Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.

Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.

Bitoscanate is a tasteless, odorless, colorless, needle-like crystalline solid material prepared from mustard powder acid and used as an anthelmintic against nematodes, especially hookworms (Necator sp.) and Ancylostoma duodenale. Side effects reported with therapeutic use have been nausea, vomiting, diarrhea, abdominal pain or discomfort, loss of appetite, dizziness or giddiness, vertigo, weakness, headache, and an itching sensation over the body. Such side effects have most often been mild and required no treatment. Bitoscanate is classified as an extremely hazardous substance in the United States as defined in Section 302 of the U.S. Emergency Planning and Community Right-to-Know Act (42 U.S.C. 11002), and is subject to strict reporting requirements by facilities which produce, store, or use it in significant quantities.

Mepiprazole is a psychotropic pyrazole derivative. Mepiprazole is a serotonin reuptake inhibitor and adrenolytic. In clinical studies, it demonstrated anxiolytic properties.

Detrothyronine is the (R)-(D)-form of triiodothyronine and has antihyperlipidaemic actions with beneficial effects upon coronary disease and hypertension. Detrothyronine has been tried in the treatment of hypercholesterolemia but its toxic effects outweigh any therapeutic advantage.

Pyroxamine (also known as AHR 224) is benzhydryl ethers of 3-pyrrolidinol patented by A. H. Robins Co., Inc. as antihistamine with bronchodilation activity. In preclinical studies, Pyroxamine shows moderate inhibition of histamine-induced ulceration in guinea pigs

Iomethin I-131 is radioiodinated quinoline derivative with potential tumor localizing activity. In animal models, Iomethin I-131 administrations lead to regression of the malignant melanoma and its metastases.

Imanixil (also known as HOE-402) was developed as a potent cholesterol-lowering compound, which inhibits VLDL production, and consequently attenuates atherosclerosis development. This drug participated in phase I clinical trial for the treatment of hyperlipidemia, however, this study was discontinued.

Dimetamfetamine is the N-methylated analog of methamphetamine, produces behavioral effects that are generally comparable to those of methamphetamine, but with reduced potency. It is often found as an impurity in preparations of methamphetamine. Dimetamfetamine itself is less neurotoxic than methamphetamine. Dimetamfetamine is metabolized to p-hydroxyl methamphetamine, p-hydroxyl dimetamfetamine, amphetamine, methamphetamine, and N,N-dimethylamphetamine N-oxide in humans, and flavin-containing monooxygenase-1 and CYP2D6 are mainly involved in the N-oxidation and N-demethylation of dimetamfetamine, respectively. Dimetamfetamine has also been used illegally in Korea, and the Korean government placed DMA on the official list of controlled substances on December 4, 2006.

Loxoribine [RWJ 217C7] is an immunostimulant which was developed by Johnson and Johnson. It is a selective agonist for TLR7 (Toll-like receptor 7), which possesses antitumor and antiviral properties and was investigated in a rat model of endometriosis and in addition, in phase I of a clinical trial for patients with advanced cancer.