Sipoglitazar (TAK 654) was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARγ, PPARα, and PPARδ. Sipoglitazar was developed to improve peripheral insulin sensitivity, normalize circulating lipid profiles, and reduce body weight in patients with metabolic syndrome and type 2 diabetes mellitus (T2DM). Sipoglitazar was being developed by Takeda for the treatment of diabetes mellitus, however in September 2006, development was discontinued.

Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.

Fenclonine, also known as p-chlorophenylalanine, is an inhibitor of tryptophan hydroxylase, the enzyme that plays a rate-limiting role in the biosynthesis of serotonin. Fenclonine was studied for the treatment of carcinoid syndrome, but the psychological side effects, prevented for the further development for this use.

Lesogaberan is a peripherally restricted high-affinity GABAB-R-specific agonist, originally developed for the treatment of gastroesophageal reflux disease (GERD) that appears to be safe for human use. The toxicity profile shows no indication of hepatic effect. Lesogaberan has been shown to induce decreased body weight and decreased food consumption. A dose-dependent diuretic effect was also noted in rats. Treatment with lesogaberan significantly enhanced replication of human islet cells in vitro, which was abrogated by a GABAB-R antagonist. Lesogaberan may be a promising drug candidate for clinical studies of diabetes intervention and islet transplantation. Disappointingly, in phase IIb study it was shown that lesogaberan is only marginally superior to placebo in gastroesophageal reflux disease (GERD) patients who are partially responsive to proton pump inhibitor (PPI) therapy.

Pracinostat is a pan-histone deacetylase inhibitor being tested in phase II of clinical trials for the treatment of sarcoma, prostate cancer, acute myeloid leukemia, myelofibrosis, myelodysplastic syndrome. The drug was shown to be active in vitro on HCT116 and HL-60 cells.

Lidadronic acid is the calcium metabolism regulator.

Hexacyclonic Acid (aka gevilon) has been clinically demonstrated to produce hypolipidemic effects. It has been investigated as a treatment for coronary heart disease, and hypertensive disease with severe lipid metabolic disturbances. Gevilon has been found to have a hypolipidemic effect in reducing the levels of total cholesterol, beta-cholesterol, triglycerides, increasing alpha-cholesterol levels and normalizing the atherogenicity coefficient; especially in patients with Type IIb dyslipoproteinemia.

Iolixanic Acid is triiodophenoxyalkoxyalkanoic acid derivative patented by Bracco Industria Chimica S.p.A. as a diagnostic agent for cholecystography and urinary tract imaging