BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability[1].
BI-1622 (0-100mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo[1].
| Animal Model: | Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)[1] |
| Dosage: | 10, 30 and 100mg/kg |
| Administration: | orally, twice daily |
| Result: | In the NCI-H2170 HER2YVMA mechanistic model, 100mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100mg/kg twice daily) resulted in tumor regressions. |
| Animal Model: | NMRI Foxn1nu mice (n=3 per group)[1] |
| Dosage: | 1 mg/kg (IV); 10 and 100 mg/kg (Orally) |
| Administration: | IV, Orally; once (Pharmacokinetic Analysis) |
| Result: | Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%. |
