Tofetridine is an analgesic agent.

Tesmilifene is a small-molecule antineoplastic drug and chemopotentiator that was under development by YM BioSciences for the treatment of breast cancer. Tesmilifene was developed as a selective ligand of the antiestrogen binding sites without estrogen receptor affinity. Tesmilifene potentiates the cytotoxicity of a variety of chemotherapy drugs in vitro and in vivo. Tesmilifene in combination with doxorubicin provides an unexpected and very large survival advantage over doxorubicin alone in a randomized trial in phase III clinical trial in advanced breast cancer. Unfortunately, Tesmilifene application associated with high rate disease and treatment-related adverse events and poor quality of life. Based on these results further development of Tesmilifene was discontinued

Selprazine was developed as a sedative agent for inhibition of aggression. Information about the current use of this compound is not available.

Saterinone, a dual-action drug combines both alpha-1 blocking vasodilatory property and phosphodiesterase III (PDE III) inhibition--mediated inotropism. PDE III inhibitors are well established in the acute intravenous treatment of patients with decompensated chronic congestive heart failure. Saterinone was demonstrated to be a safe and potent drug on short-term application without major changes in myocardial oxygen consumption. Saterinone was studied in phase II trials in Germany for the treatment of heart failure. However, the development of this drug has been discontinued.

Naftypramide is a nonsteroidal anti-inflammatory drug. It was used in the treatment of gynecological inflammatory diseases.

Mitonafide is a nitro-containing antitumor drug. Mitonafide participated in clinical trials phase II in colorectal cancer patients, however, the results have shown that the drug was not active and induced severe myelotoxicity. Besides, the drug was involved in phase II for the patients with non-small cell lung cancer (NSCLC), where it was not active in spite of the safe administration. Information about the current development of this drug is not available.

Metitepine, a psychotropic agent was developed as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors. Metitepine has never been marketed.

Aranotin, a metabolite of Arachniotus aureus, possesses the antiviral and antibiotic properties. It inhibits viral RNA synthesis against strains of rhino-, coxsackie, polio- and parainfluenza viruses.