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verapamil (verapamil, Mylan / verapamil SR, Mylan / verapamil ER)

✓ Approved

Mylan · CACNA1C · 小分子

什么是 verapamil？

verapamil 是一种小分子，由Mylan研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名verapamil, Mylan, verapamil SR, Mylan, verapamil ER
公司Mylan
药物类别小分子
分子靶点CACNA1C
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Mylan

作用机制

分子靶点

verapamil 作用于 1 个分子靶点：

CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

verapamil 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedZhongguo shi yan xue ye xue za zhi2026-08-03

[Establishment of a Doxorubicin-Resistant Acute Myeloid Leukemia Cell Line and Study on Its Drug Resistance Mechanisms].

Feng Lu-Lu LL, Wang Yu-Ting YT, Huang Chao-Fan CF, Sun Cong-Yong CY et al.

To establish a doxorubicin (DOX)-resistant acute myeloid leukemia (AML) cell line and explore the mechanisms of its drug resistance. A DOX-resistant THP1 cell line (THP1-Rdox) was established using a low-dose, concentration-gradient intermittent induction method. The resistance effect was evaluated by calculating the resistance index (RI). The expression levels of resistance-related proteins ［P-glycoprotein (P-gp) and lung resistance-related protein (LRP)］ and cell cycle-related proteins (Cyclin A2, Cyclin B1 and Cyclin D1) were examined by Western blot. Intracellular DOX accumulation was observed using confocal laser scanning microscopy. Apoptosis rate and cell cycle distribution were analyzed by flow cytometry. RNA sequencing (RNA-seq) was performed to compare the differential gene expression profiles between DOX-sensitive parental THP1 cells and DOX-resistant THP1-Rdox cells. The DOX-resistant cell line THP1-Rdox was successfully established. The THP1-Rdox cells could stably proliferate at a DOX concentration of 500 ng/ml with a resistance index as high as 198.7. The THP1-Rdox cells exhibited cross-resistance to homoharringtonine (HHT) and paclitaxel (PTX) but no significant resistance to cytarabine (Ara-C). Compared with parental THP1 cells, the expression levels of drug resistance-related proteins P-gp and LRP in THP1-Rdox cells were significantly upregulated. Additionally, THP1-Rdox cells showed decreased uptake and increased efflux of DOX. Notably, after treatment with verapamil (Ver), a specific inhibitor of P-gp, intracellular DOX accumulation was significantly increased in THP1-Rdox cells. Compared with parental THP1 cells, the THP1-Rdox cells exhibited a significantly decreased apoptosis rate, a reduced proportion of cells in the S phase, an increased proportion of cells in the G1 phase, and a marked upregulation in the expression level of the cell cycle regulatory protein Cyclin D1. RNA-seq analysis showed that among the differentially expressed genes between THP1-Rdox and parental THP1 cells, the top 10 most significantly upregulated genes in THP1-Rdox cells were ABCB1, HNRNPA1P9, SEMA3E, MICB, JAML, FGL2, VSIG1, CLEC1B, DLGAP1-AS3, and HOOK1; the top 10 most significantly downregulated genes were MAGEB2, NPTX2, CGREF1, CDO1, GBP5, ZNF595, ZNF630, DTX3, KLHL4 and ZBED6CL. Low-dose, concentration-gradient intermittent induction method can successfully establish a DOX-resistant AML cell line, THP1-Rdox. The drug resistance of this cell line is likely attributed to enhanced drug efflux mediated by the elevated expression of P-gp and LRP, as well as cell cycle dysregulation resulting from the upregulation of Cyclin D1 protein.

PMID 42544649
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PubMedJACC. Case reports2026-07-30

Wide-Complex Tachycardia in a Neonate.

Aldawsari Khalifah A KA, Wilson Kelsey K, von Alvensleben Johannes C JC, Collins Kathryn K KK et al.

