Eletriptan is a selective serotonin 5-HT1B/1D receptor agonist belonging to the triptan class of antimigraine medicines. It is an orally active small-molecule pharmaceutical ingredient developed for the acute treatment of migraine attacks, with or without aura.
Eletriptan works primarily by activating serotonin 5-HT1B and 5-HT1D receptors. This produces constriction of certain intracranial blood vessels and inhibits the release of vasoactive neuropeptides involved in migraine pathophysiology.
Eletriptan is available pharmaceutically as eletriptan hydrobromide, the salt form used in marketed tablets. The free base has CAS Number 143322-58-1, while eletriptan hydrobromide is identified by CAS Number 177834-92-3.
Eletriptan API is a pharmaceutical active ingredient belonging to the triptan class. It is used in pharmaceutical formulation development for products intended for the acute treatment of migraine.
Eletriptan has the molecular formula C22H26N2O2S and molecular weight approximately 382.52 g/mol. The hydrobromide salt has the molecular formula C22H27BrN2O2S and molecular weight approximately 463.44 g/mol.
Eletriptan binds with high affinity to serotonin 5-HT1B and 5-HT1D receptors. Activation of these receptors contributes to cranial vasoconstriction and inhibition of trigeminal neuropeptide release, helping to interrupt the processes associated with an acute migraine attack.
Eletriptan is primarily associated with:
It is intended for acute treatment rather than preventive treatment of migraine.
Eletriptan API should be manufactured, tested and released according to the applicable approved specification and pharmaceutical quality requirements.
Relevant quality attributes may include:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |