Summary of PK Parameters of BIM23B065 and BIM23B133 During the Last Day of Dosing for the MAD Cohorts
| Parameter . | BIM23B065 . | BIM23B133 . | |||||
|---|---|---|---|---|---|---|---|
| 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | ||
| Cmax, ng/mL | Post morning dose | 11.6 (14.9) | 7.8 (23.9) | 8.1 (32.2) | 3.5 (36.8) | 4.6 (32.3) | 3.5 (8.6) |
| Post evening dose at 8 h | — | 7.9 (39.6) | 10.8 (12.3) | — | 5.0 (11.8) | 5.9 (26.5) | |
| tmax, ha | Post morning dose | 0.51 (0.50, 0.55) | 0.50 (0.50, 0.50) | 0.50 (0.50, 0.52) | 3.01 (2.00, 4.02) | 2.00 (0.97, 6.00) | 4.00 (4.00, 6.00) |
| Post evening dose at 8 h | — | 8.50 (8.50, 8.50) | 8.50 (8.50, 8.50) | — | 12.0 (10.0, 12.0) | 12.0 (12.0, 12.0) | |
| AUC0-t, h·ng/mL | 30.1 (16.7) | 25.9 (29.1) | 41.2 (3.8) | 66.0 (20.3) | 118 (20.2) | 121 (6.0) | |
| AUC0-∞, h·ng/mL | 31.1 (16.9) | 26.2 (28.6) | 42.3 (4.3) | 79.5 (19.5) | 140 (22.6) | 146 (17.3) | |
| t1/2, h | 13.4 (70.9) | 4.69 (68.0) | 12.4 (142) | 29.1 (38.7) | 31.9 (38.9) | 28.8 (41.8) | |
| Parameter . | BIM23B065 . | BIM23B133 . | |||||
|---|---|---|---|---|---|---|---|
| 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | ||
| Cmax, ng/mL | Post morning dose | 11.6 (14.9) | 7.8 (23.9) | 8.1 (32.2) | 3.5 (36.8) | 4.6 (32.3) | 3.5 (8.6) |
| Post evening dose at 8 h | — | 7.9 (39.6) | 10.8 (12.3) | — | 5.0 (11.8) | 5.9 (26.5) | |
| tmax, ha | Post morning dose | 0.51 (0.50, 0.55) | 0.50 (0.50, 0.50) | 0.50 (0.50, 0.52) | 3.01 (2.00, 4.02) | 2.00 (0.97, 6.00) | 4.00 (4.00, 6.00) |
| Post evening dose at 8 h | — | 8.50 (8.50, 8.50) | 8.50 (8.50, 8.50) | — | 12.0 (10.0, 12.0) | 12.0 (12.0, 12.0) | |
| AUC0-t, h·ng/mL | 30.1 (16.7) | 25.9 (29.1) | 41.2 (3.8) | 66.0 (20.3) | 118 (20.2) | 121 (6.0) | |
| AUC0-∞, h·ng/mL | 31.1 (16.9) | 26.2 (28.6) | 42.3 (4.3) | 79.5 (19.5) | 140 (22.6) | 146 (17.3) | |
| t1/2, h | 13.4 (70.9) | 4.69 (68.0) | 12.4 (142) | 29.1 (38.7) | 31.9 (38.9) | 28.8 (41.8) | |
Data are presented as the geometric means (% coefficient of variation).
Abbreviations: AUC0-∞, area under the plasma concentration-time curve from time 0 to infinity; AUC0-t, area under the plasma concentration-time curve from 0 hours to last measurable concentration; b.i.d., twice-daily dosing; q.d., once-daily dosing.
Median (minimum, maximum) presented for tmax.
Summary of PK Parameters of BIM23B065 and BIM23B133 During the Last Day of Dosing for the MAD Cohorts
| Parameter . | BIM23B065 . | BIM23B133 . | |||||
|---|---|---|---|---|---|---|---|
| 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | ||
| Cmax, ng/mL | Post morning dose | 11.6 (14.9) | 7.8 (23.9) | 8.1 (32.2) | 3.5 (36.8) | 4.6 (32.3) | 3.5 (8.6) |
| Post evening dose at 8 h | — | 7.9 (39.6) | 10.8 (12.3) | — | 5.0 (11.8) | 5.9 (26.5) | |
| tmax, ha | Post morning dose | 0.51 (0.50, 0.55) | 0.50 (0.50, 0.50) | 0.50 (0.50, 0.52) | 3.01 (2.00, 4.02) | 2.00 (0.97, 6.00) | 4.00 (4.00, 6.00) |
| Post evening dose at 8 h | — | 8.50 (8.50, 8.50) | 8.50 (8.50, 8.50) | — | 12.0 (10.0, 12.0) | 12.0 (12.0, 12.0) | |
| AUC0-t, h·ng/mL | 30.1 (16.7) | 25.9 (29.1) | 41.2 (3.8) | 66.0 (20.3) | 118 (20.2) | 121 (6.0) | |
| AUC0-∞, h·ng/mL | 31.1 (16.9) | 26.2 (28.6) | 42.3 (4.3) | 79.5 (19.5) | 140 (22.6) | 146 (17.3) | |
| t1/2, h | 13.4 (70.9) | 4.69 (68.0) | 12.4 (142) | 29.1 (38.7) | 31.9 (38.9) | 28.8 (41.8) | |
| Parameter . | BIM23B065 . | BIM23B133 . | |||||
|---|---|---|---|---|---|---|---|
| 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | 1.2 mg q.d. (n = 6) . | 0.8 mg b.i.d. (n = 6) . | 1.0 mg b.i.d. (n = 3) . | ||
| Cmax, ng/mL | Post morning dose | 11.6 (14.9) | 7.8 (23.9) | 8.1 (32.2) | 3.5 (36.8) | 4.6 (32.3) | 3.5 (8.6) |
| Post evening dose at 8 h | — | 7.9 (39.6) | 10.8 (12.3) | — | 5.0 (11.8) | 5.9 (26.5) | |
| tmax, ha | Post morning dose | 0.51 (0.50, 0.55) | 0.50 (0.50, 0.50) | 0.50 (0.50, 0.52) | 3.01 (2.00, 4.02) | 2.00 (0.97, 6.00) | 4.00 (4.00, 6.00) |
| Post evening dose at 8 h | — | 8.50 (8.50, 8.50) | 8.50 (8.50, 8.50) | — | 12.0 (10.0, 12.0) | 12.0 (12.0, 12.0) | |
| AUC0-t, h·ng/mL | 30.1 (16.7) | 25.9 (29.1) | 41.2 (3.8) | 66.0 (20.3) | 118 (20.2) | 121 (6.0) | |
| AUC0-∞, h·ng/mL | 31.1 (16.9) | 26.2 (28.6) | 42.3 (4.3) | 79.5 (19.5) | 140 (22.6) | 146 (17.3) | |
| t1/2, h | 13.4 (70.9) | 4.69 (68.0) | 12.4 (142) | 29.1 (38.7) | 31.9 (38.9) | 28.8 (41.8) | |
Data are presented as the geometric means (% coefficient of variation).
Abbreviations: AUC0-∞, area under the plasma concentration-time curve from time 0 to infinity; AUC0-t, area under the plasma concentration-time curve from 0 hours to last measurable concentration; b.i.d., twice-daily dosing; q.d., once-daily dosing.
Median (minimum, maximum) presented for tmax.
This PDF is available to Subscribers Only
View Article Abstract & Purchase OptionsFor full access to this pdf, sign in to an existing account, or purchase an annual subscription.
