Ticagrelor The 1st reversible P2Y12 ADP receptor antagonist Better than Clopidogrel ADP Ticagrelor BRILINTA Brilique & Possia US (2011/06/20) in the EU (2010/12/03) N Engl J Med 2009; 361:1045-1057September 10, 2009DOI: 10.1056/NEJMoa0904327 26 Core Evid. 2011; 6: 31–42. Published online 2011 March 17. doi: 10.2147/CE.S9510
Edaravone • Free Radical Scavengers •1st free radical scavenger for stroke •Exerts antioxidant effects •Inhibiting radical- dependent and -independent lipid peroxidation •Marketed solely in JapanFor the treatment of acute brain ischemia and subsequentcerebral infarction. Recent Pat Cardiovasc Drug Discov. 2006 Jan;1(1):85-93. BMC Neuroscience 2008, 9:75 doi:10.1186/1471-2202-9-75 BIOMEDICAL REPORTS 1: 7-12, 2013 DOI: 10.3892/br.2012.7 34METABOLIC BRAIN DISEASE Volume 23, Number 3 (2008), 335-349, DOI: 10.1007/s11011-008-9096-3
NXY-059 (CeroviveR) • Free Radical Scavengers •Nitroxide spin trap • Stable free radicals that react with O2-. •Marginally positive clinical trial (SAINT I) http://www.nitrone.com/ http://www.centpharm.com/ Stroke. 2006 Dec;37(12):2970-8. Epub 2006 Oct 26. N Engl J Med 2006; 354:588-600February 9, 2006DOI: 10.1056/NEJMoa052980 35 N Engl J Med 2007; 357:562-571August 9, 2007DOI: 10.1056/NEJMoa070240
Why did NXY-059 fail???• Physiochemical shortcomings polar, nonlipophilic nature, poor blood–brain barrierpenetrability, nonphysiological oxidation potential, and lowpotency (Ginsburg, Stroke 2007)• Lack of biomarker assessing oxidative stress• Heterogeneity in individual responses to drug treatment• Stroke is a formidable disorder only one approved therapy to date Ann Pharmacother March 200640:461-471 36 The Journal of Experimental Biology 207, 3221-3231
Minocycline • Antibiotics acne vulgaris Exert inhibition of microglial activity, glutamate toxicity and caspase 1-dependent apoptosis produced by ischemic insults. Lampl Y, Boaz M, Gilad R et al. (2007): Neurology 69 (14): 1404–10 37
SurgeryA. carotid angioplasty B. Carotid stenting C. craniotomyremove stenosis large metal coil (stent) a type of surgery to(atherosclerotic is placed in the carotid remove blood clots ornarrowing) of the artery much like a stent repair bleeding in thecarotid artery. is placed in a coronary brain. 39 artery.
Advancement of anti-platelet therapymay be achieved either by doseadjustment of the drug based onfunctional testing by changing drugcombination or by the introduction ofmore potent and safer drugs. 43