cilnidipine / Generic mfg. - LARVOL DELTA

EFFECT ON BP AND RENAL OUTCOMES WITH CILNIDIPINE-BASED THERAPY IN HYPERTENSIVE CKD PATIENTS WITH OR WITHOUT T2DM: A TWO-YEAR REAL-WORLD ANALYSIS (ISN-WCN 2026) - "Although the decline in urinary albumin excretion did not reach statistical significance between groups, the magnitude of reduction was clinically meaningful, reflecting cilnidipine's potential reno-protective action. These findings reinforce the benefits of cilnidipine-based therapy for hypertension management in CKD, offering sustained BP control with proteinuria reduction, particularly also valuable in those with concomitant diabetes."

Clinical • Real-world • Real-world evidence • Cardiovascular • Chronic Kidney Disease • Diabetic Nephropathy • Hypertension • Nephrology • Type 2 Diabetes Mellitus

TIRZEPATIDE FOR RESISTANT HYPERTENSION IN NON-DIABETIC IGA NEPHROPATHY (ISN-WCN 2026) - "SGLT2 inhibitors and spironolactone were previously discontinued due to recurrent balanoposthitis and hyperkalemia...BP normalized dramatically (200/100→118/70 mmHg, 82/30 mmHg reduction), achieving KDIGO targets and enabling 50% medication reduction (6→3 drugs: discontinued minoxidil, prazosin, clonidine; continued telmisartan, chlorthalidone, cilnidipine)...This represents a paradigm shift toward metabolic intervention in proteinuric non-diabetic CKD with obesity and resistant hypertension. GLP-1 receptor agonists merit investigation as cornerstone therapies alongside RAAS inhibitors and SGLT2 inhibitors, particularly in advanced fibrosis where immunosuppression risks may outweigh benefits."

Cardiovascular • Chronic Kidney Disease • Diabetic Nephropathy • Fibrosis • Genetic Disorders • Glomerulonephritis • Hypertension • IgA Nephropathy • Immunology • Lupus Nephritis • Obesity • Renal Disease

Hypertension Management Beyond Blood Pressure Control in India: An Expert Consensus on Angiotensin II Receptor Blocker and Calcium Channel Blocker Combination Therapy With Reference to Telmisartan and Cilnidipine. (PubMed, Cureus) - "Available evidence suggests that cilnidipine and telmisartan may offer potential benefits beyond BP reduction, largely based on pharmacologic properties and surrogate outcomes. Future large-scale, randomized, comparative outcome trials are needed to better define the relative clinical benefits of this combination."

Journal • Review • Cardiovascular • Chronic Kidney Disease • Diabetes • Hypertension • Metabolic Disorders • Nephrology • Renal Disease • Tobacco Cessation • Type 2 Diabetes Mellitus

Pharmacokinetic Insights and Therapeutic Potential of Calcium Channel Blockers in Cardiovascular and Non-Cardiovascular Disorders. (PubMed, Curr Pharm Des) - "Since the introduction of verapamil in the 1960s, newer drugs with improved selectivity and safety, such as cilnidipine and azelnidipine, have been developed. This review provides an updated overview of the pharmacokinetics, pharmacodynamics, and therapeutic applications of dihydropyridine and non-dihydropyridine CCBs, while identifying research gaps and future directions to enhance their clinical utility. By integrating established pharmacological knowledge with recent advances, this study underscores the continued relevance of CCBs in modern medicine."

Journal • PK/PD data • Cardiovascular • CNS Disorders • Genito-urinary Cancer • Hypertension • Oncology • Vascular Neurology

A fast method to predict solubility of neutral co-crystals in aqueous media. (PubMed, Eur J Pharm Sci) - "The method was validated using two example systems: carbamazepine-benzamide and cilnidipine-p-toluenesulfonamide, which are co-crystals of neutral components. The prediction method appears suitable for a fast and reasonably accurate estimation of co-crystal solubility during early phase of drug development and solid form selection. The method is currently limited to 1:1 co-crystals of neutral components."

