Evaluation of new benzoporphyrin derivatives with enhanced PDT efficacy.
A first report on the biological evaluation of a series of isomerically pure benzoporphyrin derivatives (cis- and trans-isomers) as methyl esters is described. In preliminary in vivo studies, the n-hexyl ether analogues of both cis- and trans-isomers of benzoporphyrin derivatives were found to be more active than the industrially prepared benzoporphyrin derivative, a mixture of monocarboxylic acids (BPDMA, Quadralogic Technologies, Vancouver). Further studies with 4-de-vinyl-4- (1-hexyloxyethyl) benzoporphyrin derivative showed that, like BPDMA, it had reduced residual skin phototoxicity compared in mice with Photofrin. The uptake and clearance characteristics of BPDMA were also compared with the 4-(1-hexyloxyethyl)-derivative by in vivo reflection spectroscopy.
D000818:Animals; D005260:Female; D017324:Hematoporphyrin Derivative / Q000633:toxicity; D007536:Isomerism; D008657:Metabolic Clearance Rate; D051379:Mice; D008811:Mice, Inbred DBA; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D017319:Photosensitizing Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use / Q000633:toxicity*; D011166:Porphyrins / Q000493:pharmacokinetics* / Q000633:toxicity*; D012867:Skin / Q000187:drug effects / Q000473:pathology*; D013329:Structure-Activity Relationship
D017319:Photosensitizing Agents; D011166:Porphyrins; D017324:Hematoporphyrin Derivative