{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,21]],"date-time":"2026-09-21T08:55:36Z","timestamp":1789980936819,"version":"4.0.1"},"reference-count":24,"publisher":"American Society for Microbiology","issue":"4","license":[{"start":{"date-parts":[[2018,4,1]],"date-time":"2018-04-01T00:00:00Z","timestamp":1522540800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2018,4]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>\n                    This study was performed to investigate the intrapulmonary penetration of lascufloxacin in humans. Thirty healthy adult male Japanese subjects, allocated into five groups, received lascufloxacin in a single oral dose of 75 mg. Bronchoalveolar lavage and blood sampling were performed simultaneously in each subject at 1, 2, 4, 6, or 24 h after administration, and lascufloxacin concentrations in plasma, epithelial lining fluid, and alveolar macrophages were determined. Lascufloxacin was rapidly distributed to the epithelial lining fluid with a time to maximum drug concentration (\n                    <jats:italic>T<\/jats:italic>\n                    <jats:sub>max<\/jats:sub>\n                    ) of 1 h, which was identical to that in plasma. The maximum concentration of drug (\n                    <jats:italic>C<\/jats:italic>\n                    <jats:sub>max<\/jats:sub>\n                    ) values in plasma, epithelial lining fluid, and alveolar macrophages were 0.576, 12.3, and 21.8 \u03bcg\/ml, respectively. The corresponding area under the concentration-time curve from 0 to 24 h (AUC\n                    <jats:sub>0\u201324<\/jats:sub>\n                    ) values were 7.67, 123, and 325 \u03bcg \u00b7 h\/ml. The mean drug concentrations in the epithelial lining fluid and alveolar macrophages were much higher than those in plasma at all time points examined, and the average site-to-free plasma concentration ratios fell within the ranges of 57.5 to 86.4 and 71.0 to 217, respectively. Drug levels in epithelial lining fluid and alveolar macrophages exceeded the MIC\n                    <jats:sub>90<\/jats:sub>\n                    values for common respiratory pathogens. (This study was registered at JAPIC under registration number JapicCTI-142547.)\n                  <\/jats:p>","DOI":"10.1128\/aac.02169-17","type":"journal-article","created":{"date-parts":[[2018,1,17]],"date-time":"2018-01-17T06:41:04Z","timestamp":1516171264000},"update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":22,"title":["Intrapulmonary Pharmacokinetics of Lascufloxacin in Healthy Adult Volunteers"],"prefix":"10.1128","volume":"62","author":[{"given":"Hidetoshi","family":"Furuie","sequence":"first","affiliation":[{"name":"Osaka Pharmacology Clinical Research Hospital, Osaka, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sayoko","family":"Tanioka","sequence":"additional","affiliation":[{"name":"Kyorin Pharmaceutical Co., Ltd., Tokyo, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Keiko","family":"Shimizu","sequence":"additional","affiliation":[{"name":"Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shigeru","family":"Manita","sequence":"additional","affiliation":[{"name":"Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Masaharu","family":"Nishimura","sequence":"additional","affiliation":[{"name":"Department of Respiratory Medicine, Faculty of Medicine (and Graduate School of Medicine), Hokkaido University, Sapporo, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hisao","family":"Yoshida","sequence":"additional","affiliation":[{"name":"Kyorin Pharmaceutical Co., Ltd., Tokyo, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00120-17"},{"key":"e_1_3_2_3_2","volume-title":"abstr SUNDAY-467","author":"Totsuka K","year":"2016","unstructured":"Totsuka K, Odajima M, Nakauchi M, Sesoko S, Nakashima M. 2016. Phase I study to determine the safety and pharmacokinetics (PK) of single and multiple oral doses of lascufloxacin (AM-1977) in healthy subjects, abstr SUNDAY-467. Abstr ASM Microbe, 16 to 20 June 2016, Boston, MA."},{"key":"e_1_3_2_4_2","volume-title":"abstr SUNDAY-471","author":"Kishii R","year":"2016","unstructured":"Kishii R, Yamamuro N, Yamaguchi Y, Abukawa H, Takei M. 2016. In vivo bactericidal activity of lascufloxacin (AM-1977), a newly developed fluoroquinolone, against mouse pulmonary infection model caused by Streptococcus pneumoniae, abstr SUNDAY-471. Abstr ASM Microbe, 16 to 20 June 2016, Boston, MA."},{"key":"e_1_3_2_5_2","volume-title":"abstr SUNDAY-470","author":"Totsuka K","year":"2016","unstructured":"Totsuka K, Odajima M, Nakauchi M, Sesoko S, Nakashima M. 2016. Phase I study to determine the safety and pharmacokinetics (PK) of single and multiple intravenous infusion of lascufloxacin (AM-1977) in healthy subjects, abstr SUNDAY-470. Abstr ASM Microbe, 16 to 20 June 2016, Boston, MA."},{"key":"e_1_3_2_6_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.36.6.1171"},{"key":"e_1_3_2_7_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00133-06"},{"key":"e_1_3_2_8_2","doi-asserted-by":"publisher","DOI":"10.2165\/11594090-000000000-00000"},{"key":"e_1_3_2_9_2","doi-asserted-by":"publisher","DOI":"10.1016\/S0954-6111(05)80262-8"},{"key":"e_1_3_2_10_2","doi-asserted-by":"publisher","DOI":"10.1183\/09031936.97.10051130"},{"key":"e_1_3_2_11_2","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/40.4.573"},{"key":"e_1_3_2_12_2","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/44.6.835"},{"key":"e_1_3_2_13_2","doi-asserted-by":"publisher","DOI":"10.1378\/chest.119.4.1114"},{"key":"e_1_3_2_14_2","doi-asserted-by":"publisher","DOI":"10.1093\/jac\/dkg110"},{"key":"e_1_3_2_15_2","doi-asserted-by":"publisher","DOI":"10.1378\/chest.125.3.965"},{"key":"e_1_3_2_16_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijantimicag.2006.03.022"},{"key":"e_1_3_2_17_2","doi-asserted-by":"publisher","DOI":"10.1152\/jappl.1986.60.2.532"},{"key":"e_1_3_2_18_2","first-page":"430","article-title":"Interactions between quinolone antibiotics and phospholipid membrane for prediction of alveolar macrophage uptake in vitro","volume":"23","author":"Sun J","year":"2002","unstructured":"Sun J, Deguchi Y, Chen JM, Zhang RH, Morimoto K. 2002. Interactions between quinolone antibiotics and phospholipid membrane for prediction of alveolar macrophage uptake in vitro. 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