Galocitabine is an orally available 5-fluorouracil (5-FU) prodrug with potential antineoplastic activity. Upon administration, galocitabine is converted to 5’-deoxy-fluorocytidine (5’-DFCR) by acylamidase in the liver and is then converted to 5’-DFUR by cytidine deaminase. Efficient conversion of galocitabine to 5-FU is necessary for galocitabine to have a therapeutic effect. 5-FU is further metabolized into other cytotoxic metabolites that interfere with RNA and DNA synthesis via inhibition of thymidylate synthase. As a result, this agent eventually inhibits tumor cell growth.

Sucralox is a saccharated aluminum hydroxide patented by Combe, Inc. as antacid agent. Sucralox shows potent antacid properties in vitro and in vivo. Currently Sucralox is used to support gastric and intestinal health in horses.

Cetocycline (formerly chelocardin or cetotetrine) is tetracycline derivative with potent antibacterial activity against a number of Gram-positive and Gram-negative multi-resistant pathogens. Cetocycline was found to be more active than tetracycline against many clinical isolates of aerobic gram-negative bacilli, but is less active against staphylococci, and has no activity against Pseudomonas. At low concentrations, like classical tetracyclines, chelocardin induces the proteomic signature for peptidyl transferase inhibition demonstrating that protein biosynthesis inhibition is the dominant physiological challenge. At higher concentrations B. subtilis mainly responds to membrane stress indicating that at clinically relevant concentrations the membrane is the main antibiotic target of chelocardin.

Diflucortolone pivalate is a glucocorticoid drug. It might be used as anti-inflammatory and anti-allergic agent.

The information related to the biological or pharmacological application of fluprednisolone valerate is absent.

Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. It demonstrated a broad spectrum of in vitro cytotoxicity against tumor cell lines. According to the results of Phase II trials elsamitrucin is not an active drug in patients with metastatic breast cancer, colorectal cancer, non-small cell lung cancer or ovarian cancer, however, it showed modest activity in patients with relapsed or refractory non-Hodgkin's lymphoma.

Pamaqueside, an 11-ketotigogenin cellobioside was developed as a cholesterol absorption inhibitor for the treatment of hypercholesterolemia. This drug participated in phase III clinical trial; however, information about the further development of this drug is not available.

(S)-baclofen (or L-baclofen) is an enantiomer of baclofen, a direct GABA-B receptor mimetic. L-baclofen represents a significant improvement over racemic baclofen in the treatment of trigeminal neuralgia.

Tiqueside is the synthetic spirostane-based steroid glycoside. It precipitates cholesterol from micellar solution in vitro and reduces plasma cholesterol absorption in rats through a mechanism that is currently thought to be independent of either association of the saponin with the intestinal mucosal surface or absorption of the saponin molecule. As a consequence of this inhibition, tiqueside has been shown to reduce plasma cholesterol concentrations in cynomolgus monkeys. Inhibition of cholesterol absorption by tiqueside produces profound effects on cholesterol metabolism without affecting bile acid metabolism, and these changes lead to reductions primarily in plasma non-HDL cholesterol concentrations. Tiqueside produced a dose-dependent reduction in plasma LDL cholesterol levels in the hypercholesterolemic patients. In the mechanistic study, it decreased fractional cholesterol absorption rates and increased fecal neutral sterol excretion rates, changes associated with trends toward lower LDL cholesterol levels. Other lipoprotein levels were unaffected, as were fecal fat and bile acid excretion and fat-soluble vitamin absorption. Thus tiquesidedose-dependently inhibits cholesterol absorption in humans, resulting in a reduction in serum LDL cholesterol levels.