Vorapaxar and amyotrophic lateral sclerosis: Coincidence or adverse association?

American Journal of Therapeutics

Volumn 24, Issue 2, 2017, Pages e139-e143

  Serebruany, Victor L ^a,b   Fortmann, Seth D ^a   Hanley, Daniel F ^b   Kim, Moo Hyun ^c  

^a Heart Drug Research LLC   (United States)

^b JOHNS HOPKINS UNIVERSITY   (United States)

^c Dong A University   (South Korea)

Author keywords

Adverse events; Amyotrophic lateral sclerosis; Clinical trials; Glutamate; PAR receptors; Safety; Thrombin; Vorapaxar

Indexed keywords

GLUTAMIC ACID; PLACEBO; PROTEINASE ACTIVATED RECEPTOR; THROMBIN; VORAPAXAR; ANTITHROMBOCYTIC AGENT; LACTONE; PROTEINASE ACTIVATED RECEPTOR 1; PYRIDINE DERIVATIVE;

AMYOTROPHIC LATERAL SCLEROSIS; ARTICLE; FOOD AND DRUG ADMINISTRATION; HUMAN; INCIDENCE; LABORATORY; NONHUMAN; PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; ANTAGONISTS AND INHIBITORS; METABOLISM; RISK FACTOR; UNITED STATES;

AMYOTROPHIC LATERAL SCLEROSIS; GLUTAMIC ACID; HUMANS; INCIDENCE; LACTONES; PLATELET AGGREGATION INHIBITORS; PYRIDINES; RECEPTOR, PAR-1; RISK FACTORS; THROMBIN; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 85015351180     PISSN: 10752765     EISSN: 15363686     Source Type: Journal    
DOI: 10.1097/MJT.0000000000000395     Document Type: Article

References (41)

