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AMPA receptor negative allosteric modulator

RAP-219

Original Wikipedia articleen.wikipedia.org/wiki/RAP-219 revision used (24 October 2026)

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Part of the metabolic pathway of RAP-219. See the timeline on the metabolic highway.

Enzymes that break it down: UGT1A4. Wikipedia’s drug infobox says: “Glucuronidation (UGT1A4), sulfation” (revision 1372045630).

Overview

RAP-219, formerly known as JNJ-64300912, is an AMPA receptor negative allosteric modulator which is under development for the treatment of partial epilepsies, bipolar disorders, and neuropathic pain. It is taken orally. The drug acts specifically as a selective negative allosteric modulator of the transmembrane AMPA receptor regulatory protein (TARP) γ-8 and potently and selectively inhibits TARP γ-8-containing AMPA receptors. The time to peak levels of RAP-219 is approximately 4 hours and its elimination half-life is 278 hours. RAP-219 is under development by Rapport Therapeutics. As of May 2026, it is in phase 3 clinical trials for partial epilepsies, phase 2 trials for bipolar disorders, and phase 1 trials for neuropathic pain. The drug is an azabenzimidazole derivative of undisclosed chemical structure.[1–6] WP

Drug class

AMPA receptor negative allosteric modulator WP

From the Wikipedia article's infobox.

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Sources

  1. Journal / agency RAP 219. 26 May 2026
  2. Other Delving into the Latest Updates on RAP-219 with Synapse. 26 May 2026
  3. Journal / agency Bialer M, Johannessen SI, Koepp MJ, Perucca E, Perucca P, Tomson T, White HS. Progress report on new medications for seizures and epilepsy: A summary of the 17th Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XVII). I. Drugs in preclinical and early clinical development. Epilepsia. October 2024. doi:10.1111/epi.18056 · PMID 39008349
  4. Other Motley WW, Friedman D, Davis KA, Galer BS, Wyant N, Matta JA, Gammaitoni AR, Dlugos D, Morrell M, French JA. Novel design of a focal epilepsy proof-of-concept study of RAP-219, a negative allosteric modulator of the γ8 transmembrane AMPA receptor associated protein (TARPγ8). September 2024
  5. Other Azabenzimidazoles and their use as ampa receptor modulators
  6. Other Evolution of RAP-219 for the Treatment of Epilepsy

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