Delving into the Latest Updates on Lercanidipine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Carmen, Corifeo, Lercadip

+ [25]

Target

Cav2.1

Action

inhibitors

Mechanism

Cav2.1 inhibitors(calcium voltage-gated channel subunit alpha1 A inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Active Organization

+ [11]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Sweden (28 Mar 1998),

Hypertension

RegulationPriority Review (China)

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Structure/Sequence

Molecular FormulaC36H42ClN3O6

InChIKeyWMFYOYKPJLRMJI-UHFFFAOYSA-N

CAS Registry132866-11-6

View All Structures (2)

主要目的：以药代动力学参数作为主要终点评价指标，比较在空腹状态下口服受试制剂盐酸乐卡地平片（规格：10mg，持证商：福建省宝诺医药研发有限公司）与参比制剂盐酸乐卡地平片（规格：10mg，持证商：Recordati S.P.A.，商品名：再宁平®）后在健康受试者体内的药代动力学行为，评价两种制剂的生物等效性。次要目的：观察空腹状态下受试制剂盐酸乐卡地平片和参比制剂盐酸乐卡地平片在健康受试者中的安全性。

[Translation]

Main purpose: Using pharmacokinetic parameters as the primary endpoint evaluation index, compare the pharmacokinetic behavior of the test preparation Lercanidipine Hydrochloride Tablets (Specification: 10 mg, licensee: Fujian Province Baonuo Pharmaceutical Research and Development Co., Ltd.) and the reference preparation Lercanidipine Hydrochloride Tablets (Specification: 10 mg, licensee: Recordati S.P.A., trade name: Zainingping®) in healthy subjects after oral administration in the fasting state, and evaluate the bioequivalence of the two preparations. Secondary purpose: Observe the safety of the test preparation Lercanidipine Hydrochloride Tablets and the reference preparation Lercanidipine Hydrochloride Tablets in healthy subjects in the fasting state.

Start Date08 Jan 2025

Sponsor / Collaborator

Fujian Boro Pharmaceutical Research Co., Ltd.

CTR20244946

/ CompletedPhase 1

盐酸乐卡地平片在中国健康受试者中单次空腹口服给药的一项随机、开放、三周期、三序列部分重复交叉生物等效性试验

[Translation] A randomized, open-label, three-period, three-sequence partially repeated crossover bioequivalence study of lercanidipine hydrochloride tablets after a single oral administration on an empty stomach in healthy Chinese subjects

观察健康受试者空腹单次口服由沈阳天邦药业有限公司生产的受试制剂盐酸乐卡地平片（规格：10 mg）后血药浓度经时过程，估算其药代动力学参数，并以原研进口 Recordati S.P.A.生产的盐酸乐卡地平片（商品名：再宁平®，规格：10 mg）为参比制剂，进行人体相对生物利用度和生物等效性评价，为临床用药提供参考依据。

[Translation]

The time course of blood drug concentration after a single oral administration of the test preparation Lercanidipine Hydrochloride Tablets (Specification: 10 mg) produced by Shenyang Tianbang Pharmaceutical Co., Ltd. on an empty stomach was observed in healthy subjects, and its pharmacokinetic parameters were estimated. The Lercanidipine Hydrochloride Tablets (trade name: Zainingping®, specification: 10 mg) produced by the original imported Recordati S.P.A. was used as the reference preparation to evaluate the relative bioavailability and bioequivalence in humans, providing a reference for clinical medication.

Start Date02 Dec 2024

Sponsor / Collaborator

Shenyang Tianbang Pharmaceutical Co., Ltd.

100 Clinical Results associated with Lercanidipine Hydrochloride

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100 Translational Medicine associated with Lercanidipine Hydrochloride

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100 Patents (Medical) associated with Lercanidipine Hydrochloride

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770

Literatures (Medical) associated with Lercanidipine Hydrochloride

01 Apr 2025·Journal of Molecular Structure

Isolation and in-depth characterization of degradation products of lercanidipine hydrochloride under acid-mediated hydrolysis: Transformation of dihydropyridine moiety to cyclohexenone

Author: Nallajarla, Anil Kumar ; Goswami, Anandarup ; Doddipalla, Raju ; Modini, Arun Kumar ; Ranga, Mahesh ; Kaliyaperumal, Muralidharan

