Colterol is a beta-2 adrenoreceptor agonist. Bitolterol, a diester prodrug of colterol, was marketed by Elan Pharmaceuticals for the treatment of reversible bronchospasm associated with asthma or chronic obstructive pulmonary diseases.

Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders

Dabelotine is a cognitive-enhancing drug, developed by Servier. The drug has been shown to improve some aspects of cognitive processes, such as attention, curiosity, motivation, acquisition, and recall of memory. Dabelotine has also been shown to reduce the effect of an anticholinergic drug such as scopolamine. The drug increases the in vitro K+-induced norepinephrine release in rodent cerebral slices, and have no effect on noradrenergic and cholinergic receptor binding sites. Dabelotine was investigated in phase 2 clinical trials for the treatment of dementia, where it was demonstrated that 50-mg and 100-mg doses produced an improvement in reaction time and performance in memory tasks.

Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.

Prinomastat is a synthetic hydroxamic acid derivative with potential antineoplastic activity. Prinomastat inhibits matrix metalloproteinases (MMPs) (specifically, MMP-2, 9, 13, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. As a lipophilic agent, prinomastat crosses the blood-brain barrier. Pfizer conducted multicenter, randomized, double-bind, placebo-controlled trials to evaluate the safety and efficacy of prinomastat in combination with standard chemotherapy in patients with advanced hormone refractory prostate cancer and non-small cell lung cancer. However, this study has been terminated for the reason that Prinomastat did not improve the outcome of chemotherapy in non-small cell Lung cancer patients.

Tiliquinol in combination with tilbroquinol and tiliquinol lauryl sulfate are the active components of Intetrix, a medicine prescribed to adults who suffer from amoebiasis. Amoebiasis refers to an infection caused by the parasite Entamoeba histolytica. Intetrix is marketed as a capsule and is administered orally.

Tamolarizine (also known as NC-1100), an organic Ca2+ channel blocker, was studied in clinical trials phase II in patients with neurological disorders. However, these studies were discontinued. In addition, experiments on rodents have shown that tamolarizine treatment protected the hippocampus from ischemic brain damage and ameliorated place learning impairment. Tamolarizine was also able to reverse the multidrug-resistance phenotype in human leukemia K562 cells through direct interaction with P-glycoprotein.

NS-018 is a potent inhibitor of Janus kinase 2 (JAK2) enzyme activity and Src-family kinases. It was developed as an oral therapy for the treatment of myelofibrosis. Overall NS-018 has been used in trials studying the treatment of primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia. NS-018 is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). NS-018 also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene.

Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. In conscious spontaneously hypertensive rats intravenous injection of lidanserin caused dose-dependent blood pressure reductions. Lidanserin antagonises the excitatory effect of synaptically released 5-HT on central sympathoexcitatory neurons. Lidanserin is a potential antihypertensive compound which combines vasodilatatory effects due to selective alpha 1-receptor antagonistic action and platelet antiaggregatory, antivasospastic, and vasoprotective properties due to selective 5-HT2-receptor blockade.