Cipemastat (Ro 32-3555, tentative trade name Trocade) is a dipeptide, potent, competitive inhibitor of matrix metalloproteinases (MMP) 1, 8 and 13, which was under development by Roche for the potential treatment of rheumatoid arthritis. Cipemastat is a selective inhibitor of metalloproteinases 1, 8 and 13 over the related human matrix metalloproteinases stromelysin 1, and gelatinases A and B. Cipemastat mediated MMP inhibition leads to block the final common event in the destructive cascade resulting in the breakdown of cartilage and bone. Trocade has also been shown to inhibit cartilage destruction in vivo and to prevent structural joint damage in animal models of rheumatoid and osteoarthritis. Cipemastat was in phase II clinical trials for the treatment of rheumatoid arthritis. However, Roche discontinued the development of cipemastat because of an unfavorable risk-benefit profile.

Trecetilide is a class III antiarrhythmic agent developed for the treatment of atrial flutter and fibrillation. Trecetilide probably has effects on the cardiac myocyte membrane that are similar to ibutilide. It is being developed for both oral and intravenous administration. Unlike ibutilide, trecetilide has good oral bioavailability. Trecetilide has a good metabolic stability. As with ibutilide, its mechanism of class III action may involve both rectifier K+ current blockade and other mechanisms of prolonging repolarization.

2-(1-Hexyloxyethyl)-2-devinyl pyropheophorbide-a (HPPH), a chlorin-based photosensitize, is used in photodynamic therapy. It has been shown the therapeutic potential of HPPH in phase II clinical trials for the treatment of esophageal cancer. Besides, HPPH participated in clinical trials in treating patients with advanced non-small cell lung cancer that blocks the air passages. However, these studies were terminated.

Brolamfetamine (also known as DOB, bromo-DMA, and 4-bromo-2,5-dimethoxyphenylisopropylamine) is one of a vast number of compounds used recreationally to achieve hallucinogenic effects. Brolamfetamine is one of the most potent hallucinogens, with its hallucinogenic potency directly linked to its abuse potential. Brolamfetamine acts as a partial agonist of 5HT2A, 5HT2B, 5HT2C, and TAAR1 receptors, but it’s psychedelic effects are mainly mediated by its agonistic properties at the 5-HT2A receptor. Animal studies have shown physiologic effects including hypertension, tachycardia, hyperpyrexia, pupillary dilatation, and peripheral vasoconstriction. In general, Brolamfetamine having a similar effect to LSD, with slower onset (up to 3–4 h to peak intoxication) and longer duration of effect (up to 36 h). Brolamfetamine is not commonly available, through periods of higher circulation were reported in Australia in 1983, Ireland in 2003, and in Italy in 2015. Brolamphetamine, as well as many other synthetic hallucinogens, are increasingly being sold as LSD. Internationally Brolamfetamine is a Schedule I drug under the Convention on Psychotropic Substances. Due to its selectivity, Brolamfetamine is often used in scientific research when studying the 5-HT2 receptor subfamily.

Vinconate possesses both encephalotropic and psychotropic properties. Animal experiments have shown that this compound could induce the facilitation of phosphatidylinositide (PI) turnover via the stimulation of muscarinic acetylcholine receptors. In addition, vinconate could lead to the direct activations of PIP2-specific and cytosolic phospholipase C. The drug was on the stage of preregistration for the treatment of cognition disorders in Japan. However, information about the further fate of this drug is not available.

Vinformide (also known as N-formylleurosine), an N-formyl analog of leurosine possesses antineoplastic activity. This drug was studied for the treatment of lymphoma, leukemia and Hodkin’s disease. However, studies were discontinued, because vinformide exerted an acute cardiotoxic side effect.

Isovaleramide (also known as NPS 1776) is one of the active anticonvulsant constituents of Valeriana pavonii, it was suggested, isovaleramide can be a positive allosteric modulator of the GABAA receptor. This drug was studied in clinical trials for the treatment of A migraine, epilepsy and some others CNS disorders, but these studies were discontinued.

Lapachone (aka beta-Lapachone) is an ortho naphthoquinone, originally isolated from a tree whose extract has been used medicinally for centuries. It has garnered interest as a potential therapeutic or lead compound against a number of disease conditions including cancers, and blindness due to retinopathy of prematurity. It is lethal to a number of cancer cell types at micromolar concentrations, and it is capable of enhancing the efficacy of radiation therapies against cultured cells. A number of clinical trials have been conducted.

Tolfamide is a benzamide and urease enzyme inhibitor.

Tolnidamine belongs to the chemical class of 1H-indazole-3-carboxylic acids. These agents exert antispermatogenic activity and have two cell targets, Sertoli cells and germ cells, in the seminiferous epithelium. Tolnidamine medication induced irreversible inhibition of spermatogenesis. The addition of tolnidamine at the beginning of the culture period reduced the plating efficiency of Sertoli cells; however, tolnidamine did not induce a significant change in cell number if it was added 24 h after plating of the cells. Sertoli cell-enriched cultures prepared from tests of 10-day-old rats were highly sensitive to tolnidamine as evidenced by a marked inhibition in secretions of androgen binding protein, testibumin and transferrin. A 4-week study has been conducted in rhesus monkey fed tolnidamine orally. Dosages of 200 mg/kg and 400 mg/kg produced aplasia of the germinal epithelium with abnormal renal function.