Altoqualine (458L) is a derivative of benzylisoquinoline, it inhibited kidney histidine decarboxylase and decreased the passive anaphylactic bronchospasm in guinea pigs. Altoqualine is an antihistamine and antiallergic agent.

Amfepentorex (CB 2201) was marketed as an appetite suppressant in France in the 1970s.

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.

Altapizone is a platelet aggregation inhibitor. It is a vasodilator.

Dimeprozan is a tranquillizer. It is equipotent with chlorpromazine in producing ataxia, decreased motor activity, and loss of righting reflex in mice.

Begacestat (GSI-953 or PF-5212362), a gamma-secretase inhibitor (GSI) that selectively inhibits cleavage of APP over Notch, was discovered for the treatment of Alzheimer's disease. The drug has shown promise results in phase I clinical trials, however further studies were discontinued.

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

Bofumustine, also known as RFCNU was studied as an antitumor agent. Bofumustine participated in phase II trials in patients with digestive tract tumors. It was shown that 30% has remissions among which 13% were greater than 50%. In addition, bofumustine participated in phase II clinical trials, where it showed to be effective in 8% of digestive tumors, in 1 out of 7 pancreatic cancers and in 3 out of 10 hepatic and pulmonary metastases from an undiscovered primary adenocarcinoma. However, further information is not available.

Bisaramil, an antiarrhythmic drug was developed as an inhibitor of calcium transport and as a membrane stabilizer. In addition, the drug showed tonic and frequency-dependent block that is most potent against the heart Na+ channel. However, the phase-II for Arrhythmias in Japan was discontinued.

Mitratapide is a potent inhibitor of the microsomal triglyceride transfer protein used for the treatment of obesity in dogs. The drug was developed by Janssen Pharmaceutica and is chemically related to the antifungal drugs such as itraconazole which were also developed by Janssen. Administration of mitratapide to dogs results in reduced uptake of dietary lipids, dose dependent decreases in serum cholesterol and triglyceride and an increased presence of triglyceride containing droplets in enterocytes. Mitratapide also has a slight appetite decreasing effect that is claimed to be associated with its mode of action. Vomiting, diarrhoea or softened stools may occur during treatment. In most cases, these effects are mild and transient.