Background: Streptomyces, a prolific genus of bacteria, has been a longstanding source of bioactive compounds with diverse therapeutic applications. This review explores the multifaceted therapeutic potential of Streptomyces and its derivatives as a compelling alternative to modern therapeutic approaches. The comprehensive analysis covers the biological diversity of Streptomyces, the intricate mechanisms of its secondary metabolites, and their impact on various medical domains. Streptomyces, boasting over 500 identified species, is renowned for its production of bioactive compounds with antibacterial, antifungal, antiviral, and anticancer properties. The primary focus is on the antibiotics, such as streptomycin and tetracycline, highlighting their significance in addressing bacterial infections, especially in the context of escalating antibiotic resistance. Additionally, the review delves into the antifungal activities exhibited by Streptomyces compounds, contributing to their role in combating mycotic diseases. Streptomyces-derived compounds have also shown promise in cancer therapeutics, with specific attention to Streptozotocin and its potential in treating pancreatic cancer. Beyond their direct antimicrobial and anticancer effects, Streptomyces compounds are recognized for their immunomodulatory properties, enhancing the body's ability to combat infections and manage inflammatory conditions. This review underscores the versatility of Streptomyces in therapeutic applications, ranging from its direct effects on pathogens to its potential in regulating immune responses. As research in this field advances, the ongoing exploration of Streptomyces and its bioactive compounds holds significant promise for the development of innovative and targeted therapeutic interventions, offering an appealing alternative to contemporary medical approaches.