Bee venom (BV), a complex honeybee Apis mellifera excretion, has been vastly valued throughout centuries for its medicinal virtues, such as described in ancient documents including the Vedas, Quran, and Bible. Modern biomedicine research has elucidated principal bioactive components of BV, including melittin, phospholipase A2 (PLA2), apamin, mast cell-degranulating peptide, and adolapin, which are vested with a wide range of therapeutic properties. Melittin, the principal peptide, is strongly anticancer against a variety of cancers including breast, cervical, prostate, and hepatocellular carcinoma. With nanocarrier systems, it increases delivery and decreases systemic toxicity. Outside of cancer, BV has strong antimicrobial activity against multidrug-resistant bacteria, fungi like Candida albicans and Aspergillus fumigatus, and enveloped viruses like HIV and flu. BV controls signaling pathways like NF-κB and JAK/STAT3 to suppress oxidative stress and cytokine release. This is beneficial in the treatment of inflammatory and neurodegenerative diseases. BV promotes insulin release and protects against destruction of pancreatic β-cells, and hence can be used to treat arthritis, multiple sclerosis, Alzheimer’s, and diabetes. In dermatology and dermal cosmeceuticals, BV inhibits the 5α-reductase activity and promotes hair growth by upregulating growth factors such as FGF7, VEGF, and IGF-1. It is also useful in the treatment of acne, psoriasis, and vitiligo. Apipuncture, which is the interaction of traditional acupuncture with bee venom pharmacology, has also been shown to be useful in randomized controlled trials for musculoskeletal pain, rheumatoid arthritis, and neurological disorders. Although its multistage therapeutic potential is encouraging, clinical use is a limitation due to variability in venom composition, standardization of dosing, immunogenicity, and long-term safety. Optimal extraction methods, molecular identification, and unraveling the synergistic interaction of BV components need to be a focus of future studies to establish effective, safe, and targeted therapies. Further studies are indicated to explore the promise of bee venom as a natural addition to precision medicine across various fields.