Drug intelligence / Profile preview

JNJ-39758979

Development stage
Phase 2
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

JNJ-39758979 is a selective, orally active, high-affinity histamine H4 receptor antagonist developed by Janssen Research & Development (a Johnson & Johnson company). It exhibits potent antagonism at the human histamine H4 receptor (Ki = 12.5 nM) and shows >80-fold selectivity over other histamine receptors[1][8]. The drug was investigated for the treatment of asthma, atopic dermatitis, and rheumatoid arthritis. Clinical development was discontinued during phase II trials due to cases of idiosyncratic drug-induced agranulocytosis[3][4][5]. In clinical studies, it demonstrated efficacy in reducing histamine-induced pruritus in healthy subjects but did not significantly affect wheal or flare responses[7].

Other names
2-pyrimidinamine, 4-((3R)-3-amino-1-pyrrolidinyl)-6-(1-methylethyl)-(R)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylamine
02

Targets

HRH4 (Histamine H4 receptor)

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