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Antimicrobial Agents and Chemotherapy, March 2002, p. 917-921, Vol. 46, No. 3
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.3.917-921.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Intrapulmonary Pharmacokinetics of Telithromycin, a New Ketolide, in Healthy Japanese Volunteers

Jun-Ichi Kadota,^1* Yuji Ishimatsu,¹ Tetsuji Iwashita,¹ Yuichi Matsubara,¹ Kazunori Tomono,¹ Masao Tateno,² Roza Ishihara,³ Claudette Muller-Serieys,⁴ and Shigeru Kohno¹

Second Department of Internal Medicine, Nagasaki University School of Medicine, Nagasaki 852-8501,¹ Clinical Pharmacology Center, Niizashiki Central General Hospital, Saitama,² Aventis Pharma Ltd., Tokyo, Japan,³ Unité de microbiologie, Hôpital Bichat-Claude Bernard, 46 rue Henri Huchard, 75877 Paris, France⁴

Received 7 March 2001/ Returned for modification 18 August 2001/ Accepted 15 November 2001

The concentrations of telithromycin, a new ketolide antimicrobial agent, in alveolar macrophages (AMs) and bronchoalveolar epithelial lining fluid (ELF) were determined in order to investigate the transfer of the drug into target tissue, relative to plasma, following multiple oral doses of telithromycin. Twenty-four healthy male Japanese volunteers were randomly allocated to four groups. Each subject was given 600 or 800 mg of telithromycin once daily for 5 days, followed by bronchoalveolar lavage (BAL) 2 or 8 h after the last dose (group A and B: 600 mg, 2 and 8 h BAL time point; group C and D: 800 mg, 2 and 8 h BAL time point). The mean concentrations of the drug in AMs and ELF were 34.54 and 4.92 mg/liter in group A, 50.97 and 2.26 mg/liter in group B, 25.47 and 4.24 mg/liter in group C, and 108.22 and 4.31 mg/liter in group D, respectively, which markedly exceeded concentrations in plasma. These results demonstrated good transfer of telithromycin into AMs and ELF, suggesting good efficacy against common respiratory pathogens, including intracellular pathogens and atypical microorganisms.

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* Corresponding author. Mailing address: Second Department of Internal Medicine, Oita Medical University, 1-1 Hasama, Oita 879-5593, Japan. Phone: 81(97) 586-5804. Fax: 81(97) 549-4245. E-mail: kadota{at}oita-med.ac.jp.

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Antimicrobial Agents and Chemotherapy, March 2002, p. 917-921, Vol. 46, No. 3
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.3.917-921.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

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