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Details

Stereochemistry ACHIRAL
Molecular Formula C23H32N6
Molecular Weight 392.5404
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOREFORANT

SMILES

CN1CCC(CCCNC2=NC=C(C3=NC4=C(N3)C=C(C)C=C4C)C(C)=N2)CC1

InChI

InChIKey=FCRFVPZAXGJLPW-UHFFFAOYSA-N
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)

HIDE SMILES / InChI

Description

Toreforant (JNJ-38518168) is an orally active, selective histamine H4 receptor antagonist. Toreforant was investigated as an agent for the treatment of active rheumatoid arthritis. While some improvement in rheumatoid arthritis signs/symptoms through week 12 was observed in the phase IIa study, no efficacy was observed with toreforant at lower doses in a subsequent phase IIb study. Toreforant has been tested in clinical studies in patients with asthma and psoriasis. Toreforant failed to provide therapeutic benefit in population of patients with uncontrolled, eosinophilic, persistent asthma. Toreforant efficacy at 30 and 60 mg was greater than placebo but did not meet predefined success criterion in patients with moderate-to-severe psoriasis.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
8.4 nM [Ki]

PubMed