PMID- 35574691
OWN - NLM
STAT- MEDLINE
DCOM- 20220713
LR  - 20220720
IS  - 1744-7658 (Electronic)
IS  - 1354-3784 (Linking)
VI  - 31
IP  - 7
DP  - 2022 Jul
TI  - Pharmacokinetics, safety, and tolerability of TQC3564, a novel CRTh2 receptor 
      antagonist: report of the first-in-human single- and multiple-dose escalation 
      trials in healthy Chinese subjects.
PG  - 729-736
LID - 10.1080/13543784.2022.2078192 [doi]
AB  - BACKGROUND: This is the first-in-human study to evaluate the pharmacokinetics, 
      safety, and tolerability of TQC3564 (a novel CRTh2 receptor antagonist) in 
      healthy Chinese subjects. RESEARCH DESIGN AND METHODS: This project was a phase 
      Ia clinical study of TQC3564 as a single-ascending dose (SAD) (25 to 1200 mg) and 
      a multiple-ascending dose (MAD) (100 or 500 mg, QD) as well as a two-period 
      crossover food-effect study (300 mg). RESULTS:     In the SAD and MAD study, 
      TQC3564 were found to be safe and well tolerated, without dose-dependent adverse 
      events (AEs), and all AEs were mild or moderate in severity. In the SAD study, 
      the median t(max) of TQC3564 was 2.5-4.5 h, and t(1/2) was 8.13-35.7 h. Exposure 
      was increased after food intake. The MAD study results showed that steady-state 
      was achieved on day 4. Moreover, no apparent TQC3564 plasma accumulation was 
      detected on day 7. CONCLUSIONS: In healthy subjects, TQC3564 at a single dose of 
      25-1200 mg or 100-500 mg at multiple doses (QD) was safe and tolerable with 
      acceptable PK profiles, indicating that TQC3564 has potential as a therapeutic 
      option for asthma. (This study has been registered at 
      http://www.chinadrugtrials.org.cn/ under identifier CTR20192397.).
FAU - Li, Xiaojiao
AU  - Li X
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Li, Qianqian
AU  - Li Q
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Ji, Tianliang
AU  - Ji T
AD  - Cardiovascular Department, First Hospital, Jilin University, Jilin, China.
FAU - Zhang, Hong
AU  - Zhang H
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Liu, Jingrui
AU  - Liu J
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Wu, Min
AU  - Wu M
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Chen, Hong
AU  - Chen H
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Lou, Jinfeng
AU  - Lou J
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Liu, Chengjiao
AU  - Liu C
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
FAU - Xu, Zhongnan
AU  - Xu Z
AD  - Chia Tai Tianqing Pharmaceutical Group Co. Ltd, Nanjing, Jiangsu, China.
FAU - Ding, Yanhua
AU  - Ding Y
AD  - Clinical Trial Unit, First Hospital, Jilin UniversityPhase I , Changchun, Jilin, 
      China.
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
DEP - 20220518
PL  - England
TA  - Expert Opin Investig Drugs
JT  - Expert opinion on investigational drugs
JID - 9434197
RN  - 0 (Anti-Asthmatic Agents)
RN  - 0 (Receptors, Immunologic)
SB  - IM
MH  - Administration, Oral
MH  - *Anti-Asthmatic Agents/adverse effects/pharmacokinetics
MH  - Area Under Curve
MH  - China
MH  - Cross-Over Studies
MH  - Dose-Response Relationship, Drug
MH  - Double-Blind Method
MH  - *Healthy Volunteers
MH  - Humans
MH  - Receptors, Immunologic
OTO - NOTNLM
OT  - CRTh2 receptor antagonist
OT  - TQC3564
OT  - asthma
OT  - pharmacokinetics
OT  - safety
EDAT- 2022/05/17 06:00
MHDA- 2022/07/14 06:00
CRDT- 2022/05/16 05:24
PHST- 2022/05/17 06:00 [pubmed]
PHST- 2022/07/14 06:00 [medline]
PHST- 2022/05/16 05:24 [entrez]
AID - 10.1080/13543784.2022.2078192 [doi]
PST - ppublish
SO  - Expert Opin Investig Drugs. 2022 Jul;31(7):729-736. doi: 
      10.1080/13543784.2022.2078192. Epub 2022 May 18.