Faropenem medoxomil is an ester prodrug derivative of the beta-lactam antibiotic faropenem. The prodrug form of faropenem offers dramatically improved oral bioavailability and leads to higher systemic concentrations of the drug. Faropenem medoxomil is a broad-spectrum antibiotic that is highly resistant to beta-lactamase degradation. It was under development for the treatment of acute bacterial sinusitis, community-acquired pneumonia, acute exacerbation of chronic bronchitis, and uncomplicated skin and skin structure infections.

Dehydroascorbic acid (DHA) is an oxidized form of ascorbic acid. Ascorbic acid is transported in its oxidized form via GLUT1 across the blood-brain barrier. Dehydroascorbic acid delay low-density lipoprotein (LDL) oxidation when added before the initiation of the process, they accelerate the process if added to minimally oxidized LDL. Dehydroascorbic acid is used as biochemical markers of oxidative stress in clinical investigations. Dehydroascorbic acid has been used as a vitamin C dietary supplement.

Iomazenil (also known as Ro16-0154, benzodine) is a partial inverse agonist of central-type benzodiazepine receptors (BZR) which binds specifically to BZR with high affinity and a potential treatment for alcohol abuse. The compound was introduced in 1989 by pharmaceutical company Hoffmann-La Roche as an Iodine-123-labelled SPECT tracer for imaging benzodiazepine receptors (GABAA receptors) in the brain.

Cethromycin is a ketolide antibiotic derived from erythromycin A being investigated for use in community-acquired pneumonia and other respiratory tract infections. Cethromycin possesses reliable activity against the bacteria most commonly associated with community-acquired pneumonia including S. pneumoniae, H. influenzae, M. catarrhalis, M. pneumoniae, C. pneumoniae, and L. pneumophila. Unlike fluoroquinolones, cethromycin has a narrower spectrum of activity against gram-negative bacteria, which may reduce the risk of collateral damage and the incidence of Clostridium difficile infection. It offers an advantage over telithromycin in that hepatotoxicity does not seem to be a concern. The FDA denied approval of cethromycin for the treatment of CAP in 2009, requesting more efficacy data.

Ocaperidone [R 79598] is an equipotent antagonist of central dopamine D2 and serotonin2 receptors being investigated as a potential antipsychotic agent. Ocaperidone is a benzisoxazol piperidine antipsychotic primarily binds and with high affinity to 5-HT2 (serotonin) receptors, alpha1 and alpha 2 adrenergic receptors, dopamine D2 receptors and histamine H1 receptors. Ocaperidone is an antagonist primarily at the 5HT and D2 receptors. A proposed mechanism of action is the central D2 receptor blockade which is common to all neuroleptics that are used to treat positive symptoms of schizophrenia.

Mimbane was developed by Parke-Davis as an analgesic. Information about the current use of the drug is not available.

Rebeccamycin analog (RA, Becatecarin/ BMS 181176, rebeccamycin derivative, NSC 655649) is an antitumor antibiotic with inhibitory activity against both topoisomerase I and II, and DNA-intercalating properties. The mechanism of action of becatecarin is not exactly known, but it is thought that by inhibiting (blocking) the function of topoisomerase enzymes, it will destroy cancer cells and slow down the growth of the tumour. On 25 July 2006, orphan designation (EU/3/06/388) was granted by the European Commission to Helsinn Birex Pharmaceuticals Ltd, Ireland, for becatecarin for the treatment of cancers of the biliary tree.

Duazomycin (N-acetyl-DON) is one of the few naturally occurring compounds containing an aliphatic alpha diazoketo group, and is produced by Streptomyces ambofaciens. It is a derivative of 6-diazo-5-oxo-L-norleucine (DON) which was initially isolated from an unidentified Streptomyces species and which is produced together with N-acetyl-DON and duazomycin B (azotomycin) by S. ambofaciens. Duazomycin inhibited purine biosynthesis and caused accumulation of phosphoribosyl-N-formylglycineamide (FGAR) at low levels of inhibitor; higher levels blocked the synthesis of FGAR, indicating that the antibiotic behaved essentially like DON. Duazomycin is readily deacetylated by mammalian acylase to DON. As a glutamine antagonist, duazomycin was used in combination with azathioprine for the treatment of patients with advanced Wegener’s granulomatosis with renal involvement. Prolonged survival, remission of systemic signs and symptoms, roentogenologic improvement of pulmonary lesions, reduction in proteinuria and arrest of progression of renal insufficiency were observed.