Delving into the Latest Updates on Bisoprolol Fumarate/Amlodipine Besylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Amlodipine/bisoprolol, Bisoprolol/amlodipine, Concor-AM

+ [3]

Target

L-type calcium channel x β1-adrenergic receptor

Action

blockers, antagonists

Mechanism

L-type calcium channel blockers(Voltage-gated L-type calcium channel blockers), β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication

Essential Hypertension

Originator Organization

Merck & Co., Inc.

Active Organization

Merck Kft

Inactive Organization

Merck KGaA

Egis Gyógyszergyár Zrt.

License Organization-

Drug Highest PhaseApproved

First Approval Date

Hungary (01 Feb 2011),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC22H35NO8

InChIKeyRZPZLFIUFMNCLY-WLHGVMLRSA-N

CAS Registry104344-23-2

View All Structures (2)

考察空腹及餐后条件下，健康研究参与者单次口服由深圳市宇健生物医药有限公司提供的比索洛尔氨氯地平片【受试制剂，规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg】与相同条件下单次口服由Merck Kft持证的比索洛尔氨氯地平片【参比制剂，规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg】的药动学特征，评价两制剂间的生物等效性及安全性，为受试制剂的注册申请提供依据。

[Translation]

To investigate the pharmacokinetic characteristics of a single oral dose of bisoprolol amlodipine tablets [test preparation, strength: 5 mg bisoprolol fumarate and 5 mg amlodipine besylate (calculated as amlodipine)] provided by Shenzhen Yujian Biotechnology Co., Ltd. in healthy study participants under fasting and postprandial conditions, compared with a single oral dose of bisoprolol amlodipine tablets [reference preparation, strength: 5 mg bisoprolol fumarate and 5 mg amlodipine besylate (calculated as amlodipine)] certified by Merck Kft under the same conditions, to evaluate the bioequivalence and safety of the two preparations, and to provide a basis for the registration application of the test preparation.

Start Date20 Aug 2025

Sponsor / Collaborator

Unihealth Biopharmaceutical Limited

CTR20252203

/ CompletedNot Applicable

石家庄市普力制药有限公司生产的比索洛尔氨氯地平片（规格：5mg/5mg）与持证商为Merck Kft，生产商为Egis Pharmaceuticals PLC的比索洛尔氨氯地平片（规格：5mg/5 mg）在中国健康受试者中进行的随机、开放、单剂量、两周期、双交叉、空腹及餐后状态下的生物等效性研究。

[Translation] A randomized, open, single-dose, two-period, double-crossover bioequivalence study was conducted in healthy Chinese subjects between bisoprolol amlodipine tablets (specification: 5 mg/5 mg) produced by Shijiazhuang Puli Pharmaceutical Co., Ltd. and bisoprolol amlodipine tablets (specification: 5 mg/5 mg) whose licensee is Merck Kft and manufacturer is Egis Pharmaceuticals PLC in the fasting and fed states.

石家庄市普力制药有限公司生产的比索洛尔氨氯地平片（规格：5mg/5mg ）与持证商为Merck Kft，生产商为Egis Pharmaceuticals PLC的比索洛尔氨氯地平片（规格：5mg/5mg）在中国健康受试者中进行的随机、开放、单剂量、两周期、双交叉、空腹及餐后状态下的生物等效性研究。

[Translation]

A randomized, open, single-dose, two-period, double-crossover bioequivalence study was conducted in healthy Chinese subjects on bisoprolol amlodipine tablets (specification: 5mg/5mg) produced by Shijiazhuang Puli Pharmaceutical Co., Ltd. and bisoprolol amlodipine tablets (specification: 5mg/5mg) whose licensee is Merck Kft and manufacturer is Egis Pharmaceuticals PLC under fasting and fed conditions.

Start Date01 Jul 2025

Sponsor / Collaborator

Shijiazhuang Puli Pharmaceutical Co Ltd.

CTR20252045

/ CompletedNot Applicable

比索洛尔氨氯地平片（5mg/5mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of bisoprolol amlodipine tablets (5 mg/5 mg) in Chinese healthy subjects under fasting and fed conditions

主要研究目的：按有关生物等效性试验的规定，选择Merck Kft为持证商的比索洛尔氨氯地平片（商品名：康忻安®，规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg）为参比制剂，对山东诺禾康药业有限公司生产，山东诺明康药物研究院有限公司提供的受试制剂比索洛尔氨氯地平片（规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康受试者口服受试制剂比索洛尔氨氯地平片（规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg）和参比制剂比索洛尔氨氯地平片（商品名：康忻安®，规格：富马酸比索洛尔5mg与苯磺酸氨氯地平（按氨氯地平计）5mg）的安全性。

[Translation]

Main research purpose: According to the relevant provisions of bioequivalence test, Bisoprolol Amlodipine Tablets (trade name: Kangxinan®, specification: 5mg bisoprolol fumarate and 5mg amlodipine besylate (calculated as amlodipine)) with Merck Kft as the licensee were selected as the reference preparation, and the test preparation Bisoprolol Amlodipine Tablets (specification: 5mg bisoprolol fumarate and 5mg amlodipine besylate (calculated as amlodipine)) produced by Shandong Novocon Pharmaceutical Co., Ltd. and provided by Shandong Nomincon Pharmaceutical Research Institute Co., Ltd. were subjected to fasting and postprandial human bioequivalence test, to compare whether the absorption rate and degree of the drug in the test preparation were within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. Secondary study objective: To observe the safety of oral administration of the test preparation bisoprolol amlodipine tablets (specifications: 5 mg bisoprolol fumarate and 5 mg amlodipine besylate (calculated as amlodipine)) and the reference preparation bisoprolol amlodipine tablets (trade name: Kangxinan®, specifications: 5 mg bisoprolol fumarate and 5 mg amlodipine besylate (calculated as amlodipine)) in healthy subjects.

