Evidence map›Paper›PMID 39859273›Full record

ArticleInternational journal of molecular sciences2025

Comparative Pharmacokinetic Analysis of Aflibercept and Brolucizumab in Human Aqueous Humor Using Nano-Surface and Molecular-Orientation Limited Proteolysis.

Kosuke Nagaoka, Natsuka Kimura, Satoru Inoda, Takuya Takayama, Yusuke Arai, Yasuo Yanagi, Takashi Shimada, Ryozo Nagai, Hidenori Takahashi, Kenichi Aizawa

Abstract readComparative Study
In one paragraph

Article in International journal of molecular sciences, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Review
  2. Article
  3. Increased aqueous flare after intravitreal brolucizumab injections compared to aflibercept in neovascular age-related macular degeneration.Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie · 2026
    Article
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Kosuke NagaokaDepartment of Ophthalmology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.
Natsuka KimuraDivision of Clinical Pharmacology, Department of Pharmacology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.
Satoru InodaDepartment of Ophthalmology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.ORCID 0000-0003-4577-8169
Takuya TakayamaDepartment of Ophthalmology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.ORCID 0000-0001-5774-0016
Yusuke AraiDepartment of Ophthalmology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.
Yasuo YanagiDepartment of Ophthalmology and Micro-Technology, Yokohama City University, Yokohama-shi 232-0023, Kanagawa, Japan.
Takashi ShimadaTechnology Research Laboratory, Shimadzu Corporation, Kyoto-shi 604-8511, Kyoto, Japan.
Ryozo NagaiJichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.
Hidenori TakahashiDepartment of Ophthalmology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.ORCID 0000-0001-5331-4730
Kenichi AizawaDivision of Clinical Pharmacology, Department of Pharmacology, Jichi Medical University, Shimotsuke-shi 329-0498, Tochigi, Japan.

Funding

JSPS KAKENHI 21K16880
6 · The paper itself

Abstract

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. Aqueous humor samples were collected from 59 eyes of 59 patients treated with aflibercept and 52 eyes of 52 patients treated with brolucizumab. Samples were obtained with a median post-injection period of 30 (range, 2-49) days for aflibercept and 28 (range, 4-60) days for brolucizumab. A population pharmacokinetic (PPK) analysis revealed that the half-life of aflibercept in human aqueous humor was significantly shorter than that of brolucizumab, 2.88 days versus 9.00 days, respectively (

Indexed as

Antibodies, Monoclonal, HumanizedAqueous HumorImmunoconjugatesReceptors, Vascular Endothelial Growth FactorRecombinant Fusion ProteinsAgedAged, 80 and overChromatography, LiquidFemaleHalf-LifeHumansIntravitreal InjectionsMaleMiddle AgedProteolysisTandem Mass SpectrometryafliberceptAntibodies, Monoclonal, HumanizedbrolucizumabImmunoconjugatesReceptors, Vascular Endothelial Growth FactorRecombinant Fusion Proteinsafliberceptbrolucizumabhalf-lifehumanintravitreal injectionLC-MS/MSnSMOLvitreous humor

Identifiers

PMID39859273
PMCPMC11764841

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.