Approach Summary Licensing status Publication and contact information Drug delivery Photodynamic prodrug release system using visible light A nonenzymatic, photodynamic prodrug system could provide better control over drug delivery than systems that release drugs by enzymatic activation. With the new system, drugs bearing carbonyl groups were attached to a photosensitizer that allowed drug release upon visible light irradiation. Methyl esters of non-steroidal anti-inflammatory drugs (ibuprofen and naproxen) were linked to photosensitized porphyrin derivatives and within minutes were released by visible light illumination in high yields in vitro. Next steps were not disclosed. QLT Inc. and Novartis AG market Visudyne verteporfin photodynamic therapy to treat wet age-related macular degeneration. No fewer than six other companies have photodynamic therapies for multiple indications in developmental stages ranging from preclinical to marketed. Patent and licensing status undisclosed Jiang, M. et al.

Development of effective treatments for high-grade glioma (HGG) is hampered by (1) the blood–brain barrier (BBB), (2) an infiltrative growth pattern, (3) rapid development of therapeutic resistance, and, in many cases, (4) dose-limiting toxicity due to systemic exposure. Convection-enhanced delivery (CED) has the potential to significantly limit systemic toxicity and increase therapeutic index by directly delivering homogenous drug concentrations to the site of disease. In this review, we present clinical experiences and preclinical developments of CED in the setting of high-grade gliomas.

A meso-palladioporphyrin intermediate was isolated from a Heck reaction between an iodoporphyrin and a non-activated olefin using a Pd(PPh3)2Cl2/Et3N system; its structure was characterized by NMR, MS and X-ray crystallography. Studies on its formation indicate that the Pd(II) catalyst was reduced in situ by Et3N with the assistance of water. The catalytic activity of the intermediate was confirmed by stoichiometric and catalytic reactions using a more reactive olefin, ethyl acrylate.

Development of effective treatments for high-grade glioma (HGG) is hampered by 1) the blood-brain barrier (BBB), 2) an infiltrative growth pattern, 3) rapid development of therapeutic resistance, and, in many cases, 4) dose-limiting toxicity due to systemic exposure. Convec-tion-enhanced delivery (CED) has the potential to significantly limit systemic toxicity and in-crease therapeutic index by directly delivering homogenous drug concentrations to the site of disease. In this review, we present clinical experiences and preclinical developments of CED in the setting of high-grade gliomas.

No abstract