Garlic (Allium sativum L.) is an important and widely cultivated plant with both culinary and medicinal uses stemming from its biological activities, which include antibiotic, anticancer, anti-thrombotic, and lipid-lowering cardiovascular effects. Though such medicinal use of garlic existed for centuries, there was little scientific support for its therapeutic and pharmacological properties. However, there has been a recent upsurge of research on garlic aiming to understand its exact mechanism of action in each case so that garlic and its products may have more judicious future applications. Since garlic is vegetatively propagated, its improvement for desired traits through conventional means is difficult. The intervention of biotechnological methods such as tissue culture and gene transfer protocols developed recently hold great promise for improving this crop. Due to new innovations in instrumentation and processing technologies coupled with more judicious experimental models, better products are foreseen in the market. The objective of this article was to review the recent developments made towards understanding the mechanism by which garlic imparts different therapeutic effects as well as to review what biotechnology can offer to improve this crop and its products.