Lacidip (lacidipine) / Incepta Pharma - LARVOL DELTA

Impact of antihypertensive treatment on cardiovascular event reduction in patients with asymptomatic carotid artery stenosis: a systematic review and meta-analysis. (PubMed, Pan Afr Med J) - "The results reported that enalapril and fosinopril demonstrated dual benefits in blood pressure (BP) reduction and vascular remodeling, though meta-analysis showed statistically insignificant improvements in regional cerebral blood flow (CI: -0.84, 6.08, P = 0.14, I2= 94%). Similarly, isradipine, lacidipine, and amlodipine improved carotid hemodynamics and cerebral perfusion, with meta-analysis favoring calcium channel blocker intervention for blood pressure management (CI: -3.25 to 7.64, P = 0.43)...Moreover, beta-blockers showed specific benefits, with metoprolol improving plaque echogenicity (57.3 ± 16.8 vs. 51.8 ± 20.0, p = 0.006) and reducing cardiovascular events (17% vs. 37% placebo, p = 0.011), while labetalol effectively managed post-endarterectomy hypertension. In conclusion, antihypertensive treatments showed varying effectiveness in cardiovascular event reduction and improvements in vessel measures."

Clinical • Journal • Retrospective data • Review • Atherosclerosis • Cardiovascular • Hypertension

Inhibition of HIV-1 replication by primer RNA packaging inhibitors. (PubMed, mBio) - "In this study, we isolated molecules that inhibit viral replication by inhibiting the incorporation of tRNA3Lys into virions. The inhibitors of HIV-1 replication described in this work demonstrate that the HIV-1 tRNA packaging step can be exploited for the development of a new family of drugs with novel resistance profiles."

Journal • Human Immunodeficiency Virus • Infectious Disease

Network analysis of gene expression reveals regulators of cell viscosity and mechanical phenotype. (PubMed, Sci Rep) - "We investigated the up- and down-regulation of expression by two predicted potential small molecule regulators (lacidipine and AG879) and four predicted potential gene regulators (AKT2, ITGB6, mir-183, and CD82) through small molecule inhibition, RNA interference, and introduction of microRNAs. The effects of modulation of these regulators were measured on both cell mechanical properties and gene expression in three ovarian cancer cell types. We identified several regulators that change the viscosity and stiffness of the cell with a corresponding change to the functional migratory ability in a cell-type specific manner."

Journal • Oncology • Ovarian Cancer • Solid Tumor • AKT2 • ITGB6 • MIR183

Green first derivative synchronous spectrofluorimetric determination of lacidipine and its acid degradation product in plasma and mixtures. (PubMed, Sci Rep) - "Peak amplitude of the first derivative synchronous was measured at 409 nm by using constant wavelength difference (Δλ = λem - λex = costant) which equal 160 nm. The regression plot of the proposed first derivative synchronous spectrofluorimetric method was found to be linear over the range of 50-300 ng/mL with a determination coefficient equals 0.9997, limit of detection (LOD) was 14.51 ng/mL but limit of quantification (LOQ) was 43.97 ng/mL."

Journal

Identification of the Most Sensitive and Specific IHC Markers in Differential Diagnosis of Endocervical Gastric-Type adenocarcinoma (USCAP 2025) - "Immunohistochemical stains (IHC) for Caldine18.2, MUC6, P53, P16 were performed for all cases... Claudin 18.2 is a sensitive and specific marker for cervical gastric-type glandular lesions. It is not expressed in normal cervical tissues and 100% expressed in LEGH/ALEGH, but could not differentiate GAS from ALEGH. MUC6 is a very sensitive marker for both LEGH and GAS, but specificity is much lower than Claudin18.2."

Cervical Adenocarcinoma • Cervical Cancer • Gastric Cancer • Oncology • CLDN18 • Mucin 6 • TP53

Assessing the environmental impact of medicines in Italy using data from the Italian Medicines Agency. (PubMed, Br J Clin Pharmacol) - "This study points to the need for prioritizing targeted sampling in surface waters for medicines estimated at high risk. To prevent and mitigate the risk, a more conscious clinical practice coupled with appropriate waste management are required."

