Fevipiprant

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]

Fevipiprant
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
IUPAC name
  • {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
Chemical and physical data
FormulaC19H17F3N2O4S
Molar mass426.41 g·mol−1
3D model (JSmol)
SMILES
  • 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
  • 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

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. 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. "A 52-week, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Assess the Efficacy and Safety of QAW039 when Added to Existing Asthma Therapy in Patients with Uncontrolled Severe Asthma". 4 May 2020. {{cite journal}}: Cite journal requires |journal= (help)
  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.


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