Heteronium is an anticholinergic agent. As a bromide salt, it was investigated in the clinic for the treatment of peptic ulcer and other gastrointestinal disorders.

Befunolol is a beta-adrenergic receptor blocker approved in Japan for the treatment of open-angle glaucoma. The current drug status is unknown.

Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.

Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.

Amrubicin is a totally synthetic 9-aminoanthracycline anticancer drug, which is approved in Japan for the treatment of small cell and non-small cell lung cancer. Upon administration amrubicin is reduced to its C-13 hydroxy metabolite, amrubicinol. The cytotoxicity of amrubicinol in vitro is 10 to 100 times greater than that of amrubicin. Thus, the anticancer activity of amrubicin is considered to derive from this active metabolite. The mechanism of action of the drug is related to the inhibition of topoisomerase II by stabilizing the cleavable complex.

Oxitefonium is an anticholinergic spasmolytic medication used for the treatment of asthma.

Sitaxentan (TBC11251, trade name Thelin) is a potent and selective Endothelin A receptor antagonist. Sitaxentan was under development by Encysive Pharmaceuticals (now Pfizer) for use in the treatment of pulmonary hypertension, congestive heart failure and asthma. It was launched in the major markets of the European Union (EU) under name Thelin for the treatment of pulmonary arterial hypertension. In December 2010, Pfizer discontinued clinical trials of sitaxentan worldwide and initiated voluntary product withdrawal from markets where it is approved due to life-threatening idiosyncratic risk of liver injury.

Cefprozil, an oral cephalosporin antibiotic, is a mixture of antibiotic BMY-28100 (Z- or cis-isomer) and antibiotic BMY-28167 (E- or trans -isomer), the mixture having a Z- to E- isomer ratio in the range of 89:11 to 94:6. BMY-28167 (E- or trans -isomer) is less active when compared with BMY-28100 or isomeric mixture. There were no remarkable differences in the toxicity of the cis isomer, the trans isomer, or cefprozil (the isomeric mixture).

Cefquinome is a 4th generation cephalosporin which is active against a broad spectrum of Gram positive and Gram negative bacteria. As many cephalosporin it acts by binding to bacterial PBP and thus inhibiting the cell wall synthesis. Cefquinome is approved for veterinary use in cattles with respiratory tract infections, skin infections, bacterial mastitis and septicaemia.

Ablukast is a benzopyran derivative, a leukotriene receptor antagonist with potential as an antiasthmatic agent. Ablukast antagonized he hypotensive effect of N-methyl leukotriene C4 and leukotriene C4 (LTC4). Ablukast also antagonized the effects induced by high doses of leukotriene D4 and E4. Receptors that preferentially bind LTC4 in bullfrog vascular smooth muscle regulate the hypotensive effect and that they can be antagonized by ablukast. Ablukast has been in phase III clinical trials for the treatment of bowel disease. However, this research has been discontinued.