TABLE 1.
Pharmacologic characteristics of three irreversible TKIs.
| Drug | Pyrotinib | Neratinib | Afatinib |
|---|---|---|---|
| Brand name | Irene | Nerlynx | Gilotrif |
| Targets | HER1; HER2; HER4 | HER1; HER2; HER4 | HER1, HER2, HER4 |
| IC50(nM) | 5.6; 8.1 | 92; 59; 19 | 1.6 |
| Route of administration | Oral | oral | oral |
| Recommended dose | 400 mg once daily | 240 mg once daily | 40 mg once daily |
| Metabolism | CYP3A4 | CYP3A4 | ABCB1, ABCG2 |
| Molecular formula | C32H31CIN6O3 | C30H29CIN6O3 | C24H25ClFN5O3 |
| PubChem CID | 51039030 | 9915743 | 10184653 |
| 3D-chemical structure |
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Note: HER, Human epidermal growth factor receptor; TKIs, tyrosine kinase inhibitors.