[Translation] A randomized, double-blind, placebo-controlled, multiple-dose tolerability and pharmacokinetic study of tifentai tablets in healthy volunteers

替芬泰片随机、双盲、安慰剂对照多次给药健康人体耐受性及药代动力学试验

[Translation]

A randomized, double-blind, placebo-controlled, multiple-dose tolerability and pharmacokinetic study of tifentai tablets in healthy volunteers

Start Date08 Apr 2016

Sponsor / Collaborator

Tianjin Institute of Pharmaceutical Research Co., Ltd.

[+3]

CTR20160094 / CompletedPhase 1

评价高脂高热饮食对健康志愿者单次口服替芬泰片药代动力学影响的随机、开放、双交叉试验

[Translation] A randomized, open-label, double-crossover trial to evaluate the effect of a high-fat, high-calorie diet on the pharmacokinetics of a single oral dose of tifentanyl tablets in healthy volunteers

观察高脂高热饮食对健康成人志愿者单次口服替芬泰片药代动力学的影响

[Translation]

Effects of a high-fat and high-calorie diet on the pharmacokinetics of a single oral dose of tifentanyl tablets in healthy adult volunteers

Start Date17 Mar 2016

Sponsor / Collaborator

Tianjin Institute of Pharmaceutical Research Co., Ltd.

[+3]

CTR20140543 / CompletedPhase 1

替芬泰片随机、双盲、安慰剂对照单次给药健康人体耐受性及药代动力学试验

[Translation] A randomized, double-blind, placebo-controlled single-dose tolerability and pharmacokinetic study of tifentai tablets in healthy volunteers

从安全的初始剂量开始，研究中国健康志愿者单次口服替芬泰片后人体的安全性、耐受性和药代动力学特征，为后续临床试验提供安全的剂量范围，以及安全、合理的给药方案。

[Translation]

Starting from a safe initial dose, the safety, tolerability and pharmacokinetic characteristics of Chinese healthy volunteers after a single oral administration of tifenacet tablets were studied to provide a safe dosage range and a safe and reasonable dosing regimen for subsequent clinical trials.

Start Date22 Oct 2014

Sponsor / Collaborator

Tianjin Institute of Pharmaceutical Research Co., Ltd.

[+3]

100 Clinical Results associated with Tyrophentide

100 Translational Medicine associated with Tyrophentide

100 Patents (Medical) associated with Tyrophentide

Literatures (Medical) associated with Tyrophentide

02 Apr 2020·XenobioticaQ4 · MEDICINE

In vitrometabolism andin vivopharmacokinetics of bentysrepinine (Y101), an investigational new drug for anti-HBV-infected hepatitis: focus on interspecies comparison

Q4 · MEDICINE

Article

Author: Yang, Yuanhui ; Dong, Shiqi ; Zhang, Lihua ; Xia, Yuanyuan ; Liao, Cuiping ; Liu, Changxiao ; Liu, Jianfeng ; Fan, Huirong ; Si, Duanyun ; Zhang, Aijie

The objective of this study was to clarify the species differences of pharmacokinetics of Y101 (N-[N-benzoyl-O-(2-dimethylaminoethyl)-l-tyrosyl]-l-phenylalaninol hydrochloride), a derivative of herbal ingredient with anti-HBV hepatitis activity, in rats, dogs, monkeys and humans.The metabolic stability and metabolite identification studies using liver microsomes in vitro, plasma protein binding using a rapid equilibrium dialysis in vitro, pharmacokinetic studies in vivo were carried out to evaluate the interspecies differences. The toxicokinetic study in monkeys was also investigated.The metabolic profiles were similar in monkeys and humans, which were significant different from rats and dogs in vitro. In vitro plasma protein binding showed no major differences between species with medium to high protein binding rates. After single oral dose to rats, dogs, and monkeys, the absolute oral bioavailability of Y101 was 44.9%, 43.1%, and 19.2%, respectively. There was no accumulation for Y101 toxicokinetics in monkeys after oral administration for 90 d.The metabolic profiles indicated monkey was the very animal model for preclinical safety evaluation of Y101. Our results have demonstrated the favorable pharmacokinetics profile of Y101, which supports the clinical trials in humans.

