Diminazene aceturate is the drug most commonly used for the treatment of trypanosome infections in cattle, sheep and goat. It has been reported to also have anti-babesial, anti-inflammatory, anthelmintic, anti-viral and anti-bacterial activities unlike other trypanocides. The drug is an aromatic diamidine compound popularly marketed as Berenil®. Retention of high concentrations of diminazene aceturate in plasma and tissues can be enhanced by combining it with other drugs such as Oxytetracycline long-acting. The enhanced concentrations can lead to prevention of relapse of treated trypanosome infections and it can also act as a prophylactic treatment against trypanosomosis in dogs. The present review discussed current status of knowledge concerning therapeutic spectrum of diminazene, its chemical structure, physical properties, mechanism of actions, contraindications, formulations and combination therapeutic regimens in which diminazene has been administered together with other compounds. Analytical techniques for diminazene, the pharmacokinetics of diminazene, its toxicity, and clinical uses in livestock are also discussed.