Table 1.
Pharmacokinetic parameters of lenalidomide alone and in the presence of digoxin, quinidine, or temsirolimus
| Pharmacokinetic parameter | Lenalidomide (10 mg) | Lenalidomide (25 mg) | Lenalidomide (25 mg) | |||
|---|---|---|---|---|---|---|
| Alone (n = 17) | +Digoxin (n = 17) | Alone (n = 14) | +Quinidine (n = 14) | Alone (n = 17) | +Temsirolimus (n = 11) | |
| AUCt (h·ng/mL) | 396 (32.7) | 386 (38.9) | 1,288 (12.1) | 1,127 (9.6) | 1,276 (12.0) | 1,366 (14.5) |
| AUC∞ (h ng/mL) | 475 (23.2) | 491 (22.2) | 1,361 (12.7) | 1,190 (9.8) | 1,351 (11.9) | 1,445 (14.5) |
| Cmax (ng/mL) | 119 (20.2) | 118 (32.8) | 367 (26.3) | 337 (12.3) | 364 (30.0) | 361 (24.8) |
| Tmax (h) | 1 (1–2) | 1 (1–2) | 1 (0.5–3) | 1 (0.5–1.5) | 0.5 (0.5–2) | 1 (1–2) |
| t1/2 (h) | 2.40 (21.0) | 2.41 (17.0) | 2.81 (10.1) | 2.86 (12.9) | 2.81 (10.5) | 2.69 (9.1) |
| CLR (mL/min) | ND | ND | 227 (18.3) | 245 (11.3) | 251 (16.4) | 229 (15.6) |
| fe (% dose) | ND | ND | 74.2 (11.4) | 70.2 (6.6) | 81.0 (10.0) | 79.6 (8.0) |
Geometric mean (geometric CV %) data are presented for all parameters except for T max where median (range) data are presented
AUC area under the plasma concentration curve, AUC t, AUC from time zero to the last measurable concentration, AUC ∞ AUC from time zero to infinity, CL R renal clearance, C max maximum observed plasma concentration; fe, cumulative urinary excretion as a percentage of administered dose, ND not determined, t 1/2 z terminal-phase half-life, T max time to reach C max