Retelleptine (SR-95325 B) is an antitumoral agent. This ellipticine derivative exhibits high toxicity against several rodent tumor models. Retelliptine is thought to intercalate with DNA and inhibit topoisomerase II during DNA replication. A phase I study reported possible drug-related toxicity sporadically such as somnolence, bronchospasm, dry mouth, and vomiting.

Rifamexil (also known as MDL 62769 or P/DEA) is a derivative of rifamycin (a natural antibiotic produced by Amycolatopsis rifamycinica). This drug has greater intrinsic activity against Myobacterium avium (MAC) than rifampin. Information on current use of this compound is not available.

Funapide (also known as TV 45070; XEN 402) is a small molecule blocker of the voltage-gated sodium channels Nav1.7 (SCN9A) and Nav1.8. Funapide was developed as a potential treatment of pain conditions, including osteoarthritis, neuropathic pain, postherpetic neuralgia, and erythromelalgia, as well as dental pain. In April 2013, the US FDA granted orphan drug designation to funapide for the treatment of pain associated with erythromelalgia (EM). EM is a rare autosomal dominant condition characterized by debilitating spontaneous or easily evoked attacks of symmetrical burning pain in the feet and hands, typically associated with elevated skin temperature and erythema (redness of the skin). Funapide also was involved in phase II clinical trials in patients with post herpetic neuralgia and in participants with primary osteoarthritis (OA) affecting a single knee. On March 7, 2018, Teva Pharmaceutical and Xenon Pharmaceuticals entered into a mutual agreement to terminate the collaborative development and license agreement they entered into in 2012 for the pain drug funapide. The reason was that the top line results of funapide phase 2 study in post-herpetic neuralgia patients failed to meet the primary or secondary endpoints.

Picafibrate is clofibrate derivative. It is a hypocholesteraemic agent. Fibrates reduce plasma triglycerides by inhibiting their hepatic synthesis and increasing their catabolism. These effects are due to activation of peroxisome proliferator-activated receptors (PPAR alpha) and induction of the over-expression of genes containing a peroxisome proliferator response element (PPRE) in their promoter.

Bumepidil (also known as CS-611) is intravenously administered coronary vasodilator with antiarrhythmic action. In anesthetized, open-chest dogs Bumepidil in doses of 0.1--1 mg/kg i.v. decreased systemic blood pressure, coronary resistance and arterio-venous oxygen difference and increased coronary sinus outflow in a dose-related manner, but myocardial oxygen consumption was virtually unchanged. At 0.3 mg/kg i.v. of the drug, coronary sinus outflow was doubled, but heart rate and AV conduction time were not changed. Bumepidil shortened the action potential duration (APD) of each tissue, especially of Purkinje fibers, without any significant alterations in the resting membrane potential, action potential amplitude and maximum rate of rising. Bumepidil can be characterized as a coronary dilator virtually devoid of cardiac actions in doses sufficiently increasing coronary blood flow.

Biricodar (also known as VX-710) was developed by Vertex as a chemosensitizing agent designed to restore the effectiveness of chemotherapeutic agents in tumor multidrug resistance. The phase II trials had commenced for biricodar, in combination with chemotherapy, for five common cancer indications: breast, ovarian, soft-tissue sarcomas, small cell lung cancer, and prostate cancer. In spite of completed trials, development of biricodar was discontinued because of the adverse effects.

Divaplon is one of a series of imidazopyrimidine derivatives, which are benzodiazepine receptor ligands. This compound exhibits anxiolytic and anticonvulsant activity but little or no sedative/myorelaxant effects. Divaplon occupied a large percentage of benzodiazepine receptors, as measured with an in vivo binding technique, without inducing any deficit in a rotating drum task in mice, and it is suggested that divaplon is a partial agonist at GABA receptors. No significant anticonvulsant tolerance was seen with the divaplon.

Moguisteine is a non-narcotic antitussive compound. Moguisteine demonstrated inhibitory effect on rapidly adapting irritant receptors that could account for the antitussigenic effect of this compound. Furthermore, it is possible that ATP-sensitive K(+) channels may be involved in the anti-tussive effect of peripherally acting non-narcotic moguisteine. The drug did not show any toxic effect on the dams and their fetuses, nor did it have any teratogenic effect in either of the tested species. Finally, moguisteine had no adverse effects, either on parturition or on peri-and postnatal survival and/or development of the offspring. It was reported that moguisteine to be effective in reducing cough frequency in chronic cough of bronchitis and COPD. It was recommended for the short-term symptomatic relief of coughing. Preregistration of moguisteine in Italy is discontinued.

Ethyl dirazepate is an anticonvulsant compound.

Ethypicone is a hypnotic and sedative agent.