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.

Motesanib (AMG 706), a novel nicotinamide, was identified as a potent, orally bioavailable inhibitor of the VEGFR1/Flt1, VEGFR2/kinase domain receptor/Flk-1, VEGFR3/Flt4 and Kit receptors. Motesanib was expected to reduce vascular permeability and blood flow in human tumours. A phase III trial of motesanib in combination with paclitaxel and carboplatin in non-squamous NSCLC has been terminated by Takeda and subsequently the development was discontinued. Motesanib has also been investigated up to phase II in breast, thyroid, colorectal and gastrointestinal stromal tumours. However, development has been discontinued in these indications.

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

Iozomic Acid is triiodobenzoic acid derivative patented by Pharmacia Aktiebolag as X-ray contrast agent for Coronary Angiography.