Clinical Pharmacokinetics and Pharmacodynamics of Delafloxacin.

作者: Jennifer Shiu , Grace Ting , Tony KL Kiang

DOI: 10.1007/S13318-018-0520-8

关键词: Staphylococcus aureusPharmacokineticsPharmacologyChronic bronchitisSide effectDelafloxacinClinical pharmacologyExacerbationMedicineIn vivo

摘要: Delafloxacin has recently received approval by the US Food and Drug Administration for treatment of acute bacterial skin structure infections. This article provides a balanced comprehensive systematic critique literature in order to provide an up-to-date summary its clinical pharmacology. Oral delafloxacin is rapidly absorbed exhibits comparable exposure characteristics (300 mg intravenous versus 450 mg oral) between two formulations, allowing easy transition from oral therapy. The bioavailability high (60–70%) absorption not affected food intake, although further studies are required under clinically relevant conditions. primarily excreted renally (thus requiring renal dose adjustment setting dysfunction), but also undergoes metabolism uridine diphosphate-glucuronosyltransferase enzymes formation conjugated metabolite. Few drug-drug interaction have been identified, more characterizations vitro vivo warranted. concentration-dependent bactericidal agent that susceptibility gram-positive (notably potent activity against methicillin-resistant Staphylococcus aureus), gram-negative, anaerobic organisms. In addition infections, utility studied community-acquired pneumonia, exacerbation chronic bronchitis, gonorrhea, with potentially promising findings. Given mild side effect profile, including apparent lack association important QTc prolongation, generally well tolerated.

参考文章(37)
Wafi Siala, Marie-Paule Mingeot-Leclercq, Paul M. Tulkens, Marie Hallin, Olivier Denis, Françoise Van Bambeke, Comparison of the Antibiotic Activities of Daptomycin, Vancomycin, and the Investigational Fluoroquinolone Delafloxacin against Biofilms from Staphylococcus aureus Clinical Isolates Antimicrobial Agents and Chemotherapy. ,vol. 58, pp. 6385- 6397 ,(2014) , 10.1128/AAC.03482-14
Shana M. Gunderson, Robert A. Hayes, John P. Quinn, Larry H. Danziger, In Vitro Pharmacodynamic Activities of ABT-492, a Novel Quinolone, Compared to Those of Levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis Antimicrobial Agents and Chemotherapy. ,vol. 48, pp. 203- 208 ,(2004) , 10.1128/AAC.48.1.203-208.2004
Stephen H Zinner, Sergey N Vostrov, Irene V Alferova, Irene Yu Lubenko, Yury A Portnoy, Alexander A Firsov, Comparative pharmacodynamics of the new fluoroquinolone ABT492 and ciprofloxacin with Escherichia coli and Pseudomonas aeruginosa in an in vitro dynamic model. International Journal of Antimicrobial Agents. ,vol. 24, pp. 173- 177 ,(2004) , 10.1016/J.IJANTIMICAG.2004.02.026
Alexander A. Firsov, Irene V. Alferova, Maria V. Smirnova, Irene Yu. Lubenko, Yury A. Portnoy, Stephen H. Zinner, Comparative pharmacodynamics of the new fluoroquinolone ABT492 and levofloxacin with Streptococcus pneumoniae in an in vitro dynamic model. International Journal of Antimicrobial Agents. ,vol. 25, pp. 409- 413 ,(2005) , 10.1016/J.IJANTIMICAG.2005.02.004
William O’Riordan, Purvi Mehra, Paul Manos, Jeff Kingsley, Laura Lawrence, Sue Cammarata, A randomized phase 2 study comparing two doses of delafloxacin with tigecycline in adults with complicated skin and skin-structure infections International Journal of Infectious Diseases. ,vol. 30, pp. 67- 73 ,(2015) , 10.1016/J.IJID.2014.10.009
S. J. Harnett, Comparative study of the in vitro activity of a new fluoroquinolone, ABT-492 Journal of Antimicrobial Chemotherapy. ,vol. 53, pp. 783- 792 ,(2004) , 10.1093/JAC/DKH180
Margaret R Hammerschlag, Patricia M Roblin, The in vitro activity of a new fluoroquinolone, ABT-492, against recent clinical isolates of Chlamydia pneumoniae Journal of Antimicrobial Chemotherapy. ,vol. 54, pp. 281- 282 ,(2004) , 10.1093/JAC/DKH304
Laurel S. Almer, Jennifer B. Hoffrage, Erika L. Keller, Robert K. Flamm, Virginia D. Shortridge, In Vitro and Bactericidal Activities of ABT-492, a Novel Fluoroquinolone, against Gram-Positive and Gram-Negative Organisms Antimicrobial Agents and Chemotherapy. ,vol. 48, pp. 2771- 2777 ,(2004) , 10.1128/AAC.48.7.2771-2777.2004