Alectinib

What it is and how it works

Mechanism of Action Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity. Alectinib and M4 demonstrated in vitro and in vivo activity against multiple mutant forms of the ALK enzyme, including some mutations identified in NSCLC tumors in patients who have progressed on crizotinib.

Indications

is a kinase inhibitor indicated for: adjuvant treatment in adult patients following tumor resection of anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) (tumors ≥ 4 cm or node positive) as detected by an FDA-approved test. treatment of adult patients with ALK-positive metastatic NSCLC as detected by an FDA-approved test. Adjuvant Treatment of Resected ALK-Positive Non-Small Cell Lung Cancer (NSCLC) ALECENSA is indicated as adjuvant treatment in adult patients following tumor resection of anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) (tumors ≥ 4 cm or node positive), as detected by an FDA-approved test . Treatment of Metastatic ALK-Positive NSCLC ALECENSA is indicated for the treatment of adult patients with ALK-positive metastatic NSCLC as detected by an FDA-approved test .

Dosage and administration (summary)

600 mg orally twice daily. Administer ALECENSA with food. Patient Selection Select patients with resectable tumors for the adjuvant treatment of NSCLC with ALECENSA based on the presence of ALK positivity in tumor tissue . Select patients for the treatment of metastatic NSCLC with ALECENSA based on the presence of ALK positivity in tumor tissue or plasma specimens . If ALK rearrangements are not detected in a plasma specimen, test tumor tissue if feasible. Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics. Dosing and Administration The recommended dosage information for ALECENSA is provided in Table 1 .

Contraindications

None. None.

Warnings and precautions

Hepatotoxicity: Monitor liver laboratory tests every 2 weeks during the first 3 months of treatment, then once a month and as clinically indicated, with more frequent testing in patients who develop transaminase and bilirubin elevations. In case of severe ALT, AST, or bilirubin elevations, withhold, then reduce dose, or permanently discontinue ALECENSA. ( 2.4 , 5.1 ) Interstitial Lung Disease (ILD)/Pneumonitis: Immediately withhold ALECENSA in patients diagnosed with ILD/pneumonitis and permanently discontinue if no other potential causes of ILD/pneumonitis have been identified.

Pregnancy

Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, ALECENSA can cause fetal harm when administered to a pregnant woman . There are no available data on ALECENSA use in pregnant women.

Storage and supply

Storage and stability: Do not store above 30°C (86°F). Store in the original container to protect from light and moisture.

Source: Alectinib Hydrochloride (Alecensa) — US FDA prescribing information, 2026-08-21, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.