Elgodipine (IQB-875, CAS 119413-55-7) is a phenyldihydropyridine derivative acting as a calcium channel antagonist. Elgodipine inhibited both T- and L-type calcium channels in a concentration-dependent manner. Elgodipine was in clinical trials for the treatment of cardiovascular diseases however its development has been discontinued.

Mitemcinal (GM-611), an erythromycin-derived prokinetic agent, was developed by Chuga as an agonist of the motilin receptor. Mitemcinal acts by a novel mechanism whereby it stimulates and promotes peristalsis in the stomach and other segments of the gastrointestinal tract. This drug was studied as a potential treatment for gastric motility disorder, as well as reflux esophagitis, non-ulcer dyspepsia, and diabetic gastroparesis. Mitemcinal was involved in phase II clinical trials in Patients with diabetic gastroparesis. Although gastroparetic symptoms improved with both mitemcinal and placebo, the prominent placebo effect was not statistically exceeded by mitemcinal. That is why the development of this drug has stalled. In addition, mitemcinal has been studied in phase II for the treatment of irritable bowel syndrome, but this study was also discontinued.

Eprociclovir (A5021, 9-[[cis-1', 2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl]guanine) is a nucleoside analog with antiviral activity. Antiviral activity of eprociclovir appears to depend rapid and stable accumulation of its triphosphate in infected cells and on inhibition of viral DNA polymerase by its triphosphate. Eprociclovir was shown to be a potent inhibitor of the replication of herpes simplex virus type 1, 2, 6, Epstein-Barr virus and varicella zoster virus, both in vitro and in vivo. Eprociclovir development has been discontinued.

Aplindore (DAB-452) is a small molecule that displays potent dopamine D2 receptor partial agonist activity in in vitro and in vivo assays and is predicted to have antipsychotic efficacy without motor side effects. Aplindore had been in phase II clinical trials for the treatment of Parkinson's disease and restless legs syndrome. Aplindore was generally well tolerated and there were no withdrawals due to adverse events and no serious adverse events.

Icoduline (previously known as CBS-113 A) is a dual inhibitor of 5-lipoxygenase and cyclo-oxygenase with anti-inflammatory properties. This drug was potentially useful in ophthalmology and as an alternative to glucocorticoids. In addition, icoduline was useful to treat skin disorders. The drug participated in the clinical trial for eye disorders in France; however, this study was discontinued.

Allergan was developing the proton pump inhibitor AGN-201904 as an enteric-coated formulation for the treatment of gastric ulcer disease. AGN-201904 is a slowly absorbed, acid-stable pro-proton pump inhibitor (pro-PPI) rapidly converted to omeprazole in the systemic circulation giving a prolonged residence time. AGN-201904 has been used in trials studying the prevention of peptic ulcer.

Varlitinib (Alternative Names: ARRY-334543; ARRY-543; ASLAN-001; Varlitinib tosylate) is a small molecule based reversible pan-HER inhibitor of EGFR, HER2 and HER4. In response to the binding of various ligands, these kinases undergo heterodimerisation and homodimerization, resulting in activation of numerous growth factor signaling pathways, by inhibiting the activation of the HER receptors via drug, effects such as shrinkage of the tumor and longer survival can be anticipated. In a large variety of cancers, the overexpression and/or constitutive activation of EGFR and HER2 are often observed and frequently correlate with poor clinical prognosis. Licensed from Array BioPharma with global rights for all indications, varlitinib is being developed as first-in-class drug for cholangiocarcinoma, gastric and colorectal cancer, and as best-in-class drug for breast cancer.

Ancriviroc (SCH 351125) is a small-molecule antagonist of the human immunodeficiency virus type 1(HIV-1) coreceptor CCR5. It has in vitro activity against R5 viruses with 50% inhibitory concentrations ranging from 1.0 to 30.9 nM. Ancriviroc is an orally bioavailable small molecule inhibitor of HIV-1 entry via CCR5 coreceptor interaction. Ancriviroc has potent activity against RANTES binding (K(i) = 2 nM), possesses subnanomolar activity in blocking viral entry and has excellent antiviral potency versus a panel of primary HIV-1 viral isolates. Ancriviroc had been in phase I clinical trials by Schering-Plough (subsidiary of Merck Sharp & Dohme) for the treatment of HIV infection. However, this research has been discontinued.

Pentizidone is a prodrug which is hydrolyzed spontaneously and converted to D-cycloserine. Merck selected pentizidone as a companion product for D-fluoroalanine with the anticipation that it would be better tolerated than cycloserine itself. The expectation was that D-fluoroalanine and pentizidone would be synergistic in killing bacteria. The combination of the two enzyme inhibitors proved to have potent antibiotic activity in animal studies and abolished the self-reversal phenomenon. D-cycloserine acts on D-alanyl-D-alanine synthetase.

Altinicline (SIB-1508Y, SIB-1765F) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models, and progressed as far as Phase II clinical trials for Parkinson's disease, where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear.