Onon dry syrup (pranlukast) / Ono Pharmaceutical - LARVOL DELTA

Leukotriene Receptor Antagonists Inhibit SLC19A1 and SLC46A1-Mediated Transport of Folic Acid and Antifolates. (PubMed, Chem Biol Interact) - "In vitro studies showed that MK571, montelukast, zafirlukast, and pranlukast concentration-dependently inhibited SLC19A1 and SLC46A1-mediated uptake of folic acid, methotrexate, and pemetrexed, with IC50 values ranging from 2.34 to 31.8 μM for SLC19A1 and 2.79 to 45.4 μM for SLC46A1. Taken together, this study identified LTRAs as novel and potent inhibitors of the key folate transporters SLC19A1 and SLC46A1, and uncovered previously unrecognized transporter-mediated drug-drug interactions between LTRAs and folate-related agents. These findings highlight the necessity of careful clinical monitoring and potential dose adjustments during concurrent administration to ensure therapeutic safety and efficacy."

Journal • Allergic Rhinitis • Asthma • Immunology • Inflammation • Pulmonary Disease • Respiratory Diseases

Comparative effectiveness of pranlukast versus montelukast as add-on therapy to inhaled corticosteroid/long-acting β₂-agonist (ICS/LABA) on asthma exacerbations: a real-world retrospective cohort study (ERS 2026) - "In real-world clinical practice, pranlukast and montelukast showed comparable effectiveness as add-ons to ICS/LABA in preventing asthma exacerbations in adults."

HEOR • Real-world • Real-world evidence • Retrospective data • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Respiratory Diseases

Comparative analysis of adverse drug reaction reports for leukotriene receptor antagonists mainly indicated for allergic rhinitis and asthma: a WHO VigiAccess study. (PubMed, Front Med (Lausanne)) - "Real-world evidence from spontaneous-report databases suggests differences in the safety-reporting profiles of montelukast, pranlukast, and zafirlukast. However, under-reporting and incomplete clinical information preclude estimation of incidence or causal inference; these findings should be interpreted as safety signals."

Adverse drug reaction • Journal • Allergic Rhinitis • Asthma • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Mental Retardation • Psychiatry • Pulmonary Disease • Respiratory Diseases • Suicidal Ideation

Intrinsic AIE drug nanocrystals enable imaging-guided orchitis theranostics. (PubMed, Mater Today Bio) - "Here, we show that three clinically approved leukotriene receptor antagonists, namely Pranlukast, Zafirlukast, and Montelukast can be transformed into self-reporting, self-delivering, and self-therapeutic nanotheranostics. In a rat model of acute orchitis, AIE imaging reveals efficient testicular accumulation, which correlates with attenuated histopathological damage, restored oxidative stress balance, and downregulation of the TLR4/MyD88/NF-κB and PK2/PKR1 pathways, with no obvious adverse effects on the measured short-term reproductive indices (sperm morphology and testosterone levels) observed within the experimental timeframe. This strategy converts old drugs into minimal-excipient, self-monitoring AIE nanotheranostics for imaging-guided orchitis therapy."

Journal • MYD88 • TLR4

Assessment of the binding characteristics of three antagonists toward CysLTR1 by affinity chromatography. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "The association equilibrium constants were measured as montelukast zafirlukast > pranlukast, which were correlated to the inhibition potencies of montelukast < zafirlukast < pranlukast to CysLTR1. Additionally, thermodynamic analysis in combination with molecular docking indicated that the three antagonists were spontaneously bound to CysLTR1 and their bindings were mainly driven by hydrogen bonds and van der Waals forces. Our work demonstrated that affinity chromatography can be utilized to evaluate the binding characteristics of ligand-receptor based on their retention behaviors, aiding the selection of the best ligands for further studies to become a drug molecule."

