TABLE 3.
PET studies reporting D2 receptor occupancy and cariprazine (CP) blood concentrations (*converted; conversion factor 2.34).
| No | Author, year | PET tracer | Design | Subjects | Mean Dose (range) [mg/day] | Mean CP conc. (range) [ng/ml] | Mean receptor Occupancy (%) | EC50 [ng/mL] (*converted; conversion factor 2.34) | EC90 (estimated from EC50) [ng/ml] (*converted; conversion factor 2.34) | Comment |
| 1 | (30) | [11C]raclopride, [11C]MNPA, [11C]WAY-100635 | Animal PET study after single doses of CP, plasma samples measured with HPLC | N = 3; healthy monkeys (macaca fascicularis) 3–4 kg weight | (a) 1–5 μg/kg (b) 30–300 μg/kg |
(a) < 1.0 (b) 3.1–34.1 |
D2/3: 5–94% (antagonist); D2/3: 45–80% (agonist); 5-HT1A: 18–30% | NA | NA | Dose dependent occupancy of 5–90% of D2/D3 receptors in striatum of monkeys |
| 2 | (13) | [11C]-(+)-PHNO | Cohort study after single doses of CP, plasma samples measured with HPLC | N = 9; SCZ; age 42 ± 8; 58.3% males | 4.5 (1–12), at day 5–15 | 12.4 ± 13.1 | D2: 0.91; D3: 0.78; (regions accounted for: c, p, vs, t, globus pallidus, substantia nigra/ventral tegmental area) | D2: 4.14 ± 0.91*; D3: 3.32 ± 0.87* | D2: 37.26*; D3: 29.88* | Near complete D2 and D3 occup. after 12 mg for 2 weeks. One patient withdrew due to emesis. PK-PD analysis reports higher EC50 values of 9.0 (D3) and 30.5 (D2). |
c, cortex; p, putamen; t, thalamus; vs, ventral striatum; NA, no information available.