Cloricromen a drug that inhibits platelet aggregation in man and in experimental thrombosis. Experiments on rodents have revealed that cloricromene which reduced tumor necrosis factor production, could be useful in the treatment of periodontitis. In addition, it could be potentially useful in ischemic-retinal diseases where amelioration of blood flow and inflammation is desirable. However, experiments with patients with cerebrovascular occlusive disease didn’t shown any effect of cloricromen on coagulative variables.

Esonarimod (KE-298), a derivative of propionic acid developed in Japan, has been shown to suppress various animal models of arthritis by inhibiting the production of inflammatory cytokines, such as IL-1β, IL-6 and IL-8, from human peripheral blood mononuclear cells. In vitro, the two stereoisomers showed equivalent potency for antagonism of interleukin-1 and enhancement of lymphocyte transformation. Esonarimod also inhibited tumour necrosis factor-α-induced proliferation of synovial cells. Inhibition of proliferation of cells was not due to nonspecific cytotoxicity. Treatment with esonarimod also significantly reduced chloramphenicol acetyltransferase activity in synovial cells, and diminished activity of the transcription factor AP-1 in the nucleus of synovial fibroblast-like cells. In a phase II trial among 60 patients with rheumatoid arthritis, esonarimod 100-200 mg/day PO for 12 weeks produced significant improvements in the Lansbury index.

Racecadotril (acetorphan) is an oral enkephalinase inhibitor for use in the treatment of acute diarrhea. Racecadotril reduces hypersecretion of water and electrolytes into the intestinal lumen, by preventing the degradation of endogenous enkephalins. Treatment with racecadotril reduces the incidence and duration of acute diarrhea and reduces diarrhea-associated symptoms compared with placebo in adults. Racecadotril treatment also results in significant reductions in stool output compared with placebo in infants and young children aged 2 months to 4 years with acute diarrhea. Both rotavirus-negative and rotavirus-positive infections appear to respond to treatment in the pediatric populations investigated for this infection. Racecadotril shows similar or slightly reduced efficacy to loperamide in the treatment of diarrhea in adults and children aged up to 10 years. However, in comparative trials, racecadotril was associated with fewer adverse events than loperamide, in particular, post-treatment constipation. Racecadotril is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the UK, Spain and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States.

Deprodone is a steroid that was approved in Japan for the treatment of inflammatory skin disorders. The drug is marketed under the name Eclar and contains 0.3% of the prodrug, deprodone propionate.

Bunaprolast has been described as the most potent antioxidant inhibitor of endothelial activation of NF-kB and gene expression of E-selectin and vascular cell adhesion molecule-1. Bunaprolast is a potent inhibitor of leukotriene B4 production in human whole blood and undergoes deacetylation to an initial metabolite with similar pharmacological potency. The in vivo demonstration of inhibition of pulmonary bronchoconstriction by this compound, in a model known to be leukotriene sensitive, coupled with its potent in vitro inhibition of 5-lipoxygenase enzymes, suggests bunaprolast may be of use in 5-lypoxygenase-mediated models of asthma.

Efloxate is a coronary vasodilator developed in 1959 in Italy by Recordati and used for the treatment of angina pectoris. The drug is no longer marketed.

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. The dose is 100 mg twice daily, and should not be given to people with porphyria or breastfeeding mothers and is not recommended for children. Aceclofenac is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of prostaglandins (chemicals in the body which cause pain, swelling and inflammation). Aceclofenac is the glycolic acid ester of diclofenac. The incidence of gastric ulcerogenicity of aceclofenac has been reported to be significantly lower than that of other frequently prescribed NSAIDs: for instance, 2-fold less than naproxen, 4-fold less than diclofenac, and 7-fold less than indomethacin. Aceclofenac is metabolized in human hepatocytes and human microsomes to form [2-(2',6'-dichloro-4'-hydroxy- phenylamino)phenyl] acetoxyacetic acid as the major metabolite, which is then further conjugated.

Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.

Adafenoxate exerts nootropic and anxiolytic properties in rodents. Adafenoxate inhibits monoamine oxidase and cAMP phosphodiesterase activity. Adafenoxate inhibits monoamine uptake and regulates the density of the 5-HT1 sites in the brain.

Guacetisal (Broncaspin) is a bronchomucotropic synthesized by the Bayer Italia S.p.A. Research Laboratories. It is obtained from the esterification of acetylsalicylic acid with guaiacol. Guacetisal was used for the treatment of chronic bronchitis and other inflammatory diseases of the respiratory tract. Guacetisal, used rectally, proved to be a valuable instrument for anti-inflammatory and anti-cough treatment in acute diseases of the airways in infancy.