Pemirolast

Pemirolast (INN) is a mast cell stabilizer used as an anti-allergic drug therapy. It is marketed under the tradenames Alegysal and Alamast.

Pemirolast
Clinical data
Trade namesAlamast
AHFS/Drugs.comMonograph
Routes of
administration		Oral, ophthalmic
ATC code
  • none
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Identifiers
IUPAC name
  • 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC10H8N6O
Molar mass228.215 g·mol−1
3D model (JSmol)
SMILES
  • CC1=CC=CN2C1=NC=C(C2=O)C3=NNN=N3
 NY (what is this?)  (verify)

Clinical trials studying treatments for allergic conjunctivitis have found that an ophthalmic solution containing levocabastine with pemirolast potassium may be more effective in alleviating symptoms than levocabastine alone.[1]

It has also been studied for the treatment of asthma.

Pemirolast has appeared as a possible candidate for SARS-CoV-2 (COVID-19) spike protein disruption and interference. Such results were ascertained by molecular dynamics calculations executed on the Summit supercomputer. By simulating compounds with FDA or similar regulatory approval, the authors found 4 interfacial molecules that could potentially disrupt the SARS-CoV-2 interface with ACE-2 receptors, suggesting that such small molecules could mitigate SARS-CoV-2 infection. The 4 candidate interfacial molecules included pemirolast, isoniazid pyruvate, nitrofurantoin, and eriodictyol.[2]

References
  1. Castillo M, Scott NW, Mustafa MZ, Mustafa MS, Azuara-Blanco A (2015). "Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis". Cochrane Database Syst Rev. 6 (6): CD009566. doi:10.1002/14651858.CD009566.pub2. hdl:2164/6048. PMID 26028608.{{cite journal}}: CS1 maint: uses authors parameter (link)
  2. Smith, MD, Smith JC (April 2020). "Repurposing Therapeutics for COVID-19: Supercomputer-Based Docking to the SARS-CoV-2 Viral Spike Protein and Viral Spike Protein-Human ACE2 Interface". Preprint: 1–28.
  • Tinkelman DG, Berkowitz RB (February 1991). "A pilot study of pemirolast in patients with seasonal allergic rhinitis". Ann Allergy. 66 (2): 162–5. PMID 1994787.
  • Kawashima T, Iwamoto I, Nakagawa N, Tomioka H, Yoshida S (1994). "Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils". Int. Arch. Allergy Immunol. 103 (4): 405–9. doi:10.1159/000236662. PMID 8130655.
  • Abelson MB, Berdy GJ, Mundorf T, Amdahl LD, Graves AL (October 2002). "Pemirolast potassium 0.1% ophthalmic solution is an effective treatment for allergic conjunctivitis: a pooled analysis of two prospective, randomized, double-masked, placebo-controlled, phase III studies". J Ocul Pharmacol Ther. 18 (5): 475–88. doi:10.1089/10807680260362759. PMID 12419098.
  • Kemp JP, Bernstein IL, Bierman CW, et al. (June 1992). "Pemirolast, a new oral nonbronchodilator drug for chronic asthma". Ann Allergy. 68 (6): 488–91. PMID 1610024.


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