A 7-day-old previously healthy infant boy born at 36 6/7 weeks gestation was found in a routine well-child visit to have a heart rate of 208 beats/min. Electrocardiogram demonstrated a wide-complex tachycardia morphology while maintaining normal blood pressure and adequate perfusion. Wide-complex tachycardia in neonates is uncommon, with supraventricular tachycardia and aberrant conduction being the most frequent etiology. In the absence of congenital heart disease, a superior axis with right bundle branch block morphology on electrocardiogram is suggestive of fascicular ventricular tachycardia, for which verapamil is the preferred therapy.

PMID 42530181
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PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-07-30

Integrated Cantilever-MEA Platform for High-Sensitivity and Scalable Recording of Cardiomyocyte Electromechanics.

Sun Haolan H, Li Longlong L, Shanmugasundaram Arunkumar A, Kim Eung-Sam ES et al.

Preclinical screening is critical for reducing drug attrition; however, current electromechanical platforms are often restricted by the trade-off between miniaturization and force sensitivity. Miniaturizing sensor dimensions to enable high-throughput assays inherently increases structural stiffness, rendering conventional devices incapable of resolving the weak contractile forces of cardiomyocytes. Here, we report a miniaturized cantilever-MEA platform that overcomes this limitation to enable simultaneous, highly sensitive assessment of cardiomyocyte contractility and electrophysiology. By integrating an ultrathin nanosilicon piezoresistive strain sensor with an intrinsically compliant polymer microcantilever array, the device effectively decouples geometric scaling from sensitivity degradation. It detects cardiac forces down to 6.9 nN with a stress resolution of 0.042 nN µm-2, supporting high-density integration without compromising signal fidelity. Using neonatal rat ventricular myocytes and human induced pluripotent stem cell-derived cardiomyocytes, we evaluated functional parameters including contractile force, beating rate, and extracellular field potentials. Pharmacological testing with blebbistatin, verapamil, and astemizole produced distinct electromechanical response patterns consistent with their known mechanisms. In addition, continuous monitoring under doxorubicin exposure over 48 h captured time-dependent deterioration of both mechanical and electrical activity. This miniaturized dual-mode platform addresses the limitations of macroscopic bulk-averaging sensors, providing a scalable, label-free approach for mechanistic studies and next-generation cardiotoxicity screening.

PMID 42528395
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PubMedToxicological sciences : an official journal of the Society of Toxicology2026-07-30

Building structure activity relationships (SAR) to avoid toxicity due to unwanted CNS ion channel activity.

Zolkiewski Louisa A K LAK, Rockley Kimberly L KL, Roberts Ruth A RA, Jennings Hannah G HG et al.

We previously described an integrated in vitro liability assay for seizure, a new approach methodology (NAM) to reduce toxicity due to central nervous system (CNS) liability in drug discovery and development. Here we report the development of SAR (structure activity relationships) to guide drug design away from this liability. SAR test compounds were selected from the Enamine REadily AccesibLe (REAL) database using pharmacophore features and similarity to previous test compounds (amoxapine, diphenhydramine, quetiapine, 4-AP, linopirdine) or to ion channel positive reference compounds (bepridil, NS1619, quinidine, verapamil, XE991). These 88 compounds (10 parent compounds and 78 structurally related derivatives) were screened by automated electrophysiology in cell lines expressing human KV2.1, NaV1.2, the α1β2γ2 GABAA or α4β2 nicotinic receptors to generate IC50 values. Across all four ion channels, the derivative compounds exhibited increased, equivalent or reduced potency compared with the parent compounds, providing a complex and rich dataset for SAR. Regarding individual pharmacophoric features, statistical analysis identified 12 features significantly associated with activity at the α4β2 nicotinic receptor; 4 of these were also significantly associated with activity at KV2.1. Selected parent compounds (amoxapine, diphenhydramine, quetiapine) and structural analogues were screened for seizure-like activity in human induced pluripotent stem cell neurons using microelectrode array. The seizure-like phenotype was altered with the derivatives, as expected from the respective ion channel IC50 values. These data provide insight into specific substructures associated with seizure-like drug toxicity, offering the opportunity to avoid CNS liability in the development of novel compounds, saving time, money and resources.

