T-2000 is an oxopyrimidine derivative patented by Taro Pharmaceutical Industries Ltd. as a tranquilizing agent. T-2000 acts as a modulator of GABA A receptor with well-documented anticonvulsant activity and little sedation in animal models. In vitro, equimolar concentrations of T-2000 and phenobarbital produce equivalent enhancement of GABA-evoked chloride currents. Unfortunately, in clinical trials T-2000 failed to demonstrate efficacy in older patients with essential tremor. Moreover, daily administration of T2000 resulted in higher total blood barbiturate levels, likely accounting for the poor tolerability.

LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.

MB-07811 (VK-2809) is the liver-activated prodrug of a phosphonate-containing thyroid hormone receptor beta agonist MB-07344. In animal studies, it showed potent lipid and cholesterol lowering activity. Viking Therapeutics is developing MB-07811 hypercholesterolaemia and non-alcoholic fatty liver disease.

Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.

Othera Pharmaceuticals developed OT-551 as an antioxidant and anti-inflammatory agent. OT-551 downregulates the overexpression of the protein complex nuclear factor (NF)-kappa B. It is known that NF-kappa B is highly activated when oxidative stress, inflammation, and angiogenesis occurs. OT-551 was studied in phase II clinical trial for the treatment of age-related macular degeneration. In addition, the drug was studied for the treatment of cataracts and dry eyes; however, these studies were discontinued. Besides, phase II clinical trial for the treatment of geographic atrophy has shown that OT-551 might have limited or no benefit as a treatment for this disease.

VILANTEROL α-PHENYL CINNAMATE (GW642444H), originally developed by GlaxoSmithKline, is a long-acting β2 adrenoceptor agonist for once daily treatment of COPD and asthma. Phase III clinical trials are ongoing. GW642444H is Vilanterol a-phenylcinnimate salt. In clinical studies the study drug may been given as a dry powder in the form of either the ‘H’ salt (with the excipient lactose), or in the form of the ‘M’ salt (with the excipients lactose and cellobiose octaacetate). Its pharmacological effect is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increases in cyclic AMP are associated with relaxation of bronchial smooth muscle and inhibition of release of hypersensitivity mediators from mast cells in the lungs.

Gluceptate sodium also known as sodium glucoheptonate (H-Quest A300) is a non-toxic, a non-hazardous chelating agent, which forms stable complexes with di- and trivalent metal ions such as Ca2+, Fe2+, Fe3+, Al3+, etc. This substance is highly compatible with strong alkaline mediums and can prevent the bacterial degradation of the solution. Gluceptate sodium has various applications in water treatment, agricultural, cosmetics, textile processing and in some others fields.

LANOPEPDEN is an inhibitor of peptide deformylase, a bacterial enzyme required for protein maturation. It was in development for the treatment of complicated bacterial skin infection and hospitalized community-acquired pneumonia.