Dalmelitinib (Compound 4 d, intragastric administration, 10-60 mg/kg) significantly inhibits the tumor growth in a dose-dependent manner in MKN-45 tumor xenograft nude mice[1].
Dalmelitinib (intragastric administration, 5 mg/kg for a single dose) shows a high plasma concentration, longer half-life and mean residence time, low clearance rates in BALB/c small nude mice[1].
Dalmelitinib shows a high level of No Observed Adverse Effect Level (NOAEL) in mice long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day)[1].
| Animal Model: | MKN-45 tumor xenograft nude mice[1] |
| Dosage: | 10, 30, 60 mg/kg |
| Administration: | Intragastric administration |
| Result: | Inhibited the tumor growth with the inhibitory rates of 29.5% (10 mg/kg), 34.2% (30 mg/kg), and 61.4% (60 mg/kg).
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| Animal Model: | BALB/c small nude mice (pharmacokinetic assay)[1] |
| Dosage: | 5 mg/kg for a single dose |
| Administration: | Intragastric administration |
| Result: | Pharmacokinetic profile of Dalmelitinib (Compound 4 d)
| Compound | Cmax (ng/mL) | AUC (ng/mL/h) | t1/2 (h) | MRT (h) | CL/F (mL/min/kg) | Vz/F | | Dalmelitinib | 8628 | 122487 | 5.55 | 9.10 | 0.68 | 327 |
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