cilnidipine / Generic mfg. - LARVOL DELTA

A Re-Analysis of the RECONNOITER Phase 2 Trial of AISA-021 in the Treatment of Raynaud's Phenomenon Associated with Systemic Sclerosis - The Effects of Non-Specific Symptoms on Endpoints in Studies of Raynaud's Therapies (ACR Convergence 2026) - "The re-analysis using the specific attack definition suggested a stronger treatment effect than had been found with the non-specific attack definition and greatly decreased the variability and standard error associated with attack reporting, resulting in finding a reduction in weekly attack frequency that achieved statistical significance. Of the 31 patients in the study who received treatment with both AISA-021 and placebo treatment in either sequence in the crossover study, 4/31 (13%) saw a complete resolution of attacks while on AISA-021 and 9/31 (29%) had a reduction of 70% or more while being treated with cilnidipine. Regression to the mean could account for the improved placebo effect seen in period 2, though the treatment effect seen of AISA-021 when given in Period 2 was slightly less than seen in period 1."

P2 data • Cardiovascular • Immunology • Rheumatology • Scleroderma • Systemic Sclerosis

Ambulatory Blood Pressure Comparison of Amlodipine, Cilnidipine, and Azelnidipine in Hypertension: The AMCILAZ-EH Multicentre, Prospective, Observational Study. (PubMed, Cureus) - "However, these findings should be interpreted in the context of the limited sample size and reduced statistical power. Larger randomized studies with possible home BP monitoring are required."

Journal • Observational data • Cardiovascular • Hypertension

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 | Completed | Sponsor: AISA Pharma Australia Pty. Ltd. | Recruiting ➔ Completed

Trial completion • Cardiovascular • Rheumatology

Preclinical Evaluation of Cilnidipine Nanosponges for Enhanced Oral Bioavailability and Sustained Antihypertensive Efficacy. (PubMed, Ann Pharm Fr) - "CIL-NS significantly improved oral bioavailability with a 2.65-fold increase in systemic exposure, prolonged drug release, and enhanced antihypertensive efficacy without altering elimination kinetics, thereby demonstrating its potential as a promising oral nanosponge delivery system for dose reduction and improved patient compliance in hypertension management."

Journal • Preclinical • Cardiovascular • Hypertension

Effectiveness and Safety of Telmisartan Plus Amlodipine Compared to Telmisartan Plus Cilnidipine in Indian Patients with Hypertension and Renal Impairment: A Randomized, Open Label, Post Marketing Study (START Renal). (PubMed, Int J Nephrol Renovasc Dis) - "Both the TA and TC FDCs were effective and well tolerated when treating hypertension with renal impairment. The TA FDC may provide better BP reduction with similar reno-protective benefits than the TC FDC."

Clinical • Journal • P4 data • Cardiovascular • Hypertension • Renal Disease

Pharmacokinetic Studies and Toxicity Assessment of Nisoldipine and Cilnidipine Analogues for Drug Development. (PubMed, Cardiovasc Hematol Disord Drug Targets) - "More rapid absorption and action may offer quicker control of blood pressure and relief of symptoms in acute angina or hypertensive crises. The short elimination half-life (t½) observed indicates that multiple dosing and/or modified-release formulations may be required to maintain clinical benefit. The Nisoldipine and Cilnidipine ODT analogues show potential for further preclinical cardiovascular drug development."

Journal • PK/PD data • Cardiovascular

Telmisartan vs. other antihypertensives on cardiometabolic and vascular outcomes in diabetic hypertension: A randomised trial. (PubMed, Indian J Med Res) - "Seventy eligible patients were enrolled and randomised 1:1 to receive telmisartan (n=34) or other antihypertensive agents (amlodipine, n=22; cilnidipine, n=12; ramipril, n=2; total n=36) for 12 weeks. However, the reduction in ET-1 levels was similar across groups, suggesting a comparable effect on endothelial function over 12 weeks. These findings suggest that, beyond its antihypertensive action, telmisartan may offer favourable metabolic benefits that could help limit diabetes-related micro- and macrovascular complications compared with other commonly prescribed antihypertensives."

Clinical • Journal • Cardiovascular • Diabetes • Hypertension • Metabolic Disorders • Type 2 Diabetes Mellitus • EDN1

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