In this chapter, the potential medical-pharmaceutical use of molecules derived from toad skin secretions is discussed. Over the past decades, numerous bioactive components from toad poisons, with diverse biological activities, have been studied. They present diversified chemical structures, such as steroids, alkaloids, peptides, proteins, and biogenic amines. Toad poison components are the result of pharmacological and biochemical refinement that occurred during the process of evolution, which made them highly effective. They present a broad spectrum of physiological and defense functions. The dried secretion from the skin glands of toads has been used clinically for over a millennium as an anodyne cardiotonic, antimicrobial, local anesthetic, and antineoplastic agent. The discovery of poison components with biological activity, such as anticancer, antimicrobial, antiviral, antiparasitic, modulators of blood coagulation, neurotransmission, analgesic, and anti-inflammatory, among others, aiming to discover new drugs, is a challenge. However, despite the difficulties, these studies have been conducted and many poison components with therapeutic potential have been identified.