Delving into the Latest Updates on Pemirolast sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Action

inhibitors

Mechanism

Mast cells inhibitors

Therapeutic Areas

Immune System DiseasesNervous System DiseasesCardiovascular Diseases+ [4]

Active Indication-

Inactive Indication

Aortic Aneurysm, AbdominalAsthmaBecker Muscular Dystrophy+ [1]

Originator Organization

RSPR Pharma AB

Active Organization-

Inactive Organization

RSPR Pharma AB

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC10H8N6O

InChIKeyHIANJWSAHKJQTH-UHFFFAOYSA-N

CAS Registry69372-19-6

View All Structures (2)

The purpose of this study is to establish the influence of the non-steroidal candidate-drug pemirolast on allergen-induced airway obstruction and inflammation in allergic subjects with asthma. Pemirolast is an orally available inhibitor of the release of mast cell mediators. The study will therefore test the hypothesis that global inhibition of the mast cell, resulting in decreased production of most of its mediator molecules, will provide a highly significant anti-asthmatic effect.

Start Date01 Nov 2016

Sponsor / Collaborator

Karolinska University Hospital

[+3]

EUCTR2015-002656-26-BG

/ Not yet recruitingPhase 2

A Double-Blind, Randomised, Placebo-controlled, Parallel Group, International, Multi-centre Phase 2 Trial Investigating the Safety and Efficacy of CRD007 in Adult Subjects with Asthma - RSPR-008

Start Date15 Jun 2016

Sponsor / Collaborator

RSPR Pharma AB

NCT02615080

/ CompletedPhase 2

A Double-Blind, Randomised, Placebo-controlled, Parallel Group, International, Multi-centre Phase 2 Trial Investigating the Safety and Efficacy of CRD007 in Adult Subjects With Asthma

This is a double-blind, randomised, placebo-controlled, parallel group, Phase 2 trial evaluating CRD007 administered orally b.i.d for 14 weeks for the treatment of asthma. CRD007 will be given as add on to a background of commonly used controller medication, i.e. inhaled corticosteroid (ICS) with or without long-acting beta2-agonist (LABA). By gradually reducing the background controller medication, the efficacy and safety of CRD007 will be evaluated on top of several dose levels of this medication.

Start Date30 Nov 2015

Sponsor / Collaborator

RSPR Pharma AB

100 Clinical Results associated with Pemirolast sodium

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100 Translational Medicine associated with Pemirolast sodium

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100 Patents (Medical) associated with Pemirolast sodium

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83

Literatures (Medical) associated with Pemirolast sodium

01 Apr 2024·Molecular Diversity

Evaluation of the interaction between potent small molecules against the Nipah virus Glycoprotein in Malaysia and Bangladesh strains, accompanied by the human Ephrin-B2 and Ephrin-B3 receptors; a simulation approach

Article

Author: Alijanianzadeh, Mahdi ; Ebrahimi, Maryam

Malaysia reported the first human case of Nipah virus (NiV) in late September 1998 with encephalitis and respiratory symptoms. As a result of viral genomic mutations, two main strains (NiV-Malaysia and NiV-Bangladesh) have spread around the world. There are no licensed molecular therapeutics available for this biosafety level 4 pathogen. NiV attachment glycoprotein plays a critical role in viral transmission through its human receptors (Ephrin-B2 and Ephrin-B3), so identifying small molecules that can be repurposed to inhibit them is crucial to developing anti-NiV drugs. Consequently, in this study annealing simulations, pharmacophore modeling, molecular docking, and molecular dynamics were used to evaluate seven potential drugs (Pemirolast, Nitrofurantoin, Isoniazid Pyruvate, Eriodictyol, Cepharanthine, Ergoloid, and Hypericin) against NiV-G, Ephrin-B2, and Ephrin-B3 receptors. Based on the annealing analysis, Pemirolast for efnb2 protein and Isoniazid Pyruvate for efnb3 receptor were repurposed as the most promising small molecule candidates. Furthermore, Hypericin and Cepharanthine, with notable interaction values, are the top Glycoprotein inhibitors in Malaysia and Bangladesh strains, respectively. In addition, docking calculations revealed that their binding affinity scores are related to efnb2-pem (- 7.1 kcal/mol), efnb3-iso (- 5.8 kcal/mol), gm-hyp (- 9.6 kcal/mol), gb-ceph (- 9.2 kcal/mol). Finally, our computational research minimizes the time-consuming aspects and provides options for dealing with any new variants of Nipah virus that might emerge in the future.

