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Merck

Clinical disposition, metabolism and in vitro drug-drug interaction properties of omadacycline.

Xenobiotica; the fate of foreign compounds in biological systems (2016-08-09)
Jimmy Flarakos, Yancy Du, Helen Gu, Lai Wang, Heidi J Einolf, Dung Y Chun, Bing Zhu, Natalia Alexander, Adrienne Natrillo, Imad Hanna, Lillian Ting, Wei Zhou, Kiran Dole, Haiying Sun, Steven J Kovacs, Daniel S Stein, S Ken Tanaka, Stephen Villano, James B Mangold
ABSTRACT

1. Absorption, distribution, metabolism, transport and elimination properties of omadacycline, an aminomethylcycline antibiotic, were investigated in vitro and in a study in healthy male subjects. 2. Omadacycline was metabolically stable in human liver microsomes and hepatocytes and did not inhibit or induce any of the nine cytochrome P450 or five transporters tested. Omadacycline was a substrate of P-glycoprotein, but not of the other transporters. 3. Omadacycline metabolic stability was confirmed in six healthy male subjects who received a single 300 mg oral dose of [

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Sigma-Aldrich
Uridine 5′-diphosphoglucuronic acid ammonium salt, 98-100%