Journal

RECONNOITER-1: A PHASE 2, PROSPECTIVE, BLINDED, RANDOMIZED, PARALLEL-GROUP AND CROSSOVER CLINICAL TRIAL EVALUATING AISA-021, A NOVEL CCB, IN SUBJECTS WITH RAYNAUD'S PHENOMENON (SSC-RP) (SSWC 2026) - "We studied AISA-021(cilnidipine), a dual N + L-type CCB approved for hypertension in Japan in 1995 for SSc-RP...In Part A, 27 patients from two sites were rando- mized into six groups of 10 mg, 20 mg with/without tadalafil 5mg and placebo... In this first-in-class clinical trial for CTD-RP, significant impact on symptoms with ORAL COMMUNICATIONS 87 minimal side effects was found. Dual N- and L-type channel blocking actions, versus primarily L-type activity of approved CCBs, may explain this. CCB's exacerbate GI symptoms and were improved here."

Clinical • P2 data • Cardiovascular • Fibrosis • Hypertension • Inflammatory Arthritis • Rheumatology

Repurposing Cilnidipine as an entry inhibitor against Crimean-Congo Hemorrhagic Fever pseudovirus infection. (PubMed, Arch Virol) - "Overall, this study highlights Cilnidipine as a promising repurposed antiviral candidate targeting viral entry pathways. The findings provide a foundation for future mechanistic and pre-clinical evaluations aimed at developing effective therapeutics against CCHFV."

Journal • Hematological Disorders • Infectious Disease

Relative Evaluation of the benefit of Cilnidipine ON the Nature, Observational Indices, Temperature changes, and overall Effect in secondary Raynaud’s disease (RECONNOITER-1) (ANZCTR) - P2 | N=36 | Completed | Sponsor: AISA Pharma Australia Pty. Ltd. | Recruiting ➔ Completed | N=76 ➔ 36

Enrollment change • Trial completion • Cardiovascular • Rheumatology

Greenness Assessment of HPLC-UV Method for Simultaneous Estimation of Four Antihypertensive Drugs. (PubMed, J Chromatogr Sci) - "An environmentally friendly HPLC method was developed to estimate angiotensin receptor blocker (telmisartan) and calcium channel blockers (cilnidipine, benidipine and azelnidipine) in a single run. To assess the environmental impact of the method, five greenness evaluation criteria, namely, the Green Analytical Procedure Index, Analytical GREEness, Chlortox Scale, Blue Applicability Grade Index, and Red-Blue-Green 12, were adopted. Concerning all the tools, the proposed method was found to be green."

Journal

Cilnidipine Cubosomal Nanogel Patch: Polymer-Nanostructure Synergy for Advanced Transdermal Drug Delivery. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "The safety and biocompatibility were analyzed by skin irritancy studies and histology of rat skin, which revealed that the transdermal patches were non-irritant and safe for skin application. The study demonstrates an innovative drug delivery approach using cubosomes in transdermal patches for improved permeability, therapeutic efficacy, and sustained release."

Journal

Cost-Effective, Scalable Synthesis of Cilnidipine Nanocrystals for Enhanced Oral Bioavailability and Hypertension Treatment. (PubMed, Drug Dev Ind Pharm) - "CLN-NCs significantly improved in vitro solubility and dissolution, demonstrating a scalable preparation method suitable for industrial translation. This approach offers a promising pathway to enhance CLN's therapeutic efficacy in hypertension management."

HEOR • Journal • Cardiovascular • Hypertension

Anti-inflammatory potential of telmisartan compared to other antihypertensives: secondary outcomes from a randomized trial. (PubMed, Inflammopharmacology) - "The anti-inflammatory markers were reduced in both groups at 12 weeks without any statistically significant difference across groups. However, telmisartan was associated with greater reductions in hsCRP, IL-6, and TNF-α in patients with T2DM and hypertension following 12 weeks of treatment. These findings may indicate a potential anti-inflammatory effect of telmisartan that requires confirmation in adequately powered trials."

