Instituut voor Neuropathische Pijn
English articles Research & Development PH-797804 in neuropathic pain: a Novel N-Phenyl Pyridinone Inhibitor of p38 MAP
| PH-797804 in neuropathic pain: a Novel N-Phenyl Pyridinone Inhibitor of p38 MAP |
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A proof-of-concept study to determine if PH-797804 reduces neuropathic pain associated with post-herpetic neuralgia is under way (2010). Patients will be randomized to receive either PH-797804 or placebo for 4 weeks, during which time they will also record their pain symptoms using various pain scales. PH-797804 is a compound from Pfizer.
N-phenyl pyridinone p38 MAP kinase inhibitor benzamide [3- [3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2- oxo-1(2H)-pyridinyl]-N,4-dimethyl-, (−)-(9CI); PH-797804] is the full name of the compound PH-797804. It is is an ATP-competitive inhibitor of the α isoform of human p38 MAP kinase, and it blocks inflammation-induced production of cytokines and proinflammatory mediators. After oral dosing, PH-797804 inhibits acute inflammatory responses induced by systemically administered endotoxin in animal models. Furthermore, PH-797804 demonstrates robust anti-inflammatory activity. [1] The rationale to test this compound in neuropathic pain is not very clear, as we do not have access to animal model data supporting this pain indication. March 2010, Jan M. Keppel Hesselink, MD, PhD Referenties[1]: Hope HR, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, Keith RH, Li X, Mbalaviele G, Messing DM, Saabye MJ, Schindler JF, Selness SR, Stillwell LI, Webb EG, Zhang J, Monahan JB. | Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. | J Pharmacol Exp Ther. | 2009 Dec;331(3):882-95. Epub 2009 Aug 31. |