Pharmacokinetics of Intravitreal Bevacizumab (Avastin)

Sophie J. Bakri, Melissa R. Snyder, Joel M Reid, Jose S Pulido, Ravinder Jit Singh

Research output: Contribution to journalArticle

488 Citations (Scopus)

Abstract

Purpose: To describe the pharmacokinetics of 1.25 mg of intravitreal bevacizumab (Avastin). Design: Experimental animal study. Participants: Twenty Dutch-belted rabbits. Methods: One eye of each of 20 rabbits was injected with 1.25 mg of intravitreal bevacizumab. Both eyes of each of 4 rabbits were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in aqueous fluid, whole vitreous, and serum. Main Outcome Measures: Bevacizumab concentrations in the aqueous, vitreous, and serum. Results: Whereas vitreous concentrations of bevacizumab declined in a monoexponential fashion with a half-life of 4.32 days, concentrations of >10μg/ml bevacizumab were maintained in the vitreous humor for 30 days. Bevacizumab concentrations in the aqueous humor of the injected eye reached a peak concentration of 37.7 μg/ml 3 days after drug administration. A maximum serum concentration of 3.3 μg/ml was achieved 8 days after intravitreal injection and the concentration fell below 1 μg/ml 29 days after injection. Elimination of bevacizumab from the aqueous humor and serum paralleled that found in the vitreous humor, with half-life values of 4.88 days and 6.86 days, respectively. Very low concentrations of bevacizumab were detected in the fellow uninjected eye. Concentrations of bevacizumab in the vitreous of the fellow eye varied incrementally, from 0.35 ng/ml at 1 day to 11.17 ng/ml at 4 weeks. Concentrations of bevacizumab in the aqueous humor of the fellow eye reached their peak at 1 week, at 29.4 ng/ml, and declined to 4.56 ng/ml at 4 weeks. Conclusion: The vitreous half-life of 1.25 mg intravitreal bevacizumab is 4.32 days in a rabbit eye. Very small amounts of bevacizumab were detected in the serum and in the fellow uninjected eye.

Original languageEnglish (US)
Pages (from-to)855-859
Number of pages5
JournalOphthalmology
Volume114
Issue number5
DOIs
StatePublished - May 2007

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Pharmacokinetics
Aqueous Humor
Rabbits
Half-Life
Vitreous Body
Serum
Bevacizumab
Intravitreal Injections
Research Design
Outcome Assessment (Health Care)
Injections

ASJC Scopus subject areas

  • Ophthalmology

Cite this

Pharmacokinetics of Intravitreal Bevacizumab (Avastin). / Bakri, Sophie J.; Snyder, Melissa R.; Reid, Joel M; Pulido, Jose S; Singh, Ravinder Jit.

In: Ophthalmology, Vol. 114, No. 5, 05.2007, p. 855-859.

Research output: Contribution to journalArticle

Bakri, Sophie J. ; Snyder, Melissa R. ; Reid, Joel M ; Pulido, Jose S ; Singh, Ravinder Jit. / Pharmacokinetics of Intravitreal Bevacizumab (Avastin). In: Ophthalmology. 2007 ; Vol. 114, No. 5. pp. 855-859.
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abstract = "Purpose: To describe the pharmacokinetics of 1.25 mg of intravitreal bevacizumab (Avastin). Design: Experimental animal study. Participants: Twenty Dutch-belted rabbits. Methods: One eye of each of 20 rabbits was injected with 1.25 mg of intravitreal bevacizumab. Both eyes of each of 4 rabbits were enucleated at days 1, 3, 8, 15, and 29. Bevacizumab concentrations were measured in aqueous fluid, whole vitreous, and serum. Main Outcome Measures: Bevacizumab concentrations in the aqueous, vitreous, and serum. Results: Whereas vitreous concentrations of bevacizumab declined in a monoexponential fashion with a half-life of 4.32 days, concentrations of >10μg/ml bevacizumab were maintained in the vitreous humor for 30 days. Bevacizumab concentrations in the aqueous humor of the injected eye reached a peak concentration of 37.7 μg/ml 3 days after drug administration. A maximum serum concentration of 3.3 μg/ml was achieved 8 days after intravitreal injection and the concentration fell below 1 μg/ml 29 days after injection. Elimination of bevacizumab from the aqueous humor and serum paralleled that found in the vitreous humor, with half-life values of 4.88 days and 6.86 days, respectively. Very low concentrations of bevacizumab were detected in the fellow uninjected eye. Concentrations of bevacizumab in the vitreous of the fellow eye varied incrementally, from 0.35 ng/ml at 1 day to 11.17 ng/ml at 4 weeks. Concentrations of bevacizumab in the aqueous humor of the fellow eye reached their peak at 1 week, at 29.4 ng/ml, and declined to 4.56 ng/ml at 4 weeks. Conclusion: The vitreous half-life of 1.25 mg intravitreal bevacizumab is 4.32 days in a rabbit eye. Very small amounts of bevacizumab were detected in the serum and in the fellow uninjected eye.",
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