What are the half-lives of ranibizumab and aflibercept (VEGF Trap-eye) in human eyes? Calculations with a mathematical model
DOI:
https://doi.org/10.16964/er.v1i1.42Keywords:
age-related macular degeneration, ranibizumab, bevacizumab, VEGF Trap, aflibercept, half-lives, pharmacokinetics.Abstract
The aim of the article is to estimate the intravitreal half-lives of ranibizumab and aflibercept (VEGF Trap-eye; VTE) in human eyes. Using a published mathematical model for rabbits, the intravitreal half-lives of ranibizumab and bevacizumab were calculated and compared to empirical data. The slope coefficient within the model was changed to set the bevacizumab output equal to experimental values to meet 3 goals: firstly, to validate the model in rabbit eyes; secondly, to test the mutability of the model to monkey eyes; thirdly, to calculate the half-lives of ranibizumab and the VTE in human eyes. The half-life calculations for ranibizumab deviate from published rabbit and monkey values by only 8.3% and 4.2%. Using the experimentally determined half-life of bevacizumab in human eyes (8.25 days) to set the equation, the half-lives of ranibizumab and the VTE are calculated to be 4.75 days and 7.13 days in human eyes. The intraocular half-lives of ranibizumab and the VTE are estimated using existing published animal and human data and a mathematical model. The validity of these half-lives and binding activities, however, awaits clinical correlation.
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Published
2011-08-02
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An Open Access Publication is one that meets the following two conditions:
1. The author(s) and copyright holder(s) grant(s) to all users a free, irrevocable, worldwide, perpetual right of access to, and a license to copy, use, distribute, transmit and display the work publicly and to make and distribute derivative works, in any digital medium for any responsible purpose, subject to proper attribution of authorship, as well as the right to make small numbers of printed copies for their personal use.
2. A complete version of the work and all supplemental materials, including a copy of the permission as stated above, in a suitable standard electronic format is deposited immediately upon initial publication in at least one online repository that is supported by an academic institution, scholarly society, government agency, or other well-established organization that seeks to enable open access, unrestricted distribution, interoperability, and long-term archiving.
Authors who publish with this journal agree to the following terms: 1. Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal. 2. Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal. 3. Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work.