Journal

Targeting α6β1 Integrin Signaling with Pranlukast to Modulate Venous Endothelium Function and Reduce Post-Thrombotic Vein Wall Injury. (PubMed, J Vasc Surg Venous Lymphat Disord) - "This study demonstrates that targeting α6β1 integrin with PLK reduces vein wall fibrotic injury following experimental DVT without altering thrombus formation. These findings identify a novel, non-anticoagulant therapeutic strategy for PTS prevention that warrants further investigation in chronic models and translational studies."

Journal • Cardiovascular • Fibrosis • Hematological Disorders • Inflammation • Thrombosis • CCR2 • ITGA6 • ITGB1

Machine learning-driven drug repurposing for GPR17: activity prediction via graph neural networks and multistage computational validation. (PubMed, J Biomol Struct Dyn) - "Candidate molecules, including barmastine, astemizole, sulukast, and iralukast, were evaluated alongside reference ligands pranlukast and cangrelor. Importantly, this study proposes computationally prioritized candidates rather than experimentally validated inhibitors. Overall, the proposed hybrid workflow provides a practical strategy for early-stage GPR17 ligand discovery and future CNS-oriented drug development."

Journal • CNS Disorders • Inflammation • Multiple Sclerosis • Solid Tumor

Drug repurposing for glucosyltransferase inhibition for targeted oral biofilm disruption. (PubMed, NPJ Biofilms Microbiomes) - "Importantly, Radotinib selectively inhibited S.m. growth while preserving commensal species. This study identified at least two compounds capable of specifically inactivating a primary virulence factor of S.m. without inhibiting its growth, with a much lower selective pressure for drug resistance development, while simultaneously providing a growth advantage to commensal species that promote oral health."

Journal

Biocatalytic Bamberger Rearrangement for the Synthesis of 3-Amino-2-hydroxyacetophenone via Hydroxylaminobenzene Mutase Engineering and Multi-Enzyme System Assembly. (PubMed, Biotechnol J) - "This was overcome by implementing a RIAD/RIDD-based scaffold to spatially organize NR, HabM, GDH, and NADK, thereby promoting intermediate channeling and suppressing over-reduction. Overall, this study elucidates the structure of HabM and established a successful paradigm for optimizing complex multi-enzyme cascades for sustainable production of high-value biopharmaceutical intermediates."

Journal

Leukotriene receptor antagonists and eosinophilic granulomatosis with polyangiitis: a disproportionality analysis from FAERS, JADER, CVAR databases integrated with network pharmacology. (PubMed, PLoS One) - "Our study revealed LTRAs could increase the risk of EGPA, and initially explored potential genes and mechanisms of LTRAs-induced EGPA. It is helpful for clinicians to be alerted to the risk of EGPA during LTRAs administration."

Journal • Eosinophilic Granulomatosis With Polyangiitis • Immunology • Langerhans Cell Histiocytosis • Rare Diseases • Vasculitis • EDN1 • HMOX1 • KDR • OCLN • PACERR • PTGS2

Target Class Repurposing Across Membrane Transporter Families Provides Privileged Ligands to Address Specific and Undruggable Pharmacological Targets. (PubMed, ACS Pharmacol Transl Sci) - "The polypharmacology of selected drugs could be transferred to ABCA1 and Oatp1d1, two transporters for which almost no modulators have been reported before. This strategy provided privileged ligands with high potency at high hit rates to challenge transporter undruggability."

Journal • ABCA1 • SLC22A1

Activation of TMEM175 lysosomal ion channels by CysLT1 receptor antagonists. (PubMed, Am J Physiol Cell Physiol) - "DCPIB, zafirlukast, and pranlukast activated TMEM175 independently of AKT activation, whereas the AKT inhibitor MK2206 partially inhibited montelukast-dependent TMEM175 activation. Not only did T119A and H449A mutations decrease apparent potencies of DCPIB, zafirlukast, and montelukast, but the T119A mutation produced a constitutively open channel phenotype. This study adds zafirlukast to the short list of moderately potent TMEM175 activators and identifies a region of the channel that contributes to activation gating."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease

G Protein: β-Arrestin Bias Confers Differential Regulation of Gαq Signaling by GPR17 Antagonists. (PubMed, ACS Chem Neurosci) - "These findings highlight an unappreciated potential for biased signaling in the pharmacology of GPR17 ligands. We anticipate that these insights will help to inform the translation of GPR17-targeted therapies and improve our understanding of GPR17-mediated signaling pathways in governing myelination."

