Saracatinib

Saracatinib

Clinical data
Routes of administration	Oral
Legal status
Legal status	Investigational
Identifiers
IUPAC name N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
CAS Number	379231-04-6
PubChem CID	10302451
ChemSpider	8477917
KEGG	D09664
Chemical and physical data
Formula	C27H32ClN5O5
Molar mass	542.025 g/mol
3D model (Jmol)	Interactive image
SMILES C4CN(C)CCN4CCOc(cc2ncn3)cc(OC6CCOCC6)c2c3Nc1c(Cl)ccc5OCOc15
InChI InChI=1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31) Key:OUKYUETWWIPKQR-UHFFFAOYSA-N

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. 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. However saracatinib has subsequently been researched for other applications such as Alzheimer's disease. AZD0530 is an inhibitor of Src and Abl family kinases1. It has been developed as treatment for malignancies because these kinases play a role in tumor invasion and proliferation. However, the Src family kinases (SFKs) are highly expressed in brain and have major effects on synaptic plasticity2. Moreover, the investigators have recently shown that a specific SFK, namely Fyn, is aberrantly activated by specific conformations of the Amyloid Beta (Aß) peptide from Alzheimer's disease (AD). Genetic deletion of Fyn rescues AD deficits in preclinical models. This clinical trial will test the potential benefit of AZD0530 for Alzheimer's disease modification. and schizophrenia.