TG-100115 is a potent dual inhibitor of PI3K-gamma and PI3K-delta. TG-100115 has broad anti-inflammatory activities. TG-100115 provided potent cardioprotection, reducing infarct development and preserving myocardial function. In murine models of asthma and acute stages of chronic obstructive pulmonary disease, aerosolized TG100-115 demonstrated not only markedly inhibited anti-inflammatory activity but also, in the case of the asthma model, improved functional outcome for the test animals. TG-100115 can be used as a potent TRPM7 kinase inhibitor and a potent inhibitor of breast cancer cell migration.

Antienite oxalate is an anthelmintic agent. Antienite (R 8141) is a metabolite of antazonite (R 6438), which is about 4 times as active as the original compound. R 8141 is active as an anthelmintic in poultry and in rats.

Motexafin lutetium is pentadentate aromatic metallotexaphyrin with photosensitizing properties patented by Pharmacyclics, Inc. as anticancer agent that enhances the cytotoxic potential of photodynamic therapy through several mechanisms, including depleting intracellular reducing metabolites that are necessary for repairing the oxidative damage induced by irradiation. Motexafin lutetium catalyzes the oxidation of intracellular reducing metabolites such as ascorbate, glutathione, nicotinamide adenine dinucleotide phosphate, and protein thiols, generating reactive oxygen species in a process known as futile redox cycling. The depletion (through oxidation) of these reducing metabolites removes the substrate necessary in a cell to repair oxidative damage induced by photodynamic therapy and, left unrepaired, such oxidative DNA damage is converted into lethal double-stranded breaks. Motexafin lutetium has the potential to combine the features of selective localization, ability to be activated by deeply penetrating far-red light, low incidence of skin photosensitization and water solubility. The product was in clinical development as a treatment for several types of solid tumors (as Lutrin), age-related macular degeneration (as Optrin), atherosclerosis and prevention of restenosis (as Antrin).

GlaxoSmithKline was developing GSK-376501 as an oral peroxisome proliferator-activated receptor gamma partial agonist. This compound participated in phase I clinical trials for the treatment and diagnostic of patients with Type 2 Diabetes Mellitus, however, GSK discontinued the study of GSK-376501.

(R)-Ibuprofen, a nonsteroidal anti-inflammatory, is the less active enantiomer of ibuprofen. (S)-enantiomer of ibuprofen has the desired therapeutic effect (160 times more active than its (R)-enantiomer) in the in vitro inhibition of prostaglandin synthesis, while the (R)- ibuprofen is inactive. The accumulation of (R)- ibuprofen can cause serious side effects to the human body such as gastrointestinal pain and production of “hybrid” triglycerides between (R)- ibuprofen and Coenzyme A, which disrupt normal lipid metabolism and membrane function. The R(-)-isomer is almost inactive in inhibiting COX-2.

PX-102 is a methoxyphenylcyclopropane derivative patented by Phenex Pharmaceuticals AG as Farnesoid X receptor agonists useful in the treatment and prophylaxis of FXR-mediated diseases. The Farnesoid X Receptor (FXR) is a bile acid receptor which when activated by Px-102 has a profound positive impact on cholesterol, triglyceride and glucose metabolism in liver and intestine. In preclinical studies, Px-102 potently reduces intestinal uptake of neutral lipids and cholesterol and at the same time enhances the excretion of these lipid species. In addition, Px-102 improves hepatic insulin sensitivity and shows massive hepatoprotective effects in animal models of liver cirrhosis or fibrosis. Phenex Pharmaceuticals completes a phase I trial in Healthy volunteers in Germany in 2012 and no further development report has been published.