Journal • CNS Disorders • Solid Tumor • ARRB1

A FRET-Based High-Throughput Screening Assay for the Discovery of Mycobacterium tuberculosis DNA ADP-Ribosylglycohydrolase DarG Inhibitors. (PubMed, ACS Infect Dis) - "Notably, pranlukast did not inhibit human macrodomains, indicating strong selectivity for bacterial targets. Since pranlukast has previously been reported to reduce M. tuberculosis burden, further investigation into its action mechanism in this context would be valuable."

Journal • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

LC-MS-based metabolomics revealed promising role of leukotriene receptor antagonists against colorectal cancer. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "These findings demonstrate the antiproliferative potential of montelukast and zafirlukast in CRC and provide new insights into their distinct molecular mechanisms of action. This supports their potential repurposing as adjunctive therapies in CRC treatment."

Journal • Colorectal Cancer • Metabolic Disorders • Oncology • Solid Tumor

Recent advances in mucopolysaccharidosis IVA treatment. (PubMed, Orphanet J Rare Dis) - "Although enzyme replacement therapy (ERT) with elosulfase alfa is currently the only approved treatment, its clinical benefit on bone pathology is limited due to rapid clearance and poor penetration into avascular cartilage. Strategies to enhance enzyme stability and targeting, such as PEGylated hydrogels and extracellular vesicles, have shown promise in enhancing the biodistribution and stability of GALNS, while pharmacological chaperones, including ezetimibe, pranlukast, and bromocriptine, seem to stabilize GALNS in vitro...Importantly, recent evidence revealed that mitochondrial dysfunction in chondrocytes may contribute to the pathology of MPS IVA, uncovering new targets beyond GALNS enzyme activity recovery. This review highlights recent advances in the treatment of MPS IVA and discusses new directions to improve outcomes in MPS IVA treatment."

Journal • Review • Gene Therapies • Lysosomal Storage Diseases • Metabolic Disorders • Rare Diseases

Predicting Food Effect On Oral Drug Absorption For Solubility-Epithelial Membrane Permeation-Limited Cases With Bile Micelle Solubilization. (PubMed, Pharm Res) - "FaRLS appropriately predicted the food effect for the SL-E drugs. The mechanism was experimentally confirmed by μFlux."

Journal

First-time exploitation of Pranlukast's intrinsic fluorescence: a novel cetrimide-enhanced spectrofluorimetric platform for pharmaceutical, plasma, and content uniformity analysis. (PubMed, RSC Adv) - "This work introduces the first spectrofluorimetric approach for PNK, offering advantages of simplicity, low cost, high sensitivity, and environmental sustainability compared to previously reported UV and chromatographic methods. The method's limitation lies in its reliance on a micellar medium, which may require optimization for other surfactants or biological matrices."

Journal

A conserved mechanism of LRRC8 channel inhibition by two structurally distinct drugs. (PubMed, Commun Biol) - "We employed a structurally defined homomeric channel chimera (8C-8A(IL125)) and heteromeric LRRC8A/LRRC8C (8A/8C) channels to investigate the mechanism of action of two structurally distinct LRRC8 inhibitors: zafirlukast and pranlukast. The association between voltage-dependent inactivation induced by mutations or low pH and inhibitor sensitivity suggests that drug inhibition involves disruption of protein-lipid interactions and destabilization of the pore. This may represent a common mechanism of LRRC8 channel inhibition by lipophilic drugs."

