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TOPIC

Discovery of MK-5661, a Once-Daily Oral NaV1.8 Inhibitor for the Treatment of Pain

Journal

ACS Medicinal Chemistry Letters

Author(s)

Bungard, C. J., Breslin, M. J., Boyce, C. W., Chobanian, H. R., Clements, M. K., Dalby, S. M., Ehrhart, J., Huang, C., Jones, K. G., Kraus, R. L., Layton, M. E., Li, Y., Madeira, M., Perkins, J. J., Stachel, S. J., Vardigan, J. D., Wang, D., Zhou, X., Santarelli, V. P., Burgey, C. S.

Year

2026

NaV1.8 is a key mediator of peripheral nociceptive signaling and an attractive nonopioid target for pain therapeutics. We report the discovery of MK 5661, a potent, selective, and orally bioavailable NaV1.8 inhibitor amenable to once-daily dosing. Optimization of an initial lead, guided by reduction of PXR activation, and dose optimization focusing on half-life and volume ligand efficiency are described. MK-5661 demonstrates a favorable pharmacokinetic profile in preclinical species, as well as efficacy in preclinical models for pain.

Keywords: Q2 2026

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