Snake venoms represent a vast reservoir of bioactive molecules with both toxic and therapeutic potential. The Saharan horned viper (Cerastes cerastes), distributed across North Africa and the Middle East, produces a venom rich in proteins and peptides that modulate key physiological processes. This review synthesizes current knowledge on the pharmacological activities of Cerastes cerastes venom and its purified components, emphasizing their potential applications in medicine. Enzymes such as phospholipases A2, serine proteinases, metalloproteinases, L-amino acid oxidases, and disintegrins have been isolated and characterized, displaying diverse biological effects. These include pro- and anticoagulant activities relevant to hemostasis, cytotoxic and anti-angiogenic properties with implications in cancer therapy, and antiparasitic effects against Leishmania and Schistosoma species. Furthermore, venom-derived LAAOs exhibit strong antibacterial activity, particularly against resistant pathogens such as MRSA, while emerging evidence highlights immunomodulatory and radioprotective roles. Despite their promise, challenges related to toxicity, stability, delivery, and potential immunogenicity must be addressed for successful clinical translation. Collectively, Cerastes cerastes venom exemplifies the therapeutic versatility of natural toxins and offers a valuable platform for the discovery and development of novel agents targeting cancer, infectious diseases, hemostatic disorders, and immune-mediated conditions.