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Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Doses of Empagliflozin, a Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitor, in Healthy Japanese Subjects.
MedLine Citation:
PMID:  23149871     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
This randomized, placebo-controlled within dose groups, double-blind, single rising dose study investigated the safety, tolerability, pharmacokinetics and pharmacodynamics of 1 mg to 100 mg doses of empagliflozin in 48 healthy Japanese male subjects. Empagliflozin was rapidly absorbed, reaching peak levels in 1.25 to 2.50 hours; thereafter, plasma concentrations declined in a biphasic fashion, with mean terminal elimination half-life ranging from 7.76 to 11.7 hours. Increase in empagliflozin exposure was proportional to dose. Oral clearance was dose independent and ranged from 140 to 172 mL/min. In the 24 hours following 100 mg empagliflozin administration, the mean (%CV) amount of glucose excreted in urine was 74.3 (17.1) g. The amount and the maximum rate of glucose excreted via urine increased with dose of empagliflozin. Nine adverse events, all of mild intensity, were reported by 8 subjects (7 with empagliflozin and 1 with placebo). No hypoglycemia was reported. In conclusion, 1 mg to 100 mg doses of empagliflozin had a good safety and tolerability profile in healthy Japanese male subjects. Exposure to empagliflozin was dose-proportional. The amount and rate of urinary glucose excretion were higher with empagliflozin than with placebo, and increased with empagliflozin dose.
Authors:
Akiko Sarashina; Kazuki Koiwai; Leo J Seman; Norio Yamamura; Atsushi Taniguchi; Takahiro Negishi; Shogo Sesoko; Hans J Woerle; Klaus A Dugi
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-13
Journal Detail:
Title:  Drug metabolism and pharmacokinetics     Volume:  -     ISSN:  1880-0920     ISO Abbreviation:  Drug Metab. Pharmacokinet.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-14     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101164773     Medline TA:  Drug Metab Pharmacokinet     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Nippon Boehringer Ingelheim Co., Ltd.
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