Sunagrel is a phenylethanolamine derivative patented by Maggioni Farmaceutici S.p.A. as platelet aggregation inhibitor and antilipidaemic agent.

MK-0873 is a novel selective phosphodiesterase-4 inhibitor, which has been in development for the treatment of chronic obstructive pulmonary disease (COPD). In preclinical studies, intravenous administration of MK-0873 produced potent, dose-dependent inhibition of antigen-induced bronchoconstriction in sensitized guinea pigs. MK-0873 protected against both the early- and late-phase bronchoconstrictor response to antigen challenge in Ascaris-sensitive sheep. In healthy volunteers, MK-0873 has been shown to be safe and generally well tolerated in single oral doses up to 6 mg and in multiple oral doses up to 4 mg for 28 days. The most commonly reported adverse events were similar to those reported in other studies with drugs in its class: i.e. headaches and gastrointestinal complaints.

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.

Thiacetarsamide is a drug containing trivalent arsenic. In the USA it was used for the treatment of Heartworm Infection in dogs and cats under tradename Caparsolate, however, it was discontinued because of the availability of safer alternatives. The mechanism of action for thiacetarsamide is modulation of glucose uptake and metabolism; inhibition of glutathione reductase, and alteration of the structure and function of the surface of the intestinal epithelium of the parasites.

CTS-1027 (Ro-1130830) is a hydroxamic acid matrix metalloprotease (MMP) inhibitor. CTS-1027 was originally designed as a strong inhibitor of MMP-2, -3, -8, -9, -12, -13 and -14, without inhibiting MMP-1 and MMP-7. CTS-1027 was proved to be safe in clinical trials for osteoarthritis conducted by Roche. CTS-1027 was then licensed from Roche to Conatus Pharmaceuticals and was investigated as a protector from liver fibrosis in hepatitis C virus patients. The development of the drug was discontinued due to laboratory abnormalities and adverse events in a subset of clinical trial participants.

Carboxyamidotriazole (L651582) is a carboxyamide-amino-imidazole compound originally developed as a coccidiostat, an antiprotozoal agent that acts upon Coccidia parasites. Carboxyamidotriazole (L651582) is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2 channels, blocking both Ca2 influx into cells and Ca2 release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion, and metastasis.

GW 590735 is a selective and potent agonist of peroxisome proliferator-activated receptor alpha (PPARα), a ligand-activated transcription factor that plays a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein. GW 590735 was in phase II clinical trial for the treatment of dyslipidemia, but that study was discontinued.

Besunide was studied as a diuretic agent.

Piriprost (U-60, 257) is a structural analog of prostaglandin I2 (PGI2) with low IP receptor-mediated activity. It inhibits 5-LO (5-lipoxygenase). Piriprost inhibits the release of histamine and leukotrienes, implicating its role in inflammation and allergic responses. However, it was shown, that piriprost did not influence the airway responses after allergen in asthma. Nevertheless, even more, the drug was irritant to the respiratory tract than was placebo.