Table 3.
Mean (standard deviation) PK parameters of nemonoxacin after oral single-dose administration
| Dose (mg) | Cmax (mg/L) | Tmax (h) | AUC72 (mg · h/L) | AUC0–∞ (mg · h/L) | T1/2 (h) | CLT (L/h/kg) | CLR (L/h/kg) | Vd (L/kg) | Ae(72h) (%) |
|---|---|---|---|---|---|---|---|---|---|
| Guo et al23,a | |||||||||
| 250 (n=12) | 3.24 | 1.04 | 21.40 | 21.52 | 10.73 | 0.20 | 0.14 | 3.08 | 70.28 |
| (0.67) | (0.69) | (3.35) | (3.36) | (2.71) | (0.035) | (0.034) | (1.09) | (7.55) | |
| 500 (n=11) | 5.91 | 1.14 | 42.17 | 42.41 | 12.83 | 0.20 | 0.14 | 3.81 | 69.12 |
| (1.35) | (0.64) | (5.84) | (5.83) | (3.72) | (0.033) | (0.037) | (1.43) | (10.80) | |
| 750 (n=12) | 8.20 | 1.64 | 64.75 | 65.04 | 10.92 | 0.19 | 0.13 | 3.00 | 66.00 |
| (1.37) | (0.60) | (6.24) | (6.23) | (3.78) | (0.033) | (0.027) | (1.02) | (8.66) | |
| 500 after meal (n=11) | 3.90 | 3.64 | 34.24 | 34.53 | 14.99 | 0.25 | 0.14 | 5.35 | 54.25 |
| (0.87) | (1.12) | (4.60) | (4.58) | (4.96) | (0.045) | (0.030) | (2.00) | (4.58) | |
| Lin et al21,b | |||||||||
| 250 (n=8) | 2.40 | 0.92 | 15.45 | 10.86 | 0.24 | 0.11 | 3.58 | 44.85 | |
| (0.66) | (0.20) | (3.94) | (3.91) | (0.056) | (0.055) | (0.89) | (17.48) | ||
| 500 (n=8) | 3.41 | 2.0 | 32.36 | 14.75 | 0.20 | 0.068 | 4.25 | 34.15 | |
| (0.58) | (0.87) | (3.01) | (3.06) | (0.024) | (0.021) | (1.31) | (9.05) | ||
| 1,000 (n=8) | 7.22 | 1.67 | 63.31 | 16.41 | 0.22 | 0.084 | 5.28 | 36.54 | |
| (0.88) | (0.26) | (10.01) | (2.54) | (0.025) | (0.031) | (0.78) | (12.03) | ||
Notes: Copyright © 2010. Amended with permission from American Society for Microbiology. Lin L, Chang LW, Tsai CY, et al. Dose Escalation Study of the Safety, Tolerability, and Pharmacokinetics of Nemonoxacin (TG-873870), a Novel Potent Broad-Spectrum Nonfluorinated Quinolone, in Healthy Volunteers. Antimicrob Agents Chemother. 2010;54(1):405–410. doi: 10.1128/AAC.00682-09.21 Copyright © 2012. Adapted with kind permission from Springer Science and Business Media. Guo B, Wu X, Zhang Y, et al. Safety and clinical pharmacokinetics of nemonoxacin, a novel non-fluorinated quinolone, in healthy Chinese volunteers following single and multiple oral doses. Clin Drug Investig. 2012;32(7):475–486.23
Chinese population
multiracial group including Hispanic (71%), African American (13%), and Caucasian (9%).
Abbreviations: PK, pharmacokinetics; Cmax, maximum concentration; Tmax, time that Cmax occurs; AUC, area under concentration–time curve; T½, elimination half-life; CLT, total clearance; CLR, renal clearance; Vd, apparent volume of distribution; Ae(72h), percentage of the administered dose recovered in urine over 72 hours.