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Toreforant, an orally active histamine H(4)-receptor antagonist, in patients with active rheumatoid arthritis despite methotrexate: mechanism of action results from a phase 2, multicenter, randomized, double-blind, placebo-controlled synovial biopsy study.
Boyle DL, DePrimo SE, Calderon C, Chen D, Dunford PJ, Barchuk W, Firestein GS, Thurmond RL. Boyle DL, et al. Inflamm Res. 2019 Apr;68(4):261-274. doi: 10.1007/s00011-019-01218-y. Epub 2019 Feb 9. Inflamm Res. 2019. PMID: 30739130 Clinical Trial.
OBJECTIVE/DESIGN: In a double-blind, placebo-controlled, multiple-dose study, we assessed the molecular mechanism of action of the selective histamine-4-receptor antagonist toreforant. PATIENTS/TREATMENT: Patients with active rheumatoid arthritis (RA) despite …
OBJECTIVE/DESIGN: In a double-blind, placebo-controlled, multiple-dose study, we assessed the molecular mechanism of action of the selective …
Clinical Development of Histamine H(4) Receptor Antagonists.
Thurmond RL, Venable J, Savall B, La D, Snook S, Dunford PJ, Edwards JP. Thurmond RL, et al. Handb Exp Pharmacol. 2017;241:301-320. doi: 10.1007/164_2016_130. Handb Exp Pharmacol. 2017. PMID: 28233185 Review.
The discovery of the histamine H(4) receptor (H(4)R) provided a new avenue for the exploration of the physiological role of histamine, as well as providing a new drug target for the development of novel antihistamines. The first step in this process was the i …
The discovery of the histamine H(4) receptor (H(4)R) provided a new avenue for the exploration of the physiological role of …
Efficacy and Safety of Toreforant, a Selective Histamine H4 Receptor Antagonist, for the Treatment of Moderate-to-Severe Plaque Psoriasis: Results from a Phase 2 Multicenter, Randomized, Double-blind, Placebo-controlled Trial.
Frankel E, Song M, Li S, Jiang J, Thurmond RL, Randazzo B. Frankel E, et al. J Drugs Dermatol. 2018 Aug 1;17(8):873-879. J Drugs Dermatol. 2018. PMID: 30124726 Clinical Trial.
BACKGROUND: Toreforant is a selective histamine H4 receptor antagonist. H4 receptor activation may play a role in immune-mediated inflammation in psoriasis. OBJECTIVE: To evaluate Toreforant efficacy and safety in patients with moderate-to-sever …
BACKGROUND: Toreforant is a selective histamine H4 receptor antagonist. H4 receptor activation may play a role i …
A phase 2a study of toreforant, a histamine H(4) receptor antagonist, in eosinophilic asthma.
Kollmeier AP, Barnathan ES, O'Brien C, Chen B, Xia YK, Zhou B, Loza MJ, Silkoff PE, Ge M, Thurmond RL. Kollmeier AP, et al. Ann Allergy Asthma Immunol. 2018 Nov;121(5):568-574. doi: 10.1016/j.anai.2018.08.001. Epub 2018 Aug 11. Ann Allergy Asthma Immunol. 2018. PMID: 30102965 Clinical Trial.
BACKGROUND: Data from preclinical and clinical studies support the evaluation of histamine 4 receptor antagonists in the treatment of asthma. Toreforant is a selective histamine 4 receptor antagonist that could be effective in patients with eosi …
BACKGROUND: Data from preclinical and clinical studies support the evaluation of histamine 4 receptor antagonists in the treat …
Toreforant, A Histamine H4 Receptor Antagonist, in Patients with Active Rheumatoid Arthritis Despite Methotrexate Therapy: Results of 2 Phase II Studies.
Thurmond RL, Greenspan A, Radziszewski W, Xu XL, Miao Y, Chen B, Ge T, Zhou B, Baker DG, Pavlova D, Ritchlin CT, Tanaka Y, Takeuchi T, Smolen JS. Thurmond RL, et al. J Rheumatol. 2016 Sep;43(9):1637-42. doi: 10.3899/jrheum.160164. Epub 2016 Jul 15. J Rheumatol. 2016. PMID: 27422891 Clinical Trial.
OBJECTIVE: To assess toreforant (selective histamine H4 receptor antagonist) in active rheumatoid arthritis (RA). ...CONCLUSION: Toreforant was not effective in phase IIb testing....
OBJECTIVE: To assess toreforant (selective histamine H4 receptor antagonist) in active rheumatoid arthritis (RA). ...CO …
An Immunohistochemical Investigation of Renal Phospholipidosis and Toxicity in Rats.
Ma JY, Snook S, Garrovillo S, Johnson C, La D. Ma JY, et al. Int J Toxicol. 2017 Sep/Oct;36(5):386-394. doi: 10.1177/1091581817726040. Epub 2017 Aug 18. Int J Toxicol. 2017. PMID: 28820006
This study used LAMP-2 immunohistochemistry (IHC) to diagnose phospholipidosis in rats exhibiting renal tubular injury. Rats were administered toreforant, a histamine H4 receptor antagonist by oral gavage at a dose of 3, 10, or 100 mg/kg/d for 6 months. ...Th …
This study used LAMP-2 immunohistochemistry (IHC) to diagnose phospholipidosis in rats exhibiting renal tubular injury. Rats were administer …