Falnidamol is a novel ErbB receptor kinase inhibitor that is more potent at inhibiting signaling induced by TGF-α than that induced by neuregulin1-β1 or anti-ErbB2 agonist antibodies.
BIBX 1382 Dihydrochloride, is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM).
ChEBI: N4-(3-chloro-4-fluorophenyl)-N6-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-4,6-diamine is a substituted aniline.
Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC 50 = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC 50 = 3.4 μ M) and a range of other related tyrosine kinases (IC 50 > 10 μ M). Oral administration inhibits growth of established human xenografts in athymic mice.
Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment[2].
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice[2].
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM[2].
| Animal Model: | Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2] |
| Dosage: | 10 mg/kg |
| Administration: | p.o.; daily; 16 days |
| Result: | Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
|
| Animal Model: | Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells[2] |
| Dosage: | 10 mg/kg (Pharmacokinetic Analysis) |
| Administration: | p.o.; daily; 16 days |
| Result: | The C4h is 2222 nM and the C24h is 244 nM.
|
EGFR: 3 nM (IC50); ErbB2: 3.4 μM (IC50)
1. f. f. solca, a. baum, e. langkopf, g. dahmann, k. h. heider, f. himmelsbach and j. c. van meel, j pharmacol exp ther 2004, 311, 502-509.
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