Ethonam is an antifungal compound. Its activity was evaluated in the treatment of chronic athlete's foot.

Detorubicin is a semi-synthetic derivative of the anthracycline antineoplastic antibiotic. It intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also produces toxic free-radical intermediates and interacts with cell membrane lipids causing lipid peroxidation. Detorubicin is less toxic than daunorubicin. Although it showed some clinical activity, the drug appeared to have no particular advantage over doxorubicin except for demonstrated activity against malignant melanoma. Unfortunately, detorubicin clearly has cardiac toxicity – in clinical trial, one patient developed congestive heart failure and other patients revealed endomyocardial biopsy evidence of cardiac toxicity.

Talviraline (HBY 097) was developed as a nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (NNRTI) for the treatment of HIV Infections. Talviraline participated in a phase II clinical trial. It was found that the drug caused pronounced acute suppression of HIV-1 replication both in combination with zidovudine and alone. However, further development of the drug has been discontinued.

Wyeth was developing the small molecule plasminogen activator inhibitor-1 (PAI-1) antagonist aleplasinin for the treatment of Alzheimer's disease in the US. PAZ-417 inhibits PAI-I (Plasminogen activator inhibitor-1), thereby increasing the activation of plasminogen to form plasmin. There is some evidence that plasmin can increase the cleavage of amyloid precursor protein at the alpha cleavage site, which could reduce the formation or increase the clearance of amyloid beta, a suspected culprit in Alzheimer's disease. However, it`s development for Alzheimer's disease treatment was discontinued.

Budiodarone is a chemical analog of amiodarone with mixed ion channel electrophysiological activity. Budiodarone was developed to capitalize on the proven efficacy of amiodarone and to avoid its side effects. Budiodarone has a short plasma half-life (7 h) and a lower volume of distribution (13 L/kg). It is cleared from the body in 48 h. Like amiodarone, Budiodarone has balanced, multiple cardiac ion channel inhibiting activity, giving it properties of all four Vaughan Williams antiarrhythmic drug classes. Budiodarone, unlike amiodarone, undergoes rapid metabolism by plasma and tissue esterases. In clinical trials, Budiodarone effectively reduces the number and duration of atrial tachycardia/atrial fibrillation episodes.

Nacartocin is synthetic oxytocin analogue patented by Ceskoslovenska Akademie as a specific natriuretic agent. The natriuretic effect is mainly due to the inhibitory action of the peptide on tubular sodium resorption. Nacartocin decreased the blood pressure of anesthetized rats by the decrease of the total peripheral resistance which was greater than that observed after oxytocin administration.

Almurtide (CGP 11637) is a synthetic muramyl dipeptide (MDP) analogue with potential immunostimulating and antineoplastic activity. As a derivative of the mycobacterial cell wall component MDP, almurtide activates both monocytes and macrophages. This results in the secretion of cytokines and induces the recruitment and activation of other immune cells, which may result in indirect tumoricidal or cytostatic effects. CGP 11637 has been shown to prevent oncogenic viral infections in mice.

Arbaclofen (STX209, R-baclofen), a selective agonist of GABA-B receptors, has been investigated in clinical trials for the treatment of autism spectrum disorder ASD, phase II and for the treatment of patients with fragile X syndrome in phase III. As a result, the drug did not meet the primary outcome of improved social avoidance in FXS in either study. In spite of positive results in some children with ASD, further study will be needed to replicate and extend these initial findings. Arbaclofen has also been investigated in phase III clinical trials as a treatment for spasticity due to multiple sclerosis.

Sulfachrysoidine is a sulfamylchrysoidine derivative and lipid-soluble azo dye with antibacterial activity.

Folitixorin, a thymidylate synthase inhibitor is a substrate used by the enzyme methylenetetrahydrofolate reductase (MTHFR) to generate 5-methyltetrahydrofolate. Folitixorin was studied in clinical trials for the treatment of breast cancer, metastatic colorectal cancer and for the treatment of advanced pancreatic cancer. Folitixorin had been granted orphan drug status for the treatment of pancreatic cancer in both the U.S. and EU. However, further development of this drug was discontinued.