Introduction: Pathological formation of blood vessels plays a key role in the growth and metastasis of tumors and also in several serious ophthalmological diseases such as wet age-related macular degeneration (AMD) or diabetic retinopathy. In AMD treatment, aflibercept (tradename EYLEA) is used to deactivate the underlying pathological neovascularisation. Aflibercept is a recombinant fusion protein which binds to vascular endothelial growth factor (VEGF) receptors, thereby inhibiting VEGF pathway activation. VEGF is one of the most important angiogenesis factors.
Objective: This analysis investigates lasting efficacy of aflibercept in vitro for later application as therapeutic agent against macular degeneration (AMD).
Material And Methods: VEGF-ELISA assays were performed to investigate binding affinities at different aflibercept concentrations. The impact of VEGF on the proliferation of human umbilical vein endothelial cells (HUVEC) was investigated using proliferation assays. Moreover, time-dependent kinetic studies were performed to analyze different aflibercept storage durations with regard to its inhibitory capabilities on human VEGF.
Results And Conclusion: Our results reveal that aflibercept significantly lowers the amount of unbound VEGF as well as the proliferation rate of HUVEC. Moreover, in contrast to specifications given by the manufacturer, aflibercept retains its full inhibitory effect up to at least 120h after transference from the original vial into the injection syringe.
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http://dx.doi.org/10.1016/j.aanat.2017.02.005 | DOI Listing |
Int J Mol Sci
January 2025
Division of Clinical Pharmacology, Department of Pharmacology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.
Aflibercept and brolucizumab, two anti-VEGF agents used as intravitreal injections in ophthalmology, differ significantly in molecular weight (aflibercept-115 kDa and brolucizumab-26 kDa). Using aqueous humor samples collected after drug administration, we measured and performed a comparative analysis of pharmacokinetics and half-lives of these drugs in the human eye. Since the quantification of monoclonal antibodies (mAbs) using antigen-antibody reactions, such as ELISA, is influenced by endogenous ligands or anti-drug antibodies, we employed nano-surface and molecular-orientation limited proteolysis (nSMOL), combined with liquid chromatography-tandem mass spectrometry (LC-MS/MS), for accurate measurements.
View Article and Find Full Text PDFClin Colorectal Cancer
January 2025
Operative Research Unit of Medical Oncology, Fondazione Policlinico Universitario Campus Bio-Medico, Roma, Italy; Department of Medicine and Surgery, Università Campus Bio-Medico di Roma, Roma, Italy.
Background: Both aflibercept and bevacizumab-based regimens are available II-line treatment options for patients with metastatic colorectal cancer (mCRC). However, no head-to-head trials established the optimal anti-angiogenic strategy for this setting.
Methods: We launched a multicenter, retrospective, observational study to assess and compare clinical efficacy of II-line treatments for patients with mCRC.
J AAPOS
January 2025
Cleveland Clinic Cole Eye Institute, Cleveland, Ohio. Electronic address:
Background: Choroidal neovascular membranes (CNVM) associated with optic nerve head drusen (ONHD) are rare but vision threatening. A variety of treatments, including laser photocoagulation, subretinal surgery, and anti-VEGF injections, are effective but pose risks, particularly in pediatric patients, underscoring the need for a comprehensive review.
Methods: A systematic review was conducted using PubMed, Embase, and Web of Science.
Ophthalmic Surg Lasers Imaging Retina
January 2025
Background And Objective: To assess the efficacy of intravitreal aflibercept 8 mg in treating neovascular age-related macular degeneration (nAMD) in patients previously treated with faricimab.
Patients And Methods: A retrospective study was conducted on nAMD patients with suboptimal response to faricimab injections who were switched to intravitreal aflibercept 8 mg. Visual acuity (VA) and optical coherence tomography features were evaluated.
Int Ophthalmol
January 2025
Beyoglu Eye Training and Research Hospital, University of Health Sciences, Bereketzade Camii Sk. No:2 Beyoğlu, 34421, Istanbul, Turkey.
Background: To evaluate the efficacy and safety of intravitreal injections of 4 mg (high dose) of aflibercept in treatment-naive patients with neovascular AMD(nAMD) with treat and extend(TREX) dosing regimens, and to determine the frequency of injections.
Methods: In this interventional, retrospective study a total of 15 eyes of 14 patients (eight female and 9 male) with nAMD were included. All patients were examined and OCT imaging was performed at the time of initial presentation, on the day of each injection and at subsequent follow-up visits.
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