Delving into the Latest Updates on Felbinac Trometamol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Binaprofen, Felbinac

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Nervous System Diseases

Active Indication

Pain, PostoperativePain

Inactive Indication

CalculiCancer PainCarcinoma+ [8]

Originator Organization

Dalian Tianyu Pharmaceutical Co.,Ltd.

Active Organization

Guangdong Zhongke Pharmaceutical Research Co., Ltd.

Shijiazhuang Yiling Pharmaceutical Co., Ltd.

Hebei Kaiwei Pharmaceutical Co. Ltd.

Inactive Organization

Dalian Tianyu Pharmaceutical Co.,Ltd.

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC14H12O2

InChIKeyQRZAKQDHEVVFRX-UHFFFAOYSA-N

CAS Registry5728-52-9

View All Structures (2)

主要目的：（1）评价氟康唑胶囊对中国健康受试者静脉滴注苯胺洛芬注射液的药代动力学影响；（2）评价利福平胶囊对中国健康受试者静脉滴注苯胺洛芬注射液的药代动力学影响；次要目的：评价健康受试者单剂量静脉滴注苯胺洛芬注射液与口服氟康唑胶囊/利福平胶囊联合用药的安全性。

[Translation]

Primary objectives: (1) To evaluate the effect of fluconazole capsules on the pharmacokinetics of intravenous anilinoprofen injection in healthy Chinese subjects; (2) To evaluate the effect of rifampicin capsules on the pharmacokinetics of intravenous anilinoprofen injection in healthy Chinese subjects; Secondary objectives: To evaluate the safety of single-dose intravenous anilinoprofen injection combined with oral fluconazole capsules/rifampicin capsules in healthy subjects.

Start Date28 Sep 2021

Sponsor / Collaborator

Dalian Tianyu Pharmaceutical Co.,Ltd.

[+1]

CTR20211806 / CompletedPhase 1

苯胺洛芬滴眼液单中心、随机、双盲、安慰剂对照健康受试者多次给药人体耐受性和药代动力学研究

[Translation] A single-center, randomized, double-blind, placebo-controlled study of the tolerability and pharmacokinetics of fenprofen eye drops in healthy subjects after multiple doses

主要目的：评价苯胺洛芬滴眼液多次给药在中国健康受试者中的安全性和耐受性。次要目的：评价苯胺洛芬滴眼液多次给药在中国健康受试者中的药代动力学特征。

[Translation]

Primary objective: To evaluate the safety and tolerability of multiple-dose anilinoprofen eye drops in healthy Chinese subjects. Secondary objective: To evaluate the pharmacokinetic characteristics of multiple-dose anilinoprofen eye drops in healthy Chinese subjects.

Start Date07 Sep 2021

Sponsor / Collaborator

Guangdong Zhongke Pharmaceutical Research Co., Ltd.

CTR20212131 / CompletedPhase 1

[14C]苯胺洛芬注射液在中国成年男性健康受试者体内吸收、代谢和排泄临床试验——[14C]苯胺洛芬注射液人体物质平衡与生物转化研究

[Translation] Clinical trial on absorption, metabolism and excretion of [14C]anilinoprofen injection in healthy adult male subjects in China——Study on material balance and biotransformation of [14C]anilinoprofen injection in humans

主要目的：评价中国男性健康受试者单次静脉滴注[14C]苯胺洛芬注射液的物质平衡及生物转化途径。次要目的：评价苯胺洛芬在人体内的药代动力学整体特征及安全性。

[Translation]

Primary objective: To evaluate the material balance and biotransformation pathways of a single intravenous infusion of [14C]anilinoprofen injection in healthy Chinese male subjects. Secondary objective: To evaluate the overall pharmacokinetic characteristics and safety of anilinoprofen in humans.

Start Date01 Sep 2021

Sponsor / Collaborator

Dalian Tianyu Pharmaceutical Co.,Ltd.

[+1]

100 Clinical Results associated with Felbinac Trometamol

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100 Translational Medicine associated with Felbinac Trometamol

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100 Patents (Medical) associated with Felbinac Trometamol

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4

Literatures (Medical) associated with Felbinac Trometamol

01 Aug 2020·CNS DrugsQ2 · MEDICINE

Pharmacokinetics, Safety, and Tolerability of Intravenous Felbinac Trometamol in Healthy Chinese Volunteers: A First-in-Human Single- and Multiple-Dose Escalation Phase I Study with a Randomized, Double-Blind, Placebo-Controlled Design

Q2 · MEDICINE

Article

Author: Li, Cuiyun ; Zhang, Hong ; Sun, Jixuan ; Li, Xiaojiao ; Ding, Yanhua ; Gao, Xuedong ; Wang, Wei ; Wu, Min ; Zhu, Xiaoxue

