Toreforant

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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Toreforant

Names
IUPAC name 5-(4,6-dimethyl-1H-benzimidazol-2-yl)-4-methyl-N-[3-(1-methylpiperidin-4-yl)propyl]pyrimidin-2-amine
Identifiers
CAS Number	952494-46-1
3D model (JSmol)	Interactive image
ChEMBL	ChEMBL3301609
ChemSpider	31389942
DrugBank	DB12522
KEGG	D10735
PubChem CID	23650961
UNII	U6LA7G393X
CompTox Dashboard (EPA)	DTXSID701336756
InChI InChI=1S/C23H32N6/c1-15-12-16(2)21-20(13-15)27-22(28-21)19-14-25-23(26-17(19)3)24-9-5-6-18-7-10-29(4)11-8-18/h12-14,18H,5-11H2,1-4H3,(H,27,28)(H,24,25,26) Key: FCRFVPZAXGJLPW-UHFFFAOYSA-N
SMILES CC1=CC(=C2C(=C1)NC(=N2)C3=CN=C(N=C3C)NCCCC4CCN(CC4)C)C
Properties
Chemical formula	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). Infobox references

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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]