The International Council for Harmonisation of Tech. Requirements for Pharmaceuticals for Human Use (ICH) guidelines are commonly used in the pharmaceutical industry to assess drug degradationWhile most studies focus on anal. protocols like impurity isolation and stability assessment, they often neglect detailed structural characterization of degradants thus potentially limiting the development of new chem.The present study investigates the degradation profile of Lercanidipine hydrochloride (LER.HCl), an antihypertensive drug belonging to the calcium channel blocker class with a dihydropyridine moiety, under ICH-guided acidic hydrolytic conditions and subsequent detailed characterization of the isolated degradation products.The acid-mediated hydrolytic condition (at 60 °C for 12 h) led to degradation of LER HCl (20.3 %) to five degradation products (LER-P1- 3.2 %, LER-P2- 4.3 %, LER-P3-5.5 %, LER-P4- 2.1 % and LER-P5-5.2 %).The compounds were initially detected by a simple mass-compatible UHPLC-MS and tentatively characterized by HRMS.The reaction mixture was separated using preparative HPLC with high recovery percentage (>90 %) and their structures were characterized comprehensively using a variety of techniques including 1D (¹H, ¹³C) and 2D (COSY, HSQC, and HMBC) NMR spectroscopy, FT-IR spectroscopy, and Single Crystal X-ray Diffraction (SC-XRD).LER-P1, previously identified as a process impurity with min. characterization data, was thoroughly characterized using advanced spectroscopic techniques.Moreover, the exhaustive characterization of LER-P2, LER-P3, LER-P4, and LER-P5 (which were not reported in previous LER degradation studies) confirmed the transformation of dihydropyridine ring to cyclohexenone with multiple chiral centers under acidic hydrolysis.The proposed mechanisms rationalized all structures, aiming to connect the thorough characterization of new degradation products with their transformation process.The present study provides a guideline about systematic investigations of the stress-induced degradation of pharmaceutical candidates.

01 Mar 2025·British Journal of Clinical Pharmacology

Calcium channel blocker overdose: Not all the same toxicity

Article

Author: Isbister, Geoffrey K. ; Jenkins, Shane ; Harris, Keith ; Isoardi, Katherine Z. ; Downes, Michael A.

AbstractAimsCalcium channel blocker (CCB) overdose remains an important poisoning, with increasing availability of dihydropyridines. We aimed to compare the severity and treatment of CCB overdoses.MethodsWe reviewed CCB overdoses presenting to two toxicology services from 2014 to 2023. We extracted prospectively collected data from a clinical database, including demographics, dose, co‐ingestants, complications, treatments and outcomes, to compare different CCBs.ResultsThere were 236 overdoses; median age 55 years (interquartile range [IQR]: 41–65 years); 130 (55%) were females. Dihydropyridine overdoses increased significantly: median of nine cases annually (IQR: 8.8–12.3) during the study compared to a median of three cases annually (IQR: 1–4.3; P < 0.001) in the 10 years prior. The commonest agent was amlodipine (147), then lercanidipine (28), diltiazem (27), verapamil (23) and felodipine (11). Median defined daily dose ingested was higher for dihydropyridines, and cardiac co‐ingestants were common except verapamil. Median length of stay was 21 h (IQR: 13–43 h), which was similar except longer for diltiazem (median, 39 h). Fifty‐six patients (24%) were admitted to intensive care, more often for diltiazem (14; 52%) and verapamil (7; 30%). Dysrhythmias occurred in 19 patients (diltiazem [9], verapamil [8], amlodipine [2]), and included 13 junctional dysrhythmias. Hypotension occurred in 91 patients (39%), 62 (26%) received inotropes/vasopressors (adrenaline 32 [52%], noradrenaline 48 [77%]), 21 (9%) high‐dose insulin and 44 (19%) calcium. Adrenaline and high‐dose insulin were more commonly given in diltiazem and verapamil overdoses, compared to vasopressors in dihydropyridine overdoses. Acute kidney injury occurred in 39 patients. Seven (3%) patients died.ConclusionsDihydropyridines were the commonest CCB overdoses, with amlodipine making up half. More severe toxicity occurred with diltiazem and verapamil.