Journal • Cardiovascular • Pain

Efficacy and Safety of Dihydropyridine Calcium Channel Blockers for Primary Hypertension: A Bayesian Network Meta-analysis. (PubMed, Curr Hypertens Rev) - "In the office setting, levamlodipine may be the best treatment for primary hypertension, and lacidipine shows good safety."

Clinical • Journal • Retrospective data • Cardiovascular • Hypertension

Exploration of Enalapril-Lacidipine Co-Amorphous System with Superior Dissolution, In vivo Absorption and Physical Stability via Incorporated into Mesoporous Silica. (PubMed, Eur J Pharm Sci) - "Raman mapping revealed that the less microstructure phase separation could be the main reason for the better stability in presence of mesoporous SiO2. In conclusion, ENP could be successfully used as a potential co-former to fabricate co-amorphous system with poorly water-soluble drugs and collaborates the co-amorphous with mesoporous SiO2 become a promising strategy to achieve stable amorphous formulation for further enhancement of dissolution rate and bioavailability."

Journal • Preclinical

UHPLC-MS/MS method for the simultaneous quantification of five calcium channel antagonists' drugs in human plasma. (PubMed, Biomed Pharmacother) - "Drug concentrations in the patient's serum or urine (also known as therapeutic drug monitoring, or TDM) and blood pressure measurements following supervised medication ingestion are two techniques for assessing treatment adherence. In alignment with guideline from the Food and Drug Administration (FDA) and European Medicines Agency (EMA), this study aims to design, develop, and validate a single UHPLC method for the plasma quantification of five antihypertensive drugs within the calcium channel blocker class: amlodipine, nifedipine, barnidipine, lercanidipine and lacidipine."

Journal • Cardiovascular • Hypertension

Novel ecofriendly spectrophotometric methods for the determination of six dihydropyridines calcium channel blockers through derivatization with sulfophtalein dye: application to tablet analysis. (PubMed, BMC Chem) - "Novel, «green» and simple visible spectrophotometric procedures for the determination of six dihydropyridines CCBs (amlodipine besylate (AML), lacidipine (LAC), levamlodipine besylate (LAML), nifedipine (NIF), nimodipine (NIM) and nitrendipine (NIT)) through derivatization with the sulfophthalein dye bromophenol blue (BPB) have been developed. The developed methods are colorimetric and therefore does not require a UV instrument to quantify these drugs. The proposed approach was more efficient in terms of time reliability, sensitivity and «greenness» than other recorded spectrophotometric methods and can be easily implemented for routine pharmaceutical analysis."

Journal • Acute Myelogenous Leukemia

Calcium Channel Blocker Lacidipine Promotes Antitumor Immunity by Reprogramming Tryptophan Metabolism. (PubMed, Adv Sci (Weinh)) - "Mechanistically, lacidipine targets calcium channels (CaV1.2/1.3) to inhibit Pyk2-JAK1-calmodulin complex-mediated IDO1 transcription suppression, which suppresses the kynurenine pathway and maintains the total nicotinamide adenine dinucleotide (NAD) pool by regulating NAD biosynthesis. These results reveal a new function of calcium channels in IDO1-mediated tryptophan metabolism in tumor immunity and warrant further development of lacidipine for the metabolic immunotherapy in breast cancer."

IO biomarker • Journal • Breast Cancer • Immunology • Oncology • Solid Tumor • IDO1 • JAK1

Reproducibility and Treatment Effect on Office and Ambulatory Pressure Relation. (PubMed, Hypertension) - "In 2397 patients of the ELSA (European Lacidipine Study on Atherosclerosis) and PHYLLIS (Plaque Hypertension Lipid-Lowering Italian Study) trials, we calculated the office and 24-hour BP relationship according to the linear regression model, with office systolic BP as the independent variable, at baseline and yearly during a 3-year treatment...In treated patients with hypertension the slope of the office/24-hour BP linear regression is reproducible over time. However, the slopes are steeper in untreated individuals, indicating that information on ambulatory BP values corresponding to office BP values can be more accurate if separately estimated in these 2 conditions."

