Drug intelligence / Profile preview

sumatriptan + telcagepant

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**sumatriptan + telcagepant** is an oral combination of two drugs from distinct migraine therapeutic classes: sumatriptan, a selective serotonin (5-HT1B/1D) receptor agonist (triptan), and telcagepant, a small molecule calcitonin gene-related peptide (CGRP) receptor antagonist. Sumatriptan induces cranial vasoconstriction and inhibits neurogenic inflammation by activating 5-HT1B/1D receptors, reducing pain transmission, and reversing blood vessel dilation involved in migraine pathogenesis[2][3]. Telcagepant functions by blocking CGRP-induced vasodilation, exerting antidromic action at the CGRP receptor with high affinity, thereby limiting migraines without direct vasoconstrictive effects[4][6]. When coadministered, telcagepant slightly increases plasma levels of sumatriptan via weak MAO-A inhibition, but clinical effects on blood pressure do not exceed those of sumatriptan alone[1][3]. The combination has been investigated in controlled studies for acute migraine therapy[1][3], with no additive vascular safety risks noted.

Other names
sumatriptan + telcagepantCGRP antagonist + triptan combo
02

Targets

Calcitonin gene-related peptide type 1 receptorHTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)MAOA (Monoamine oxidase A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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