Melittin, a cationic amphiphilic peptide from bee venom, has been studied for its pharmacological effects, including antitumor, antiviral, and anti-inflammatory properties. It can enhance the therapeutic effects of first-line drugs and has potential for clinical applications. However, its hemolytic activity and cytotoxicity limit its use. Strategies such as nanomodification, immuno-conjugation, structural regulation, and gene technology have been developed to reduce its toxicity and improve its specificity. Melittin has shown antiviral activity against herpes simplex virus (HSV), human immunodeficiency virus (HIV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and influenza A virus. It also exhibits antitumor potential against colon, gastric, breast, and hepatocellular carcinoma (HCC) cells, by inducing apoptosis, inhibiting cell proliferation, and suppressing metastasis. Melittin has anti-inflammatory effects by reducing pro-inflammatory cytokines, inhibiting NF-κB activation, and mitigating oxidative stress. It has been shown to alleviate symptoms of inflammatory diseases such as rheumatoid arthritis, ulcerative colitis, and acute liver failure. Melittin's therapeutic potential is being explored through various modifications to enhance its efficacy and reduce side effects. The article summarizes the current research on melittin's antiviral, antitumor, and anti-inflammatory properties and discusses strategies for its future clinical applications.Melittin, a cationic amphiphilic peptide from bee venom, has been studied for its pharmacological effects, including antitumor, antiviral, and anti-inflammatory properties. It can enhance the therapeutic effects of first-line drugs and has potential for clinical applications. However, its hemolytic activity and cytotoxicity limit its use. Strategies such as nanomodification, immuno-conjugation, structural regulation, and gene technology have been developed to reduce its toxicity and improve its specificity. Melittin has shown antiviral activity against herpes simplex virus (HSV), human immunodeficiency virus (HIV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and influenza A virus. It also exhibits antitumor potential against colon, gastric, breast, and hepatocellular carcinoma (HCC) cells, by inducing apoptosis, inhibiting cell proliferation, and suppressing metastasis. Melittin has anti-inflammatory effects by reducing pro-inflammatory cytokines, inhibiting NF-κB activation, and mitigating oxidative stress. It has been shown to alleviate symptoms of inflammatory diseases such as rheumatoid arthritis, ulcerative colitis, and acute liver failure. Melittin's therapeutic potential is being explored through various modifications to enhance its efficacy and reduce side effects. The article summarizes the current research on melittin's antiviral, antitumor, and anti-inflammatory properties and discusses strategies for its future clinical applications.