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The disposition and tissue distribution of 14C-labeled N-[[(trimethylamino)boryl]carbonyl]-L-phenylalanine methyl esther (1) determined in CF1 mice following i.v., p.o., and i.p. administration. Compound 1 was found to undergo rapid and extensive metabolism, and the majority of the radioactivity was found in the skin and carcass regardless of the route of administration. Approximately 55% of the radioactivity was recovered in urine and feces after 78 h; however, excretion via these routes was not complete. Degradation of compound 1 occurred at the amide bond at low pH (0.8) but at the ester bond a physiological pH. This difference in degradation was reflected in elevation of the blood radioactivity levels after p.o. administration compared to i.p. and i.v. administration.


M C Miller, R P Shrewsbury, A L Elkins, A Sood, B F Spielvogel, I H Hall. The disposition, tissue distribution, and cellular transport of N-[[(trimethylamino)boryl]carbonyl]-L-phenylalanine methyl ester in CF1 mice. Journal of pharmaceutical sciences. 1995 Aug;84(8):933-6

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PMID: 7500276

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