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PK optimization of QD394. Microsomal stability, plasma stability, and PK studies were performed to evaluate the PK profiles of QD394 and its analog QD394-Me. Key parameters for each experiment are listed.
| Compound | Microsomal stability T1/2 (min) | Plasma stability T1/2 (min) | Concentration at 7 h in mouse plasma (ng/mL) | |||
|---|---|---|---|---|---|---|
| mouse | mouse | human | IP (n=2) | PO (n=2) | IV (n=3) | |
| QD394 | > 60 | 6 | NA | 5.0, 4.5 | 23.3, 25.8 | 2 out of 3 mice died |
| QD394-Me | 44.6 | > 120 | > 120 | 6.7, 1.1 | 4.2, 3.4 | 3.4 ± 1.2 |
