Betaprodine is an opioid analgesic under international control according to the UN Single Convention 1961. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures.

Ciprostene is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.

Cloxestradiol is a chlorinated derivative of estradiol, invented by Danish company Leo Pharma AS in 1963. The compound is claimed to have estrogenic activity, as was demonstrated by the extended duration of oestrus caused by the injection of cloxestradiol to castrated female rats.

Somantadine, an adamantane derivative, is an antiviral agent. Somantadine was synthesized by Pennwalt and has been undergoing tests for the treatment of herpes virus for nearly five years.

Glunicate (LG 13979) is a long-acting nicotinic acid derivative that can lower plasma triglyceride levels, while leaving other lipoprotein parameters unaffected. It exerts a dose‐dependent reduction of plasma triglycerides and cholesterol. In rabbits, glunicate provided dose-dependent protection of the arterial wall from atheromatous lesions and from cholesterol and collagen accumulation. It has been shown that glunicate has prolonged activity on plasma free fatty acids and triglycerides, with long lasting and intense activity on plasma cholesterol.

Feloprentan is an endothelin receptor antagonist.

Esorubicin (4'-deoxydoxorubicin, NSC 267469) is a synthetic derivative of the anthracycline antineoplastic antibiotic doxorubicin with potential antineoplastic activity. Esorubicin intercalates into DNA and inhibits topoisomerase II, thereby inhibiting DNA replication and ultimately, interfering with RNA and protein synthesis. This agent exhibits less cardiotoxicity than the parent antibiotic doxorubicin, but may cause more severe myelosupression compared to other compounds within the anthracycline class. Esorubicin was being clinically tested for the treatment of solid tumors as well as lymphomas an leukemias. Esorubicin development has been discontinued.

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.

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

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.