levocabastine / Generic mfg. - LARVOL DELTA

Montelukast sodium combined with levocabastine nasal spray demonstrates high efficacy in treating pediatric allergic rhinitis. (PubMed, Am J Transl Res) - "The combination of MKS and LEVO nasal spray demonstrates superior efficacy and safety in pediatric AR treatment, significantly improving patients' quality of life. Moreover, treatment failure is closely linked to passive secondhand smoke exposure and elevated EOS levels."

Journal • Allergic Rhinitis • Conjunctivitis • Dental Disorders • Dermatology • Gastrointestinal Disorder • Immunology • Inflammation • Ocular Infections • Ocular Inflammation • Ophthalmology • Pain • Pediatrics • Pruritus • Xerostomia • CXCL8 • IL10 • IL4

Levocabastine ameliorates cyclophosphamide-induced nephrotoxicity in Swiss albino mice via NF-κB/cleaved caspase-3/TGF-β signaling pathways. (PubMed, Drug Res (Stuttg)) - "LEV (0.05 and 0.1 mg/kg, i.p.) and fenofibrate (FF) (80 mg/kg, p.o.) were given daily for 14 days. LEV 0.1 and FF 80 significantly reversed these changes toward normal and showed nephroprotective potential. Thus, seeing the protective effect of LEV on CP-intoxicated mice, we conclude that LEV may be used as an adjuvant with CP in cancer, however, it needs more studies with the direct cancer model to confirm the claim."

Journal • Preclinical • Fibrosis • Immunology • Oncology • CASP3 • CAT • IL1B • IL6 • TGFB1 • TNFA

Levocabastine ameliorates cyclophosphamide-induced hepatotoxicity in Swiss albino mice: modulation of Nrf2, NF-κB p65, cleaved caspase-3 and TGF-β signaling molecules. (PubMed, J Mol Histol) - "LEV can be helpful as an adjuvant in cancer patients who are on CP treatment, to minimize toxicity. However, its role in in-vivo cancer model is further needed to be confirmed."

Journal • Preclinical • Fibrosis • Hepatology • Immunology • Inflammation • Liver Failure • Oncology • CASP3 • CAT • IL1B • IL6 • NFE2L2 • NFKB1 • TGFB1 • TNFA

Evaluation methods using tear volume in a conjunctivitis mice model. (PubMed, J Pharmacol Toxicol Methods) - "Furthermore, levocabastine inhibited the increase in tear volume in antigen-induced allergic conjunctivitis and histamine- and compound 48/80-induced conjunctivitis models...Evaluation of tear volume in a conjunctivitis mice model is highly quantitative; therefore, it is possible to evaluate drug efficacy. This is considered a useful index compared with conventional methods."

Journal • Preclinical • Conjunctivitis • Inflammation • Ocular Infections • Ocular Inflammation • Ophthalmology

Levocabastine ameliorates cyclophosphamide-induced cardiotoxicity in Swiss albino mice: Targeting TLR4/NF-κB/NLRP3 signaling pathway. (PubMed, Toxicol Appl Pharmacol) - "LEV and fenofibrate (FF) treatment reversed these changes towards normal and showed a significant protective effect against CP. The results showed the protective role of LEV in restoring CP-induced cardiotoxicity in terms of inflammation, apoptosis, oxidative stress, cardiac injury and histopathological damage. Thus, levocabastine can be used as an adjuvant to cyclophosphamide in cancer treatment but a thorough study with various animal cancer models is further needed to establish the fact."

Journal • Preclinical • Cardiovascular • Fibrosis • Hematological Disorders • Inflammation • Oncology • CASP3 • IL1B • IL6 • NFKB1 • NLRP3 • TLR4 • TNFA

The Efficacy of Budesonide, Levocabastine, and Their Combination in Treatment of Vasomotor Rhinitis. (PubMed, ORL J Otorhinolaryngol Relat Spec) - "Budesonide or levocabastine hydrochloride alone improved the nasal symptoms of patients with vasomotor rhinitis and reduced the levels of ECP, HA, LTB4, and VIP in nasal secretions. However, their combination improved the symptoms of patients more significantly than each drug alone."

Journal • Inflammation

In-silico identification of novel DDI2 inhibitor in glioblastoma via repurposing FDA approved drugs using molecular docking and MD simulation study. (PubMed, J Biomol Struct Dyn) - "Here in this study, we performed molecular docking against DDI2 with the 20 FDA-approved drugs and identified Alvimopan and Levocabastine as the top two compounds with the best binding score along with the standard drug Nelfinavir. MD simulation (100 ns) of these protein-ligand docked complexes reveals that the stability and compactness of Alvimopan are high in comparison with Nelfinavir. Our in-silico (Molecular docking and Molecular dynamics simulation) studies pointed out that Alvimopan may be repurposed as a DDI2 inhibitor and can be used as a potential anticancer agent for the treatment of brain tumors.Communicated by Ramaswamy H. Sarma."

FDA event • Journal • Brain Cancer • CNS Tumor • Glioblastoma • Oncology • Solid Tumor • Targeted Protein Degradation • NRF1

Design, Synthesis, and Biological Evaluation of the First Radio-Metalated Neurotensin Analogue Targeting Neurotensin Receptor 2. (PubMed, ACS Omega) - "Efflux was as high as 66 ± 9% at 45 min for [Ga]Ga-JMV 7488 on HT-29 and increased for [In]In-JMV 7488 up to 73 ± 16% on HT-29 and 78 ± 9% on MCF-7 cells at 2 h. Maximum intracellular calcium mobilization of JMV 7488 was 91 ± 11% to that of levocabastine, a known NTS agonist on HT-29 cells demonstrating the agonist behavior of JMV 7488...Significant uptake was also depicted in lungs. Interestingly, mice prostate also demonstrated [Ga]Ga-JMV 7488 uptake although the mechanism was not NTS-mediated."

