PMID- 31588657
OWN - NLM
STAT- MEDLINE
DCOM- 20210402
LR  - 20221207
IS  - 1463-1326 (Electronic)
IS  - 1462-8902 (Linking)
VI  - 22
IP  - 2
DP  - 2020 Feb
TI  - Pharmacokinetics and pharmacodynamics of rongliflozin, a novel selective 
      inhibitor of sodium-glucose co-transporter-2, in people with type 2 diabetes 
      mellitus.
PG  - 191-202
LID - 10.1111/dom.13887 [doi]
AB  - AIMS: To evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) 
      characteristics of rongliflozin in a cohort of healthy Chinese people and people 
      with type 2 diabetes mellitus (T2DM). MATERIALS AND METHODS: We examined the 
      effects of a single ascending dose (SAD) of rongliflozin (10-200 mg) in 
      combination with food (20 mg) in 50 healthy people, and a multiple ascending dose 
      (MAD) of rongliflozin (10-50 mg once daily for 12 days) in 36 people with T2DM. 
      RESULTS: No serious adverse events (AEs) or discontinuations as a result of AEs 
      (related to rongliflozin) occurred in either study. In healthy participants and 
      those with T2DM, rongliflozin was rapidly absorbed, with a time to maximum plasma 
      concentration of 0.63 to 1.75 hours. Systemic exposure (maximum observed serum 
      concentration and area under the curve) to rongliflozin and its inactive major 
      metabolites (T1444, T1454 and T1830) increased in proportion to dose. In the SAD 
      and MAD studies, there was a dose-related increase in urinary glucose excretion 
      (UGE) ranging from 10 to 50 mg rongliflozin. This increase in UGE was associated 
      with dose-related decreases in serum glucose values in people with T2DM in the 
      MAD group. In the SAD group, UGE plateaued at 50 to 200 mg. CONCLUSIONS: 
      Rongliflozin was well tolerated in all participants. The PK and PD measurements 
      obtained for rongliflozin demonstrate a dose-response relationship when the drug 
      is administered at doses ranging from 10 to 50 mg in healthy people and in people 
      with T2DM.
CI  - (c) 2019 John Wiley & Sons Ltd.
FAU - Zhang, Hong
AU  - Zhang H
AUID- ORCID: 0000-0002-8546-8555
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Zhu, Xiaoxue
AU  - Zhu X
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Li, Xiaojiao
AU  - Li X
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Chen, Hong
AU  - Chen H
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Wu, Min
AU  - Wu M
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Li, Cuiyun
AU  - Li C
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Liu, Jingrui
AU  - Liu J
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Liu, Chengjiao
AU  - Liu C
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
FAU - Zhang, Yingjun
AU  - Zhang Y
AD  - State Key Laboratory of Anti-Infective Drug Development, HEC R&D Centre, Sunshine 
      Lake Pharma Co., Ltd, Dongguan, Guangzhou, China.
FAU - Ding, Yanhua
AU  - Ding Y
AD  - Phase I Clinical Research Centre, First Hospital of Jilin University, Jilin, 
      China.
LA  - eng
GR  - Project: 2017ZX09304004, 2017ZX09101001-002-004/National Major Scientific and 
      Technological Special Project for Significant New Drug Development during the 
      13th 5-Year Plan Period of China/International
GR  - 2018ZX09301007005/National Major Scientific and Technological Special Project for 
      Significant New Drug Development during the 13th 5-Year Plan Period of 
      China/International
GR  - Project: 81602897/National Natural Science Foundation of China/International
GR  - HEC R&D Centre, Sunshine Lake Pharma Co., Ltd./International
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20191105
PL  - England
TA  - Diabetes Obes Metab
JT  - Diabetes, obesity & metabolism
JID - 100883645
RN  - 0 (Blood Glucose)
RN  - 0 (Placebos)
RN  - 0 (Sodium-Glucose Transporter 2 Inhibitors)
RN  - 0 (rongliflozin)
RN  - 0SAC974Z85 (Canagliflozin)
SB  - IM
MH  - Adolescent
MH  - Adult
MH  - Asian People
MH  - Blood Glucose/drug effects/metabolism
MH  - Canagliflozin/administration & dosage/adverse effects/*analogs & 
      derivatives/pharmacokinetics
MH  - China
MH  - Diabetes Mellitus, Type 2/*drug therapy/*metabolism
MH  - Dose-Response Relationship, Drug
MH  - Double-Blind Method
MH  - Female
MH  - Glycosuria/metabolism/urine
MH  - Humans
MH  - Male
MH  - Maximum Tolerated Dose
MH  - Middle Aged
MH  - Placebos
MH  - Sodium-Glucose Transporter 2 Inhibitors/administration & dosage/adverse 
      effects/pharmacokinetics
MH  - Young Adult
OTO - NOTNLM
OT  - Chinese
OT  - SGLT2 inhibitor
OT  - clinical trial
OT  - pharmacodynamics
OT  - pharmacokinetics
OT  - type 2 diabetes
EDAT- 2019/10/08 06:00
MHDA- 2021/04/07 06:00
CRDT- 2019/10/08 06:00
PHST- 2019/08/06 00:00 [received]
PHST- 2019/09/18 00:00 [revised]
PHST- 2019/09/27 00:00 [accepted]
PHST- 2019/10/08 06:00 [pubmed]
PHST- 2021/04/07 06:00 [medline]
PHST- 2019/10/08 06:00 [entrez]
AID - 10.1111/dom.13887 [doi]
PST - ppublish
SO  - Diabetes Obes Metab. 2020 Feb;22(2):191-202. doi: 10.1111/dom.13887. Epub 2019 
      Nov 5.