Chemistry:RAP-219
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.[1][2][3][4] It is taken orally.[1][3] 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.[3][4] The time to peak levels of RAP-219 is approximately 4 hours and its elimination half-life is 278 hours.[3] RAP-219 is under development by Rapport Therapeutics.[1][2] 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.[1][2] The drug is an azabenzimidazole derivative of undisclosed chemical structure.[3][5][6]
See also
- List of investigational bipolar disorder drugs
References
- ↑ 1.0 1.1 1.2 1.3 "RAP 219". 26 May 2026. https://adisinsight.springer.com/drugs/800072876.
- ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on RAP-219 with Synapse". 26 May 2026. https://synapse.patsnap.com/drug/0f5b900d3eef49d3aa3266b6d448173b.
- ↑ 3.0 3.1 3.2 3.3 3.4 "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 65 (10): 2831–2857. October 2024. doi:10.1111/epi.18056. PMID 39008349.
- ↑ 4.0 4.1 "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).". 15th European Epilepsy Congress. Rome, Italy. September 2024. https://www.rapportrx.com/wp-content/uploads/2024/09/53391-EEC-Poster-2024-08-08_FINAL.pdf.
- ↑ Berry CG, Chen G, Jourdan FL, Lebold TP, Lin DW, Piñón MA, Ravula S, Savall BM, Swanson DM, Wu D, Zhang W, Ameriks MK, "Azabenzimidazoles and their use as ampa receptor modulators", WO patent 2016176460, published 28 April 2016, assigned to Janssen Pharmaceutica NV
- ↑ "Evolution of RAP-219 for the Treatment of Epilepsy". https://www.rapportrx.com/wp-content/uploads/2025/12/53741-History-Poster-2025-12-04_FINAL.pdf.
 |  |
