Fasiplon (RU 33203), an imidazo[1,2-a]pyrimidine derivative, is agonist of GABA(A) receptors at benzodiazepine binding site. It was in preclinical studies for the treatment of anxiety.

Nicofibrate is an antilipidemic drug. Treatment of diabetics led to a significant reduction in plasma cholesterol and triglycerides and brought the lipoprotein picture back within the norm. Nicofibrate did not lead to significant increases in uricaemia nor to any worsening in carbohydrate tolerance. Nicofibrate may also lead to a significant drop in plasma prothrombinic activity.

Semorphone (previously known as Mr 2264), a partial opiate receptor agonist that was in two times more potent than morphine. Semorphone has a ceiling effect on both analgesia and respiratory depression; it means that these effects stop becoming any stronger after a certain maximum dose.

Sermetacin, an indometacin derivative, is a nonsteroidal anti-inflammatory agent.

Iomeglamic Acid is an iodinated aryldicarboxylic acid monoamide used as insoluble X-ray contrast media. Iomeglamic acid has been successfully applied for radioscopy of the gall-bladder since 1972 but currently discontinued.

Calcimycin is an ionophore, polyether antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems. Calcimycin has antibiotic properties against gram-positive bacteria and fungi. Inex Pharmaceuticals Corporation (Canada) reported an innovative application of Calcimycin. "Inex" used Calcimycin as a molecular tool in order to make artificial liposomes loaded with anti-cancer drugs such as Topotecan. In in vitro fertilization (IVF) field, Ca Ionophore can be used in case of low fertilization rate after ICSI procedure, particularly with Globozoospermia (Round Head sperm syndrome), Ca Ionophore plays role in oocyte activation after ICSI. Recommended use is 0.5 microgram/ml twice for 10 min interrupted with fresh media with 30 min incubation, followed with regular injected eggs culture for IVF

Rosabulin (STA 5312) is an antineoplastic compound (inhibiting or halting neoplasm development). This compound was developed for the treatment of drug resistant tumors. By acting as a tubulin inhibitor, rosabulin hinders the microtubule assembly necessary to shape endothelial (vascular) cells, and blocks their cell division. As a result, blood flow to the tumor is reduced and tumor cell proliferation is decreased. Phase I clinical trials in patients with advanced or metastatic tumors, leukemia, lymphoma and hematological malignancies have evaluated the safety and toxicity of rosabulin. Development of rosabulin has been discontinued in 2008.

CP-195543 is a selective and potent leukotriene B4 (LTB4) receptor antagonist developed by Pfizer. CP-195543 inhibited human and mouse neutrophil chemotaxis mediated by LTB4. In vivo, after oral administration, CP-195543 blocked LTB4-mediated neutrophil infiltration in guinea pig and murine skin. CP-195543 reduced the clinical symptoms and attendant weight loss in an IL-1-exacerbated murine model of collagen-induced arthritis. Combination of CP-195543 and celecoxib was investigated in phase 2 clinical trials against rheumatoid arthritis, but the drug failed to achieve superiority over placebo, and its development was discontinued.

Pralnacasan is a potent, non-peptide inhibitor of interleukin-1beta converting enzyme (ICE, aka Caspase-1). It was originally discovered by Vertex Pharmaceuticals and licensed for development to Aventis Pharma. In 2003 Aventis and Vertex Pharmaceuticals agreed to voluntarily discontinue development based on results from a 9-month animal toxicity trial that showed liver abnormalities due to chronic high doses of pralnacasan. Pralnacasan has also been investigated for the treatment of Partial Epilepsy; advancing to Phase II clinical trials.