01 Mar 2025·International Journal of Cardiology Cardiovascular Risk and Prevention

Effects of antihypertensives with and without IL-6 lowering properties on long-term blood pressure control: The prospective HELIUS cohort

Article

Author: Galenkamp, Henrike ; Batuo, Hillman ; van der Linden, Eva ; Born, Bert-Jan van der ; Chilunga, Felix P ; Moll van Charante, Eric

BackgroundChronic inflammation is a well-recognized contributor to hypertension pathogenesis. However, the role of targeting inflammation in hypertension treatment, particularly through modulation of inflammatory markers like interleukin-6 (IL-6), remains less understood. We investigated the effects of antihypertensive medications with and without IL-6-lowering properties on long-term blood pressure (BP) control in a multi-ethnic cohort in the Netherlands.MethodsParticipants from HELIUS cohort receiving hypertension treatment were followed over six years. BP control at follow-up was determined using WHO criteria. Due to unavailability of IL-6 data, a literature review was conducted to classify antihypertensives based on their IL-6-lowering properties - a proxy approach. Logistic regression models were used to assess associations between the IL-6-lowering potential of antihypertensives and BP control, both within and between antihypertensive classes. Effect modification by ethnicity was explored.ResultsA total of 1510 participants were included (mean age 57 years, 62 % women). Within the calcium channel blocker (CCB) class, medications with IL-6-lowering properties (amlodipine and barnidipine) were associated with superior BP control (aOR 1.41, 95 % confidence interval 1.05-1.90) compared to other CCBs (lercanidipine, nifedipine, verapamil, clevidipine, diltiazem). No significant associations were observed within angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs), between different antihypertensive drug classes, nor across ethnic groups.ConclusionAmlodipine and barnidipine were associated with better BP control compared to other CCBs. Our findings provide an important starting point for understanding the role of IL-6 in hypertension management. Further studies are warranted to confirm these observations by directly measuring IL-6 levels and investigating underlying mechanisms.

100 Deals associated with Lercanidipine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D01849	Lercanidipine Hydrochloride	C08CA13	DB00528

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	Sweden	Meda AB	28 Mar 1998

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESH2024	Not Applicable	Hypertension	-	Amlodipine	(udatuzmdvg) = sapyniiano qcntpnozoq (bsaxbjeouz )	Positive	01 May 2024
				Lercanidipine	(udatuzmdvg) = czunkvvifq qcntpnozoq (bsaxbjeouz )
NCT01093807 (Pubmed \| J Hypertens)	Phase 2	Hypertension	1,039	Placebo	xewoubjkog(nawyizowql) = ytuhdbwhvq bgtdjplqhr (vkaoidaqai ) View more	-	01 Jan 2016
				Lercanidipine 10mg	xewoubjkog(nawyizowql) = ixtmoxarcn bgtdjplqhr (vkaoidaqai ) View more
[PP.35.33] (ESH2015)	Not Applicable	Diabetes Mellitus, Type 2 \| Hypertension fasting plasma glucose \| glycated hemoglobin \| high-sensitivity C-reactive protein ... View more	151	Barnidipine 20 mg/day + Losartan 100 mg/day	(ggkjczrpge) = bdczxmtkfr lwjovfobxc (ngolctsgkv ) View more	Positive	01 Jun 2015
				Lercanidipine 20 mg/day + Losartan 100 mg/day	(ggkjczrpge) = cwjvffleek lwjovfobxc (ngolctsgkv ) View more
PP.5.213 (ESH2010)	Not Applicable	Hypertension	60	Lercanidipine monotherapy	(gouctlyxdh) = tgpqfeaoti uhdszcyywb (ayflynlbct ) View more	Positive	01 Jun 2010
				Lercanidipine + Perindopril combination therapy	(gouctlyxdh) = peztfbfulv uhdszcyywb (ayflynlbct ) View more
PP.5.176 (ESH2010)	Not Applicable	-	162	Lercanidipine + Beta-blockers	(vwhkqfaifj) = smfhitihot xngcxkkmsb (xfbhkbhynn ) View more	Positive	01 Jun 2010
				Lercanidipine + Diuretics	(vwhkqfaifj) = soakablubr xngcxkkmsb (xfbhkbhynn ) View more