Ensifentrine
Template:Short description Template:Use dmy dates Template:Cs1 config Template:Short description <templatestyles src="Infobox drug/styles.css"/> Script error: No such module "Infobox".Template:Template otherScript error: No such module "TemplatePar".{{Infobox drug/maintenance categoriesTemplate:Yesno | drug_name = | INN = | _drugtype =
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| _other_data=N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea
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Ensifentrine, sold under the brand name Ohtuvayre, is a medication used for the treatment of chronic obstructive pulmonary disease (COPD) in adults.[1] It is a phosphodiesterase 3 inhibitor and phosphodiesterase 4 inhibitor.[1] It is given by inhalation.[1]
PDE3 inhibitors act as bronchodilators, while PDE4 inhibitors have an anti-inflammatory effect.[2][3]
Ensifentrine was approved for medical use in the United States in June 2024.[1][4][5]
Medical uses
Ensifentrine is indicated for the maintenance treatment of chronic obstructive pulmonary disease in adults.[1]
Pharmacology
It is an analog of trequinsin and, like trequinsin, it is a highly selective inhibitor of the phosphodiesterase enzyme, PDE3; it is >3000-times more potent against PDE3 than PDE4.[2]
History
Ensifentrine was part of a family of compounds invented by Sir David Jack, former head of R&D for GlaxoSmithKline, and Alexander Oxford, a medicinal chemist; the patents on their work were assigned to Vernalis plc.[6][7][8]Template:Rp
In 2005, Rhinopharma Ltd, acquired the rights to the intellectual property from Vernalis.[8]Template:Rp Rhinopharma was a startup founded in Vancouver, Canada in 2004 by Michael Walker, Clive Page, and David Saint, to discover and develop drugs for chronic respiratory diseases,[8]Template:Rp and intended to develop ensifentrine, delivered with an inhaler, first for allergic rhinitis, then asthma, then for COPD.[8]Template:Rp Ensifentrine was synthesized at a contract research organization, under the supervision of Oxford, and was studied in collaboration with Page's lab at King’s College, London.[2] In 2006 Rhinopharma recapitalized and was renamed Verona Pharma plc.[8]
Society and culture
Legal status
Ensifentrine was approved for medical use in the United States in June 2024.[1][4]
Research
As of October 2015, inhaled RPL-554 delivered via a nebulizer was in development for COPD and had been studied in asthma.[9]
References
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- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Oxford AW, Jack D, "Derivatives of pyrimido[6,1-a]isoquinolin-4-one", published Script error: No such module "auto date formatter"., assigned to Verona Pharma plcScript error: No such module "Check for unknown parameters".
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