Oxophenarsine was developed as an antisyphilis drug that can inhibit HIV-1 production. However, information about the further development of this drug is not available.

Naronapride (ATI-7505), an orally administered, cisapride analogue and serotonin4 (5HT4) receptor agonist, is being developed by Renexxion for the treatment of multiple gastrointestinal disorders. Sinovant is initially developing naronapride for the treatment of irritable bowel syndrome – constipation (IBS-C), a disease that affects millions of Chinese patients and for which few effective treatment options are available. Naronapride has been evaluated in over 900 subjects in multiple randomized controlled clinical studies and has demonstrated promising results in patients with gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and chronic idiopathic constipation (CIC). Naronapride’s low systemic absorption and high specificity for 5HT4 and D2 receptors is thought to improve its safety and tolerability profile relative to other members of the class.

Meletimide (R 5183) is a powerful anticholinergic agent with pronounced peripheral and central action.

IPROPLATIN is a quadrivalent second-generation platinum complex. It binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and tumor cell death. IPROPLATIN was discontinued in phase III clinical trials.

FLUBEPRIDE, a substituted benzamide, is an antidepressant drug. Its activity resides in the R-(+)-enantiomer.

Elinafide (LU 79553) is a bisintercalating naphthalamide and a topoisomerase II inhibitor has demonstrated a higher binding affinity for DNA and significant antitumour efficacy against a panel of established tumour cell lines, including several multidrug resistant-positive sublines. Elinafide had been in phase II clinical trial for the treatment of ovarian cancer and phase I trials for the treatment of various solid tumours. The major haematological toxicities observed were anaemia and neutropenia. The major non-haematological toxicities observed in the 3-weekly schedule were neuro-muscular presenting clinically as a mixed syndrome of severe weakness (sometimes with pain in both legs), myalgia and arthralgia, asthenia/fatigue/malaise. One fatality was considered related to LU 79553, as the patient had fever and neutropenia. Clinical study of this drug candidate was discontinued due to its neuromuscular dose-limiting toxicity.

Levophenacylmorphan is the synthetic narcotic analgesic and sedative agent. Levophenacylmorphan have been used as pre-anaesthetic medication. Phenazocine and levophenacylmorphan have similar pharmacologic properties and similar analgesic potency. Levophenacylmorphan is under international control according to the UN Single Convention 1961 and its amendments. It is not found in any pharmaceutical preparations sold in the United States.

Pobilukast is the Leukotriene D4 receptor antagonist. Pobilukast significantly attenuated the Salmonella enteritidis endotoxin-induced thrombocytopenia but had no effect on either the endotoxin-induced early leukopenia or late leukocytosis. Additionally, Pobilukast significantly reduced the endotoxin-induced hemoconcentration and improved survival to 30% at 48 hr. Pobilukast dose-dependently inhibited the immediate hemodynamic changes after leukotriene D4 (LTD4) injections. Pobilukast also attenuated the increase in vascular permeability and the prolonged decrease in CO, suggesting that the observed cardiac and vascular effects of LTs were mediated by stimulation of LT receptors. A shift toward the right of the dose-response curves to histamine with pobilukast compared to that with placebo in three subjects was demonstrated, whereas the active compound did not exhibit any protective effect against histamine in the remaining nine subjects. It was concluded that there is a leukotriene component to the bronchial responses to histamine in some, but not all, subjects. Pobilukast had been in phase II clinical trial for the treatment of asthma. However, this development was discontinued.

EC-18 (now known as mosedipimod), a synthetic copy of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) that was developed by Enzychem Lifescience for oral administration for the treatment of immune and inflammatory related diseases, including psoriasis, rheumatoid arthritis, asthma, atopic dermatitis, and sepsis. The US Food and Drug Administration (FDA) has granted Orphan Drug Designation to EC-18 for the treatment of Acute Radiation Syndrome (ARS) and for the for the neutropenia treatment. Besides, the EC-18 is participating in phase II clinical trials to investigate the efficacy and safety of the agent for chemoradiation-induced oral mucositis and chemotherapy-induced neutropenia. This drug has a multimodal mechanism of action. It stimulates calcium influx into T lymphocytes and increases the production of various cytokines. In addition, EC-18 enhances the cytolytic activity of natural killer (NK) cells and suppresses the expression of the transmembrane protein tumor cell toll-like receptor 4 (TLR-4) on cancer cells, thus suppresses tumor cell proliferation.