PMID- 26692004
OWN - NLM
STAT- MEDLINE
DCOM- 20160927
LR  - 20221207
IS  - 1179-1918 (Electronic)
IS  - 1173-2563 (Linking)
VI  - 36
IP  - 3
DP  - 2016 Mar
TI  - Pharmacokinetics and Pharmacodynamics of Henagliflozin, a Sodium Glucose 
      Co-Transporter 2 Inhibitor, in Chinese Patients with Type 2 Diabetes Mellitus.
PG  - 195-202
LID - 10.1007/s40261-015-0366-7 [doi]
AB  - BACKGROUND AND OBJECTIVE: Henagliflozin, a selective inhibitor of the renal 
      sodium glucose cotransporter-2, was developed for type 2 diabetes mellitus 
      (T2DM). This study characterized single- and multiple-dose pharmacokinetics and 
      pharmacodynamics of henagliflozin in Chinese patients with T2DM. METHODS: Thirty 
      T2DM patients were randomized in a 4:1 ratio to orally receive either 
      henagliflozin 5, 10, 20 mg/day or placebo for 10 days, except on day 2 and day 3. 
      Pharmacokinetic and pharmacodynamic profiles were measured on day 1 and day 10. 
      RESULTS: Henagliflozin exhibited dose-proportional plasma concentrations with a 
      half-life ranging from 9.1 to 14 h. Steady-state plasma henagliflozin 
      concentration was reached by day 7 in all active treatment groups. Henagliflozin 
      decreased the 24-h mean plasma glucose by -0.3, -1.0 and -1.0 mmol/L with doses 
      of 5, 10 and 20 mg on day 1, respectively. The corresponding values on day 10 
      were -0.8, -0.9 and -1.2 mmol/L. Twenty-four-hour urinary glucose excretion 
      increased by 11, 65 and 82 times with doses of 5, 10 and 20 mg on day 1, 
      respectively, with a similar trend on day 10. No treatment-related serious 
      adverse events or discontinuations due to adverse events occurred. CONCLUSIONS: 
      The observed pharmacokinetic and pharmacodynamic profiles of henagliflozin 
      support a once-daily dosing regimen in Chinese T2DM patients.
FAU - Yong, Xiaolan
AU  - Yong X
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Wen, Aidong
AU  - Wen A
AD  - Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, 
      Xi'an, Shanxi, China.
FAU - Liu, Xiangyang
AU  - Liu X
AD  - Department of Endocrine and Metabolism, Xijing Hospital, Fourth Military Medical 
      University, Xi'an, Shanxi, China.
FAU - Liu, Haiyan
AU  - Liu H
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China.
FAU - Liu, Yan-Ping
AU  - Liu YP
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China.
FAU - Li, Nan
AU  - Li N
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Hu, Tingting
AU  - Hu T
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Chen, Ying
AU  - Chen Y
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China.
FAU - Wang, Minquan
AU  - Wang M
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China.
FAU - Wang, Lantian
AU  - Wang L
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Dai, Xiaojiao
AU  - Dai X
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Huang, Juan
AU  - Huang J
AD  - Clinical Pharmacy Lab, General Hospital of Chengdu Military Region PLA, Chengdu, 
      Sichuan, China.
FAU - Li, Jia
AU  - Li J
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China.
FAU - Shen, Huaqiong
AU  - Shen H
AD  - Department of Clinical Medicine, Jiangsu Hengrui Medicine Co., Ltd., Shanghai, 
      200122, China. maoweitaoliu@126.com.
LA  - eng
PT  - Journal Article
PT  - Multicenter Study
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - New Zealand
TA  - Clin Drug Investig
JT  - Clinical drug investigation
JID - 9504817
RN  - 0 (Bridged Bicyclo Compounds, Heterocyclic)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (SLC5A2 protein, human)
RN  - 0 (Sodium-Glucose Transporter 2)
RN  - 0 (Sodium-Glucose Transporter 2 Inhibitors)
RN  - 21P2M98388 (henagliflozin)
RN  - IY9XDZ35W2 (Glucose)
SB  - IM
MH  - Adult
MH  - Asian People
MH  - Bridged Bicyclo Compounds, Heterocyclic/*administration & dosage/pharmacokinetics
MH  - Diabetes Mellitus, Type 2/*drug therapy
MH  - Dose-Response Relationship, Drug
MH  - Double-Blind Method
MH  - Female
MH  - Glucose/metabolism
MH  - Half-Life
MH  - Humans
MH  - Hypoglycemic Agents/*administration & dosage/pharmacokinetics
MH  - Male
MH  - Middle Aged
MH  - Sodium-Glucose Transporter 2
MH  - *Sodium-Glucose Transporter 2 Inhibitors
EDAT- 2015/12/23 06:00
MHDA- 2016/09/28 06:00
CRDT- 2015/12/23 06:00
PHST- 2015/12/23 06:00 [entrez]
PHST- 2015/12/23 06:00 [pubmed]
PHST- 2016/09/28 06:00 [medline]
AID - 10.1007/s40261-015-0366-7 [pii]
AID - 10.1007/s40261-015-0366-7 [doi]
PST - ppublish
SO  - Clin Drug Investig. 2016 Mar;36(3):195-202. doi: 10.1007/s40261-015-0366-7.