Journal • LRRC8A

Evidence that Mast Cells Regulate the Cough Hypersensitivity Associated with Eosinophilic Bronchitis. (PubMed, Lung) - "These results suggest that mast cells and not eosinophils may be essential to the emergence of cough hypersensitivity in EB. We speculate that therapeutic strategies targeting mast cells, cysLT1 receptors, and TP receptors may represent endotype-specific treatments for chronic cough."

Journal • Asthma • Chronic Cough • Cough • Immunology • Inflammation • Pulmonary Disease • Respiratory Diseases

Polypharmacology translates between species and phylogenetic distance: A functional, bioinformatic, and structural study on organic anion transporting polypeptides. (PubMed, Biochem Pharmacol) - "The bioactivity of Pranlukast (PRA) on human OATPs could be accurately predicted based on its activity on drOatp1d1. The collection of pan-ABC transporter modulators also showed activity against other zebrafish (i.e., drAbcb4) and non-zebrafish (i.e., mumAbca1) membrane transporters, ultimately rendering it a suitable tool to translate between species to tackle the undruggability of membrane transporters and potentially other proteins by addressing conserved structural motifs."

Journal • ABCA1 • SLCO2B1

Distinct effects of synthetic GPR17 antagonists on cellular signaling in recombinant HEK293 cells and native oligodendroglial cell backgrounds (CINP-AsCNP 2025) - "These findings reveal a hitherto unappreciated potential for biased signalling in the pharmacology of GPR17 ligands with implications for their regulation of downstream cellular signalling relevant to myelination. We anticipate these insights will expedite the translation of GPR17 targeted therapies and improve our understanding of signaling pathways used by this receptor for governing myelination."

CNS Disorders • Psychiatry • Solid Tumor • ARRB1

Therapeutic potential of Pranlukast against cuprizone-induced inflammatory demyelination and sensory impairment in mice: comparison with Fingolimod. (PubMed, Neurotoxicology) - "Cuprizone and Pranlukast groups presented more microglia/macrophages in the CC, but fewer presenting reactive microglia/macrophages and less NOS2 staining in pranlukast-treated when compared to the cuprizone group, while fingolimod treatment prevented the increase in Iba1 in the CC. In summary, this study demonstrated that pranlukast is a good candidate as a novel drug for use in conditions of inflammatory demyelination, such as MS, by restoring function through modulation of the inflammatory environment."

Journal • Preclinical • CNS Disorders • Inflammation • Multiple Sclerosis • MBP • NOS2

Practical Application and Caution for Interaction Between Antiseizure Medications and Popular Pediatric Medications (AES 2024) - "The patients in Group A had combination of some of CBZ, CLB, CZP, perampanel (PER), ZNS, RUF, STP, VPA, LTG and bromide. Five cases took clarithromycin (CAM) (with pranlukast (PK) in one case and with PK and acetaminophen (AA) in one case), four cases had dextromethorphan (DM) (with cyproheptadine (CH), with tipepidine (TP), and with CH and TP in one case each), and two cases had TP (with AA in one case)... As ASM levels are elevated by concomitant CPMs which metabolizing enzymes inhibit or compete with those of ASM, we must be aware of metabolizing enzymes in both medications. It may lead to detect effective ASMs and to avoid adverse effects, particularly for CPMs which inhibit metabolic enzymes of ASMs. Pediatricians are not aware of interaction of ASMs and CPMs, and we should remind this to patients who take corresponding ASMs and PCMs to avoid adverse events."

Clinical • CNS Disorders • Epilepsy • Infectious Disease • Pediatrics • Pneumonia • Respiratory Diseases • CYP3A4

In silico Prediction of Pranlukast as a Stabilizer of PD-L1 Homodimers. (PubMed, Anticancer Agents Med Chem) - "Our results suggest that pranlukast inhibits the PD-1/PD-L1 axis, meriting its repurposing as an antitumor drug."

Journal • Asthma • Immunology • Oncology • Pulmonary Disease • Respiratory Diseases • PD-L1