Neurally Acting Anti-Migraine Agents

Neurally Acting Anti-Migraine Agents (NAAMAs) are a new class of drugs that provide safe, effective migraine relief without vasoconstriction. Lasmiditan is a first-in-class therapy that selectively targets 5-HT1F receptors expressed in the trigeminal pathway.

Localization of 5-HT Receptors in Migraine Pathways

Studies have demonstrated the following:

It's in the Data

Concentration causing 50% of maximal stimulation of GTPγS binding (nM)

Data 5-HT1B 5-HT1D 5-HT1F
COL-144 ~10,000 >1,000 43

Lasmiditan (COL-144) is a highly potent and selective 5-HT1F receptor agonist (Ki at human 5-HT1F receptors of 2.21nM), possessing >450-fold higher affinity for the 5-HT1F receptor versus 5-HT1B or 1D receptors based on binding affinity in vitro.