Chemistry:BP1.4979

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BP1.4979 is a selective dopamine D3 receptor agonist which is under development for the treatment of binge-eating disorder, obsessive–compulsive disorder (OCD), restless legs syndrome (RLS), and smoking withdrawal.[1][2][3] It is taken orally.[1] The drug acts as a highly potent weak partial agonist of the dopamine D3 receptor (Ki = ~1 nM; EC50 = 0.7 nM; Emax = 32%).[3] It has around 200-fold higher affinity for the dopamine D3 receptor than for the dopamine D2 receptor (Ki = 192 nM), where it is an antagonist.[3] BP1.4979 showed 66% dopamine D3 receptor occupancy and 8% dopamine D2 receptor occupancy with positron emission tomography (PET) imaging in a clinical study.[2][3] The time to peak levels of BP1.4979 is 1 hour and its elimination half-life is about 8 hours.[3] The drug is under development by Bioprojet.[1] As of January 2026, it is in phase 2 clinical trials for all indications.[1]

See also

References

  1. 1.0 1.1 1.2 1.3 "BP 14979". 16 January 2026. https://adisinsight.springer.com/drugs/800037563. 
  2. 2.0 2.1 "A Historical Perspective on the Dopamine D3 Receptor". Therapeutic Applications of Dopamine D3 Receptor Function. Current Topics in Behavioral Neurosciences. 60. Cham: Springer International Publishing. 2022. pp. 1–28. doi:10.1007/7854_2022_315. ISBN 978-3-031-23057-8. https://link.springer.com/10.1007/7854_2022_315. Retrieved 18 January 2026. 
  3. 3.0 3.1 3.2 3.3 3.4 "Occupancy of dopamine D2 and D3 receptors by a novel D3 partial agonist BP1.4979: a [11C-(+)-PHNO PET study in humans"]. Neuropsychopharmacology 44 (7): 1284–1290. June 2019. doi:10.1038/s41386-018-0285-4. PMID 30659274. "The purpose of the present study was to investigate, for the first time in healthy controls, the in vivo occupancy of the DRD3 and DRD2 by a selective DRD3 partial agonist. BP1.4979 has an affinity for the human DRD3 of ~1 nM and presents a partial agonist behaviour with an intrinsic activity of 32% ± 2.6% and EC50 of 0.7 ± 0.3 nM. In contrast, it behaves as an antagonist at the hDRD2 with Ki of 192 nM. After oral administration in humans, it reaches peak serum concentrations in one hour and has a half-life of about 8 h.".