Chemistry:Fevipiprant
From HandWiki
Short description: Chemical compound
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| Routes of administration | Oral |
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| Bioavailability | Unaffected by food[1] |
| Metabolism | Hepatic glucuronidation |
| Elimination half-life | ~20 hours |
| Excretion | Renal (≤30%) |
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| Formula | C19H17F3N2O4S |
| Molar mass | 426.41 g·mol−1 |
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Fevipiprant (INN; code name QAW039) is a drug of the piprant class that was being developed by Novartis. It is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2 or CRTh2).[1][2][3]
By 2016 it had advanced to phase III[4] clinical trials for the treatment of asthma.[5] However, in 2019 Novartis announced that it was removing fevipiprant from its development program, given that the medicine has failed in two 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
- ↑ 1.0 1.1 "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. 2016. doi:10.1002/cpdd.244. PMID 27310331.
- ↑ "Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy". Mol Pharmacol 89 (5): 593–605. May 2016. doi:10.1124/mol.115.101832. PMID 26916831.
- ↑ "The oral CRTh2 antagonist QAW039 (fevipiprant): A phase II study in uncontrolled allergic asthma". Pulm Pharmacol Ther 39: 54–63. 2016. doi:10.1016/j.pupt.2016.06.005. PMID 27354118.
- ↑ "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. https://clinicaltrials.gov/ct2/show/NCT02555683.
- ↑ "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. 2016. doi:10.1016/S2213-2600(16)30179-5. PMID 27503237. https://ora.ox.ac.uk/objects/uuid:f07c58de-6462-4d8d-92c4-6960249f2623.
- ↑ "Novartis drops asthma drug fevipiprant after trial failures" (in en). Reuters. 2019-12-16. https://www.reuters.com/article/us-novartis-asthma-idUSKBN1YK0DR.
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