Journal • Cardiovascular • Diabetes • Hypertension • Metabolic Disorders • Oncology • Type 2 Diabetes Mellitus • CRP • IL6 • PPARG • TNFA

LC-MS/MS-based simultaneous quantification of chlorthalidone and cilnidipine in rat plasma: Pharmacokinetic evaluation, green analytical assessment, and DoE-driven optimization. (PubMed, J Pharmacol Toxicol Methods) - "Detection was achieved in positive electrospray ionization mode using multiple reaction monitoring, with transitions of m/z 339.8909 → 85.0951 for chlorthalidone, m/z 493.5237 → 300.1587 for cilnidipine, and m/z 515.6423 → 342.6158 for telmisartan, employed as the internal standard. The method exhibited strong analyte stability and was successfully applied to the pharmacokinetic evaluation of both drugs in Wistar rats. This DoE-optimized LC-MS/MS platform offers a selective, reliable, and environmentally conscious analytical solution for the preclinical assessment of chlorthalidone and cilnidipine."

Journal • PK/PD data • Preclinical

Patterns of Prescription Switching in a Uniform-Pricing System for Multi-Source Drugs: A Retrospective Population-Based Cohort Study. (PubMed, Healthcare (Basel)) - "Switching rates varied substantially (coefficient of variation = 227%) by physician practice setting (e.g., public health center branches: 26%; tertiary hospitals: 15%) and by drug market size (e.g., glimepiride: 29%; cilnidipine: 1%). In Korea, physicians frequently switch prescriptions between originator and generic drugs, even as generic substitution at the pharmacy level remains uncommon. The substantial variation in MSPS across provider settings and drug markets-but not by patient characteristics-underscores the need for targeted pharmacy benefit policies to promote effective substitutability and competition among multi-source drugs."

Journal • Pricing • Retrospective data • Cardiovascular • Diabetes • Hypertension • Metabolic Disorders

Green and White Analytical Chemistry: Advances, Comparisons, Future Perspectives, and a Proposal for Green Financing Model for Analytical Chemistry. (PubMed, J Pharm Sci) - "We analyze WAC's aspects within the development of stability-indicating High-Performance Thin-Layer Chromatography (HPTLC) methods for thiocolchicoside and aceclofenac. We further illustrate WAC's practical utility through the development of a green RP-HPLC method for azilsartan, medoxomil, chlorthalidone, and cilnidipine in human plasma, where a WAC-assisted AQbD strategy led to a validated, sustainable, and cost-effective procedure with an excellent white WAC score...This paper conducts a NOISE (needs, opportunities, improvements, strengths, exceptions) analysis of WAC, emphasizing the change it brings to existing Green Analytical Chemistry methodology. Finally, it proposes Green Financing for Analytical Chemistry (GFAC), a dedicated funding model designed to promote innovations which are aligned to GAC and WAC goals and bridge the gaps in current practices."

Financing • Journal • Review

Relative Evaluation of the benefit of Cilnidipine ON the Nature, Observational Indices, Temperature changes, and overall Effect in secondary Raynaud’s disease (RECONNOITER-1): Part B (ANZCTR) - P2 | N=38 | Recruiting | Sponsor: AISA Pharma Australia Pty. Ltd.

New P2 trial • Cardiovascular • Rheumatology

Reversion of a RND transporter pseudogene reveals latent stress resistance potential in Brucella ovis. (PubMed, PLoS Genet) - "Conversely, deleting bepE in Brucella abortus, a closely related zoonotic species that retains an intact version of the gene, increased its sensitivity to envelope disruptors in vitro and to cilnidipine in the intracellular niche. We conclude that bepE is a key determinant of chemical stress resistance in Brucella spp., and that its pseudogenization in B. ovis contributes to the documented hypersensitivity of this host-restricted lineage to chemical stressors."

Journal • Immunology

Reversion of a RND transporter pseudogene uncovers latent stress resistance in Brucella ovis. (PubMed, bioRxiv) - "To investigate the genetic basis of B. ovis susceptibility to dihydropyridine treatment, we selected for mutants capable of growing in the presence of cilnidipine...In other Brucella species, bepE remains intact, and we show that deleting this gene in the zoonotic pathogen Brucella abortus increases susceptibility to both dihydropyridine treatment and membrane-disrupting stress. Our study provides evidence that pseudogenes like bepE can serve as a latent reservoir of adaptive functions in B. ovis , including drug and stress resistance."