01 Mar 2024·European Journal of Pharmaceutical Sciences

Pitfalls in evaluating permeability experiments with Caco-2/MDCK cell monolayers

Article

Author: Goss, Kai-Uwe ; Dahley, Carolin ; Ebert, Andrea

When studying the transport of molecules across biological membranes, intrinsic membrane permeability (P₀) is more informative than apparent permeability (P_app), because it eliminates external (setup-specific) factors, provides consistency across experiments and mechanistic insight. It is thus an important building block for modeling the total permeability in any given scenario. However, extracting P₀ is often difficult, if not impossible, when the membrane is not the dominant transport resistance. In this work, we set out to analyze P_app values measured with Caco-2/MDCK cell monolayers of 69 literature references. We checked the P_app values for a total of 318 different compounds for the extractability of P₀, considering possible limitations by aqueous boundary layers, paracellular transport, recovery issues, active transport, a possible proton flux limitation, and sink conditions. Overall, we were able to extract 77 reliable P₀ values, which corresponds to about one quarter of the total compounds analyzed, while about half were limited by the diffusion through the aqueous layers. Compared to an existing data set of P₀ values published by Avdeef, our approach resulted in a much higher exclusion of compounds. This is a consequence of stricter compound- and reference-specific exclusion criteria, but also because we considered possible concentration-shift effects due to different pH values in the aqueous layers, an effect only recently described in literature. We thus provide a consistent and reliable set of P₀, e.g. as a basis for future modeling.

13 Oct 2023·Journal of Biomolecular Structure and Dynamics

Quantum chemical studies on the binding domain of SARS-CoV-2 S-protein: human ACE2 interface complex

Article

Author: Suresh, Cherumuttathu H. ; Haritha, Mambatta

A two-layer ONIOM(B3LYP/6-31G*:PM7) method is used to model the binding of several drug/drug-like molecules (L) at the SARS-CoV-2 S-protein: human ACE2 protein interface cavity. The selected molecules include a set of thirty-five ligands from the study of Smith and Smith which showed a high docking score in the range of -7.0 to -7.7 kcal/mol and another set of seven repurposing drugs, viz. favipiravir, remdesivir, EIDD, galidesivir, triazavirin, ruxolitinib, and baricitinib. The ONIOM model of the cavity (M) showed a highly polarized electron distribution along its top-to-bottom direction while Ls with lengths in the range 1.0 - 1.5 nm fitted well inside the cavity in a head-to-tail fashion to yield ML complexes. The ligands showed a large variation in the ONIOM-level binding energy (E_b), in the range -2.7 to -85.4 kcal/mol. The E_b of ML complexes better than -40.0 kcal/mol is observed for myricetin, fidarestat, protirelin, m-digallic acid, glucogallin, benserazide hydrochlorideseradie, remdesivir, tazobactum, sapropterin, nitrofurantoin, quinonoid, pyruvic acid calcium isoniazid, and aspartame, and among them the highest E_b -85.4 kcal/mol is observed for myricetin. A hydroxy substitution is suggested for the phenyl ring of aspartame to improve its binding behavior at the cavity, and the resulting ligand 43 showed the best E_b -84.5 kcal/mol. The ONIOM-level study is found to be effective for the interpretation of the noncovalent interactions resulting from residues such as arginine, histidine, tyrosine, lysine, carboxylate, and amide moieties in the active site and suggests rational design strategies for COVID-19 drug development.Communicated by Ramaswamy H. Sarma.

100 Deals associated with Pemirolast sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Pemirolast sodium	-	DB00885

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	Denmark	RSPR Pharma AB	01 Mar 2015
Becker Muscular Dystrophy	Phase 2	Sweden	RSPR Pharma AB	29 Feb 2012
Muscular Dystrophy, Duchenne	Phase 2	Sweden	RSPR Pharma AB	29 Feb 2012
Aortic Aneurysm, Abdominal	Phase 2	United Kingdom	RSPR Pharma AB	16 May 2011
Aortic Aneurysm, Abdominal	Phase 2	Sweden	RSPR Pharma AB	16 May 2011
Aortic Aneurysm, Abdominal	Phase 2	Denmark	RSPR Pharma AB	16 May 2011