Objective To evaluate the feasibility of Bama miniture pigs to be used as a model on pharmacokenetic properties of CYP3A by comparing enzyme kinetics of lovastatin metabolism in liver microsomes of Bama miniture pigs, humans and rats. Methods Liver microsomes were prepared from Bama miniature pigs, humans and rats, respectively. To evaluate the biotransformation activity in the minipig liver microsomes and compare with those of humans and rats, incubation with lovastatin was carried out. The inhibitory effects were observed by using chemical inhibitor specific to the CYP3A in humans. Results The enzyme kinetics in liver microsomes of minipigs were more similar to humans than rats. The metabolism of lovastatin in three various genera was significantly inhibited by ketoconazole. Conclusion Compared with rats, Bama miniature pigs are more suitable for the pharmacological studies related to CYP3A.