1. Histamine H1 receptor antagonist
TAK-427
Histamine H1 receptor antagonist
Summary
TAK-427 is a novel anti-allergic agent that has both histamine H1-receptor antagonist and anti-inflammatory activities.
Safety, tolerability and adverse events
Pre-clinical pharmacology
TAK-427 inhibited ligand binding to rhH1R with an IC50 value of 17.3 nmol/l. TAK-427 inhibited histamine induced skin reactions in guinea pigs and mice with an ID50 value of and mg/kg, p.o., respectively; significant inhibition associated with 10 mg/kg of TAK-427 was still observed 24 h after dosing in guinea pigs.
Clinical studies
Phase II trials for Allergic dermatitis, rhinitis
Exclusion/restrictions to future studies
Other relevant information