Lasmiditan is a novel, centrally acting selective 5-HT?F receptor agonist approved for the acute treatment of migraine with or without aura. Unlike triptans, it does not cause vasoconstriction, making it a safer therapeutic option for patients with cardiovascular risk factors. Chemically, lasmiditan is 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-pyridin-2-yl] benzamide with a molecular formula of C??H??F?N?O? and molecular weight of 377.367 g/mol. It is available as lasmiditan hemi-succinate in 50 mg film-coated tablets. Lasmiditan exerts its antimigraine effect by selectively activating central 5-HT?F receptors located on trigeminal neurons, thereby inhibiting calcitonin gene-related peptide (CGRP) release and suppressing nociceptive transmission within the trigeminovascular pathway. The drug demonstrates rapid oral absorption, moderate protein binding, central nervous system penetration, hepatic non-CYP metabolism, and an elimination half-life of approximately 5–7 hours. Common adverse effects include dizziness, fatigue, somnolence, and paresthesia. Various analytical methods such as UV–Visible spectroscopy, HPLC, RP-HPLC, and LC-MS/MS have been developed and validated for its quantitative estimation, demonstrating high linearity, accuracy, and precision. This review highlights the physicochemical properties, pharmacodynamics, pharmacokinetics, mechanism of action, therapeutic uses, adverse effects, and analytical methods of lasmiditan.