ArticleInvestigative ophthalmology & visual science2010
Delivery of SAR 1118 to the retina via ophthalmic drops and its effectiveness in a rat streptozotocin (STZ) model of diabetic retinopathy (DR).
Article in Investigative ophthalmology & visual science, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers, 1 of them a synthesis that pooled it.
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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.
The trial behind it
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Who cites it
41 citing papers in PubMed, 1 synthesis or guideline pooled it, 70 citations in OpenAlex.
- Association between the neutrophil-to-lymphocyte ratio and the incidence of diabetic retinopathy: a systematic review and meta-analysis.Frontiers in endocrinology · 2025Pooled it
- Safety, tolerability, and bioavailability of topical SAR 1118, a novel antagonist of lymphocyte function-associated antigen-1: a phase 1b study.Eye (London, England) · 2012Trial
- Cytokines in age-related eye diseases: pathogenesis and potential targets for innovative therapies.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Topical lifitegrast therapy for dry eye disease.The Cochrane database of systematic reviews · 2025Article
- Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data.Pharmaceuticals (Basel, Switzerland) · 2024Article
- The Role of Immune Cells and Signaling Pathways in Diabetic Eye Disease: A Comprehensive Review.Biomedicines · 2024Review
- Cell and molecular targeted therapies for diabetic retinopathy.Frontiers in endocrinology · 2024Review
- Inflammation: The Link between Neural and Vascular Impairment in the Diabetic Retina and Therapeutic Implications.International journal of molecular sciences · 2023Review
- Inflammation in diabetic retinopathy: possible roles in pathogenesis and potential implications for therapy.Neural regeneration research · 2023Review
- LFA-1/ ICAM-1 promotes NK cell cytotoxicity associated with the pathogenesis of ocular toxoplasmosis in murine model.PLoS neglected tropical diseases · 2022Article
- Inflammatory mediators in diabetic retinopathy: Deriving clinicopathological correlations for potential targeted therapy.Indian journal of ophthalmology · 2021Review
- Effects of ranibizumab on growth factors and mediators of inflammation in the aqueous humor of patients with diabetic macular edema.Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie · 2021Article
- Involvement of Cytokines in the Pathogenesis of Diabetic Macular Edema.International journal of molecular sciences · 2021Review
- Endothelial activation and dysfunction in COVID-19: from basic mechanisms to potential therapeutic approaches.Signal transduction and targeted therapy · 2020Review
- The involvement of the mGluR5-mediated JNK signaling pathway in rats with diabetic retinopathy.International ophthalmology · 2019Article
- Translational Preclinical Pharmacologic Disease Models for Ophthalmic Drug Development.Pharmaceutical research · 2019Review
- Aqueous Humor Cytokine Levels and Anatomic Response to Intravitreal Ranibizumab in Diabetic Macular Edema.JAMA ophthalmology · 2018Article
- Dry eye syndrome: developments and lifitegrast in perspective.Clinical ophthalmology (Auckland, N.Z.) · 2018Review
- Review
- Lifitegrast ophthalmic solution in the treatment of signs and symptoms of dry eye disease: design, development, and place in therapy.Clinical ophthalmology (Auckland, N.Z.) · 2017Review
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
purposeTo determine the pharmacokinetics of SAR 1118, a small-molecule antagonist of leukocyte function-associated antigen (LFA)-1, after administration of ophthalmic drops in normal rats, and to determine its pharmacologic activity by assessing the inhibition of retinal leukostasis and vascular leakiness in a streptozotocin (STZ)-induced diabetic retinopathy model.
methodsThe ocular pharmacokinetics of SAR 1118 were studied in rats after a single topical dose of (14)C-SAR 1118 (1 mg/eye; 40 μCi; 15.5 μL). SAR 1118 concentration time profiles in plasma and ocular tissues were quantified by liquid scintillation counting (LSC). The pharmacologic activity of SAR 1118 eye drops administered thrice daily for 2 months at 1% (0.3 mg/eye/d) and 5% (1.5 mg/eye/d) was assessed in an STZ-induced diabetic rat model by determining retinal leukostasis and blood-retinal barrier breakdown. Diabetic rats treated with periocularly administered celecoxib microparticles served as the positive control, and vehicle-treated rats served as the negative control.
resultsA single dose of 6.5% (14)C-radiolabeled SAR 1118 ophthalmic drops delivered retinal drug levels greater than 1 μM in less than 30 minutes and sustained levels greater than 100 nM for 8 hours. SAR 1118 eye drops significantly reduced leukostasis and blood-retinal barrier breakdown in a dose-dependent manner.
conclusionsSAR 1118 ophthalmic drops administered thrice daily deliver therapeutic levels of SAR 1118 in the retina and can alleviate the retinal complications associated with diabetes.
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What OpenQuestion holds
Registered trials
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