Trovafloxacin

Products

Trovafloxacin was commercially available in many countries as film-coated tablets and as an infusion concentrate (Trovan, Pfizer). It was withdrawn from the market in 1999 because of potential adverse effects.

Structure and properties

Trovafloxacin (C20H15F3N4O3, Mr = 416.4 g/mol) is a fluoronaphthyridone. It is present in tablets as trovafloxacin mesilate. In parenteral dosage forms, it is also present as alatrofloxacin, an alanine prodrug that is rapidly hydrolyzed in the body to the active trovafloxacin.

Effects

Trovafloxacin (ATC J01MA13) has bactericidal properties against Gram-positive, Gram-negative, and anaerobic pathogens. The effects are due to inhibition of bacterial topoisomerase II (gyrase) and topoisomerase IV, which play a central role in bacterial proliferation.

Indications

For the treatment of bacterial infectious diseases.

Adverse effects

Trovafloxacin is hepatotoxic and rarely can cause severe liver disease requiring transplantation or even death. Therefore, it has been withdrawn from the market in many countries.