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Metformin is a popular biguanide medicine because of its efficacy and inexpensive cost. Over time, other applications of metformin were found, and the advantages of metformin for diverse conditions such as anticancer, anti-inflammatory, anticoagulant, antimicrobial, and many more were studied. Although the underlying mechanism of these numerous benefits remains unknown, repurposing it is a smart concept, as it offers several advantages, including reduced development and research costs. However, taking it as-is may result in unwanted pharmacokinetics and mild to severe adverse effects. To overcome these, several researchers experimented and reported modified metformin derivatives that had better pharmacological potential, favorable pharmacokinetics, and fewer side effects. This review, therefore, sheds light on the current therapeutic expansion of non-metal derivatives of metformin along with their synthesis methods and evaluated outcomes. This will support researchers studying these modified or replaced metformins in the scientific community.
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