Kopetz S, Morris J, Parikh N, Qiao W, Overman MJ, Fogelman D, Shureiqi I, Jacobs C, Malik Z, Jimenez CA, Wolff RA, Abbruzzese JL, Gallick G, Eng C. Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer. ''Invest New Drugs''. 2015 Aug;33(4):977-84. doi: 10.1007/s10637-015-0257-z PMID 26062928〕 However saracatinib has subsequently been researched for other applications such as Alzheimer's disease〔Kaufman AC, Salazar SV, Haas LT, Yang J, Kostylev MA, Jeng AT, Robinson SA, Gunther EC, van Dyck CH, Nygaard HB, Strittmatter SM. Fyn inhibition rescues established memory and synapse loss in Alzheimer mice. ''Ann Neurol''. 2015 Jun;77(6):953-71. doi: 10.1002/ana.24394 PMID 25707991〕〔Nygaard HB, Wagner AF, Bowen GS, Good SP, MacAvoy MG, Strittmatter KA, Kaufman AC, Rosenberg BJ, Sekine-Konno T, Varma P, Chen K, Koleske AJ, Reiman EM, Strittmatter SM, van Dyck CH. A phase Ib multiple ascending dose study of the safety, tolerability, and central nervous system availability of AZD0530 (saracatinib) in Alzheimer's disease. ''Alzheimers Res Ther''. 2015 Apr 14;7(1):35. doi: 10.1186/s13195-015-0119-0. PMID 25874001〕 and schizophrenia.〔(MICA: SRC inhibitors as potential antipsychotics: human testing with psilocybin. Imperial College London. 27 July 2015 )〕
==See also==
* Bosutinib
* Dasatinib
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