Filorexant (MK-6096) is a novel, structurally distinct dual orexin receptor antagonist, conclusively validates orexin signalling mechanism as a specific and effective target for the treatment of insomnia and potentially other disorders in which sleep/wake dysregulation occurs. Also, it is being investigated as a possible agent against diabetic neuropathies, major depressive disorder and for the a migraine prophylaxis. Detected adverse events are: sleep-onset paralysis, excessive daytime sleepiness. As of May 2015, filorexant is no longer listed on Merck's online development pipeline.

Quinazosin is a diaminoquinazoline derivative patented by Pfizer, Chas., and Co., Inc. as a hypotensive agent. Quinazosin acts as adrenoreceptor antagonist and in preclinical studies lowered systolic blood pressure in conscious hypertensive dogs, without having any significant effect on their heart rate. Quinazosin lowered blood pressure and reduced total peripheral vascular resistance, while the duration of these effects was dose-dependent. In cats, Quinazosin reduced or reversed the pressor effects of epinephrine, but did not alter those of angiotensin amide.

Evodenoson (ATL-313) is an agonist of adenosine A2A receptor. It exerts anti-inflammatory activity through activation of adenosine A2A receptors on CD4+ T cells and neutrophils. Evodenoson demonstrates efficacy in animal models of sepsis, myocardial infarction, allograft rejection and enteritis.

Tyroserleutide (YSL) is a tripeptide treatment being developed by Shenzhen Kangzhe Pharmaceutical Co Ltd, a subsidary of China Medical System Holdings (CMS), for the treatment of liver cancer. It is initially separated and purified from the hydrolyzates of pig’s spleen, but now can be obtained by chemical synthesis, its chemical name is L-tyrosine-L-serine-L-leucine. Tyroserleutide is an active, low-molecular-weight polypeptide, comprised of three amino acids, that has shown antitumor effects on human hepatocarcinoma BEL-7402 in vitro and in vivo. Tyroserleutide has various advantages over the other bioactive peptides such as its low molecular weight, simple construction, nonimmunogenicity, specificity, few side effects, and ease of synthesis. Tyroserleutide is in Phase-III clinical trials for the treatment of liver cancer.

Esuberaprost (314d) is an active enantiomer of beraprost, a prostacyclin analog. The pharmacologic action of esuberaprost is mediated by specifically binding to PGI2 receptors in smooth muscle cells (the blood vessel’s endothelium) and platelets. Upon binding, the compound widened blood vessels, preventing the formation of blood clots, and lowering blood pressure in the lungs. As a result, it was expected to improve the symptoms of pulmonary arterial hypertension. United Therapeutics announced it has ended its Phase 3 BEAT trial testing esuberaprost as an add-on therapy to its product Tyvaso (inhaled treprostinil) for clinically symptomatic patients with pulmonary arterial hypertension (PAH). According to a company press release, the study failed to reach its main endpoint of delaying the time to first clinical worsening events.