Scorpionism (scorpion sting) is a major public health issue in many regions of the world. Globally, 1.2 million scorpion stings happen annually, specifically in the tropical regions. Mortality due to these venomous stings is serious health problem in absence of suitable medication. Awareness of this problem is fundamental for preventive measures. Scorpion venom is composed of water, mucosa, enzymes, free amino acids, biogenic amines, neurotoxins, low molecular weight peptides, and proteins having maximum molecular activities. Neurotoxins are potent and are highly selective ligands for voltage-gated sodium, potassium, chloride, and calcium ion channels. Therefore, they depict interesting compounds for the development of novel drugs, for example, drugs for cancer, neurological disorders, cardiovascular diseases, and analgesics. Scorpion venom has apoptogenic, cytotoxic, immunosuppressive, and antiproliferative effects. Therefore, scorpion venom can be utilized against various cancers like glioma, leukemia, human neuroblastoma, brain tumor, melanoma, prostate cancer, and breast cancer. This review explains the details of toxin receptor interactions and provides details about opportunities for the development of peptide-based therapeutics.