PMID- 37980573
OWN - NLM
STAT- MEDLINE
DCOM- 20231127
LR  - 20240222
IS  - 1365-2060 (Electronic)
IS  - 0785-3890 (Print)
IS  - 0785-3890 (Linking)
VI  - 55
IP  - 2
DP  - 2023
TI  - Safety, tolerability and pharmacokinetics of forsythin in healthy subjects: a 
      double-blinded, placebo-controlled single-dose and multiple-dose escalation and 
      food effect study.
PG  - 2274512
LID - 10.1080/07853890.2023.2274512 [doi]
LID - 2274512
AB  - BACKGROUND: Forsythin, an active compound from Forsythiae Fructus, has the 
      potential to treat the common cold and influenza through its 
      antipyretic-analgesic, anti-inflammatory and antiviral effects. The safety, 
      tolerability and pharmacokinetic (PK) profile of forsythin were evaluated in 
      healthy Chinese subjects. METHODS: This phase 1a study included three parts: 
      double-blind, randomized, placebo-controlled single-ascending-dose (SAD) (50, 
      100, 200, 400, 600 or 800 mg), food effect investigation (100 mg) and 
      multiple-ascending-dose (MAD) (50, 100 or 200 mg TID for 5 days). RESULTS: 
      Forsythin is safe and tolerable in healthy Chinese subjects. The rates of adverse 
      events (AEs) in the forsythin cohort were similar to those in the placebo cohort. 
      Forsythin is well-absorbed after single or multiple doses and is extensively 
      metabolized. The primary metabolites were aglycone M1, M1 sulphate (M2) and M1 
      glucuronide (M7). Exposure to forsythin (100 mg) was higher after food intake by 
      approximately 1.4-fold, whereas M2 and M7 did not change. The steady state was 
      reached around three days in the MAD study. Forsythin, M2 and M7 accumulation on 
      day 5 was 1, 3 and 2, respectively. CONCLUSIONS: The safety and PK profiles of 
      forsythin support further evaluation of its efficacy in individuals with the 
      common cold or influenza.
FAU - Li, Cuiyun
AU  - Li C
AD  - Phase I Clinical Trial Unit, First Hospital, Jilin University, Changchun, China.
FAU - Wu, Min
AU  - Wu M
AD  - Phase I Clinical Trial Unit, First Hospital, Jilin University, Changchun, China.
FAU - Zhang, Hong
AU  - Zhang H
AD  - Phase I Clinical Trial Unit, First Hospital, Jilin University, Changchun, China.
FAU - Zhu, Xiaoxue
AU  - Zhu X
AD  - Phase I Clinical Trial Unit, First Hospital, Jilin University, Changchun, China.
FAU - Fu, Li
AU  - Fu L
AD  - Dalian Fusheng Institute of Natural Medicine, Dalian, China.
FAU - Wang, Shuo
AU  - Wang S
AD  - Dalian Fusheng Institute of Natural Medicine, Dalian, China.
FAU - Lu, Mingming
AU  - Lu M
AD  - Dalian Fusheng Institute of Natural Medicine, Dalian, China.
FAU - Zhong, Dafang
AU  - Zhong D
AD  - State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, 
      Chinese Academy of Sciences, Shanghai, China.
FAU - Ding, Yanhua
AU  - Ding Y
AD  - Phase I Clinical Trial Unit, First Hospital, Jilin University, Changchun, China.
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20231119
PL  - England
TA  - Ann Med
JT  - Annals of medicine
JID - 8906388
RN  - VE9P4964MG (phillyrin)
SB  - IM
MH  - Humans
MH  - Healthy Volunteers
MH  - *Common Cold/drug therapy
MH  - *Influenza, Human
MH  - Area Under Curve
MH  - Double-Blind Method
MH  - Dose-Response Relationship, Drug
PMC - PMC10836277
OTO - NOTNLM
OT  - Forsythin
OT  - food effect
OT  - pharmacokinetics
OT  - safety
OT  - tolerability
COIS- The authors declare no competing interests.
EDAT- 2023/11/19 18:41
MHDA- 2023/11/27 12:42
PMCR- 2023/11/19
CRDT- 2023/11/19 15:14
PHST- 2023/11/27 12:42 [medline]
PHST- 2023/11/19 18:41 [pubmed]
PHST- 2023/11/19 15:14 [entrez]
PHST- 2023/11/19 00:00 [pmc-release]
AID - 2274512 [pii]
AID - 10.1080/07853890.2023.2274512 [doi]
PST - ppublish
SO  - Ann Med. 2023;55(2):2274512. doi: 10.1080/07853890.2023.2274512. Epub 2023 Nov 
      19.