Elsibucol (AGI-1096) is a phenolic intracellular antioxidant with anti-inflammatory and antiproliferative properties. In vitro, elsibucol inhibited the inducible expression of vascular cell adhesion molecule (VCAM)-1, E-selectin, and monocyte chemoattractant protein (MCP)-1 in endothelial cells and tumor necrosis factor (TNF)-alpha and interleukin (IL)-1beta secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells. It also inhibited serum-stimulated proliferation of aortic smooth-muscle cells. In vivo, elsibucol demonstrated anti-inflammatory properties in a murine delayed-type hypersensitivity model. In hypercholesterolemic animals, elsibucol inhibits atherosclerosis and preserves endothelial healing following arterial injury. Elsibucol development for the prevention of transplant rejection has been discontinued.

Pimetacin is the thio-ester of indometacin. It is antithrombotic and anti-inflammatory agent. Pimetacin produced dose-related enhancement of the OpZ-induced chemiluminescence from resident peritoneal macrophages.

Diflumidone is a non-steroidal antiinflammatory drug. It inhibits the biosynthesis of prostaglandin by bovine seminal vesicle microsomes and arachidonic acid-induced aggregation of human platelets in a concentration-dependent manner. Diflumidone is a competitive inhibitor of prostaglandin synthetase. Diflumidone also inhibits equally the formation of PGE2 and PGF2a, which suggests blockade of endoperoxide formation. The relative topical efficacy of indomethacin and diflumidone for the suppression of ultraviolet-light-induced erythema has been compared in a randomized, double-blind, placebo-controlled study in man. At 24 h after application, the indomethacin-treated sites had significantly less erythema than did the diflumidone-treated sites.

Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.

Ramifenazone is pyrazolone derivative with analgesic, antipyretic, and anti-inflammatory activity. In preclinical studies, Ramifenazone shows potent inhibition of prostaglandin production, carrageenan edema, and yeast fever.

Prefenamate is an esters of N-substituted anthranilic acid patented by Ferrer Internacional S. A. as antiinflammatory agent

Tesimide is an isoquinolinedione derivative patented by Warner-Lambert Co. as anti-inflammatory agent.

Timegadine Is a quinolylguanidine derivative patented by Loevens Kemiske Fabrik Produktionsaktieselskab as an anti-arthritic agent. Timegadine acts as a potent, competitive inhibitor of cyclo-oxygenase and lipo-oxygenase. Timegadine significantly inhibits both the primary and secondary lesions of rats adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide. In clinical trials, Timegadine significantly improves both biochemical and clinical markers of disease activity, i.e. ESR, serum IgG and IgM, leukocyte and platelet counts, duration of morning stiffness, Ritchie index, number of swollen joints and pain. Timegadine treatment associated with gastrointestinal and allergic side effects.