LAPISTERIDE is an inhibitor of 5alpha-reductase (5aR), converting testosterone to the more potent androgen dihydrotestosterone. It has dual inhibitory activity on both 5aR isoenzymes. It was under investigation for the treatment of benign prostatic hyperplasia and androgenic alopecia, but its development was discontinued.

LASINAVIR, a hydroxyethylene derivative, is highly specific human immunodeficiency virus (HIV) protease inhibitor with an IC50 of 1 nM. Its clinical development was discontinued.

Nupafant (BB-960) is a potent platelet activating factor antagonist that is active both orally and intravenously. Nupafant was in phase I clinical trials in the UK for the treatment of ischemia-reperfusion injury, however this compound has since been suspended.

Difencloxazine is a tranquilizing agent.

Entasobulin (ZEN-012; AEZS-112) is a small molecule with several mechanisms of action, such as DNA fragmentation via inhibition of topoisomerase II as well as inhibition of tubulin polymerization. It exerts antineoplastic activity. It was being developed for the treatment of cancers.

Forfenimex (also known as forphenicinol), a low molecular weight immunomodifier was studied as an antineoplastic agent. Preclinical experiments in vitro have shown that forfenimex enhanced the antitumor effects of cyclophosphamide in a model of squamous cell carcinoma. Experiments on rodents have revealed that this compound possessed protective effect against P. aeruginosa infection. This influence achieved due to macrophage activation followed by the enhancement of the bactericidal activity of polymorphonuclear cells (PMN).

Estrofurate (AY-11483) is an impeded estrogen. it prevents ovulation and implantation.

IRTEMAZOLE is a uricosuric agent exhibiting a rapid uricosuric effect in normouricemic as well as in hyperuricemic persons.

Acetorphine is a synthetic narcotic analgesic. Acetorphine was reported to have uses in veterinary medicine with pronounced advantages in the immobilization of the giraffe in which toxic effects were reduced as compared to the effects of etorphine. In July 1966, the Director-General of the World Health Organization informed the Secretary-General that WHO had arrived at the conclusion that etorphine and acetorphine should be included in Schedule I of the Convention, since they could give rise to similar abuse, and produce similar ill effects as the substances already listed therein. Acetorphine is a Schedule I controlled substance in the United States.

Brofezil (ICI 54594) is an ibuprofen derivative with anti-inflammatory and analgesic activity.