García-Quintanilla Laura, Luaces-Rodríguez Andrea, Gil-Martínez María, Mondelo-García Cristina, Maroñas Olalla, Mangas-Sanjuan Víctor, González-Barcia Miguel, Zarra-Ferro Irene, Aguiar Pablo, Otero-Espinar Francisco J, Fernández-Ferreiro Anxo
Pharmacy Department, University Clinical Hospital of Santiago de Compostela (SERGAS), 15706 Santiago de Compostela, Spain.
Pharmacology Group, Health Research Institute of Santiago de Compostela (FIDIS), 15706 Santiago de Compostela, Spain.
Pharmaceutics. 2019 Jul 31;11(8):365. doi: 10.3390/pharmaceutics11080365.
Intravitreal administration of anti-vascular endothelial growth factor (VEGF) antibodies has become the standard treatment for Age-Related Macular Degeneration; however, the knowledge of their pharmacokinetics is limited. A comprehensive review of the preclinical and clinical pharmacokinetic data that were obtained in different studies with intravitreal bevacizumab, ranibizumab, and aflibercept has been conducted. Moreover, the factors that can influence the vitreous pharmacokinetics of these drugs, as well as the methods that were used in the studies for analytical determination, have been exposed. These anti-VEGF drugs present different charge and molecular weights, which play an important role in vitreous distribution and elimination. The pharmacokinetic parameters that were collected differ depending on the species that were involved in the studies and on physiological and pathological conditions, such as vitrectomy and lensectomy. Knowledge of the intravitreal pharmacokinetics of the anti-VEGF drugs that were used in clinical practice is of vital importance.
玻璃体内注射抗血管内皮生长因子（VEGF）抗体已成为年龄相关性黄斑变性的标准治疗方法；然而，其药代动力学知识有限。已对在不同研究中使用玻璃体内注射贝伐单抗、雷珠单抗和阿柏西普获得的临床前和临床药代动力学数据进行了全面综述。此外，还阐述了可影响这些药物玻璃体药代动力学的因素以及研究中用于分析测定的方法。这些抗VEGF药物具有不同的电荷和分子量，这在玻璃体分布和消除中起重要作用。所收集的药代动力学参数因研究涉及的物种以及生理和病理状况（如玻璃体切除术和晶状体切除术）而异。了解临床实践中使用的抗VEGF药物的玻璃体内药代动力学至关重要。
