Background: Classified as a Group IIIA metal, gallium, as well as its compounds, has been presenting several therapeutic activities in the last decades. Gallium compounds garnered considerable attention mainly due to their ability to mimic iron, presenting antimicrobial activities and showing antiproliferative and antimitotic activity against some cancers. Method: This review article provides a survey of the main therapeutic applications and analysis of the characteristics of in vivo and in vitro preclinical trials with gallium and its respective compounds. Results: Given the therapeutic potential of gallium, its compounds are promising at various stages of preclinical studies for promoting therapeutic action. In this work we discussed about Gallium antimicrobial and antineoplasic activities, its effects in bone metabolism and hypercalcemia, as well as immunosuppressive, anti-inflammatory and antimalarial properties. Conclusion: Gallium and its complexes show promising pharmacological options for various diseases, representing a major breakthrough in therapy as they have potential for new drug candidates. However, more studies are still necessary.