Manifaxine (GW 320659) is a highly selective neuronal norepinephrine and dopamine re-uptake inhibitor. It has been in phase II clinical trials by GlaxoSmithKline for the treatment of attention deficit hyperactivity disorder and obesity. Manifaxine development has been discontinued.

Bemarinone (ORF 16600) is a positive inotropic and vasodilator agent with potential clinical utility in the management of congestive heart failure. The compound selectively and competitively inhibited cyclic AMP phosphodiesterase fraction III. However, further studies were discontinued

Nanterinone [UK 61260], a phosphodiesterase III inhibitor, was undergoing II evaluation with Pfizer in the US for the treatment of heart failure. Nanterinone is a positive inotropic and balanced-type vasodilating drug, only partially based on phosphodiesterase III inhibition. Preliminary data from controlled studies suggest satisfactory long-term efficacy and safety.

Veribulin is a novel microtubule destabilizer that both functions as a potent cytotoxin and acts as a vascular disrupting agent (VDA). It binds to the same (or nearby) sites on β-tubulin as colchicine. It is capable of evading multidrug resistance pumps and, thus, achieves high CNS concentrations. It is efficacious in multiple xenograft models without CNS toxicity. Veribulin had previously demonstrated pre-clinical and clinical activity in multiple tumor types. Veribulin is in phase II clinical trial for the treatment of Glioblastoma and Malignant melanoma.

Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.

Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.

Acolbifene, the active metabolite of EM-800, was identified as a pure antagonist that acts on both activation domains of the ERs. It is in Phase III clinical trials for the prevention of breast cancer and vasomotor symptoms (Hot flush) in postmenopausal women. Most commonly reported adverse events included irregular menses, leg/muscle cramps, diarrhea, and hot flashes. No serious adverse events were reported.

Thiphencillin is a penicillin analog patented by Abbott Laboratories as an antibacterial agent. Thiphencillin shows potent antibacterial activity against various species and genera of pathogenic bacteria.

Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.

Liarozole is an imidazole-containing compound that inhibits the cytochrome P-450-dependent metabolism of all-trans-retinoic acid (RA). Liarozole, a retinoic acid (RA) metabolism-blocking agent (RAMBA) in clinical development, has been granted orphan drug designation for congenital ichthyosis by the European Commission and the U.S. Food and Drug Administration. Later, based on the mixed results from a phase II/III trial of liarozole for the treatment of ichthyosis, Barrier decided to discontinue the development of liarozole. Liarozole displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.A large phase III international study was completed comparing liarozole 300 mg twice daily with cyproterone acetate (CPA) 100 mg twice daily in a total of 321 patients with metastatic prostate cancer in relapse after first-line endocrine therapy. The results indicate that liarozole might be a possible treatment option for prostate cancer (PCA) following failure of first-line endocrine therapy.