Diminazene is an aromatic diamidine derived from Surfen C. Diminazene is used as aceturate salt. Diminazene is highly active against both Trypanosoma and Babesia spp. It is also of value in the treatment of theileriosis due to Theileria annulata. Diminazene has become the most commonly used therapeutic agent for trypanosomiasis in animals. It is said to be effective in canine, ovine and bovine babesiosis and, unlike some drugs, is less susceptible to relapse. It may also possess antibacterial properties. Diminazene binds to trypanosomal kDNA. This binding does not occur by intercalation but via specific interaction with sites rich in adenine-thymine (A-T) base pairs. Diminazene specifically inhibits mitochondrial type II topoisomerase in viable trypanosomes. Thus, inhibition of DNA replication may also occur via this interaction. Diminazene is extensively distributed in the body of treated animals. Residues of the compound may persist for several weeks, principally in the liver and kidneys, and also, to a lesser extent, in the gastrointestinal tract, lungs, muscle, brain and fat.

Gimatecan is a topoisomerase I inhibitor that is presently tested in phase II of clinical trials for the treatment of different cancers: glioma, glioblastoma, epithelial ovarian cancer, fallopian tube or peritoneal cancer. The drug recieved orphan designation for the treatment of glioma.

Pelitrexol (also known as AG2037) was developed by Pfizer as a glycinamide ribonucleotide formyltransferase inhibitor. This drug was studied in phase II clinical trials in patients with metastatic non-small cell lung cancer and in patients with metastatic colorectal cancer who failed treatment. In addition, the drug participated in a phase I clinical trial in treating patients who have advanced, metastatic, or recurrent solid tumors. Information about the further development of pelitrexol is not available.

Enofelast (BI-L-239) is a potent and selective 5-lipoxygenase inhibitor. It inhibited leukotriene B4 and C4 generation. In animal models, enofelast attenuates bronchoconstriction, leukocyte infiltration, inflammation and hyperresponsiveness that characterize asthma.

Topixantrone (BBR 3576) is a hetero-analog of the anthrapyrazole class of compounds. The mechanism of action of BBR 3576 is similar to that of mitoxantrone in terms of DNA intercalation, DNA affinity, topoisomerase II interaction and formation of single-strand breaks. BBR 3576 showed curative antitumor activity at the maximum tolerated dose (MTD) with a number of long-term survivors and showed greater activity than mitoxantrone and doxorubicin in preclinical studies. BBR 3576 retained a high level of activity across a wide range of doses. In human xenograft studies, equivalent antitumor activity was observed when compared with doxorubicin and mitoxantrone. The compound showed reduced cardiotoxicity when repeatedly administered in rodent models. Topixantrone has a manageable toxicity profile on a 4-week schedule.

Clonixeril is a glyceryl ester of a nonsteroid anti-inflammatory drug clonixin, developed by Scherico Ltd in the 1970s. Oral administration of clonixeril delays the onset of castor oil-induced diarrhoea in rats.

Tanogitran (also called as BIBT986) is a dual inhibitor of thrombin/factor Xa. Tanogitran participated in a clinical trial in endotoxin-induced coagulation, where was shown that tanogitran was a potent anticoagulant. In addition, the drug was studied in phase II clinical trial for the treatment of septic shock; however, information about the further development of this drug is not available.

Dacemazine is a derivative of phenothiazine which acts as an antagonist of a histamine H1 receptor. The compound demonstrates local anesthetic activity and reduced the spasms produced by acetylcholine and histamine. In combination with di-tert-butylnaphthalenesulfonate, dacemazine was marketed under tradename Codopectyl as a spasmolytic and antitussive agent.

ISOTIQUIMIDE is an anti-ulcerative agent.

Subendazole is an antiparasitic and antispirochete agent used to treat helminth infection.