Table II.
Overview of the PET Data Sources Used in the Development of the D2 Occupancy–Pharmacokinetic Model
| Agent | Dosesa | Population | No. of PET observationsb | D2 occupancy range (%) | Data source |
|---|---|---|---|---|---|
| Asenapine | 0.1 mg | Healthy volunteers | 3 | 12–23 | (11) |
| Asenapine | 0.6 mg/day | Healthy volunteers | 24 | 0–45 | (12) |
| Asenapine | 4–9.6 mg/day | Schizophrenia patients | 18 | 9–93 | (12) |
| Haloperidol | 4–12 mg/day | Schizophrenia patients | 5 | 75–89 | (3) |
| Haloperidol | 2 mg/day | Schizophrenia patients | 6 | 53–74 | (5) |
| Haloperidol | 1–5 mg/day | Schizophrenia patients | 21 | 38–87 | (21) |
| Haloperidol | 7.5 mg | Schizophrenia patients | 4 | 83–92 | (33) |
| Olanzapine | 5–60 mg/day | Schizophrenia patients | 17 | 43–89 | (2) |
| Olanzapine | 10 mg | Healthy volunteers | 3 | 59–63 | (34) |
| Risperidone | 2–6 mg/day | Schizophrenia patients | 9 | 59–83 | (35) |
| Risperidone | 2–12 mg/day | Schizophrenia patients | 16 | 63–89 | (2) |
| Risperidone | 1 mg | Healthy volunteers | 3 | 40–55 | (36) |
| Risperidone | 3–6 mg/day | Schizophrenia patients | 15 | 53–85 | (37) |
| Ziprasidone | 40 mg | Healthy volunteers | 1 | 77 | (38) |
| Ziprasidone | 0–40 mg | Healthy volunteers | 7 | 0–79 | (39) |
PET positron emission tomography
aDose regimens labeled as “mg” refer to single-dose administrations; “mg/day” refers to multiple-dose administration prior to PET scan
bOnly PET observations with pharmacokinetic information were included in the analysis