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Clinical data | |
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Trade names | Ohtuvayre |
Other names | RPL-554, LS-193,855 |
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ECHA InfoCard | 100.245.423 |
Chemical and physical data | |
Formula | C26H31N5O4 |
Molar mass | 477.565 g·mol−1 |
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Ensifentrine, sold under the brand name Ohtuvayre, is a medication indicated for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in adults.
It is an analog of trequinsin and, like trequinsin, is a highly selective inhibitor of the phosphodiesterase enzyme, PDE3; indeed, it is >3000-times more potent against PDE3 than PDE4. [1] As of October 2015, inhaled RPL-554 delivered via a nebulizer was in development for COPD and had been studied in asthma. [2]
PDE3 inhibitors act as bronchodilators, while PDE4 inhibitors have an anti-inflammatory effect. [1] [3]
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. [4] [5] [6] : 19–20
In 2005, Rhinopharma Ltd, acquired the rights to the intellectual property from Vernalis. [6] : 19–20 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, [6] : 16 and intended to develop ensifentrine, delivered with an inhaler, first for allergic rhinitis, then asthma, then for COPD. [6] : 16–17 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. [1] In 2006 Rhinopharma recapitalized and was renamed Verona Pharma plc. [6]
Benzodiazepines, colloquially called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and was made available in 1960 by Hoffmann–La Roche, which followed with the development of diazepam (Valium) three years later, in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide.
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