Didrovaltrate is an active compound derived from Valeriana plant. In experiments with rat HTC cells, didrovaltrate showed considerable cytotoxicity which made it a promising agent for the treatment of cancer. There are no clinical trials available on the drug, however, there are studies reporting its clinical use (under the name Valmane) in patients with kidney cancer, oral cavity cancer, breast cancer and lung cancer. It is believed that the drugs acts by inhibiting the protein synthesis. The current marketing status of the drug is unknown and supposed to be "discontinued".

Aceclidine is a parasympathomimetic agent used in the treatment of open-angle glaucoma as topical eye drop solution. It is as a muscarinic acetylcholine receptor agonist with weak anticholinesterase activity. Acting directly on the motor end-plate (cholinergic nerve endings) it decreases intraocular pressure and mediates the contraction of iris muscle. Aceclidine increased outflow facility in human eyes in vitro by a direct stimulation of the outflow tissues in the absence of an intact ciliary muscle. This effect was biphasic, occurring at concentrations of 10 uM and lower with no effect at higher concentrations. Passed numerous clinical trials in Russia, France, Italy and other countries and was widely used in Europe but never been in clinical use in USA.

Chloroprednisone acetate is the 21-acetate ester of chloroprednisone. Chloroprednisone acetate was sold under the brand name Topilan as an anti-inflammatory agent.

Cyproterone belongs to a group of medications known as steroidal antiandrogens. It suppresses testosterone and its metabolites. It has approximately three-fold lower potency as an antagonist of the androgen receptor relative to cyproterone acetate. Cyproterone acetate is used to treat advanced prostate cancer and acne.

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.