PMID 42530889
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PubMedBiomolecules2026-07-28

Solvent-Free Mechanochemical Synthesis, Antispasmodic Activity, and Integrated In Silico Mechanistic Analysis of a Dapsone-Derived Phenylaminojuglone.

Zavaleta-Miñano Ricardo E RE, Mantilla-Rodríguez Elena E, Ybañez-Julca Roberto O RO, Asunción-Alvarez Daniel D et al.

The structural hybridization of bioactive quinones is a promising strategy for generating pharmacologically active compounds through sustainable synthetic approaches. This study aimed to synthesize and evaluate a dapsone-derived phenylaminojuglone as a potential intestinal smooth muscle relaxant. Juglone (AJ) was functionalized with dapsone (D) via a solvent-free mechanochemical aza-Michael reaction using silica gel as a mild acid catalyst. The resulting compound (AJ-D) was characterized and evaluated in isolated rat ileum preparations. Pharmacological studies were complemented by molecular docking, density functional theory (DFT) calculations, and in silico ADMET predictions. AJ-D was obtained with complete regioselectivity at the C-3 position and required shorter reaction times than conventional solution-based methods. The compound exhibited significant spasmolytic and antispasmodic effects under basal conditions and against acetylcholine- and KCl-induced contractions. Its relaxant activity was not significantly affected by muscarinic receptor blockade or K+ channel inhibition, whereas verapamil reduced its potency. Calcium reintroduction experiments suggested the involvement of extracellular Ca2+ influx pathways. Docking studies suggested favorable interactions with the CaV1.2 L-type calcium channel, whereas DFT and ADMET analyses indicated suitable electronic and drug-like properties. AJ-D is a promising juglone-derived scaffold with antispasmodic activity, likely associated with the modulation of extracellular calcium influx pathways involved in intestinal smooth muscle contraction.

PMID 42509837
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PubMedCephalalgia : an international journal of headache2026-07-27

Treatment patterns and Reasons for Discontinuing Preventive Treatment in Cluster Headache: A prospective cohort study.

Petersen Anja Sofie AS, Laursen Sophie Bryde SB, Søborg Marie-Louise Kulas MK, Barløse Mads M et al.

BackgroundPharmacological prevention of cluster headache aims to reduce the frequency and intensity of attacks, but the long-term effect and tolerance of treatments remain uncertain. The aim of the study was twofold. First, to quantify the discontinuation rates of preventive treatment due to side effects; and second, to assess the proportion of verapamil responders who maintained preventive effectiveness at follow-up.MethodsIn total, 596 participants with cluster headache fulfilling the ICHD-criteria (the baseline cohort) completed a semi-structured interview between 2017 and 2023. Of these, 430 were re-interviewed after a median time of 4.6 years constituting the follow-up cohort.ResultsIn the baseline cohort, 457 participants (76.7%) had taken a preventive medicine for cluster headache. Among these, 123 (26.9%) had discontinued a treatment due to intolerable side effects. The discontinuation rate for the first-line treatment verapamil was 18%, whereas the second-line treatments with lithium or topiramate had been discontinued in nearly half. The odds of discontinuing due to intolerable side effects of lithium or topiramate therapy were four times higher than for verapamil (p < 0.0001).In the follow-up cohort, only 143 participants (33.3%) still received a preventive treatment at the time of the second interview. Of the initial 182 verapamil users, 77 (42.3%) continued, 54 (29.7%) had discontinued due to remission, and 51 (28%) discontinued due to intolerable side effects, lack of effect, or for other reasons. At follow-up including new users, a total of 91 participants were treated with verapamil and 50 of them (54.9%) were 50% responders.ConclusionEffective therapeutic prevention of cluster headache is hindered by intolerance and insufficient efficacy of the available preventives. Though verapamil remains effective over time for initial responders, there is a high rate of discontinuation due to side effects or lack of efficacy. Taken together with the low proportion of 50% responders, the findings underscore the need for new tolerable and effective preventive treatment for cluster headache.

PMID 42506063
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