Milveterol (also known as GSK159797) was developed as a longer-acting beta2 adrenoceptor agonist for the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Milveterol completed phase II clinical trials for asthmatic subjects. However further development of the drug was discontinued.

Fluazuron (N-[[4-chloro-3-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]carbamoyl]-2,6-difluorobenzamide, trade name Acatak) is an insect growth regulator belonging to the class of benzoyl phenyl urea derivatives, a class of chitin synthesis inhibitors. Fluazuron specifically interferes with chitin formation in ticks during engorgement, molt, and hatching. The substance is intended for tick control in beef cattle applied topically as a pour-on for use at single dose levels of 1.5 and 2.5 mg/kg BW with a possible additional treatment after 3 to 6 months.

FETOXYLATE, a phenoxyethyl ester of diphenoxylate, is an opioid receptor agonist. It is used as antidiarrheal.

Peliglitazar (also known as BMS 426707-01), a dual α/γ peroxisome proliferator-activated receptor agonist, has been studied in phase I/II clinical trial in patients with type 2 diabetes mellitus. However, this study was discontinued.

Dersalazine is a locally-acting compound. It is a potent platelet activating factor (PAF)-antagonist. Dersalazine inhibited IL-1beta or TNF-alpha production in THP-1 or U937 cells, respectively. Dersalazine sodium reduced colonic proinflammatory cytokines IL-1b, IL-6, and IL-17 in dextran sodium sulphate (DSS)–induced colitis. After oral administration, dersalazine sodium is mostly unabsorbed until it reaches the large bowel where the azo bond is reduced by bacteria releasing the active compound. Dersalazine had been in phase I clinical trial for the treatment of ulcerative colitis. No serious adverse reactions were detected in clinical trial. However, no recent development has been reported.

Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.

Benafentrine (also known as AH 21-132), an inhibitor of the phosphodiesterase (PDE) III and IV isoenzymes, had an anti-allergic effect and was studied for the treatment of allergic bronchial asthma. However, the development of the drug was discontinued at phase I.