Nifurethazone, a 5-nitrofuran derivative, is an antibacterial agent. It was used for controlling Salmonella choleraesuis in swine. The mode of action of 5-nitrofuran analogues is based on red-ox biotransformation.

Oxapadol (MD 720111), a non-narcotic analgesic that caused a significant increase in the threshold of the reflex whereas no change was noted with placebo. The current use of this drug is unknown.

Nicothiazone (nicotinaldehyde thiosemicarbazone), an antituberculosis drug, was apparently responsible for inducing vacuoles in the corneal epithelium and thus caused discomfort and photophobia from corneal disturbance.

Nictiazem, diltiazem derivative, is a calcium channel blocker. Calcium antagonists and compounds which lower intraocular pressure may be combined in ophthalmic compositions to treat glaucoma.

Saviprazole (also known as HOE 731) is a potent inhibitor of gastric H+/K(+)-ATPase that has been studied in phase I clinical trial for the treatment of gastric ulcer. However, this study was discontinued.

Axitirome (also known as CGS 26214), a thyroid hormone receptor β selective agonist and an LDL receptor function stimulant, has a cholesterol-lowering activity. This drug was in phase I clinical trials for the treatment of hyperlipidemia, but studies were discontinued because of the unexpected side effects.

Naxifylline [CVT 124, BG 9719], a small molecule diuretic, is one of a new class of potent and highly selective adenosine A1 receptor antagonists discovered at University of Florida. Naxifylline is an A1 adenosine receptor antagonist used for the treatment of edema associated with congestive heart failure. Naxifylline appears to be one of the more potent and clearly the most A1-selective antagonist reported to date, with K1 values of 0.67 and 0.45 nM, respectively, at the rat and cloned human A1-receptors and with 1800-fold (rat) and 2400-fold (human) subtype selectivity. Naxifylline protects against the decline in renal function observed with diuretic therapy by promoting urine output.

IROFULVEN is a semisynthetic derivative of a natural sesquiterpene toxin illudin S, isolated from the fungus Omphalotus illudens. It alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. It requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. IROFULVEN is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and P-glycoprotein than other alkylating agents. IROFULVEN has been evaluated in 19 clinical trials, predominantly in refractory prostate and ovarian cancer patients. Results were positive, including a 10% response rate in patients with prostate cancer previously treated with docetaxel and 13% in ovarian cancer patients relapsing between 6 and 12 months after standard treatment with carboplatin and paclitaxel.

Upidosin [REC 152739, REC 22009] is an α1-blocker that was in phase II trials with Recordati in Belgium and Israel for the treatment of benign prostatic hyperplasia. When evaluated in radioligand binding assays with expressed animal or human alpha-1 ARs, Upidosin shows marked to moderate selectivity for the alpha-1a AR subtype. Its affinity for the recombinant alpha-2 AR subtypes or native dopaminergic D2 receptor was about 100-fold lower than that for alpha-1a AR subtype.