Start Date11 Jun 2025

Sponsor / Collaborator

Shandong Nuomingkang Pharmaceutical Research Institute Co., Ltd.

100 Clinical Results associated with Bisoprolol Fumarate/Amlodipine Besylate

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100 Translational Medicine associated with Bisoprolol Fumarate/Amlodipine Besylate

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100 Patents (Medical) associated with Bisoprolol Fumarate/Amlodipine Besylate

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1

Literatures (Medical) associated with Bisoprolol Fumarate/Amlodipine Besylate

01 Dec 2018·Clinical Drug Investigation

Bioequivalence and Pharmacokinetics of Bisoprolol–Amlodipine 5 mg/5 mg Combination Tablet versus Bisoprolol 5 mg Tablet and Amlodipine 5 mg Tablet: An Open-Label, Randomized, Two-Sequence Crossover Study in Healthy Chinese Subjects

Article

Author: Zhou, Dongli ; Zhao, Zirun ; Zhang, Lan ; Gao, Dan ; Huang, Yue ; Li, Lin ; Wang, Chunhua ; Hu, Xiao ; Chen, Xiaoping ; Hu, Chaoying

BACKGROUND:

The pharmacokinetics of bisoprolol and amlodipine administered as a fixed-dose combination (FDC) tablet have not been sufficiently studied in healthy Chinese subjects to support a medical need for using the FDC in hypertension.

OBJECTIVE:

This study was conducted to compare the pharmacokinetic profiles of the bisoprolol-amlodipine FDC tablet with the bisoprolol tablet and amlodipine tablet administered concomitantly under both fasting and fed conditions.

METHODS:

An open-label, randomized, two-period, two-sequence crossover study was designed under both fasting and fed conditions. The plasma concentrations of bisoprolol and amlodipine were analyzed using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay, and the pharmacokinetic parameters of maximum concentration (C_max) and area under the concentration-time curve (AUC) were used to evaluate bioequivalence.

RESULTS:

The point estimate of geometric mean ratios of C_max and AUC from the time of dosing to the last measurable concentration (AUC_t) for bisoprolol were 97.85% and 99.46% in the fasting state, and 93.87% and 98.95% in the fed state, respectively. For amlodipine, the geometric mean ratios of C_max and AUC_t were 100.03% and 96.76% in the fasting state, and 106.56% and 103.07% in the fed state. No cases of treatment-emergent adverse events were reported during the entire study period.

CONCLUSIONS:

Bioequivalence was achieved for bisoprolol and amlodipine FDC under both fasting and fed conditions, and all treatments were safe and well tolerated by all study subjects.

TRIAL REGISTRATION:

ClinicalTrials.gov: NCT03226275.

100 Deals associated with Bisoprolol Fumarate/Amlodipine Besylate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	C07FB07	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	Hungary	Merck Kft	01 Feb 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	Phase 3	Germany	Merck KGaA	01 Mar 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03226275 (CTgov)	Phase 1	-	32	Amlodipine+Bisoprolol (Fasting: Bisoprolol-Amlodipine FDC)	pqfooucrld(zvbuuvtjyd) = kqcahdifbr qlazusubpb (mezoyovmyx, 16.7) View more	-	20 Feb 2019
				Amlodipine+Bisoprolol (Fasting: Bisoprolol and Amlodipine Separately)	pqfooucrld(zvbuuvtjyd) = mecjyhfsow qlazusubpb (mezoyovmyx, 21.5) View more
NCT03226275 (Pubmed \| Clin Drug Investig)	Phase 1	-	-	Bisoprolol-Amlodipine 5 mg/5 mg Combination Tablet	lmjyntnwrs(bknfqsvreo) = lskksopasr tuclubjgak (rtyavyxutl ) View more	-	01 Dec 2018
				Amlodipine 5 mg Tablet	lmjyntnwrs(bknfqsvreo) = zqexxovvcc tuclubjgak (rtyavyxutl ) View more
NCT01977794 (CTgov)	Phase 3	Essential Hypertension	200	Bisoprolol/Amlodipine (Amlodipine failed group) (Amlodipine Failed Group)	fckrxkceed(rxrbcqijka) = ptqhgfwjaz ftdvbmqzke (agdwpaodje, 8.21) View more	-	11 Aug 2016
				Bisoprolol/Amlodipine (Bisoprolol failed group) (Bisoprolol Failed Group)	fckrxkceed(rxrbcqijka) = pbtjikqvsg ftdvbmqzke (agdwpaodje, 11.57) View more