Methylenedioxymethamphetamine (or 3,4-methylenedioxymethamphetamine (MDMA)), a synthetic, psychoactive drug also known as ecstasy that was used as a recreational drug. This drug acts as both a stimulant and psychedelic and exerts its effects in the brain on neurons that use the chemicals serotonin, dopamine and norepinephrine to communicate with other neurons. In spite of the presence of this compound in the List of control and forbidden compounds, it was studied in psychotherapy for patients with chronic, treatment-resistant posttraumatic stress disorder. Initial results showed efficacy for the treatment approach, although further studies are needed.

Bromacrylide is an acrylamide-based alkylating agent with antineoplastic activity. Bromacrylide after oral or intraperitoneal administration decrease tumor growth in animal models. Unfortunately, Bromacrylide demonstrates severe toxicity, including severe bone marrow suppression and weight loss.

Lurtotecan is a semisynthetic analog of camptothecin with antineoplastic activity. It is an inhibitor of DNA topoisomerase I. Liposomal formulation of lurtotecan was being studied in the treatment of cancer. Lurtotecan development has been discontinued.

Mitoflaxone, also known as flavone acetic acid is a synthetic flavonoid that has been studied as an antitumor agent. Mitoflaxone was involved in phase II clinical trials in Europe for patients with advanced colorectal carcinoma and for patients with advanced malignant melanoma. Despite the promising preclinical activity, this drug didn’t demonstrate any clinical activity. Further studies of the drug were suspended.

Ethyl cartrizoate has been used in diagnostics as a bronchographic agent.

Azimexon, a synthetic derivative of the 2-cyanaziridines, possesses the immunorestorative properties that were shown for patients with acquired immunodeficiency syndrome. Besides, azimexon had a role in managing cancer-associated dysregulation of the immune response. It was studied in clinical trials phase I to determine the drug's tolerable dose, toxicity, and effects on immune and nonimmune host defense parameters.

Iclazepam (also known as Clazepam) was used as a tranquilliser.

Clocoumarol is a synthetic antagonist of vitamin K, developed in the 1970s. Clocoumarol exhibits strong anticoagulant properties in rat and rabbit.

Timcodar (also known as VX-853) is a benzenepropanamide derivative patented by Vertex Pharmaceuticals Incorporated as an efflux pump inhibitor for the treatment of multi-drug resistant bacterial infection. Timcodar potentiates the activity of ethidium bromide (EtBr), a model efflux substrate, against three clinically significant gram-positive pathogens: Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pneumoniae. Timcodar weakly inhibits M. tuberculosis growth in broth culture but shows a 10-fold increase in the growth inhibition of M. Tuberculosis cultured in host macrophage cells and demonstrated synergy with rifampin, moxifloxacin, and bedaquiline. In a mouse model of tuberculosis lung infection, timcodar reduces the likelihood of a relapse infection and potentiates the efficacies of rifampin and isoniazid. Timcodar in combination with Doxorubicin was studied in phase 1/2 clinical trials in patients with solid tumors, but no results have been published.

KETORFANOL, a morphinan derivative, is an opioid analgesic. It showed potent antiwrithing activity in the animal assay. It was equipotent with morphine as an agonist and lacked antagonist activity up to 10 mg/kg.