PMID- 33440080
OWN - NLM
STAT- MEDLINE
DCOM- 20220127
LR  - 20221207
IS  - 2160-7648 (Electronic)
IS  - 2160-763X (Linking)
VI  - 10
IP  - 6
DP  - 2021 Jun
TI  - Safety, Pharmacokinetics, and Pharmacodynamics of a Dipeptidyl Peptidase-4 
      Inhibitor: A Randomized, Double-Blinded, Placebo-Controlled Daily Administration 
      of Fotagliptin Benzoate for 14 Days for Type 2 Diabetes Mellitus.
PG  - 660-668
LID - 10.1002/cpdd.895 [doi]
AB  - This study investigated the pharmacokinetics, pharmacodynamics, and safety of 
      fotagliptin benzoate (fotagliptin), a dipeptidyl peptidase-4 (DPP-4) inhibitor, 
      in Chinese patients with type 2 diabetes mellitus (T2DM). In a randomized, 
      double-blinded, placebo-controlled study, 10 and 4 patients with T2DM were 
      randomized and received, respectively, once-daily oral fotagliptin (24 mg) or 
      placebo, for 14 days. The pharmacokinetics and pharmacodynamics were assessed 
      throughout the study, including monitoring DPP-4, glucagon-like peptide-1 
      (GLP-1), glycosylated hemoglobin, and fasting blood glucose. Fotagliptin was 
      rapidly absorbed, and the median time to maximum concentration value was  approximately 1.5 
      hours. Plasma fotagliptin levels were stable after 14 days of once-daily dosage. 
      The accumulation ratios for the area under the plasma concentration-time curve of 
      fotagliptin, M1, and M2-1, were 1.19 +/- 0.10, 1.59 +/- 0.27, and 1.39 +/- 0.26, 
      respectively. The durations for DPP-4 inhibition >80% in the fotagliptin group on 
      days 1 and 14 were 23.5 and 24.0 hours, respectively. The concentrations of GLP-1 
      were higher on days 1 and 14 than at the baseline. No serious complications 
      occurred. Fotagliptin showed favorable pharmacokinetics and pharmacodynamics and 
      was well tolerated. Treatment with fotagliptin can achieve high DPP-4 inhibition 
      and increase plasma GLP-1. A once-per-day dosing regimen may be recommended as 
      clinically efficacious.
CI  - (c) 2021, The American College of Clinical Pharmacology.
FAU - Wu, Min
AU  - Wu M
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
FAU - Li, Qian-Qian
AU  - Li QQ
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
FAU - Zhang, Hong
AU  - Zhang H
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
FAU - Zhu, Xiao-Xue
AU  - Zhu XX
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
FAU - Li, Xiao-Jiao
AU  - Li XJ
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
FAU - Li, Ying
AU  - Li Y
AD  - Shenzhen Salubris Pharmaceuticals Co., Ltd. Shenzhen, Guangdong, China.
FAU - Sun, Hai-Gang
AU  - Sun HG
AD  - Shenzhen Salubris Pharmaceuticals Co., Ltd. Shenzhen, Guangdong, China.
FAU - Ding, Yan-Hua
AU  - Ding YH
AD  - Department of Phase I Clinical Trial Unit, First Hospital of Jilin University, 
      Changchun, Jilin, China.
LA  - eng
GR  - 2017ZX09101001-002-004/National Major Scientific and Technological Special 
      Project for Significant New Drug Development/
GR  - 2017ZX09304004/National Major Scientific and Technological Special Project for 
      Significant New Drug Development/
GR  - 81602897/National Natural Science Foundation of China/
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20210113
PL  - United States
TA  - Clin Pharmacol Drug Dev
JT  - Clinical pharmacology in drug development
JID - 101572899
RN  - 0 (Blood Glucose)
RN  - 0 (Dipeptidyl-Peptidase IV Inhibitors)
RN  - 0 (Glycated Hemoglobin A)
RN  - 0 (Piperidines)
RN  - 0 (Triazines)
RN  - 0 (fotagliptin)
RN  - 89750-14-1 (Glucagon-Like Peptide 1)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Area Under Curve
MH  - Blood Glucose/drug effects
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Dipeptidyl-Peptidase IV Inhibitors/*administration & dosage/adverse 
      effects/pharmacokinetics
MH  - Double-Blind Method
MH  - Female
MH  - Glucagon-Like Peptide 1/blood
MH  - Glycated Hemoglobin/metabolism
MH  - Humans
MH  - Male
MH  - Middle Aged
MH  - Piperidines/*administration & dosage/adverse effects/pharmacokinetics
MH  - Triazines/*administration & dosage/adverse effects/pharmacokinetics
OTO - NOTNLM
OT  - fotagliptin benzoate, pharmacodynamics, pharmacokinetics, safety
OT  - type 2 diabetes mellitus
EDAT- 2021/01/14 06:00
MHDA- 2022/01/28 06:00
CRDT- 2021/01/13 17:11
PHST- 2020/07/30 00:00 [received]
PHST- 2020/11/23 00:00 [accepted]
PHST- 2021/01/14 06:00 [pubmed]
PHST- 2022/01/28 06:00 [medline]
PHST- 2021/01/13 17:11 [entrez]
AID - 10.1002/cpdd.895 [doi]
PST - ppublish
SO  - Clin Pharmacol Drug Dev. 2021 Jun;10(6):660-668. doi: 10.1002/cpdd.895. Epub 2021 
      Jan 13.