Drug intelligence / Profile preview

avitriptan

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Avitriptan is an **antimigraine drug** from the triptan family that was developed but never marketed[1][2][3]. It is a **small molecule serotonin receptor agonist** acting primarily as an agonist of the **serotonin 5-HT1B and 5-HT1D receptors**, with weaker agonist activity at the **serotonin 5-HT2A receptor**[1]. Furthermore, avitriptan is a **low-affinity agonist of the aryl hydrocarbon receptor (AhR)**, inducing CYP1A1 gene expression in a cell-type-specific manner[3]. The drug was developed by Bristol-Myers Squibb and reached phase III trials but was discontinued due to transient elevation of liver enzymes at high doses[3]. Its main indication was **migraine**[1][3], and its AhR agonist activity suggested potential repurposing for **intestinal diseases**, including inflammatory bowel disease[3]. Avitriptan is chemically classified as a **tryptamine derivative**.

Other names
AvitriptanAvitriptan [INN]151140-96-4UNII-6RS056L04PUNII6RS056L04PUNII 6RS056L04Pavitriptanum
02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)AHR (Aryl hydrocarbon receptor)HTR1D (5-hydroxytryptamine receptor 1D)

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