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Pharmacokinetics, safety, and tolerability of QAW039 (fevipiprant), a novel CRTh2 receptor antagonist: Results from two randomized, phase I, placebo-controlled studies in healthy volunteers

Erpenbeck, Veit and Weiss, Markus and Sandham, David and Neelakantham, Srikanth Raju (2016) Pharmacokinetics, safety, and tolerability of QAW039 (fevipiprant), a novel CRTh2 receptor antagonist: Results from two randomized, phase I, placebo-controlled studies in healthy volunteers. Clinical Pharmacology in Drug Development.

Abstract

We evaluated the pharmacokinetics (PK), safety and tolerability of a novel oral CRTh2 antagonist, QAW039 (fevipiprant); in healthy subjects. QAW039 peak concentrations in plasma were observed 1‒3 hours post-dosing. Concentrations declined in a multi-exponential manner, followed by an apparent terminal phase (t1/2 ~ 20 hours). Steady state was achieved in 4 days with < 2-fold accumulation. Elimination was partly by renal excretion (≤ 30% of the dose) and glucuronidation. Food had minimal impact on the PK of QAW039 and it was well tolerated at single and multiple oral doses up to 500 mg/day. No dose dependent adverse events were observed and all the events were mild or moderate in severity. Systemic concentrations were sufficiently high to achieve relevant target occupancy, considering in vitro pharmacology data.
In summary, the data support further development as a once-daily oral therapy for allergic diseases.

Item Type: Article
Date Deposited: 13 Apr 2016 23:45
Last Modified: 13 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/25722

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