V. Panajotova et al., PHARMACOLOGICAL PROFILE OF THE NOVEL POTENT ANTIRHEUMATIC ',4'-DIFLUOROBIPHENYL-4-YL)-2-METHYL-4-OXOBUTANOIC ACID, Arzneimittel-Forschung, 47(5), 1997, pp. 648-652
On the basis of basic screening for novel, more potent antiarthritics
VUFB-16066 ',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid, CA
S 112344-52-2) was chosen as a compound with pronounced anti-inflammat
ory and immunomodulatory effects, with good gastric tolerance and rela
tively low toxicity. VUFB-16066 Is a dual cyclooxygenase and 5-lipoxyg
enase inhibitor, and it suppresses alloantigen-driven cellular immune
response and phagocytosis of stimulated peritoneal cells. VUFB-16066 e
xhibits prolonged pharmacological activity connected with its major me
tabolite having a very long half-life. In the model of adjuvant arthri
tis VUFB-16066 improves most of disease symptoms including immunopatho
logical disturbances, which indicates possible disease-modifying activ
ity of the drug. The beneficial antiarthritic effect of VUFB-16066 has
been also confirmed in patients with rheumatoid arthritis.