The effects of topical everolimus and sunitinib on corneal neovascularization

Çakmak, Harun; Ergin, Kemal; Bozkurt, Gökay; Kocatürk, Tolga; Evliçoglu, Gökhan Evren

doi:10.3109/15569527.2015.1034360

Cited by 11 publications

(12 citation statements)

References 38 publications

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“…Other experiments showed that topical application of both sunitinib and everolimus could decrease VEGFR2 levels and suppress CNV. Further, everolimus could decrease ERK 1/2 levels, which appeared to be more useful than sunitinib on the treatment of CNV …”

Section: The Drug Treatment Of Cnvmentioning

confidence: 97%

Recent drug therapies for corneal neovascularization

Liu

Wang

et al. 2017

Chem Biol Drug Des

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Corneal neovascularization (CNV) is a common pathological change in ocular surface diseases. It is not only the factor that affects vision but also the main cause for corneal graft failure. Based on the mechanism of CNV, many achievements have been developed to suppress the formation of CNV. There are certain novel drugs such as aflibercept, gold nanoparticles, and netrins which provide us with new clues to treat CNV. However, we still need to develop more effective therapeutic drugs. It is of great significance to develop new effective drugs to suppress the occurrence of CNV. In this paper, recent drug therapies for CNV are reviewed. The electronic database (PubMed) is searched for relative basic research and randomized clinical trials that are published recently.

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Section: The Drug Treatment Of Cnvmentioning

confidence: 97%

Recent drug therapies for corneal neovascularization

Liu

Wang

et al. 2017

Chem Biol Drug Des

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“…Its design was based on sunitinib. Preclinical studies have indicated that sunitinib can inhibit corneal neovascularization [ 31 ]. Vatalanib, pazopanib, and sorafenib are tyrosine kinase inhibitors similar to sunitinib.…”

Section: Discussionmentioning

confidence: 99%

The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

Ren

Shi

Jiang

et al. 2017

Journal of Ophthalmology

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The aims of this study were to evaluate the effects of CM082 on the development of choroidal neovascularization (CNV) in a laser-induced CNV rat model and to determine the drug concentration in the ocular tissues. After the laser-induced CNV model was established in rats, CM082 was orally administered. The effects of CM082 on the CNV lesions were assessed using fundus fluorescein angiography (FFA), CNV histology, and retinal pigment epithelium- (RPE-) choroid-sclera eyecup analysis. The concentrations of CM082 in the plasma and eye tissues were determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Results of FFA, histology, and RPE-choroid-sclera eyecup analysis demonstrated that the CM082-treated (10 mg/kg/d or 30 mg/kg/d) rats exhibited significantly less neovascularization than did the control group. The total concentration of CM082 in the eyes (172.86 ± 57.11 ng/g) was similar to that in the plasma (196.87 ± 73.13 ng/ml). Within the eye, the concentrations of CM082 and its metabolites were highest in the retina-sclera. The orally administered CM082 thus effectively passed through the blood-retina barrier (BRB) to reach the retina in the Brown Norway rats. Therefore, at both 10 mg/kg/d and 30 mg/kg/d, CM082 was able to reduce CNV lesions in the laser-induced CNV rat model.

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“…143 Both agents have recently been shown to effectively reduce VEGFR-2 levels and inhibit CoNV in a rat model. 144…”

Section: Vegf Pathwaymentioning

confidence: 99%

The Management of Corneal Neovascularisation – Update on New Clinical Data and Recommendations of Treatment

Spiteri¹,

Romano²,

Brunner³

et al. 2016

European Ophthalmic Review

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Vascularisation of the cornea may occur as a sight-threatening response to various insults to the cornea, such as infection, trauma and inflammation, and is a well-recognised risk factor for rejection and subsequent failure of corneal grafts. Various different treatment modalities have been used in the past, with varying levels of success. In this review, we discuss the pathogenesis of corneal neovascularisation, look at recent advances in the assessment of these patients and give an overview of currently available treatment options, both medical and surgical. We also discuss current experimental treatment for corneal neovascularisation, such as gene therapy, which may provide further treatment options in the future.

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The effects of topical everolimus and sunitinib on corneal neovascularization

Abstract: Topical administration of both everolimus and sunitinib reduced VEGFR-2 levels and inhibited CNV. In additon, everolimus reduced ERK 1/2 levels and seems to be more effective than sunitinib on CNV.

Cited by 11 publications

References 38 publications

Recent drug therapies for corneal neovascularization

Recent drug therapies for corneal neovascularization

The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

The Management of Corneal Neovascularisation – Update on New Clinical Data and Recommendations of Treatment

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