01 Feb 2018·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Simultaneous determination of bentysrepinine (Y101) and its metabolites M8 and M9 in human plasma by UPLC–MS/MS and its application to a pharmacokinetic study

Q3 · MEDICINE

Article

Author: Huang, Chenrong ; Miao, Liyan ; Xia, Wen ; Xue, Ling ; Xu, Qingqing ; Li, Xing ; Liu, Xiaoxue

A rapid and highly sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of a novel anti-HBV compound Y101 and its metabolites M8 and M9 in human plasma. The plasma samples were deproteinated with acetonitrile after addition of Peramivir (internal standard, IS) and separated on a 40 °C ACQUITY UPLC BEH C₁₈ column (2.1 mm × 50 mm, 1.7 μm). The mobile phase consisted of water (containing 5 mM ammonium acetate and 0.1% formic acid) and acetonitrile (74:26, v/v) at a flow rate of 0.3 mL/min. The detection was performed on a Triple Quad 5500 tandem mass spectrometer coupled with electrospray ionization (ESI) source in positive mode. Quantification was conducted by multiple reaction monitoring (MRM) of the transitions of m/z 490.1 → 339.0 for Y101, m/z 357.2 → 105.2 for metabolite M8, m/z 373.1 → 105.1 for metabolite M9 and m/z 329.1 → 270.2 for IS, respectively. The method was validated over the calibration curve range of 1.000-1000 ng/mL for Y101, 2.000-2000 ng/mL for metabolite M8 and 0.3000-300.0 ng/mL for metabolite M9, using linear regression and 1/x² weighting. No matrix effect and carryover effect was observed. The intra- and inter-batch precision and accuracy of Y101, metabolite M8 and M9 were all within the acceptable criteria. This method allows a rapid and simple determination of Y101 and its metabolites M8 and M9 in human plasma. It was successfully applied in a pharmacokinetic study in human for the first time.

01 Jan 2017·Journal of Chromatography BQ3 · MEDICINE

Metabolite identification of bentysrepinine (Y101), a novel anti-HBV agent in rats using a five-step strategy based on a combined workflow with two different platforms of liquid chromatography–tandem mass spectrometry

Q3 · MEDICINE

Article

Author: Liu, Changxiao ; Dong, Shiqi ; Hu, Zhanxing ; Liu, Ting ; Fan, Huirong ; Si, Duanyun ; Liang, Guangyi ; Li, Ruixing ; Gu, Yuan

Bentysrepinine (Y101), a derivative of repensine (a compound isolated from Dichondrarepens Forst), is a novel phenyalanine dipeptide inhibiting DNA-HBV and cccDNA activities and is currently under development for the treatment of hepatitis B virus (HBV)-infected hepatitis. Our previous study implied that there might be an existence of extensive metabolism of Y101 in rats. Therefore, it is necessary to perform metabolic profiling study to further evaluate its safety and drug-like properties. In this study, the metabolism of Y101 in rats was investigated by a convincible five-step strategy to characterize metabolites in plasma and that excreted into urine, bile and feces. The five-step strategy was realized by using an combined workflow on two different MS platforms, including various scan modes of liquid chromatography with hybrid quadruple-linear ion trap mass spectrometry (LC-QTRAP-MS/MS) and various post-acquiring data mining tools of liquid chromatography-quadrupole time-of-flight tandem mass spectrometry (LC-QTOF-MS/MS). QTOF MS/MS was employed as a powerful complementary tool to enable high confidence of metabolites identification using its functions of accurate MS and MS/MS fragmentation. As a result, a total of 30 metabolites were detected, including 25 phase I and 5 phase II metabolites. Among them, four primary metabolites (M6-M9) were further identified by comparing with the authentic standards chemically synthesized. The possible metabolic pathways of Y101 in rats were proposed to be amide hydrolysis, monohydroxylation, dihydroxylation, N-oxidation, demethylation, methylation, glucosidation and glucuronidation. This is the first study of the metabolism of Y101 in rats. The five-step strategy was successfully used to systematically characterize metabolites of Y101 in rats, and it would be generally applied for metabolite identification of new drug candidate.

100 Deals associated with Tyrophentide

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis B, Chronic	Phase 1	CN	Chinese Academy of Sciences	25 Aug 2014

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