TTT 3002 (6 mg/kg, Oral gavage, twice per day, for 2 to 4 weeks) is effective in vivo in several mouse tumor models of FLT3/ITD-associated AML (acute myeloid leukemia) with minimal toxicity[1].
TTT 3002 (6 mg/kg, Oral gavage, single) is rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay[1].
| Animal Model: | BALB/C mice (female, age 6 to 8 weeks, received Ba/F3-ITD Luc+ cells by tail vein injection on day 0)[1] |
| Dosage: | 6 mg/kg |
| Administration: | Oral gavage, twice per day, for 2 to 4 weeks |
| Result: | Showed no significant changes in animal weight and was sufficient to eliminate the presence of Ba/F3-ITD Luc+ cells by day 17 (10 days of treatment). |
| Animal Model: | Leukemic engrafted mice (female, age 6 to 8 weeks)[1] |
| Dosage: | 6 mg/kg |
| Administration: | Oral gavage, single (Pharmacokinetic Analysis) |
| Result: | After oral administration, TTT 3002 was rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay. The Cmax and area under the concentration-time curve from time 0 to infinity (AUC0→∞) were 613 nM and 3127 nM?h, respectively. The half-life, apparent volume of distribution, and apparent clearance were 3.6 hours, 21 L/kg, and 4.1 L/h per kilogram, respectively. |
