Girish Mahajan (Editor)

RPL 554

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit
PubChem CID
  
9934746

Formula
  
C26H31N5O4

Molar mass
  
477.554 g/mol

ChemSpider
  
8110374

3D model (Jmol)
  
Interactive image

RPL-554 httpsuploadwikimediaorgwikipediacommonsthu

Synonyms
  
9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one

RPL-554 (LS-193,855) is a drug candidate for respiratory diseases. It is an analog of trequinsin, and like trequinsin, is a dual inhibitor of the phosphodiesterase enzymes PDE-3 and PDE-4. As of October 2015, inhaled RPL-554 delivered via a nebulizer was in development for COPD and had been studied in asthma.

PDE3 inhibitors act as bronchodilators, while PDE4 inhibitors have an anti-inflammatory effect.

RPL554 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.

In 2005, Rhinopharma Ltd, acquired the rights to the intellectual property from Vernalis. 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, and intended to develop RPL-554, delivered with an inhaler, first for allergic rhinitis, then asthma, then for COPD. RPL554 was synthesized at Tocris, a contract research organization, under the supervision of Oxford, and was studied in collaboration with Page's lab at King’s College, London. In 2006 Rhinopharma recapitalized and was renamed Verona Pharma plc.

References

RPL-554 Wikipedia