Toreforant (JNJ-38518168) is an orally-dosed selective antagonist of the histamine H4 receptor that has been studied for various health conditions. It is the successor of a number of H4-selective compounds developed by Johnson & Johnson.[1] Phase IIa clinical trials completed as recently as November 2018 continue to suggest that toreforant is safe.[2]
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IUPAC name
5-(4,6-dimethyl-1H-benzimidazol-2-yl)-4-methyl-N-[3-(1-methylpiperidin-4-yl)propyl]pyrimidin-2-amine
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C23H32N6 | |
Molar mass | 392.551 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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As of the end of 2020, there is no regulator-approved H4 antagonist. In U.S. Phase II clinical trials, toreforant, by itself, did not show efficacy against eosinophilic asthma.[2] The drug did show at least partial efficacy against rheumatoid arthritis in patients who were nonresponsive to methotrexate.[3] As the H4 receptor is widely implicated in the regulation of inflammatory states, the potential uses for an H4 antagonist remain significant.[4][5][6]