RAP-219

RAP-219
Clinical data
Other namesRAP219; JNJ-64300912; JNJ64300912
Routes of
administration		Oral
Drug classAMPA receptor negative allosteric modulator
Pharmacokinetic data
Protein binding98.8%
MetabolismGlucuronidation (UGT1A4), sulfation
Elimination half-life278 hours

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.

See also

References

  1. 1 2 3 4 5 "RAP 219". AdisInsight. 26 May 2026. Retrieved 30 May 2026.
  2. 1 2 3 4 5 6 7 8 9 Bialer M, Johannessen SI, Koepp MJ, Perucca E, Perucca P, Tomson T, et al. (October 2024). "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. doi:10.1111/epi.18056. PMID 39008349.
  3. 1 2 3 "Delving into the Latest Updates on RAP-219 with Synapse". Synapse. 26 May 2026. Retrieved 30 May 2026.
  4. 1 2 Motley WW, Friedman D, Davis KA, Galer BS, Wyant N, Matta JA, et al. (September 2024). 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) (PDF). 15th European Epilepsy Congress. Rome, Italy.
  5. ↑ WO 2016176460, 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", published 28 April 2016, assigned to Janssen Pharmaceutica NV
  6. ↑ "Evolution of RAP-219 for the Treatment of Epilepsy" (PDF). www.rapportrx.com.