Betamethadol or β-methadol is an opioid analgesic under international control according to the UN Single Convention 1961. Betamethadol is an isomer of the racemic mixture of dimepheptanol.

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.

Berubicin, an anthracycline derivative, is a DNA binding agent and potent topoisomerase II poison. Reata Pharmaceuticals were developing it as a treatment for brain cancer as it can breach the blood-brain barrier. It had also been in early clinical trials for the treatment of lung cancer and malignant gliomas. However, studies have been terminated. In October 2006, it was granted orphan drug designation from the FDA for the treatment of malignant gliomas. According to a CNS Pharmaceuticals media release in April 2018, berubicin will be studied for glioblastoma patients, these investigations will be funded in part by an equity crowdfunding campaign.

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.

Elucaine is local anesthetic and anti-ulcerative agent, acting as a gastric muscarinic acetylcholine receptor antagonist.

Eflucimibe is a new and potent Acyl coenzyme A:cholesterol acyltransferases inhibitor. Eflucimibe effectively decreased plasma cholesterol in cholesterol-fed animals. In animal models, drug restores normolipodemia in endogenous hypercholesterolemic rabbits and prevents the progression of atherosclerosis by decreasing the number of macrophages in the foam cells. Eflucimibe has been in phase II clinical trials for the treatment of atherosclerosis and hyperlipidemia. However, this research has been discontinued.

Alphamethadol is a synthetic opioid analgesic. Alphamethadol is composed of two isomers itself, L-α-methadol, and D-α-methadol. L-α-methadol is an important active metabolite of levacetylmethadol (LAAM), a medication therapy for individuals addicted to opiates that provides an alternative to methadone. Isomers of Alphamethadol bind to and activate the μ-opioid receptor; they are active as opioid analgesics.

Bolazine is a synthetic anabolic steroid that uses as the ester prodrug bolazine capronate.

Giracodazole (also Girodazole or RP 49532A) is a marine compound has been isolated from the sponge Pseudaxinyssa cantharella. It has shown broad antitumor activity in experimental models and has been studied as a potential antitumor compound that inhibits protein synthesis in cell cultures and in cell free systems. Dose-limiting toxic effects that were observed were delayed hypotension and severe asthenia. Independent of dose level, transient nausea and vomiting were reported during infusion. As a result of this toxicity profile, no phase II clinical trial was conducted for Giracodazole.