Fevipiprant

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Fevipiprant
Fevipiprant.svg
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Pharmacokinetic data
BioavailabilityUnaffected by food[1]
MetabolismHepatic glucuronidation
Elimination half-life~20 hours
ExcretionRenal (≤30%)
Identifiers
  • {2-methyl-1-[4-(methylsulfonyl)-2-(trifluoromethyl)benzyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetic acid
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ECHA InfoCard100.243.911 Edit this at Wikidata
Chemical and physical data
FormulaC19H17F3N2O4S
Molar mass426.41 g·mol−1
3D model (JSmol)
  • CC1=C(C2=C(N1CC3=C(C=C(C=C3)S(=O)(=O)C)C(F)(F)F)N=CC=C2)CC(=O)O
  • InChI=1S/C19H17F3N2O4S/c1-11-15(9-17(25)26)14-4-3-7-23-18(14)24(11)10-12-5-6-13(29(2,27)28)8-16(12)19(20,21)22/h3-8H,9-10H2,1-2H3,(H,25,26)
  • Key:GFPPXZDRVCSVNR-UHFFFAOYSA-N

Fevipiprant (INN; code name QAW039) is a drug being developed by Novartis which acts as a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2 or CRTh2).[1][2][3]

As of 2016, it is in phase III[4] clinical trials for the treatment of asthma.[5]

On Monday, December 16, 2019, Switzerland-based Novartis officially announced that it was jettisoning fevipiprant from its development program, given that the medicine has failed in two additional clinical trials in patients with moderate-to-severe asthma. The firm said that it had hoped fevipiprant would be a billion-dollar-selling asthma drug.[6]

See also

References

  1. ^ a b Erpenbeck VJ, Vets E, Gheyle L, Osuntokun W, Larbig M, Neelakantham S, et al. (2016). "Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo-Controlled Studies in Healthy Volunteers". Clinical Pharmacology in Drug Development. 5 (4): 306–13. doi:10.1002/cpdd.244. PMC 5071756. PMID 27310331.
  2. ^ Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G, Charlton SJ (May 2016). "Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy". Mol Pharmacol. 89 (5): 593–605. doi:10.1124/mol.115.101832. PMID 26916831.
  3. ^ Erpenbeck VJ, Popov TA, Miller D, Weinstein SF, Spector S, Magnusson B, et al. (2016). "The oral CRTh2 antagonist QAW039 (fevipiprant): A phase II study in uncontrolled allergic asthma". Pulm Pharmacol Ther. 39: 54–63. doi:10.1016/j.pupt.2016.06.005. PMID 27354118.
  4. ^ https://clinicaltrials.gov/ct2/show/NCT02555683
  5. ^ Gonem S, Berair R, Singapuri A, Hartley R, Laurencin M, Bacher G, et al. (2016). "Fevipiprant, a prostaglandin D2 receptor 2 antagonist, in patients with persistent eosinophilic asthma: a single-centre, randomised, double-blind, parallel-group, placebo-controlled trial". Lancet Respir Med. 4 (9): 699–707. doi:10.1016/S2213-2600(16)30179-5. hdl:2381/38430. PMID 27503237.
  6. ^ Novartis drops asthma drug fevipiprant after trial failures. Reuters News. https://www.reuters.com/article/us-novartis-asthma/novartis-drops-asthma-drug-fevipiprant-after-trial-failures-idUSKBN1YK0DR - Accessed Sunday, December 15, 2019, from North America.