Voltage-gated calcium channels are one of the major ion channels distributed in the human central nervous system, and mediate an influx of extracellular Ca2+ in response to membrane depolarization. Calcium channels are of particular interest in a broad range of cellular functions including cell proliferation and differentiation, gene expression, neurite outgrowth, transmitter and hormone release, and brain plasticity. The dysfunction of calcium channels is related to a variety of clinical disorders such as migraine, hemiplegia, and epilepsy. Therefore, calcium channels have gained great pharmaceutical interest as a privileged target class for the treatment of a wide range of human diseases. This review will examine the known marketed peptide drugs for calcium channels and address the development of some important patented peptide molecules targeting calcium channels.