Leurubicin was developed as a prodrug of doxorubicin (Dox) with the aim of lowering the cardiotoxicity and improving the therapeutic index produced by Dox. Antineoplastic agent Dox was rapidly formed from leurubicin, reaching peak levels in plasma within 5 min and in tissues within 1 h after i.v. administration of leurubicin. The incorporation of leurubicin into the MES-SA human uterine sarcoma cell line and its Dox resistant counterpart, MES-SA/Dx5 cell line and the subsequent transformation of leurubicin into Dox and its subcellular distribution, were investigated. In both cell lines the cellular uptakes of Dox and leurubicin were similar at equimolar doses, while the percent transformation of leurubicin into Dox in MES-SA/Dx5 cells was about twice as great as its transformation in MES-SA cells, which is beneficial for reaching Dox cytotoxic levels in this resistant cell line. The highest Dox/ leurubicin ratio was found in the nuclear fraction, followed by the ratio in the low density organelle fraction that contains lysosomes, organelles in which lysosomal hydrolytic enzymes, capthesins, transform leurubicin into Dox.

Eniclobrate (Sgd 33374), a diphenylmethane derivative, is a lipid-lowering compound. In rodents, eniclobrate lower serum and liver cholesterol levels and reduced the percentage of esterified cholesterol present in the serum but raised liver triglyceride levels. In a clinical trial for the treatment of hyperlipidemia type IIa and type IIb eniclobrate effectively reduced LDL-cholesterol in type IIa, however, there was a remarkable increase in HDL-cholesterol in both types of hyperlipidemia.

Butikacin is deoxystreptamine aminoglycoside with bactericidal activity with good activity against Staphylococcus aureus and a range of gram-negative bacteria.

Colterol is a beta-2 adrenoreceptor agonist. Bitolterol, a diester prodrug of colterol, was marketed by Elan Pharmaceuticals for the treatment of reversible bronchospasm associated with asthma or chronic obstructive pulmonary diseases.

Metostilenol was developed as an antidepressant. However, it has never been marketed.

ISOPROFEN is an anti-inflammatory agent with analgesic and antipyretic properties. Its anti-inflammatory potency is greater than that of phenylbutazone but lower than that of indomethacin. Its antipyretic action can be explained by an effect of this substance on the metabolism of arachidonic acid in the brain.

Pancopride (LAS 30451) is a 5-hydroxytryptamine 3 receptor antagonist and was developed against cytotoxic drug-induced emesis. Pancopride was studied in clinical trials in patients treated with highly emetogenic chemotherapy. It was found a combination of Pancopride with dexamethasone was the most effective against chemotherapy-induced vomiting. However, information about the further development of this drug is not available.

Febuverine is a spasmolytic and local anesthetic.

Etisomicin is a semisynthetic aminoglycoside antibiotic.