Timcodar (also known as VX-853) is a benzenepropanamide derivative patented by Vertex Pharmaceuticals Incorporated as an efflux pump inhibitor for the treatment of multi-drug resistant bacterial infection. Timcodar potentiates the activity of ethidium bromide (EtBr), a model efflux substrate, against three clinically significant gram-positive pathogens: Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pneumoniae. Timcodar weakly inhibits M. tuberculosis growth in broth culture but shows a 10-fold increase in the growth inhibition of M. Tuberculosis cultured in host macrophage cells and demonstrated synergy with rifampin, moxifloxacin, and bedaquiline. In a mouse model of tuberculosis lung infection, timcodar reduces the likelihood of a relapse infection and potentiates the efficacies of rifampin and isoniazid. Timcodar in combination with Doxorubicin was studied in phase 1/2 clinical trials in patients with solid tumors, but no results have been published.

KETORFANOL, a morphinan derivative, is an opioid analgesic. It showed potent antiwrithing activity in the animal assay. It was equipotent with morphine as an agonist and lacked antagonist activity up to 10 mg/kg.

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.