Daconib

Dacomitinib irreversibly blocks the kinase activity of the human EGFR family, which includes EGFR/HER1, HER2 and HER4. It also acts on certain EGFR activating mutations, namely the exon 19 deletion and the exon 21 L858R substitution mutation. In vitro, dacomitinib also inhibited DDR1, EPHA6, LCK, DDR2 and MNK1 at clinically relevant concentrations.

In mice carrying human tumor xenografts implanted under the skin, the tumors being driven by HER family targets (including mutated EGFR), dacomitinib reduced EGFR and HER2 autophosphorylation and slowed tumor growth, and the effect increased with the dose. It also showed antitumor activity when given orally to mice with intracranial human tumor xenografts driven by EGFR amplifications.

Dacomitinib can harm an unborn baby when a pregnant woman takes it. No one knows whether dacomitinib or its breakdown products pass into human milk, or what they might do to a breastfed infant or to milk production. Because a breastfed baby could have serious side effects from dacomitinib, women should be advised not to breastfeed while on treatment, and for at least 17 days after the last dose.

Pediatric Use: The safety and effectiveness of Dacomitinib in children have not been established.

Renal Impairment: Patients with mild or moderate renal impairment (ClCr 30 to 89 mL/min, estimated by Cockcroft-Gault) don't need any change in dose. For patients with severe renal impairment (ClCr<30 mL/min), the recommended dose of Dacomitinib has not been established.

Store Dacomitinib at a temperature no higher than 30⁰C. Keep it away from light, and keep it out of the reach of children.