BACKGROUNDFelbinac trometamol, an anti-inflammatory and analgesic drug, has been used to treat immediate postoperative pain.OBJECTIVEThe aim of this study was to evaluate the safety, tolerability, and pharmacokinetics of single or multiple intravenous infusions of felbinac trometamol in healthy Chinese volunteers.METHODSA total of 56 healthy subjects were enrolled in a single-ascending dose study (11.78-377.00 mg), meanwhile 36 subjects were enrolled in a multiple-ascending dose study (47.13-188.50 mg). Safety endpoints included treatment-emergent adverse events, vital signs, electrocardiograms, and laboratory parameters. Pharmacokinetic endpoints included exposure of subjects to felblinac and metabolites of the drug in plasma, urine, and feces.RESULTSFelblinac time to maximum plasma concentration was obtained at 0.5 h, corresponding to the end of the infusion. Maximum plasma concentration and area under the curve increased in a dose-dependent manner for felblinac and its metabolite, showing linear pharmacokinetic characteristics at single and multiple doses. After intravenous infusions of multiple doses three times (30 min each time) per day, the accumulation ratio of felblinac and its metabolite based on the area under the curve had a range of 1.34-1.45 and 1.60-1.87, respectively, across cohorts. After administration of the fourth dose, the plasma concentration of both felblinac and its metabolites was maintained at a steady state. Felbinac trometamol was well tolerated. Neither treatment-emergent adverse event frequency nor severity increased with increasing felbinac trometamol dose.CONCLUSIONSFelbinac trometamol was well tolerated in our study. Based on the dose range in this study, 94.25 mg is the recommended target dose for a phase II study.CLINICAL TRIAL REGISTRATIONCTR20170496 and CTR20180896. The dates of registration are 2017-06-19 and 2018-07-02 ( https://www.chinadrugtrials.org.cn/ ).

01 Apr 2015·Journal of Chromatography BQ3 · MEDICINE

Qualitative and quantitative analysis of felbinac and its major metabolites in human plasma and urine by liquid chromatography tandem mass spectrometry and its application after intravenous administration of felbinac trometamol injection

Q3 · MEDICINE

Article

Author: Wu, Guolan ; Hu, Xingjiang ; Zhai, You ; Wu, Lihua ; Zheng, Yunliang ; Shentu, Jianzhong ; Liu, Jian

We present a method for the qualitative and quantitative analysis of felbinac and its major metabolites in human plasma and urine by HPLC-MS/MS and its application. Qualitative analysis through LC-Triple-TOF-MS/MS indicated that oxidization was the main phase-I metabolic pathway of felbinac in human, conjugation with sulfate and glucuronide groups produced at least 7 phase-II metabolites. Quantitative analysis through HPLC-MS/MS in MRM mode was developed and validated for the quantification of felbinac and its major metabolite (4'-hydroxyfelbinac) in human plasma and urine. Linear calibration curves were obtained for felbinac and 4'-hydroxyfelbinac in plasma and urine (r>0.996); intra- and inter-day precision values (RSD%) obtained were ranged from 1.13 to 6.49%, and the accuracy were between 95.9% and 108.6% for the two analytes. The pharmacokinetics and excretion analysis showed that the t1/2 of 4'-hydroxyfelbinac (8.25 ± 4.15 h) is a litter longer than that of felbinac (6.13 ± 2.01 h), but the mean AUC(0-t) value of felbinac was about 20 times higher than that of 4'-hydroxyfelbinac; excretion of felbinac and 4'-hydroxyfelbinac reached their peak values at about 3-6h after intravenous administration of felbinac trometamol in human.

01 Apr 2011·XenobioticaQ4 · MEDICINE

Pharmacokinetics of felbinac after intravenous administration of felbinac trometamol in rats

Q4 · MEDICINE

Article

Author: Feng Gao ; Yantong Sun ; Jingkai Gu ; Wei Yang ; Chao Zhang ; Wei Wang ; Xiangyong Cui ; J. Paul Fawcett ; Yan Yang

Felbinac trometamol (trishydroxymethylaminomethane 4-biphenylacetate) is a new water-soluble salt of felbinac currently undergoing clinical evaluation as an intravenous (i.v.) formulation for the treatment of severe post-operative pain. This article reports the pharmacokinetics of felbinac after i.v. administration of felbinac trometamol in Sprague-Dawley rats. The maximum plasma concentration (C(0)) and area under the plasma concentration-time curve (AUC) of felbinac administered at doses of 3.36, 8.40 and 21.0 mg/kg felbinac trometamol increased linearly with dose. Felbinac was highly protein bound (~95%) at plasma concentrations up to 75 μg/ml and extensively metabolized with only small amounts being excreted unchanged in urine (0.318%), feces (0.530%) and bile (0.465%). 4'-Hydroxyfelbinac was the principal metabolite in urine, feces and bile together with felbinac glucuronide, 4'-hydroxyfelbinac glucuronide and sulfate. The majority of the administered dose was excreted in urine (63.6%) mostly as 4'-hydroxyfelbinac. Total drug in urine and feces accounted for about 72% of the dose. It would appear that felbinac trometamol has the potential to replace lipid-based NSAID formulations and progress to clinical evaluation.

100 Deals associated with Felbinac Trometamol

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB07477

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain, Postoperative	NDA/BLA	CN	Hebei Kaiwei Pharmaceutical Co. Ltd.	10 Jul 2024
Pain, Postoperative	NDA/BLA	CN	Shijiazhuang Yiling Pharmaceutical Co., Ltd.	10 Jul 2024
Pain	NDA/BLA	-	Shijiazhuang Yiling Pharmaceutical Co., Ltd.	-
Neuralgia	Discovery	CN	Dalian Tianyu Pharmaceutical Co.,Ltd.	10 May 2021
Cancer Pain	Discovery	CN	Guangdong Zhongke Pharmaceutical Research Co., Ltd.	08 Apr 2021
Cancer Pain	Discovery	CN	Dalian Tianyu Pharmaceutical Co.,Ltd.	08 Apr 2021
Gout	Discovery	CN	Dalian Tianyu Pharmaceutical Co.,Ltd.	08 Apr 2021
Gout	Discovery	CN	Guangdong Zhongke Pharmaceutical Research Co., Ltd.	08 Apr 2021
Lithiasis	Discovery	CN	Dalian Tianyu Pharmaceutical Co.,Ltd.	08 Apr 2021
Lithiasis	Discovery	CN	Guangdong Zhongke Pharmaceutical Research Co., Ltd.	08 Apr 2021