Pharmacokinetic study of lascufloxacin in non-elderly healthy men and elderly men

We conducted this phase I clinical study to examine the pharmacokinetic profiles and safety of lascufloxacin (LSFX), a novel quinolone antibacterial agent, in non-elderly Japanese healthy men and the effects of aging on LSFX pharmacokinetics in elderly Japanese healthy men. 1. After single-dose oral...

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Bibliographic Details
Published in:Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy 2020-03, Vol.26 (3), p.231-239
Main Authors: Totsuka, Kyoichi, Sesoko, Shogo, Fukase, Hiroyuki, Ikushima, Ippei, Odajima, Masaaki, Niwayama, Yutaka
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Aged
Elderly
Fasting
Fluoroquinolones - adverse effects
Fluoroquinolones - blood
Fluoroquinolones - pharmacokinetics
Food effect
Healthy Volunteers
Humans
Japan
Lascufloxacin
Male
Pharmacokinetics
Phase I
Young Adult
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Summary:We conducted this phase I clinical study to examine the pharmacokinetic profiles and safety of lascufloxacin (LSFX), a novel quinolone antibacterial agent, in non-elderly Japanese healthy men and the effects of aging on LSFX pharmacokinetics in elderly Japanese healthy men. 1. After single-dose oral administration of LSFX 100–800 mg (capsules) to six healthy adults in fasting state, the Cmax and AUClast roughly increased in proportion to the doses. 2. After multiple-dose oral administration of LSFX 75 mg (tablets) once daily for 7 days to six healthy adults, plasma LSFX reached the steady state by Day 7. The cumulative factor of LSFX on Day 7 to Day 1 was 1.65 for the Cmax and 1.96 for the AUCtau. 3. Regarding pharmacokinetic parameters of plasma LSFX after single-dose administration of LSFX 75 mg tablets (final product) to 24 healthy adults in fed state, the Cmax was somewhat higher, 1.28 times more than that in fasting state, whereas no changes were found in the AUClast. We therefore proposed that food effects of LSFX on absorption were negligible. 4. No clinically significant safety problems of LSFX were found in a series of studies involving healthy adults conducted this time. 5. After single-dose oral administration of LSFX 200 mg (capsules) to six elderly people in fasting state, its pharmacokinetic parameters were similar to those in non-elderly people, with no significant safety concerns. Therefore, adjustment of dosage and administration was considered to be unnecessary for LSFX administration to elderly individuals.
ISSN:1341-321X
1437-7780
DOI:10.1016/j.jiac.2019.09.010