Brigatinib is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC).
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It inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of downstream signaling proteins such as STAT3, AKT, ERK1/2, and S6 in vitro and in vivo assays.
Demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice.
Primarily metabolized by CYP2C8 and CYP3A4 in vitro. The major metabolite, AP26123, has lower potency against ALK compared to Brigatinib.
Excreted mainly through feces (65%) and urine (25%).
The recommended dosing regimen for Brigatinib is as follows:
Note: Patients should follow the dosage instructions as directed by the registered physician.
Avoid strong CYP3A inhibitors; if unavoidable, reduce the Biganib dose by approximately 50%. Strong CYP3A inducers should be avoided as they may decrease Brigatinib efficacy.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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