Journal • Cardiovascular • Hypertension • Immunology

Mechanistic investigation of methadone, tolfenamic acid, and cilnidipine in traumatic brain injury: a novel multi-target perspective outcome of network pharmacology. (PubMed, Inflammopharmacology) - "This study identified a primary target for MTD such as NOS1, NOS2, NOS3, DRD2, DAT (SLC6A3), MPO, SLC6A4, CXCR4-C-X-C, AKT1, SLC/8A2, HTR1A; for TA: MAPK1, GRIN1 and for CLD: IGF1R, DRD2, SHH, MAP2K1, CACNA1D, HTR2A, PDE4D, CASP3, MTOR, FASN, PTGS2, SCN9N, CNR1, CACNA1C, ABCB1, PIK3CA, GSK3B in the mechanistic regulation of TBI by reducing the activation of several pathways linked to development of TBI."

Journal • CNS Disorders • Vascular Neurology • ABCB1 • CASP3 • CXCR4 • DRD2 • FASN • HTR2A • MAP2K1 • MAPK1 • NOS1 • NOS2 • NOS3 • PACERR • PIK3CA • PTGS2 • SLC6A3 • SLC6A4

Thermodynamic Perspectives on the Impact of a Second Drug on Amorphous Drug Solubility. (PubMed, Mol Pharm) - "In this study, we experimentally determined how a second drug affects the amorphous solubility of ritonavir (RTV) and analyzed these effects from a thermodynamic perspective. Lopinavir (LPV), cilnidipine (CND), and probucol (PBC) were used as second drugs...In contrast, in the RTV/PBC system, the water content of the RTV-rich phase was more substantially decreased, leading to a higher experimentally determined value of RTV amorphous solubility than that predicted by ideal mixing of RTV and PBC. Overall, this study elucidates the impact of a second drug on the amorphous solubility of a primary drug and provides valuable insights for the design of supersaturated formulations containing multiple drugs."

Journal

Discovery of Cilnidipine Cocrystals with Enhanced Dissolution by the Use of Computational Tools and Semiautomatic High-Throughput Screening. (PubMed, Cryst Growth Des) - "Dissolution rates of drug and coformer were compared for better mechanistic understanding of the cocrystal dissolution-supersaturation-precipitation behavior. The case of cilnidipine with a rare occurrence of cocrystals emphasized the importance of using joint computational and HTS approaches to enable successful cocrystal identification for pharmaceutical development."

Journal

Cilnidipine: An L- and N-Type Blocker of Calcium Channels Ameliorating Renal Damage in Experimental Hypertensive Rats. (PubMed, Cureus) - "These results showed that in hypertensive experimental rats, cilnidipine, apart from its hypotensive actions, decreases proteinuria and urinary creatinine and Ang II levels. These actions of cilnidipine may be because of blocking N-type calcium channels. Therefore, cilnidipine dual L/N type CCB may act as a renoprotective drug and decrease glomerular damage. Further mechanistic studies using selective N-type channel blockers or knockout mice are needed to prove the findings."

Journal • Preclinical • Renal Disease

Formulation and evaluation of HPMC and pullulan-based rapidly dissolving films containing cilnidipine nanosuspension. (PubMed, Int J Biol Macromol) - "The CLD NS-RDF exhibited a significant increase in AUC0-24h, Cmax, and a decrease in Tmax and MRT as compared to the CLD CD-RDF. The CLD NS-RDF also had a superior effect to control the blood pressure in rats as compared to the CLD CD-RDF."

Journal • Cardiovascular • Hypertension

Synergistic action of cilnidipine and bexarotene in mitigating cholestatic liver damage: role of FXR signaling cascade. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Furthermore, the combined treatment upregulated the expression of FXR and its target genes, suggesting that the protective effects may be mediated through the activation of the FXR signaling cascade. These findings highlight the potential of cilnidipine and bexarotene as a novel therapeutic approach for the management of cholestatic liver disorders and provide insights into the underlying molecular mechanisms involving the FXR signaling pathway."

Journal • Cholestasis • Hepatology • Inflammation

Cilnidipine exerts antiviral effects in vitro and in vivo by inhibiting the internalization and fusion of influenza A virus. (PubMed, BMC Med) - "These findings highlight the promising anti-IAV properties of cilnidipine both in vitro and in vivo, suggesting its potential as a clinical agent for emergencies against influenza outbreaks."

Journal • Preclinical • Infectious Disease • Influenza • Respiratory Diseases