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Management of endophthalmitis
Published in A Peyman MD Gholam, A Meffert MD Stephen, D Conway MD FACS Mandi, Chiasson Trisha, Vitreoretinal Surgical Techniques, 2019
Mandi D Conway, Gholam A Peyman
Pegaptanib (Macugen, Pfizer Ophthalmics) has been used to treat choroidal neovascularization secondary to age-related macular degeneration,35 and is in clinical trials for treatment of diabetic macular edema and CME related to retinal venous occlusive disease. Among the adverse events to eyes in the Neovascular Age-Related Macular Degeneration Study, endophthalmitis occurred in 1.3% of eyes and was associated with severe visual loss. The range of endophthalmitis after cataract surgery is comparatively 0.06–0.4%. Review of data suggested that appropriate aseptic technique was broken, especially with regard to the use of a lid speculum. The per-injection rate of endophthalmitis (0.16%) in the age-related macular degeneration trial was reportedly similar to rates identified in a comprehensive review by Jager et al140 of more than 15 000 intravitreous injections. Gragoudas et al35 and Aiello et al141 concluded that careful attention to aseptic technique would probably minimize the risk. After aseptic technique education, the incidence of endophthalmitis associated with the injection decreased significantly to 0.03% per injection.142 Importantly, these eyes are treated like other acute postoperative endophthalmitis cases, with intravitreal tap, cultures, and injections of antibiotics or vitrectomy.
Age-Related Macular Degeneration Drug Delivery
Published in Glenn J. Jaffe, Paul Ashton, P. Andrew Pearson, Intraocular Drug Delivery, 2006
Kourous A. Rezaei, Sophie J. Bakri, Peter K. Kaiser
Based on the results described above, Eyetech received Food and Drug Administration approval to market pegaptanib sodium for treatment of patients with neovascular AMD. This drug is the first anti-angiogenic agent to receive approval to treat AMD.
Updates on the Management of Ocular Vasculopathies with VEGF Inhibitor Conbercept
Published in Current Eye Research, 2020
Huan Liu, Yue Ma, Hong-Chang Xu, Li-Ying Huang, Li-Ying Zhai, Xiao-Rong Zhang
According to the guidelines from American Academy of Ophthalmology (AAO) and the European Society of Retina Specialists (EURETINA), VEGF inhibitors (e.g., aflibercept, Ranibizumab (Lucentis; Genentech, Inc., South San Francisco, CA, USA) and bevacizumab (Avastin; Genentech and Roche, Basel, Switzerland)) are most effective to manage neovascular AMD and are considered first-line therapy for treating and stabilizing most cases of neovascular AMD patients,37,38 and a Cochrane systematic review demonstrated the effectiveness of these agents to maintain visual acuity.39 Pegaptanib has since fallen out of favor after these anti-VEGF agents demonstrated meaningful improvement in vision.40 Researchers around the world have launched various clinical studies to investigate the anti-VEGF agents for neovascular AMD. Recently, the Food and Drug Administration of China has approved conbercept for the treatment of neovascular AMD in China. Conbercept appears to offer yet another option of anti-VEGF drug for use in neovascular AMD.6,16,41
Metabolism of bioconjugate therapeutics: why, when, and how?
Published in Drug Metabolism Reviews, 2020
Hanlan Liu, Jayaprakasam Bolleddula, Andrew Nichols, Lei Tang, Zhiyang Zhao, Chandra Prakash
Aptamers are single-stranded DNA or RNA molecules (usually containing 20–60 nucleotides) with specific three-dimensional structures that can bind with high specificity and affinity to molecular targets. Pegaptanib (MacQueen®) is a 28-base ribonucleic acid aptamer (Ruckman et al. 1998) developed to bind and block the activity of vascular endothelial growth factor for the treatment of neovascular (wet) age-related macular degeneration (AMD). Like other nucleotide drugs in development, the carbohydrate backbone of pegaptanib is modified to increase stability. In addition, it is covalently linked to two branched 20-kD PEG moieties to prolong the half-life of the drug in the vitreous (Gragoudas et al. 2004). In clinical studies, it was proven safe and demonstrated a statistically significant and clinically meaningful benefit for the treatment of AMD.
Emerging PEGylated non-biologic drugs
Published in Expert Opinion on Emerging Drugs, 2019
Eun Ji Park, Jiyoung Choi, Kang Choon Lee, Dong Hee Na
Pegaptanib (Macugen®, Pfizer) was the first therapeutic aptamer approved by the US FDA in 2004 as an anti-angiogenic medicine for the treatment of neovascular age-related macular degeneration (AMD) [37,38]. It is administered by intravitreal injection at a dosage of 0.3 mg per eye every 6 weeks. Pegaptanib specifically binds to the 165-amino acid isoform of vascular endothelial growth factor (VEGF), blocks its interaction with the cognate receptor, and ultimately stops intraocular blood vessel growth [37]. The aptamer has been chemically modified by the incorporation of 2′-fluoro pyrimidine, 2′-O-methyl purines, and an inverted nucleotide at the 3′-terminus, and the conjugation of 40 kDa branched PEG to the 5′-terminus (Figure 1(c)). In a clinical study, pegaptanib exhibited prolonged blood residence, with a mean apparent terminal half-life of 10 days without unwanted immune responses [39,40].