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MK-3207
- Development stage
- Discontinued
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MK-3207 is an orally active, highly selective, and potent small molecule antagonist of the calcitonin gene-related peptide receptor (CGRP receptor). It was developed by Merck & Co for the acute treatment of migraine and migraine disorders. In clinical studies, it demonstrated high affinity for the human CGRP receptor (IC50 = 0.12 nM; Ki ≈ 0.022–0.024 nM), with selectivity over related receptors. Clinical trials showed that MK-3207 was effective in achieving pain freedom two hours after dosing in patients with moderate to severe migraine attacks. However, its development was discontinued after phase II due to concerns about asymptomatic liver test abnormalities observed during trials. The drug does not act via vasoconstriction or serotonin pathways but specifically blocks CGRP-mediated pain signaling.
- Other names
- 957118-49-9UNII-5C44M1QYCCUNII5C44M1QYCCUNII 5C44M1QYCC
02
Targets
Calcitonin gene-related peptide type 1 receptor
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