ISOMETHEPTENE, (R)- is an antimigraine drug candidate, which development was discontinued in 2016. It is a potent agonist of the imidazoline-1-receptor.

Esaprazole, also known as hexaprazole, was developed in the 1980s as a drug for the treatment of gastric and duodenal ulcers. Esaprazole exerts a dose-dependent cytoprotective effect on the gastric mucosa in man. It was shown to have a dose-dependent antisecretory activity, which was particularly evident on secretion volume and acid output. Esaprazole completed phase II clinical trials with only a few minor side effects being reported, but was shown to be less effective than Cimetidine and Ranitidine at healing ulcers. Esaprazole is a weak sigma opioid receptor and muscarinic acetylcholine receptors M3 and M5 ligand. Esaprazole analogs with many compounds showing neuroprotective properties.

PF-3758309 was developed as an ATP-competitive inhibitor of PAK4. In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). PF-3758309 blocks the growth of multiple human tumor xenografts, with a plasma EC50 value of 0.4 nM in the most sensitive model. PF-3758309 is antiproliferative and induces apoptosis in an HCT116 tumor model.

FENIROFIBRATE, (-)- is a metabolite of fenofibrate, an antilipemic agent which reduces both cholesterol and triglycerides in the blood.

Phencarbamide is an anti-spasmodic and anticholinergic drug used during parturition. It has a specific antispasmodic action on the smooth muscle, both directly like papaverine and through the autonomic nervous system (atropine effect). It has also an analgesic effect of its own. Side-effects generally associated with the atropine group of drugs.

CBL0137 (also known as Curaxin CBL0137) is a metabolically stable curaxin and belongs to the class of small molecules with anti-cancer activity. CBL0137 is in Phase I clinical trials to treat hematological malignancies and solid tumors. CBL0137 binds to Facilitates Chromatin Transcription (FACT) and sequesters the FACT complex on chromatin, which inhibits its activity. This prevents transcription of certain genes involved in cancer-associated signaling pathways; it specifically inhibits the transcription of both NF-kappa β and heat shock transcription factor 1 (HSF1) and simultaneously activates p53. In addition, CBL0137 was investigated in vitro and in models mice for pancreatic ductal adenocarcinoma (PDA) and the obtained data suggested testing of CBL0137 efficacy in Phase II trial in PDA patients alone and in combination with gemcitabine.

Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric disorders and facilitated participation in behaviour therapy. During clinical trials, unexpected observations indicated that ritanserin may be of value in treating obsessive-compulsive disorder, acute mania, negative symptoms of schizophrenia, drug addicts, etc. Clinical observations confirmed the efficacy of ritanserin in the chronic withdrawal phase after detoxification from ethanol. Ritanserin had been in phase III clinical trials by Janssen L.P. for the treatment of anxiety disorder and major depressive disorder. However, the clinical development of ritanserin was discontinued.