69081-78-3Relevant academic research and scientific papers
Synthesis of highly water-soluble fibrate derivatives via BGLation
Nemoto, Hisao,Kamiya, Masaki,Nakamoto, Aki,Matsushita, Tsuyoshi,Matsumura, Kosuke,Hattori, Hatsuhiko,Kawamura, Tomoyuki,Taoka, Chiaki,Abe, Shinji,Ishizawa, Keisuke,Miyamoto, Licht,Tsuchiya, Koichiro
supporting information, p. 6425 - 6428 (2012/11/07)
Three water-soluble fibrates (fenofibrate, bezafibrate and chlofibrate) conjugated with a symmetrically branched glyceryl trimer (BGL003) were synthesized, and an evaluation of the fenofibrate-BGL003 conjugate as a candidate for anti-hyperlipemia drug was carried out using rats. The water-solubility of the fenofibrate-BGL003 conjugate was several thousand times greater than that of the original fenofibrate. The lipid-lowering effects of the fenofibrate-BGL003 conjugate were as strong as those of the same grams of fenofibrate. The actual active species of fenofibrate, fenofibric acid, was detected in rats' blood, but neither the fenofibrate-BGL003 conjugate nor fenofibrate was detected, probably due to enzymatic hydrolysis of the ester bond. The plasma concentration of fenofibric acid derived from the fenofibrate-BGL003 conjugate was five times higher than that derived from fenofibrate 4 h after administration.
