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Pharmacokinetics of ocriplasmin in vitreous.
MedLine Citation:
PMID:  23150619     Owner:  NLM     Status:  Publisher    
PURPOSE: Ocriplasmin contains the active moiety of plasmin enzyme. At a physiologic pH, ocriplasmin is highly proteolytic and autolytic, limiting its duration of activity. Specific inhibitors of plasmin are present in the vitreous under normal and disease conditions and could affect its activity. Each may contribute to its mode of action. METHOD: Degradation characteristics were determined in porcine, human vitreous, and PBS under reducing condition with different incubation periods between 0 and 24 hours on SDS Page tris-glycine gels. Residual activity was determined by spectrophotometry of p-nitroaniline release through hydrolysis of L-Pyroglutamyl-L-phenylalanyl-L-lysine-p-nitroaniline hydrochlorid. The presence of endogenous inactivators of ocriplasmin in human vitreous was determined in a series of vitreous samples using an ELISA specific for alpha(2)-antiplasmin, antithrombin and antitrypsin. RESULTS: Degradation productions from autolysis are similar between vitreous and PBS with a significant prolongation of the effect in vitreous. Both follow a non linear pattern over time. The degradation corresponds best to a second order kinetic process. The resulting rate constants were 207±60M -1 s -1 in PBS, 81±15M -1 s -1 in porcine vitreous, and 195 M -1s -1 in human vitreous Natural inhibitors were identified in samples of donor vitreous. Amounts differed significantly between samples, which may help explain variability in human subjects. CONCLUSION: Ocriplasmin is autolytic in vitreous. Biologic activity extends to several days following injection. The exact duration will vary based on the presence and concentration of serine protease inhibitors.
Marc D de Smet; Bart Jonckx; Marc Vanhove; Joachim van Calster; Peter Stalmans; Jean Marie Stassen
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-13
Journal Detail:
Title:  Investigative ophthalmology & visual science     Volume:  -     ISSN:  1552-5783     ISO Abbreviation:  Invest. Ophthalmol. Vis. Sci.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7703701     Medline TA:  Invest Ophthalmol Vis Sci     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Retina and Inflammation Center, MIOS, Chemin des Allinges 10, Lausanne, 1001, Switzerland.
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