Dalbavancin

General information

Dalbavancin (BI 397) is a semi-synthetic derivative of A40926, a glycopeptide with a structure related to that of teicoplanin [ , ]. Dalbavancin is more active against Streptococcus pneumoniae than conventional glycopeptides are, and its activity against Staphylococcus aureus is also substantially better. However, it is not more active than teicoplanin against enterococci harboring the VanA phenotype of resistance to glycopeptides. Dalbavancin is also characterized by a marked bactericidal character and synergism with penicillin.

Dalbavancin is a lipoglycopeptide antibacterial with in vitro activity against a variety of Gram-positive pathogens [ ]. Compared with other available agents it has favorable minimum inhibitory concentration ranges against meticillin-susceptible and meticillin-resistant Staphylococcus aureus . It is highly protein bound (> 90%), which contributes to its prolonged half-life of 149–300 hours, because of which once-weekly dosing strategies have been used in clinical trials.

Preclinical studies in rats and dogs have shown that dalbavancin is well tolerated, even at dosages several-fold higher than those likely to be used clinically. In phase I, II, and III clinical trials, dalbavancin was well tolerated, without evidence of dose- or duration-related adverse effects. It is important to note that clinical and pharmacokinetic studies published to date have excluded patients with a history of glycopeptide hypersensitivity, and there is no information about the incidence of cross-reactivity [ ].