Migraine is one of the most prevalent neurological disorders known to have an immense adverse socio-economic impact. Neurogenic inflammation is thought to mediate migraine, and CGRP is known to be released during acute attacks of migraine that causes vasodilation in extracerebral arteries. Hence, CGRP is believed to play a key role in triggering migraine. Although there are several classes of medications used in the prevention and treatment of migraine pain, targeted therapies are fewer. Therefore, CGRP receptor inhibitors which bind to CGRP receptors in the cranial vasculature have been developed as drugs for migraine therapy. In this review article, we describe the basic pathophysiologic mechanism that causes migraine headaches and the pharmacotherapeutic aspects of CGRP inhibitors available for clinical use. For the purpose of this review, a search was performed on the pharmacological, pharmacokinetic, pharmaceutical, and therapeutic aspects of the FDA-approved CGRP inhibitors viz. erenumab, ubrogepant, rimegepant, atogepant, eptinezumab, fremanezumab, and galcanezumab in UpToDate database and PubMed beginning year 2000. Based on the data collected, a risk-benefit comparison of different classes of novel CGRP inhibitors available for clinical use is provided. This comparative review may help the healthcare providers in choosing the best pharmacotherapeutic agent for their patients based on patient-specific information.