Icrocaptide, also known as ITF 1697, a chemically modified LYS-Pro tetrapeptide that was studied to reduce reperfusion injury. The ability of icrocaptide to inhibit the early functions of activated endothelial cells could be used as pharmacological tool in model of pathologies of a variety of microvascular disorders. In addition, tetrapeptide was involved in phase II clinical trials for patients undergoing percutaneous transluminal coronary angioplasty with or without coronary stenting. As a result, a trend toward reperfusion improvement was seen.

Guaiapate was studied as a sedative agent for a cough. This drug has never been marketed.

Semagacestat (LY-450139) was a gamma secretase inhibitor being developed as a treatment for Alzheimer's disease by Eli Lilly. It was hoped that the drug would help to delay the onset of severe Alzheimer's disease, and thereby help preserve cognitive and executive functioning and in turn improve patient quality of life. Semagacestat (LY-450139) is designed to inhibit gamma secretase, an enzyme that is involved in the cleavage of APP to beta-amyloid. By decreasing production of beta-amyloid, it is hoped that gamma secretase inhibitors will exert a disease-modifying effect in Alzheimer's disease and thus slow or halt the destruction of nerve cells – the final stage in the amyloid cascade hypothesis. In March 2008 semagacestat (LY-450139) advanced to Phase III development, where it was evaluated in the IDENTITY (Interrupting Alzheimer's Dementia by EvaluatiNg Treatment of AmyloId PaThologY) trial, the first Phase III trial for this new anti-dementia drug. In August 2010, Eli Lilly announced its decision to halt the development of Semagacestat. The decision was taken after analysing the preliminary results of the second Phase III clinical trial of the drug, which indicated that semagacestat failed to slow disease progression. The drug, in fact, worsened cognition and the ability to perform day-to-day activities.

Paliroden is an orally active drug that activates the synthesis of endogenous neurotrophins or nerve growth factors. Paliroden was investigated in phase II clinical trial in patients with Alzheimer's disease and to evaluate its effect on 18F-Dopa PET imaging in patients with Parkinson's disease. The further development of paliroden was discontinued due to its insufficient efficacy.

Sulamserod is a methanesulfonamide derivative patented by British multinational pharmaceutical company GlaxoSmithKline as 5-HT4 receptor antagonist, with antiarrhythmic activities for the treatment of the certain cardiovascular condition. 5-HT4 receptor blockade could have antiarrhythmic effects by decreasing intracellular Ca2+ concentration and delayed rectifier potassium current and prolonging atrial refractory period. In preclinical models, Sulamserod prolongs mean atrial effective refractory period and wavelength, reduces the dispersion of effective refractory period, and minimally slows conduction velocity in pigs.

Phencarbamide is an anti-spasmodic and anticholinergic drug used during parturition. It has a specific antispasmodic action on the smooth muscle, both directly like papaverine and through the autonomic nervous system (atropine effect). It has also an analgesic effect of its own. Side-effects generally associated with the atropine group of drugs.

Cimaterol is a chemically stable nonselective agonist β1-, β2-, and β3-adrenoceptors. Cimaterol is used in sport as a stimulant and a fat burner that assists bodybuilders and strength athletes to get rid of body fats. Aside from shedding off fats, another benefit for using cimaterol for athletes is a boost in strength as well as an increase in muscle size or lean body mass. The increase in muscle size has been seen in previous animal studies when cimaterol is used. However, the reason behind the muscle gain is not identified yet, but the body has a very different response compared from taking in anabolic steroids. Experts in the field are saying that the increased nitrogen retention, that is known to cause by cimaterol, maybe the reason behind the muscle gain. Another great thing about Cimaterol is that, it can improve blood flow.

Perzinfotel (EAA-090) is a novel squaric acid amide derivative that has been identified as a potential treatment for ischemic brain damage resulting from stroke. EAA-090 is a competitive inhibitor at the NMDA-selective subtype of the glutamate receptor. The compound demonstrates potent inhibitory activity in both in vitro and in vivo models of NMDA-induced excitotoxicity and provides neuroprotective efficacy in several animal models of stroke. EAA-090 is unique among competitive NMDA antagonists in displaying a clear separation between predicted efficacious dose and doses that induce PCP-like psychotomimetic side effects in both animals and humans. This unique profile makes EAA-090 an exciting candidate for assessing the neuroprotective potential of the competitive NMDA mechanism.

AEE-788 is an orally available anticancer agent that was being developed by Novartis. AEE-788 is a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. At the enzyme level, AEE-788 inhibited EGFR and VEGF receptor tyrosine kinases in the nm range (IC(50)s: EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC(50)s: 11 and 220 nm, respectively). AEE-788 demonstrated antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibited the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells. These properties, combined with a favorable pharmacokinetic profile, were associated with a potent antitumor activity in a number of animal models of cancer, including tumors that overexpress EGFR and or ErbB2. Oral administration of AEE-788 to tumor-bearing mice resulted in high and persistent compound levels in tumor tissue. Moreover, AEE-788 efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. AEE-788 has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters. AEE-788 had been in phase Ⅱ clinical trials by Novartis for the treatment of glioblastoma multiforme. However, this research has been discontinued.