{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,17]],"date-time":"2026-10-17T07:20:31Z","timestamp":1792221631850,"version":"4.4.0"},"reference-count":21,"publisher":"American Society for Microbiology","issue":"1","license":[{"start":{"date-parts":[[2016,12,27]],"date-time":"2016-12-27T00:00:00Z","timestamp":1482796800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"},{"start":{"date-parts":[[2017,1,1]],"date-time":"2017-01-01T00:00:00Z","timestamp":1483228800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"funder":[{"name":"Paratek Pharmaceuticals"},{"DOI":"10.13039\/100008272","name":"Novartis Pharmaceuticals Corporation","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100008272","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2017,1]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>The absorption, distribution, metabolism, and excretion (ADME) of omadacycline, a first-in-class aminomethylcycline antibiotic with a broad spectrum of activity against Gram-positive, Gram-negative, anaerobic, and atypical bacteria, were evaluated in rats. Tissue distribution was investigated by quantitative whole-body autoradiography in male Long-Evans Hooded (LEH) rats. Following an intravenous (i.v.) dose of 5 mg\/kg of body weight, radioactivity widely and rapidly distributed into most tissues. The highest tissue-to-blood concentration ratios (t\/b) were observed in bone mineral, thyroid gland, and Harderian gland at 24 h post-i.v. dose. There was no evidence of stable accumulation in uveal tract tissue, suggesting the absence of a stable binding interaction with melanin. Following a 90 mg\/kg oral dose in LEH rats, the highest t\/b were observed in bone mineral, Harderian gland, liver, spleen, and salivary gland. The plasma protein binding levels were 26% in the rat and 15% to 21% in other species. Omadacycline plasma clearance was 1.2 liters\/h\/kg, and its half-life was 4.6 h; the steady-state volume of distribution (Vss) was 6.89 liters\/kg. Major circulating components in plasma were intact omadacycline and its epimer. Consistent with observations in human, approximately 80% of the dose was excreted into the feces as unchanged omadacycline after i.v. administration. Fecal excretion was primarily the result of biliary excretion (\u223c40%) and direct gastrointestinal secretion (\u223c30%). However, urinary excretion (\u223c30%) was equally prominent after i.v. dosing.<\/jats:p>","DOI":"10.1128\/aac.01784-16","type":"journal-article","created":{"date-parts":[[2016,11,8]],"date-time":"2016-11-08T03:54:40Z","timestamp":1478577280000},"update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":40,"title":["Pharmacokinetics, Distribution, Metabolism, and Excretion of Omadacycline following a Single Intravenous or Oral Dose of\n            <sup>14<\/sup>\n            C-Omadacycline in Rats"],"prefix":"10.1128","volume":"61","author":[{"given":"Wen","family":"Lin","sequence":"first","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jimmy","family":"Flarakos","sequence":"additional","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yancy","family":"Du","sequence":"additional","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenyu","family":"Hu","sequence":"additional","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Handan","family":"He","sequence":"additional","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"James","family":"Mangold","sequence":"additional","affiliation":[{"name":"Novartis Biomedical Research Institute, East Hanover, New Jersey, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"S. Ken","family":"Tanaka","sequence":"additional","affiliation":[{"name":"Paratek Pharmaceuticals, Boston, Massachusetts, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stephen","family":"Villano","sequence":"additional","affiliation":[{"name":"Paratek Pharmaceuticals, Boston, Massachusetts, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01066-13"},{"key":"e_1_3_2_3_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01242-13"},{"key":"e_1_3_2_4_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00948-12"},{"key":"e_1_3_2_5_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01393-16"},{"key":"e_1_3_2_6_2","doi-asserted-by":"publisher","DOI":"10.1080\/00498254.2016.1213465"},{"key":"e_1_3_2_7_2","unstructured":"FDA. February2008. 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Abstr 39th Intersci Conf Antimicrob Agents Chemother, abstr 413."},{"key":"e_1_3_2_15_2","doi-asserted-by":"publisher","DOI":"10.1211\/0022357023141"},{"key":"e_1_3_2_16_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejps.2010.03.011"},{"key":"e_1_3_2_17_2","volume-title":"Abstr 26th Eur Congr Clin Microbiol Infect Dis","author":"Tanaka SK","year":"2016","unstructured":"Tanaka SK VillanoS TzanisE. 2016. Single and multiple dose pharmacokinetics and tolerability of intravenous omadacycline in healthy volunteers. Abstr 26th Eur Congr Clin Microbiol Infect Dis, abstr P1319."},{"key":"e_1_3_2_18_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0731-7085(98)00268-4"},{"key":"e_1_3_2_19_2","doi-asserted-by":"publisher","DOI":"10.1124\/dmd.107.015735"},{"key":"e_1_3_2_20_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00020-07"},{"key":"e_1_3_2_21_2","volume-title":"Abstr 52nd Intersci Conf Antimicrob Agents Chemother","author":"Lawrence L","year":"2012","unstructured":"Lawrence L LongcorJ LiD ReeveM HooverR McEwenAB FordG WoodSG. 2012. Metabolism and mass balance of [14C]-delafloxacin in healthy human volunteers following intravenous administration. Abstr 52nd Intersci Conf Antimicrob Agents Chemother, abstr A-1956."},{"key":"e_1_3_2_22_2","volume-title":"Abstr 50th Intersci Conf Antimicrob Agents Chemother","author":"Pereira DE","year":"2010","unstructured":"Pereira DE DegenhardtT FernandesP. 2010. Comparison of CEM-101 metabolism in mice, rats, monkeys and humans. 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