Journal • Atherosclerosis • Cardiovascular • Dyslipidemia • Hypertension

Data mining of PubChem bioassay records reveals diverse OXPHOS inhibitory chemotypes as potential therapeutic agents against ovarian cancer. (PubMed, J Cheminform) - "Two of these four compounds, lacidipine and esbiothrin, increased in intracellular oxygen radicals (a major hallmark of most OXPHOS inhibitors) and decreased the viability of two ovarian cancer cell lines, ID8 and OVCAR5...We believe the procedure may be more broadly applied to guide compound selection in early-stage hit finding on novel multi-protein mechanistic or phenotypic targets. To demonstrate the utility of our approach, we apply a data mining strategy on a large set of public assay data to find drug-like molecules that inhibit oxidative phosphorylation (OXPHOS) as candidates for ovarian cancer therapies."

Journal • Oncology • Ovarian Cancer • Pain • Solid Tumor

Accurate determination of three new antihypertensive drugs illegally added to food using ultra-high performance liquid chromatography-tandem mass spectrometry (PubMed, Se Pu) - "In this study, a novel ultra-high performance liquid chromatography-triple-quadrupole mass spectrometry (UHPLC-MS/MS) method was developed for the simultaneous determination of three antihypertensive drugs (azilsartan, candesartan cilexetil, and lacidipine) in 12 food matrices (pressed candies, solid beverages, alternative teas, tea drinks, biscuits, jellies, mixed liquors, oral liquids, medicinal teas, tablets, hard capsules, and soft capsules). Overall, the newly developed method is simple, rapid, sensitive, accurate, and suitable for the qualitative and quantitative determination of antihypertensive drugs in different food matrices. This work could provide technical support for food safety agencies in implementing measures against the illegal addition of antihypertensive drugs to food."

Journal

Lacidipine Inhibits NF-κB and Notch Pathways and Mitigates DSS-Induced Colitis. (PubMed, Dig Dis Sci) - "Lacidipine demonstrated a protective effect in UC, reducing inflammation and modulating key signaling pathways. These findings suggest that lacidipine could be a promising candidate for the treatment of UC."

Journal • Cardiovascular • Colorectal Cancer • Gastroenterology • Gastrointestinal Disorder • Hypertension • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis • NFKBIA

Data mining of PubChem bioassay records reveals diverse OXPHOS inhibitory chemotypes with potential as therapeutic agents against ovarian cancer (ACS-Fall 2024) - "Two of these four compounds, lacidipine and esbiothrin, increased in intracellular oxygen radicals (a major hallmark of most OXPHOS inhibitors) and decreased the viability of two ovarian cancer cell lines, ID8 and OVCAR5. Finally, data from the pipeline were used to train random forest and support vector classifiers that effectively prioritized OXPHOS inhibitory compounds within a held-out test set (ROCAUC 0.962 and 0.927, respectively) and on another set containing 44 documented OXPHOS inhibitors outside of the training set (ROCAUC 0.900 and 0.823). This prototype pipeline is extensible and could be adapted for focus screening on other phenotypic targets for which sufficient public data are available."

Oncology • Ovarian Cancer • Pain • Solid Tumor

Calcium-channel blockers chyloperitoneum: an underrated complication in peritoneal dialysis (ERA-EDTA 2024) - "All of them were affected by hypertension and 10 of 16 (2 APD and 8 CAPD) were already in chronic therapy with CCBs (5 with lercanidipine, 4 with lacidipine and 1 with barnidipine), all at maximum accepted dosage. cloudy peritoneal effluent is always cause for concern for Nephrologists since that it could represent, event without any other sign or symptom of infection, an already subclinical bacterial peritonitis. Most of dialysis patients are also affected by hypertension. Since usage of ARB and ACE-I is limited by risk of hyperkalaemia, CCBs represents one of the most prescribed antihypertensive drugs."

