Drug intelligence / Profile preview

tildipirosin

Development stage
Unknown
Lead developer
Merck Animal Health
Modality
Small Molecules
Administration
Subcutaneous, Intramuscular
01

Overview

Tildipirosin is a semi-synthetic, 16-membered macrolide antibiotic developed for veterinary use, primarily in cattle and swine. It is structurally derived from tylosin and features three amine substituents on its macrocyclic lactone ring, giving it a tri-basic character[1][5][7]. Tildipirosin acts by selectively binding to the 23S ribosomal RNA of the bacterial 50S subunit, thereby inhibiting essential protein biosynthesis and blocking peptide chain elongation[1][6]. This mechanism results in bacteriostatic activity against most pathogens but can be bactericidal for certain species such as Mannheimia haemolytica and Actinobacillus pleuropneumoniae[1][7]. The drug exhibits high concentrations in lung tissue and bronchial fluid after administration, making it effective against respiratory pathogens associated with bovine respiratory disease (BRD) and swine respiratory disease (SRD), including Mannheimia haemolytica, Pasteurella multocida, Histophilus somni (cattle), Actinobacillus pleuropneumoniae, Bordetella bronchiseptica, Haemophilus parasuis (swine)[1][2][3][5]. Tildipirosin is administered as a single-dose injection—subcutaneously in cattle or intramuscularly in swine—and provides prolonged therapeutic levels due to its pharmacokinetic properties[2][5].

Brand names
Zuprevo
02

Targets

Bacterial 50S ribosomal subunit

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