1. Academic Validation
  2. Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid

Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid

  • Arzneimittelforschung. 1997 May;47(5):648-52.
V Panajotova 1 E Andĕrova A Jandera M Kuchar
Affiliations

Affiliation

  • 1 VUFB, a.s. (Research Institute for Pharmacy and Biochemistry), Prague, Czech Republic.
PMID: 9205780
Abstract

On the basis of basic screening for novel, more potent antiarthritics VUFB-16066 (4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid, CAS 112344-S2-2) was chosen as a compound with pronounced anti-inflammatory and immunomodulatory effects, with good gastric tolerance and relatively low toxicity. VUFB-16066 is a dual cyclooxygenase and 5-lipoxygenase inhibitor, and it suppresses alloantigen-driven cellular immune response and phagocytosis of stimulated peritoneal cells. VUFB-16066 exhibits prolonged pharmacological activity connected with its major metabolite having a very long half-life. In the model of Adjuvant arthritis VUFB-16066 improves most of disease symptoms including immunopathological disturbances, which indicates possible disease-modifying activity of the drug. The beneficial antiarthritic effect of VUFB-16066 has been also confirmed in patients with rheumatoid arthritis.

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