| Clinical data | |
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| Other names | BP-1.4979; BP14979; BP-14979 |
| Routes of administration | Oral |
| Drug class | Dopamine D3 receptor agonist |
| Pharmacokinetic data | |
| Onset of action | 1 hour (Tmax) |
| Elimination half-life | 8 hours |
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| CAS Number | |
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| Chemical and physical data | |
| Formula | C23H34N4O2 |
| Molar mass | 398.551 g·mol−1 |
| 3D model (JSmol) | |
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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. It is taken orally. The drug acts as a highly potent weak partial agonist of the dopamine D3 receptor (Ki = ~1 nM; EC50 = 0.7 nM; Emax = 32%). 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. BP1.4979 showed 66% dopamine D3 receptor occupancy and 8% dopamine D2 receptor occupancy with positron emission tomography (PET) imaging in a clinical study. The time to peak levels of BP1.4979 is 1 hour and its elimination half-life is about 8 hours. The drug is under development by Bioprojet. As of January 2026, it is in phase 2 clinical trials for all indications.
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.