Toreforant (JNJ-38518168) is an orally active, selective histamine H4 receptor antagonist. Toreforant was investigated as an agent for the treatment of active rheumatoid arthritis. While some improvement in rheumatoid arthritis signs/symptoms through week 12 was observed in the phase IIa study, no efficacy was observed with toreforant at lower doses in a subsequent phase IIb study. Toreforant has been tested in clinical studies in patients with asthma and psoriasis. Toreforant failed to provide therapeutic benefit in population of patients with uncontrolled, eosinophilic, persistent asthma. Toreforant efficacy at 30 and 60 mg was greater than placebo but did not meet predefined success criterion in patients with moderate-to-severe psoriasis.

CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 for potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.

Cannabidivarin is a homolog of cannabidiol, with a well-established antiepileptiform profile in preclinical studies, both in vitro and in vivo animal models of epilepsy. The oral bioavailability of cannabidivarin is very low (about 6%) due to erratic absorption and first pass metabolism. After oral administration, the maximum plasma concentration of Cannabidivarin is rising in about three hours and the drug has a large volume of distribution, because of his link to protein plasma, being highly liposoluble, so CBDV can penetrate well to the brain. Cannabidivarin is also metabolized in the liver to 7-COOH and 6-OH metabolites, but the mechanism is also unknown. There is an ongoing phase II double-blind, placebo-controlled trial that is assessing the efficacy and safety of cannabidivarin in Children With Autism Spectrum Disorder (ASD).

Fluoromisonidazole (FMISO) is a small, water-soluble molecule with a molecular weight of 189.14 Daltons. It has an octanol:water partition coefficient of 0.41, so that it would be expected to reflect plasma flow as an inert, freely-diffusible tracer immediately after injection, but later images should reflect its tissue partition coefficient in normoxic tissues. Fluoromisonidazole is used as a positron emission tomography (PET) radiotracer for imaging hypoxia when labeled with fluorine-18. It is the most widely used nitroimidazole imaging agent for use as a non-invasive way to localize and quantify hypoxia.

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates luteinizing hormone (LH)/follicle-stimulating hormone release, whereas continuous subcutaneous exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of testosterone levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. In accordance with the T reductions, TAK-448 treatment showed also more rapid reduction in plasma prostate-specific antigen(PSA) levels. TAK-448 had been in phase II clinical trials for the treatment of prostate cancer. However, this research has been discontinued.

LAUDEXIUM is a non-depolarizing neuromuscular blocking agent. It was used in surgical anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation.