Calcitonin Gene-Related Peptide (CGRP) plays a pivotal role in migraine pathophysiology. Two types of CGRP function-blocking modalities, monoclonal antibodies, and small molecules (gepants), have been developed to target the CGRP ligands and CGRP receptors. Four CGRP monoclonal antibodies have received FDA approval for the prevention of migraine: erenumab, fremanezumab, galcanezumab, and eptinezumab. Two gepants have been approved by the FDA for the acute treatment of migraine: ubrogepant and rimegepant. Multiple clinical trials of the CGRP monoclonal antibodies and gepants, and now some open-label long-term extension data, established their efficacy, safety, and tolerability. In this chapter, we summarize the major clinical trials, pharmacokinetic insights, safety and tolerability profiles, and real-world data (if available) of the CGRP monoclonal antibodies and gepants.