Table 5.

Plasma and epithelial lining fluid concentrations of fluoroquinolones

Antibacterial agent	Dosage regimen	Subjects [n]	Sampling time [h]a	ELF to plasma based on AUC	Plasma concentration [µg/mL]b	ELF concentration [µg/mL]b	References
Alalevonadifloxacinc	1000 mg PO q12h × 9 doses	6	2	1.15d	20.5 ± 6.3	26.0 ± 15.9	[74]
		6	4		17.6 ± 6.1	19.7 ± 7.2
		6	6		16.4 ± 4.7	19.9 ± 11.1
		6	8		9.49 ± 4.25	10.6 ± 6.0
		6	12		4.88 ± 1.09	4.28 ± 1.40
Sitafloxacin	200 mg PO × 1 dose	12	0.5–2	0.85e	0.60 ± 0.46	0.19 ± 0.20	[76]
		12	3-4		1.37 ± 0.51	0.48 ± 0.29
		12	5-6		1.99 ± 2.34	1.07 ± 0.93
		12	7-9		0.85 ± 0.77	0.61 ± 0.77
JNJ-Q2	250 mg PO q12h × 7 doses	2	1	NR	0.65 (26.7)f	39.8 (35.4, 44.2)	[77]
		2	2		0.78 (20.2)f	34.5 (31.8, 37.2)
		2	4		0.71 (11.3)f	11.4 (10.5, 12.3)
		2	6		0.64 (8.9)f	35.0 (34.9, 35.1)
Lascufloxacin	75 mg PO × 1 dose	6	1	61.7g	0.576 ± 0.145	12.3 ± 3.74	[79]
		6	2		0.501 ± 0.0876	9.22 ± 3.45
		6	4		0.443 ± 0.0419	7.15 ± 3.21
		6	6		0.387 ± 0.0119	5.84 ± 1.72
		6	24		0.176 ± 0.0545	2.65 ± 0.88

ELF epithelial lining fluid, AUC area under the concentration-time curve, PO by mouth, NR not reported, qxh every x hours, SD standard deviation

^aSampling time after the last dose

^bTotal plasma and ELF concentrations expressed as mean ± SD or median (minimum, maximum)

^cMeasured concentrations are levonadifloxacin, the active drug from the alalevonadifloxacin prodrug

^dBased on the ratio of AUC₁₂ in ELF to AUC₁₂ in total plasma

^eBased on the ratio of AUC₈ in ELF to AUC₈ in unbound plasma, assuming 63% protein binding in plasma

^fValues expressed as mean (percent coefficient of variation), assuming 65% protein binding in plasma

^gBased on the ratio of AUC₂₄ in ELF to AUC₂₄ in unbound plasma, assuming 74% protein binding in plasma