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List of investigational headache and migraine drugs

This is a list of investigational headache and migraine drugs, or drugs that are currently under development for clinical use in the treatment of headaches and/or migraines but are not yet approved. They may also be referred to as investigational antimigraine agents.

Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. The format of list items is "Name (Synonyms) – Mechanism of Action – Indication [Reference]".

This list was last comprehensively updated in September 2025. It is likely to become outdated with time.

Under development

Phase 3

Phase 2/3

Phase 2

Phase 1/2

  • XC-101 (XC101; XC101-D13H) – serotonin 5-HT<sub>1B</sub> and 5-HT<sub>7</sub> receptor agonist, serotonin 5-HT<sub>1D</sub> and 5-HT<sub>1F</sub> receptor partial agonist, and serotonin 5-HT<sub>2A</sub>, 5-HT<sub>2B</sub>, and 5-HT<sub>2C</sub> receptor antagonist – migraine https://adisinsight.springer.com/drugs/800051258

Phase 1

Preclinical

Research

Phase unknown

Not under development

Preregistration submission withdrawal

Suspended

No development reported

Discontinued

Clinically used drugs

Approved drugs

COX inhibitors/NSAIDs

Triptans (serotonin 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptor agonists)

Ergolines (non-selective monoamine receptor modulators)

Calcitonin gene-related peptide (CGRP) inhibitors

Combination drugs

Other drugs

Off-label drugs

See also

References

External links