Evidence map›Paper›PMID 32277364›Full record

Trial reportClinical drug investigation2020

Phase I, First-in-Human, Single and Multiple Ascending Dose- and Food-Effect Studies to Assess the Safety, Tolerability and Pharmacokinetics of a Novel Anti-hepatitis B Virus Drug, Bentysrepinine (Y101), in Healthy Chinese Subjects.

Xiaoxue Liu, Ling Xue, Hua Zhang, Qingqing Xu, Shichao Zhang, Sheng Ma, Xiaoliang Ding, Linsheng Liu, Ji Dong, Lifang Qian and 4 more

Abstract readClinical Trial, Phase IRandomized Controlled Trial
PubMed Publisher
In one paragraph

Trial report in Clinical drug investigation, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.7field-weighted citation impact, top 28% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 6 citations in OpenAlex.

  1. Article
  2. Article
  3. Frontiers in pharmacology · 2020
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors at 1 institution in 1 country.

Xiaoxue Liu *Department of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.ORCID http://orcid.org/0000-0003-1424-5853
Ling Xue *Department of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Hua Zhang *Department of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Qingqing XuDepartment of Pharmaceutics, College of Pharmaceutical Science, Soochow University, Suzhou, China.
Shichao ZhangDepartment of Pharmaceutics, College of Pharmaceutical Science, Soochow University, Suzhou, China.
Sheng MaDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Xiaoliang DingDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Linsheng LiuDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Ji DongDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Lifang QianDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China.
Wen XiaBailing Enterprise Group Pharmaceutical Co., Ltd., Guizhou, China.
Kun JiangBailing Enterprise Group Pharmaceutical Co., Ltd., Guizhou, China.
Chenrong HuangDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China. chrishuangcr@163.com.
Liyan MiaoDepartment of Clinical Pharmacology, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Street, Suzhou, 215006, China. miaoliyan@suda.edu.cn.
Soochow University · CN

Funding

Aosaikang Clinical Pharmacy Foundation A201723National Key New Drug Creation and Manufacturing Program, Ministry of Science and Technology (CN) 2017ZX09304-021the Ministry of Science and Technology of China No. 2015ZX09101012the Ministry of Science and Technology of China No. 2017ZX09304021the National Natural Science Foundation of China 81703619the Science and Technology Cooperation Major Project of Guizhou Province No. [2015]6002
6 · The paper itself

Abstract

BACKGROUND AND

objectiveBentysrepinine (Y101), a derivative of repensine (a compound isolated from Dichondra repens Forst), is a novel phenylalanine dipeptide currently under development for the treatment of hepatitis B virus (HBV). The objectives of these studies were to assess the safety, tolerability and pharmacokinetics of bentysrepinine in healthy Chinese subjects.

methodsTwo randomised, double-blind, placebo-controlled trials evaluated a single oral dose (50-900 mg, study 01) and multiple doses (300 mg and 600 mg, study 02), and a randomised, open, crossover food-effect study (600 mg, study 03) of bentysrepinine was established. Safety and tolerability were assessed by adverse event (AE) reporting, clinical laboratory tests, physical examinations, vital sign monitoring and electrocardiogram (ECG). Plasma, urine and faecal samples were analysed using validated liquid chromatography tandem mass spectrometry (LC-MS/MS) methods to investigate the pharmacokinetics of bentysrepinine.

resultsNinety-four subjects were enrolled, and bentysrepinine was well tolerated. Mild and reversible AEs occurred for single and multiple oral doses between 50 and 900 mg. The most common adverse effects were increased alanine aminotransferase (ALT) and aspartate transaminase (AST). Other clinically significant AEs included nausea and elevated urine leukocytes, urine red blood cells, transaminase, creatine kinase, total cholesterol, triglycerides, and low-density cholesterol. There were no clinically significant changes in the ECG, vital signs or laboratory assessments during the studies. The maximum tolerated dose (MTD) was not reached in the dose escalation study. Bentysrepinine was rapidly absorbed and metabolised with a mean time to reach maximum concentration (T

conclusionBentysrepinine exhibited acceptable safety and tolerability in healthy subjects in the dose range of 50-900 mg in both single- and multiple-dose studies. The drug did not exhibit linear pharmacokinetic characteristics. No accumulation was observed after the administration of multiple 300 and 600 mg doses. Bentysrepinine is extensively metabolised in the body. Food may increase its bioavailability. TRIALS REGISTRATION: CFDA registration numbers CTR20160096, CTR20160094, and CTR20140543 (www.chinadrugtrials.org.cn).

Indexed as

AdultAntiviral AgentsArea Under CurveAsian PeopleBenzamidesChromatography, LiquidCross-Over StudiesDipeptidesDouble-Blind MethodFemaleHealthy VolunteersHepatitis B virusHumansMalePlacebosTandem Mass SpectrometryAntiviral AgentsBenzamidesDipeptidesN-(N-benzoyl-O-(2-dimethylaminoethyl)tyrosyl)phenylalaninolPlacebos

Identifiers

PMID32277364
OpenAlexW3015473245

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.