Cardiovascular • Hypertension • Infectious Disease • Nephrology • Pain • Pancreatitis

Lacidipine, thiamine pyrophosphate and their combination on the ocular ischemic syndrome induced by bilateral common carotid artery ligation. (PubMed, Int J Ophthalmol) - "As a result of the study, it is concluded that LTC may be more effective than lacidipine and TPP alone in treating ocular ischemic syndrome."

Journal • Anesthesia • Cardiovascular • Ocular Inflammation • Oncology • Retinal Disorders • CAT • IL1B • IL6 • TNFA

Effects of adenosine triphosphate, Lacidipine, and Benidipine on 5-fluorouracil-induced kidney damage in rats. (PubMed, Eur Rev Med Pharmacol Sci) - "It may be possible to prevent nephrotoxicity by adding ATP + Benidipine or ATP to 5-FU treatment."

Journal • Preclinical • CAT

Fabrication, optimization, and evaluation of lyophilized lacidipine-loaded fatty-based nanovesicles as orally fast disintegrating sponge delivery system. (PubMed, Int J Pharm) - "In the In-vivo pharmacokinetic study in rabbits, the LY-OFDS showed 4.7-fold higher bioavailability compared with the marketed oral tablet. In conclusion, the LY-OFDS loaded with LCD-FNVs is a safe, and non-invasive approach that can deliver LCD effectively to the blood circulation via the buccal mucosa giving superior immediate capabilities of lowering high blood pressure and increasing the drug bioavailability."

Journal • Cardiovascular • Hypertension

Ternary solid dispersions of lacidipine: Enhancing dissolution and supersaturation maintenance through strategic formulation optimization. (PubMed, Int J Pharm) - "The formation of intermolecular hydrogen bonding within the molecules of the ternary solid dispersions significantly enhanced drug solubility and system stability. Strategic formulation optimization, coupled with judicious selection of suitable carrier types and ratios, may serve as a promising approach for designing supersaturated drug delivery systems."

Journal

Dinotefuran exposure alters biochemical, metabolomic, gut microbiome, and growth responses in decapoda pacific white shrimp Penaeus vannamei. (PubMed, J Hazard Mater) - "Biomarkers erythromycin-N-demethylase, alanine aminotransferase, and catalase increased in all exposed groups, while glutathione S-transferase is the opposite; aminopyrin-N-demethylase, malondialdehyde, and aspartate aminotransferase increased at 60 and 600 μg/L. The WGCNA results revealed a highly significant negative correlation between two key metabolites, caldine and indican, and the gut microbiota within co-expression modules. Overall, the risk of dinotefuran exposure to non-target organisms in aquatic environments still requires further attention."

Journal • Infectious Disease • CAT

Drug clustering to anticipate new aspects of drug safety profile: application to gabapentinoids and other voltage-gated calcium channel ligand drugs. (PubMed, Br J Clin Pharmacol) - "The safety profile of gabapentinoids overlaps with the one of some dihydropyridine CCBs and Ca -blocking anticonvulsants. These results could be used to anticipate some unidentified ADRs of gabapentinoids from information accumulated with older drugs and sharing a common molecular target and ADR signature."

Journal • Ataxia • Cardiovascular • Movement Disorders

Formulation and Characterization of Nanoparticulate Drug Carrier System for Lacidipine. (PubMed, Assay Drug Dev Technol) - "Short-term stability studies conducted on films at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months demonstrated no significant variation in morphological and mechanical properties. Therefore, lacidipine-loaded cubosomal rapid dissolving oral films may be a promising formulation approach for the management of hypertension."

Journal • Cardiovascular • Hypertension

Data mining of PubChem bioassay data reveals OXPHOS inhibitory chemotypes that promote oxidative stress responses in ovarian cancer cell lines (ACS-Fall 2023) - "Active compound clusters frequently contain α/β-unsaturated carbonyl groups, which are also observed in both endogenous quinone electron carriers and atovaquone–a potent inhibitor of OXPHOS. Treatment with oryzalin, allylestrenol, esbiothrin, and lacidipine decreased basal respiration rates and ATP production in ID-8 cells. Thus, 4 of 6 compound classes prioritized by the pipeline show inhibitory effects against ovarian cancer cells."

Oxidative stress • Preclinical • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Solid Tumor