1. Hashemzadeh M, Arreguin JM, Roberts T, et al. A novel inhibitor of protease-activated receptor 1: a review of chemical structure and mode of action. Rev Cardiovasc Med. 2015;16:68-73
2. Tricoci P, Huang Z, Held C, et al. Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med. 2012;366:20-33
3. Morrow DA, Braunwald E, Bonaca MP, et al. Vorapaxar in the secondary prevention of atherothrombotic events. N Engl J Med. 2012;366:1404-1413
4. NDA 294-886. Cross-Discipline Team Leader Review on Vorapaxar. 2014. Available at: http://www.accessdata.fda. gov/drugsatfda-docs/nda/2014/ 204886Orig1s000SumR.pdf. Assessed May 15, 2015
5. NDA 294-886. Medical Reviews on Vorapaxar. 2014. Available at: www.accessdata.fda.gov/drugsatfda-docs/nda/ 2014/204886Orig1s000MedR.pdf. Assessed May 15, 2015
6. Kosoglou T, Reyderman L, Tiessen RG, et al. Pharmacodynamics and pharmacokinetics of the novel PAR-1 antagonist vorapaxar (formerly SCH 530348) in healthy subjects. Eur J Clin Pharmacol. 2012;68:249-258
7. Valadi N. Evaluation and management of amyotrophic lateral sclerosis. Prim Care. 2015;42:177-187
8. Andersen JK. Oxidative stress in neurodegeneration: cause or consequence Nat Rev Neurosci. 2004;10:S18-S25
9. Ingre C, Roos PM, Piehl F, et al. Risk factors for amyotrophic lateral sclerosis. Clin Epidemiol. 2015;7:181-193
10. Malek AM, Stickler DE, Antao VC, et al. The National ALS Registry: a recruitment tool for research. Muscle Nerve. 2014;50:830-834
11. Bieniek KF, van Blitterswijk M, Baker MC, et al. Expanded C9ORF72 hexanucleotide repeat in depressive pseudodementia. JAMA Neurol. 2014;71:775-781
12. Sea K, Sohn SH, Durazo A, et al. Insights into the role of the unusual disulfide bond in copper-zinc superoxide dismutase. J Biol Chem. 2015;290:2405-2418
13. Smirnova IV, Citron BA, Arnold PM, Festoff BW. Neuroprotective signal transduction in model motor neurons exposed to thrombin: G-protein modulation effects on neurite outgrowth, Ca(2+) mobilization, and apoptosis. J Neurobiol. 2001;48:87-100
14. Smirnova IV, Zhang SX, Citron BA, et al. Thrombin is a death signal that activates intracellular death protease pathways in motor neurons. J Neurobiol. 1998;36:64-80
15. Turgeon VL, Lloyd ED, Wang SW, et al. Thrombin perturbs neurite outgrowth and induces apoptotic cell death in chick spinal motoneuron cultures through caspase activation. J Neurosci. 1998;18:6882-6891
16. Donovan FM, Pike CJ, Cotman CW, et al. Thrombin induces apoptosis in cultured neurons and astrocytes via a pathway requiring tyrosine kinase and RhoA activities. J Neurosci. 1997;17:5316-5326
17. Festoff BW, D'Andrea MR, Citron BA, et al. Motor neuron cell death in wobbler mutant mice follows overexpression of the G-protein-coupled, protease-activated receptor for thrombin. Mol Med. 2000;6:410-429
18. Festoff BW, Nelson PG, Brenneman DE. Prevention of activity-dependent neuronal death: vasoactive intestinal polypeptide stimulates astrocytes to secrete the thrombin-inhibiting neurotrophic serpin, protease nexin I. J Neurobiol. 1996;30:255-266
19. Vance KM, Rogers RC, Hermann GE. PAR1-activated astrocytes in the nucleus of the solitary tract stimulate adjacent neurons via NMDA receptors. J Neurosci. 2015;35:776-785
20. Mueller K, Michel K, Krueger D, et al. Activity of protease-activated receptors in the human submucous plexus. Gastroenterology. 2011;141:2088-2097
21. Han KS, Mannaioni G, Hamill CE, et al. Activation of protease activated receptor 1 increases the excitability of the dentate granule neurons of hippocampus. Mol Brain. 2011;4:32
22. Fujita T, Liu T, Nakatsuka T, et al. Proteinase-activated receptor-1 activation presynaptically enhances spontaneous glutamatergic excitatory transmission in adult rat substantia gelatinosa neurons. J Neurophysiol. 2009;102: 312-319
23. Saba L, Viscomi MT, Caioli S, et al. Transporter expression of cortical motor neurons from a presymptomatic mouse model of amyotrophic lateral sclerosis. Cereb Cortex. 2016;26:1512-1528
24. Chou SM, Taniguchi A, Wang HS, et al. Serpin5serine protease-like complexes within neurofilament conglomerates of motoneurons in amyotrophic lateral sclerosis. J Neurol Sci. 1998;160(Suppl 1):S73-S79
25. Rao JS, Hantaï D, Festoff BW. Thrombospondin, a platelet alpha-granule and matrix glycoprotein, is increased in muscle basement membrane of patients with amyotrophic lateral sclerosis. J Neurol Sci. 1992;113:99-107
26. Sokolova E, Reiser G. Prothrombin/thrombin and the thrombin receptors PAR-1 and PAR-4 in the brain: localization, expression and participation in neurodegenerative diseases. Thromb Haemost. 2008;100:576-581
27. Saito T, Bunnett NW. Protease-activated receptors: regulation of neuronal function. Neuromolecular Med. 2005;7:79-99
28. Vandell AG, Larson N, Laxmikanthan G, et al. Proteaseactivated receptor dependent and independent signaling by kallikreins 1 and 6 in CNS neuron and astroglial cell lines. J Neurochem. 2008;107:855-870
29. Wang H, Wu X, Li JY, et al. Functional proteaseactivated receptors in the dorsal motor nucleus of the vagus. Neurogastroenterol Motil. 2010;22:431-438
30. Bunnett NW. Protease-activated receptors: how proteases signal to cells to cause inflammation and pain. Semin Thromb Hemost. 2006;32(Suppl 1):39-48
31. Almonte AG, Hamill CE, Chhatwal JP, et al. Learning and memory deficits in mice lacking protease activated receptor-1. Neurobiol Learn Mem. 2007;88:295-304
32. Hollenberg MD, Mihara K, Polley D, et al. Biased signalling and proteinase-activated receptors (PARs): targeting inflammatory disease. Br J Pharmacol. 2014;171: 1180-1194
33. García PS, Gulati A, Levy JH. The role of thrombin and protease-activated receptors in pain mechanisms. Thromb Haemost. 2010;103:1145-1151
34. Ebert CS Jr, McKinney KA, Urrutia G, et al. Expression of protease-activated receptors in allergic fungal rhinosinusitis. Int Forum Allergy Rhinol. 2014;4:266-271
35. Rajput PS, Lyden PD, Chen B, et al. Protease activated receptor-1 mediates cytotoxicity during ischemia using in vivo and in vitro models. Neuroscience. 2014;281C: 229-240
36. Chen D, Abrahams JM, Smith LM, et al. Regenerative repair after endoluminal injury in mice with specific antagonism of protease activated receptors on CD34+ vascular progenitors. Blood. 2008;111:4155-4164
37. Flynn AN, Buret AG. Proteinase-activated receptor 1 (PAR-1) and cell apoptosis. Apoptosis. 2004;9:729-737
38. Qinan W, Ling Z, Bing C. PAR-4: a possible new target for age-related disease. Expert Opin Ther Targets. 2014;18: 917-927
39. Cannon JR, Keep RF, Schallert T, et al. Protease-activated receptor-1 mediates protection elicited by thrombin preconditioning in a rat 6-hydroxydopamine model of Parkinson's disease. Brain Res. 2006;1116:177-186
40. Afkhami-Goli A, Noorbakhsh F, Keller AJ, et al. Proteinase-activated receptor-2 exerts protective and pathogenic cell type-specific effects in Alzheimer's disease. J Immunol. 2007;179:5493-5503
41. Serebruany VL. Redesigning TRACER after TRITON. Intern J Cardiol. 2015;197:44-47.