Sampatrilat (also known as UK 81252) was developed as a dual inhibitor of both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). This drug was studied for the treatment of hypertension and congestive heart failure.

Batelapine (or CGS 13429), an antipsychotic drug, that was undergoing preclinical development, but the further studied were discontinued

Oxepinac was developed as an anti-inflammatory drug. Results of clinical trials have revealed that oxepinac was an effective and well-tolerated drug in the treatment of painful osteoarthritis. Experiments on animal have shown that oxepinac had no teratogenic effect on fetuses in mice and rabbits. Information about the current use of this drug is not available.

Sumacetamol is a acetylaminothioalkanoate derivative patented by Sterwin A.-G. as an analgesic and antipyretic agent. Sumacetamol is used in combination with free paracetamol. In clinical trials, Sumacetamol failed to demonstrate superior efficacy in pain and swelling management compare to paracetamol but shows a longer duration of analgesia. The rates of reported adverse events were similar in paracetamol and Sumacetamol, although reports of mild to moderate drowsiness were more common after the Sumacetamol combination.

Trethocanic acid is a beta-hydroxy acid. It exerts a similar effect on the skin as salicylic acid. Trethocanic acid was used as antihypercholesterolaemic agent.

Dexverapamil (R-verapamil) is an enantiomer of verapamil. R-isomer behaved as an inhibitor of multidrug-resistant protein MRP1 (involved in the cancer cell multidrug resistance phenotype). It was developed by Knoll (BASF Pharma) as a chemosensitiser and/or modulator of multidrug resistance for use in combination with cancer chemotherapy. Dexverapamil was undergoing phase II clinical studies in France, Italy, Spain, United Kingdom and the US in patients with various cancers. It was also undergoing phase I clinical trials in Japan where it was licensed to Mitsui and Mitsui Toatsu Chemicals. However, development was discontinued. Dexverapamil (R-verapamil) has been developing by AGI therapeutics for the treatment of Irritable bowel syndrome however development was discontinued.

Cilengitide is a cyclized Arg-Gly-Glu (RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins. Its precursor was first synthesized in 1995 as c(RGDfV), and later modified by the incorporation of N-methyl Val c(RGDfMetV), generating the current form of the drug. Cilengitide displays subnanomolar antagonistic activity for αvβ3 and αvβ5, and is the first integrin antagonist evaluated in clinical phase I and II trials for treatment of glioblastoma and several other tumor types. Cilengitide-induced glioma cell death and inhibition of blood vessel formation may use different molecular mechanisms, including regulation of tumor hypoxia and activation of apoptotic pathways. Cilengitide inhibits cell signaling through FAK-Src-Akt and Erk mediated pathways in endothelial and tumor cells and attenuates the effect of VEGF stimulation on growth factor signaling. Cilengitide has shown encouraging activity in patients with glioblastoma as single agent, and in association with standard RT and temozolomide.

Aleglitazar is a dual agonist of PPARalpha/PPARgamma which was developed by Hoffmann-La Roche for the treatment of type 2 diabetes. Aleglitazar activates PPAR receptors with EC50 in nanomolar range and exerts a cardioprotective effect in vitro. The drug is currently in phase III of clinical trials.

Fenclorac is a potent nonsteroidal anti-inflammatory agent with significant analgesic and antipyretic activity. It inhibits prostaglandin synthesis both in vitro and in vivo.

Vebufloxacin (OPC-7241) is a nalidixic acid analog. It exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa.