ArticlePharmaceutical research2014
Pharmacokinetics and efficacy of the spleen tyrosine kinase inhibitor r406 after ocular delivery for retinoblastoma.
Article in Pharmaceutical research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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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
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.
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- Tyrosine Kinase Receptors, Inhibition, and Potential Role in the Pharmacotherapy of Retinal Disorders.Ophthalmology and therapy · 2026Review
- Emerging New Therapeutics for Retinoblastoma.Ocular oncology and pathology · 2022Review
- Treatment of RB-deficient retinoblastoma with Aurora-A kinase inhibitor.The Kaohsiung journal of medical sciences · 2022Article
- Treatment of Retinoblastoma: What Is the Latest and What Is the Future.Frontiers in oncology · 2022Review
- Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress inAntioxidants (Basel, Switzerland) · 2020Article
- Non-coding and Coding Transcriptional Profiles Are Significantly Altered in Pediatric Retinoblastoma Tumors.Frontiers in oncology · 2019Article
- RNA-Sequencing of Primary Retinoblastoma Tumors Provides New Insights and Challenges Into Tumor Development.Frontiers in genetics · 2018Article
- Syk inhibitors in clinical development for hematological malignancies.Journal of hematology & oncology · 2017Review
- Advances in the use of prodrugs for drug delivery to the eye.Expert opinion on drug delivery · 2017Review
- RB1: a prototype tumor suppressor and an enigma.Genes & development · 2016Review
- Progress in Small Molecule Therapeutics for the Treatment of Retinoblastoma.Mini reviews in medicinal chemistry · 2016Review
- Retinoblastoma.Nature reviews. Disease primers · 2015Review
- Management of retinoblastoma in children: current status.Paediatric drugs · 2015Review
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
purposeRetinoblastoma is a childhood cancer of the retina. Clinical trials have shown that local delivery of broad spectrum chemotherapeutic agents is efficacious. Recent studies characterizing the genomic and epigenomic landscape of retinoblastoma identified spleen tyrosine kinase (SYK) as a promising candidate for targeted therapy. The purpose of this study was to conduct preclinical testing of the SYK antagonist R406 to evaluate it as a candidate for retinoblastoma treatment.
methodsThe efficacy of the SYK antagonist R406 delivered locally in a human orthotopic xenograft mouse model of retinoblastoma was tested. Intraocular exposure of R406 was determined for various routes and formulations.
resultsThere was no evidence of efficacy for subconjunctival. R406. Maximal vitreal concentration was 10-fold lower than the minimal concentration required to kill retinoblastoma cells in vitro. Dosage of R406 subconjunctivally from emulsion or suspension formulations, direct intravitreal injection of the soluble prodrug of R406 (R788), and repeated topical administration of R406 all increased vitreal exposure, but failed to reach the exposure required for retinoblastoma cell death in culture.
conclusionTaken together, these data suggest that R406 is not a viable clinical candidate for the treatment of retinoblastoma. This study highlights the importance of pharmacokinetic testing of molecular targeted retinoblastoma therapeutics.
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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.