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Pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Sinapis CI, Routsias JG, Sinapis AI, Sinapis DI, Agrogiannis GD, Pantopoulou A, Theocharis SE, Baltatzis S, Patsouris E, Perrea D - Clin Ophthalmol (2011)

Bottom Line: In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model.Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

View Article: PubMed Central - PubMed

Affiliation: Laboratory for Experimental Surgery and Surgical Research 'N.S.Christeas', School of Medicine, National and Kapodistrian University of Athens, 15b AgiouThoma Street, 11527, Athens, Greece. csinapis@yahoo.gr

ABSTRACT

Purpose: To describe the pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Methods: The right eye of 20 rabbits was injected intravitreally with 1.25 mg/0.05 mL bevacizumab. Both eyes of four rabbits each time were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in serum, aqueous humor, and vitreous.

Results: Maximum vitreous (406.25 μg/mL) and aqueous humor (5.83 μg/mL) concentrations of bevacizumab in the right eye were measured at day 1. Serum bevacizumab concentration peaked at day 8 (0.413 μg/mL) and declined to 0.032 μg/mL at 4 weeks. Half-life values in right vitreous, right aqueous humor, and serum were 6.61, 6.51, and 5.87 days, respectively. Concentration of bevacizumab in the vitreous of the noninjected eye peaked at day 8 (0.335 ng/mL) and declined to 0.218 ng/mL at 4 weeks. In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.

Conclusion: The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model. Maximum concentrations of bevacizumab were reached at day 1 in both vitreous and aqueous humor of the right eye and at day 8 in the serum. Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

No MeSH data available.


Quantification of anti-bevacizumab antibodies in serum of rabbits at day 0 (before intravitreal injection of bevacizumab) and at days 1, 3, 8, 15, and 29 after injection.Abbreviation: OD, optical density.
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f4-opth-5-697: Quantification of anti-bevacizumab antibodies in serum of rabbits at day 0 (before intravitreal injection of bevacizumab) and at days 1, 3, 8, 15, and 29 after injection.Abbreviation: OD, optical density.

Mentions: The results of high sensitivity ELISA assay for the detection of anti-bevacizumab antibodies are illustrated in Figure 4. There was a 30% increase of anti-bevacizumab antibodies at day 1, 60% at day 3, and 70% at day 8. Subsequently, the anti-bevacizumab activity of antibodies gradually decreased (to 120% of the initial levels at day 29), following the elimination of bevacizumab from blood circulation. Taking into account the absolute optical density values of the measurements of the high sensitivity ELISA, compared with the high sensitivity assay for bevacizumab, we can conclude that the concentration of anti-bevacizumab antibodies in serum is at least 200-fold lower than the bevacizumab concentration. Therefore, anti-bevacizumab antibodies cannot have an important effect on bevacizumab concentration because of their low concentration.


Pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Sinapis CI, Routsias JG, Sinapis AI, Sinapis DI, Agrogiannis GD, Pantopoulou A, Theocharis SE, Baltatzis S, Patsouris E, Perrea D - Clin Ophthalmol (2011)

Quantification of anti-bevacizumab antibodies in serum of rabbits at day 0 (before intravitreal injection of bevacizumab) and at days 1, 3, 8, 15, and 29 after injection.Abbreviation: OD, optical density.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3104800&req=5

f4-opth-5-697: Quantification of anti-bevacizumab antibodies in serum of rabbits at day 0 (before intravitreal injection of bevacizumab) and at days 1, 3, 8, 15, and 29 after injection.Abbreviation: OD, optical density.
Mentions: The results of high sensitivity ELISA assay for the detection of anti-bevacizumab antibodies are illustrated in Figure 4. There was a 30% increase of anti-bevacizumab antibodies at day 1, 60% at day 3, and 70% at day 8. Subsequently, the anti-bevacizumab activity of antibodies gradually decreased (to 120% of the initial levels at day 29), following the elimination of bevacizumab from blood circulation. Taking into account the absolute optical density values of the measurements of the high sensitivity ELISA, compared with the high sensitivity assay for bevacizumab, we can conclude that the concentration of anti-bevacizumab antibodies in serum is at least 200-fold lower than the bevacizumab concentration. Therefore, anti-bevacizumab antibodies cannot have an important effect on bevacizumab concentration because of their low concentration.

Bottom Line: In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model.Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

View Article: PubMed Central - PubMed

Affiliation: Laboratory for Experimental Surgery and Surgical Research 'N.S.Christeas', School of Medicine, National and Kapodistrian University of Athens, 15b AgiouThoma Street, 11527, Athens, Greece. csinapis@yahoo.gr

ABSTRACT

Purpose: To describe the pharmacokinetics of intravitreal bevacizumab (Avastin®) in rabbits.

Methods: The right eye of 20 rabbits was injected intravitreally with 1.25 mg/0.05 mL bevacizumab. Both eyes of four rabbits each time were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in serum, aqueous humor, and vitreous.

Results: Maximum vitreous (406.25 μg/mL) and aqueous humor (5.83 μg/mL) concentrations of bevacizumab in the right eye were measured at day 1. Serum bevacizumab concentration peaked at day 8 (0.413 μg/mL) and declined to 0.032 μg/mL at 4 weeks. Half-life values in right vitreous, right aqueous humor, and serum were 6.61, 6.51, and 5.87 days, respectively. Concentration of bevacizumab in the vitreous of the noninjected eye peaked at day 8 (0.335 ng/mL) and declined to 0.218 ng/mL at 4 weeks. In the aqueous humor of the noninjected eye, maximum concentration of bevacizumab was achieved at day 8 (1.6125 ng/mL) and declined (to 0.11 ng/mL) at 4 weeks.

Conclusion: The vitreous half-life of 1.25 mg/0.05 mL intravitreal bevacizumab was 6.61 days in this rabbit model. Maximum concentrations of bevacizumab were reached at day 1 in both vitreous and aqueous humor of the right eye and at day 8 in the serum. Very low concentrations of bevacizumab were measured in the fellow noninjected eye.

No MeSH data available.