Table 2.
Predicted Steady-State Human IOP Response to 4 Doses of Intracameral Bimatoprost SR Implants Based on PK/PD Relationship Established in Dogs
| Implant Dose Strength (µg) | |||||
|---|---|---|---|---|---|
| 8 | 15 | 30 | 60 | ||
| Dog | Cav* (ng/mL) | 3.32 | 4.18 | 7.54 | 11.0 |
| % IOP lowering (observed) | 10 | 19 | 24 | 30 | |
| Human | Cav† (ng/mL) | 6.64 | 8.36 | 15.08 | 22.0 |
| % IOP lowering (predicted) | 29 | 31 | 33 | 33 | |
Bimatoprost SR, bimatoprost sustained-release; Cav, average concentration; IOP, intraocular pressure; PK/PD, pharmacokinetic/pharmacodynamic.
*
Average aqueous humor bimatoprost and bimatoprost acid concentration (combined) calculated based on PK data at steady state.
†
Average aqueous humor bimatoprost and bimatoprost acid concentration (combined) in humans estimated based on a 2:1 ratio of drug clearance rate assuming the same in vivo drug release rate in dogs versus humans.