Journal • Addiction (Opioid and Alcohol) • Breast Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatology • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Prostate Cancer • Solid Tumor

A mouse model of allergic conjunctivitis permitting tear eosinophil quantification. (PubMed, J Pharmacol Toxicol Methods) - "This method may be useful for evaluation of the symptoms of allergic conjunctivitis. in experimental and clinical settings. In particular, the developed method, which measures the number of eosinophils in tears collected with phenol red threads, may enable the quantitative, objective, and noninvasive evaluation of the severity of allergic conjunctivitis."

Journal • Preclinical • Conjunctivitis • Inflammation • Ocular Infections • Ocular Inflammation • Ophthalmology

Bioactive components of different nasal spray solutions may defeat SARS-Cov2: repurposing and in silico studies. (PubMed, J Mol Model) - "In this study, three bioactive components namely ciclesonide (8), levocabastine (13), and triamcinolone acetonide (16) have been found as promising inhibitory agents against SARS-CoV2 spike and human ACE2 receptor proteins with excellent binding affinities, comparing to reference drugs such as nafamostat, arbidol, losartan, and benazepril. Furthermore, MD simulations were performed (triplicate) for 100 ns to confirm the stability of 8, 13, and 16 with said protein targets and to compute MM-PBSA-based binding-free energy calculations. Thus, bioactive components 8, 13, and 16 open the door for researchers and scientist globally to investigate them against SARS-CoV2 through in vitro and in vivo analysis."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

The add-on effect of an intranasal antihistamine with an intranasal corticosteroid in Japanese cedar pollinosis. (PubMed, Auris Nasus Larynx) - "The intranasal antihistamine provided better control of not only nasal symptoms, but also of ocular symptoms, and decreased the need for rescue medications when added to intranasal corticosteroid treatment in JCP patients."

Journal • Allergic Rhinitis • Immunology • Inflammation

Neurotensin and xenin stimulates pancreatic exocrine secretion through the peripheral cholinergic nerves in conscious sheep. (PubMed, Gen Comp Endocrinol) - "A single intravenous injection of NTR-2 agonist levocabastine at 0.1-3 nmol /kg did not alter pancreatic exocrine secretion. These results suggest that both NT and xenin-25 effectively stimulates pancreatic exocrine secretion through the peripheral cholinergic system in sheep and that NTR-2 is not involved in the regulation of pancreatic exocrine secretion, however, we did not precisely determine the role of NTR-1 in the actions of both the peptides on pancreatic exocrine secretion."

Journal

Discovery of adapalene and dihydrotachysterol as antiviral agents for the Omicron variant of SARS-CoV-2 through computational drug repurposing. (PubMed, Mol Divers) - "We discovered promising drug candidates for the inhibition of alarming Omicron variant such as quinestrol, adapalene, tamibarotene, and dihydrotachysterol. Particularly, adapalene, dihydrotachysterol, levocabastine and bexarotene came into prominence due to their non-interference with the normal physiological processes. Therefore, this study suggests that these approved drugs can be considered as drug candidates for further in vitro and in vivo studies to develop new treatment options for the Omicron variant of SARS-CoV-2."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

3,4-disubstituted piperidines synthesis via enantioselective Tsuji-Trost coupling and cope rearrangement (ACS-Sp 2022) - "3,4-difunctionalized piperidines are privileged structures found in numerous pharmaceuticals and biologically active natural products such as the antidepressant paroxetine and the antihistamine levocabastine. The Cope rearrangement products were derivatized by reduction and oxidative amidation demonstrating the importance of such substrates and presenting the type of products that can be access through this methodology. As such these products are of high value and will provide insights into stereoselective strategies related to the synthesis of 3,4-difunctionalized piperidines."

Optimization of a histamine-induced allergic conjunctivitis model in Guinea pigs. (PubMed, J Pharmacol Toxicol Methods) - "For observations of symptoms of conjunctivitis, we eliminated ambiguity of evaluation by adopting the Draize scale and ensured a higher objectivity on the evaluation method. The drug efficacy evaluation of levocabastine hydrochloride in the prepared model revealed that drug efficacy of the antihistamine drug was captured according to the standardized test method and highly-reproducible results were obtained."

Journal • Conjunctivitis • Immunology • Ocular Infections • Ocular Inflammation • Ophthalmology

Changes in synaptic proteins of the complex PSD-95/NMDA receptor/nNOS and mitochondrial dysfunction after levocabastine treatment. (PubMed, Neurochem Int) - "Results suggested that levocabastine administration induces alterations in synaptic proteins of the protein complex PSD-95/NMDA receptor/nNOS and in neuron cytoskeleton. Mitochondrial bioenergetics impairment may play a role in the functional link between synaptic proteins and NO synthesis."

Journal • Metabolic Disorders

Effects of xenin-25 on insulin and glucagon secretions in healthy conscious sheep. (PubMed, Domest Anim Endocrinol) - "A prior intravenous injection of the neurotensin receptor subtype-1 (NTR-1) antagonist SR 48692 at 100 nmol/kg did not modify the glucose-induced change in plasma insulin caused by xenin-25 at 300 pmol/kg, and intravenous injection of the NTR-2 agonist levocabastine at 1000 pmol/kg did not augment the insulin response to the glucose injection...The mRNAs of the three NTR subtypes were highly expressed in the ovine pancreas in comparison with the expression in the abomasum. These results suggest that xenin-25 released from the upper gastrointestinal tract plays a role of an insulinotropic factor in sheep, possibly through NTRs in the pancreatic islets, but not via NTR-2."

Clinical • Journal • Gastrointestinal Disorder