INCB9471 is a non-competitive, potent and selective CCR5 small-molecule antagonist patented by pharmaceutical company Incyte Corporation for treatment of human immunodeficiency virus infection. INCB9471 potently inhibited macrophage inflammatory protein-1beta-induced monocyte migration and infection of peripheral blood mononuclear cells by a panel of R5-HIV-1 strains. INCB9471 was shown to be safe and highly efficacious in reducing HIV viral load in phase I and II human clinical trials

Aspaminol (1,1 diphenyl-3-piperidinobutanol hydrochloride) is a nonspecific smooth muscle relaxant. It inhibits calcium uptake. The relaxation of smooth muscle induced by aspaminol may be due to a combining of aspaminol with calcium ions at the binding sites on the surface of smooth muscle, thus decreasing the supply of calcium ions to the contractile element.

Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.

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.

Elesclomol (also known as STA-4783), originally identified in a cell-based phenotypic screen for pro-apoptotic activity, is a novel small-molecule that potently induces apoptosis of cancer cells through the rapid generation of reactive oxygen species (ROS) and the induction of unmanageable levels of oxidative stress. Elesclomol exhibits antitumor activity against a broad spectrum of types of cancer cell in human tumour xenograft models due to its excessive ROS production and elevated levels of oxidative stress leading to the death of cancer cells. Elesclomol is currently being studied as novel cancer therapeutic, in which it has demonstrated the ability to prolong progression-free survival in study subjects. Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells. Elesclomol requires a redox-active metal ion to function; the Cu(II) complex is 34 times more potent than the Ni(II) complex and 1040-fold more potent than the Pt(II) complex. Elesclomol is an HSP-90 Inhibitor with pro-apoptotic and potential antineoplastic activities. Elesclomol induces oxidative stress and triggers mitochondrial-induced apoptosis in cancer cells. Elesclomol is being developed by Synta Pharmaceuticals and GlaxoSmithKline as a chemotherapy adjuvant and has received both fast track and orphan drug status from the U.S. Food and Drug Administration for the treatment of metastatic melanoma. Synta Pharmaceuticals announced on February 26, 2009, the suspension of all clinical trials involving Elesclomol due to safety concerns. In March 2010, Synta announced that the FDA had approved resuming clinical development of elesclomol, and that they expected to initiate one or more clinical trials for elesclomol in the second half of the year. In a small, randomized phase II study, elesclomol was shown to significantly increase progression-free survival in people with metastatic melanoma when given in addition to paclitaxel (Taxol).

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.

Gepotidacin (formerly GSK2140944) is a novel, first-in-class, triazaacenaphthylene antibacterial that selectively inhibits bacterial DNA gyrase and topoisomerase IV by a unique mechanism, one that is not utilized by any currently approved human therapeutic agent. As a consequence of its novel mode of action, gepotidacin is active in vitro against target pathogens carrying resistance determinants to established antibacterials, including fluoroquinolones. Gepotidacin has demonstrated in vitro activity against key pathogens, including drug-resistant strains, associated with a range of conventional and biothreat infections. GlaxoSmithKline is developing Gepotidacin for the treatment of gonorrhoea and skin and soft tissue infections.

Recilisib (also known as EX-RAD or ON-01210) is a radioprotectant, which means that this compound can protect cells from harmful effects of ionizing radiation. Unlike other radioprotectors, recilisib is not a free-radical scavenger or responsible for cell cycle arrest. Recilisib was suggested to have a different radiation protection mechanism involving DNA repair pathways. This compound has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. In studies with healthy volunteers, recilisib was rapidly absorbed and well-tolerated, with only mild adverse events. Phase I clinical trials have been completed.

AFN-1252 (now known as Debio-1452) is an antibiotic drug which is in phase II of clinical trials for the treatment of Staphylococcal skin and skin structure infections. The drug was effective in vitro against all isolates of S.aureus and its effect was explained by inhibition of enoyl-acyl carrier protein Reductase (FabI).