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.

Exherin is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. In murine melanoma xenografts, ADH-1 in combination with melphalan significantly reduced tumor growth up to 30-fold over melphalan alone. ADH-1 enhancement of response to melphalan was associated with increased formation of DNA adducts, increased apoptosis, and intracellular signaling changes. In a pilot study (phase I trial), ADH-1 intravenous pretreatment before chemotherapy in metastatic melanoma completely destroyed tumors in half of patients

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.

GSI-136 is an amyloid protein secretase inhibitor that has been tested for treatment of Alzheimer Disease. This γ-Secretase inhibitor was evaluated in a phase I clinical trial to determine its safety and tolerability in healthy subjects after administration of single oral doses.

MK-7145 is a piperazine derivative patented by Merck Sharp & Dohme Corporation as the renal outer medullary potassium channel inhibitor useful for the treatment of hypertension and heart failure. In preclinical studies, MK-7145 shows selectivity against other cardiac ion channels such as Cav1.2, Nav1.5, and Kir2.1, Kir2.3, Kir4.1, or Kir7.1. In 2011 MK-7145 was studied in phase I clinical trials but no further development reports were published.

Friulimicin B (or friulimicin) is a naturally occurring antibiotic produced by a microorganism Actinoplanes friuliensis. This drug is active against a broad spectrum of gram-positive multi drug resistant, invasive pathogens. Friulimicin B participated in phase I clinical trials provided by MerLion Pharmaceuticals for the treatment of nosocomial infections. However, information about the further development of this drug is not available.

GW 274150 was developed by GlaxoSmithKline as a selective inhibitor of inducible nitric oxide synthase (iNOS; also known as NOS2). Nitric oxide synthase (NOS) is an important chemical involved in the production of NO. Reduction of NOS, and therefore NO, may be an effective technique for the treatment of migraine headache. GW 274150 offered the potential of anti-inflammatory activity in migraine through a novel mechanism of action. The drug has completed phase II of the clinical trials for patients with rheumatoid arthritis and migraine disorders. In addition, GW 274150 was involved in phase I clinical trial for patients with mild asthma. However, all these studied were discontinued.