Lusaperidone (R107474) is a potent and relatively selective alpha(2)-adrenoceptor antagonist. It was under clinical evaluation for the treatment of depression, characterized by anergia and lack of drive. However, further clinical development has been stopped. Radiolabeled lusaperidone may be used as a potential radioligand for studying alpha(2)-adrenoceptors using PET.

Encyprate (MO-1255) is a unique drug in being inactive as an MAO inhibitor in vitro but very active in vivo. It most probably is converted by the body to ethyl-N-benzyl-N-cyclopropylcarbamate which is an active MAOI in vitro. I was studying in the treatment of depression.

Securinine is a plant-derived alkaloid from the Securinega plant that has been used clinically as a therapeutic for primarily neurological related diseases. Securinine is well-known GABAA antagonist and recently it was found that Securinine is able to up-regulate p53 protein and to modulate the related family member p73 protein in a p53-dependent fashion, inducing p73 in the HCT116 p53(-) cells and down-regulating it in the p53(+) cells. Securinine induces G1 phase cell cycle arrest, upregulates expression of p53 and Bax, and downregulates expression of Bcl-2, PI3K, mTOR, and p70s6k in breast cancer cells and promyelocytic leukemia cells. Securinine activates p38 MAPK, enhancing monocyte antibacterial activity in vitro as well. This compound also exhibits antimicrobial activity against Alternaria, Curvularia, and Helminthosporum. Additionally, securinine decreases AChE activity and suppresses amyloid-β (Aβ)-induced glial inflammatory responses in animal models of Alzheimer’s disease, improving cognitive deficits. Securinine’s activity as a GABA antagonist, likely explains its reported clinical success in limited studies for the treatment of neurological conditions such as amyotrophic lateral sclerosis (ALS), poliomyelitis and multiple sclerosis. Securinine has not been utilized in the United States, it has been used clinically in several other countries particularly China and Russia. In China, it is considered one of the 50 fundamental Chinese herbs and is used in Chinese herbal medicine.

Rifalazil (also known as KRM-1648) is a derivative of the antibiotic rifamycin. This orally administered ansamycin is under evaluation for treatment of various bacterial infections. Rifalazil kills bacterial cells by blocking off the β-subunit in RNA polymerase. This drug was originally developed as a therapeutic agent to replace rifampin in the treatment of tuberculosis. It also showed potential to treat indications caused by chlamydia trachomatis and chlamydia pneumoniae. Furthermore, it has been suggested as a potential drug in the treatment of gastric ulcer disease (which is caused by Helicobacter pylori) and antibiotic-associated colitis. Phase II studies evaluated the efficacy and safety of this drug in patients with chlamydia trachomatis and chlamydia seropositive patients. A phase 3 study was initiated including chlamydia seropositive patients. However, the development of rifalazil was terminated in 2013 due to severe side effects.

Edotecarin (J-107088 or [6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carb azo le-5,7(6H)-dione]) is a DNA topoisomerase I inhibitor. The antitumor activity of edotecarin has been tested in vitro and in vivo, and inhibition of tumor growth has been observed in breast, cervix, pharynx, lung, prostate, colon, gastric, and hepatic cancer models. Banyu Pharmaceutical Co Ltd and Pfizer Inc were developing edotecarin for the potential treatment of solid tumors. Edotecarin development has been discontinued.

Omaciclovir (previously known as H2G), a cyclic guanosine analog that is structurally similar to acyclovir and was in clinical development for the treatment of herpesvirus infections. This drug acted against varicella-zoster virus (VZV), by the formation of high concentrations of relatively stable H2G-triphosphate, which is a potent inhibitor of the viral DNA polymerases. However, further development of this drug was discontinued.

Alazanine triclofenate is a mixture of one molecule of 3-ethyl-2-(3-(3-ethyl-2-benzothiazolinylidene)propenyl)benzothiazolium 2,4,5-trichlorophenate and two molecules of 2,4,5-trichlorophenol. It is an antiparasitic agent. It is antimalarial drug, highly active against multiple Plasmodium falciparum isolates with IC50 value of 2.36E-07 M.

Nuclomedone (TEI-3096), a thiazolopyrimidine compound has been shown to suppress adjuvant arthritis in rats without any effect on conventional inflammation. TEI-3096 also enhanced the delayed type hypersensitivity in mice and rats. These results suggests that TEI-3096 restores the abnormal immune response. Nuclomedone was discovered by Teijin and investigated as a potential treatment for rheumatoid arthritis and inflammatory disorders.