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更新于：2025-05-07

Levamlodipine Besylate/Valsartan

苯磺酸左旋氨氯地平/缬沙坦

更新于：2025-05-07

概要

基本信息

药物类型

小分子化药

别名

Levosartan

靶点

AT1R x VDCCs

作用方式

拮抗剂、阻滞剂

作用机制

AT1R拮抗剂(血管紧张素II-1型受体拮抗剂)、VDCCs阻滞剂(电压门控性钙通道复合体阻滞剂)

治疗领域

心血管疾病

在研适应症

原发性高血压

非在研适应症-

原研机构

AHN-GOOK PHARMACEUTICAL Co., Ltd.

在研机构

AHN-GOOK PHARMACEUTICAL Co., Ltd.

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期

韩国 (2013-07-30),

原发性高血压

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C26H31ClN2O8S

InChIKeyZPBWCRDSRKPIDG-LMOVPXPDSA-N

CAS号150566-71-5

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关联

项与苯磺酸左旋氨氯地平/缬沙坦相关的临床试验

NCT01536353

/ Completed临床1期

A Single Dose, Randomized, Open-label, 2x2 Crossover Study to Evaluate the Bioavailability and Safety of AGSAV301 Tablet in Healthy Male Volunteers

The purpose of this study is to evaluate the bioavailability and safety of AGSAV301 tablet in healthy male volunteers.

开始日期2012-01-01

申办/合作机构

AHN-GOOK PHARMACEUTICAL Co., Ltd.

[+1]

100 项与苯磺酸左旋氨氯地平/缬沙坦相关的临床结果

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100 项与苯磺酸左旋氨氯地平/缬沙坦相关的转化医学

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100 项与苯磺酸左旋氨氯地平/缬沙坦相关的专利（医药）

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项与苯磺酸左旋氨氯地平/缬沙坦相关的文献（医药）

2014-02-01·American Journal of Cardiovascular Drugs4区 · 医学

Pharmacokinetics, Tolerability, and Safety of the Single Oral Administration of AGSAV301 vs Exforge: A Randomized Crossover Study of Healthy Male Volunteers

4区 · 医学

Article

作者: Shi Hyang Lee ; Mi Jo Kim ; Yo Han Kim ; Hyeong-Seok Lim ; Kyun-Seop Bae ; Hee Youn Choi ; Yook-Hwan Noh

BACKGROUND AND OBJECTIVEValsartan, an angiotensin receptor blocker, is often used with calcium channel blockers (CCBs) such as amlodipine to control hypertension. Recently, the fixed-dose combination (FDC) of amlodipine 10 mg/valsartan 160 mg (Exforge) was approved. Amlodipine is a racemic mixture of CCB; S-amlodipine has higher activity than R-form. Therefore, AGSAV301, the FDC of S-amlodipine 5 mg/valsartan 160 mg was recently developed. The objective of this study was to compare the pharmacokinetic (PK) characteristics of S-amlodipine and valsartan when administered as one tablet each of Exforge and AGSAV301 to healthy male subjects.METHODSThis was a single-dose, randomized, open-label, two-way, two-period crossover study. Each subject received a single dose of AGSAV301 and Exforge, separated by a 3-week washout period. Plasma samples for the PK analysis of valsartan and S-amlodipine were collected at predose (0) and 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 16, 24, 36, 48, 72, 96, 120, and 168 h after administration. Tolerability was also evaluated.RESULTSA total of 29 subjects were enrolled; 24 completed this study. The S-amlodipine maximum plasma concentration (C max) geometric mean ratio (GMR) between AGSAV301 and Exforge was 0.951 (90 % CI 0.983-1.014), and area under the concentration-time curve from time 0 to last measured time point (AUClast) was 0.917 (90 % CI 0.861-0.976). The GMR of valsartan C max was 0.994 (90 % CI 0.918-1.076), and the AUClast was 0.927 (90 % CI 0.821-1.047). All adverse events (AEs) were resolved without sequelae; no serious AEs were reported. Two drugs showed similar tendencies to lower blood pressure in healthy subjects.CONCLUSIONSThe PK profiles of AGSAV301 and Exforge were bioequivalent. Both drugs were also well tolerated, with comparable AE profiles and similar blood pressure-lowering tendencies in healthy volunteers, suggesting equivalent therapeutic indications.

100 项与苯磺酸左旋氨氯地平/缬沙坦相关的药物交易

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