Overview
11 DESCRIPTION ALECENSA (alectinib) is a kinase inhibitor for oral administration. The molecular formula for alectinib is C 30 H 34 N 4 O 2 ∙ HCl. The molecular weight is 482.62 g/mol (free base form) and 519.08 g/mol (hydrochloride salt). Alectinib is described chemically as 9-ethyl-6, 6-dimethyl-8-[4-(morpholin-4-yl)piperidin-1-yl]-11-oxo-6, 11-dihydro-5 H -benzo[ b ]carbazole-3-carbonitrile...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 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
- 1 INDICATIONS AND USAGE ALECENSA 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. ( 1.1 ) treatment of adult patients with ALK-positive metastatic NSCLC as detected by an FDA-approved test. ( 1.2 ) 1.1 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...
Common Doses
- 600 mg
- 450 mg
- 300 mg
Dosage
2 DOSAGE AND ADMINISTRATION 600 mg orally twice daily. Administer ALECENSA with food. ( 2.2 ) 2.1 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 [see Indications and Usage (1.1) and Clinical Studies (14.1) ]. Select patients for the treatment of metastatic NSCLC with ALECENSA based on the presence of ALK positivity in tumor tissue or plasma specimens [see Indications and Usage (1.2) and Clinical Studies (14.2) ] .
Contraindications
- 4 CONTRAINDICATIONS None. None. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the label: Hepatotoxicity [see Warnings and Precautions (5.1) ] Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.2) ] Renal Impairment [see Warnings and Precautions (5.3) ] Bradycardia [see Warnings and Precautions (5.4) ] Severe Myalgia and Creatine Phosphokinase (CPK) Elevation [see Warnings and Precautions (5.5) ] Hemolytic Anemia [see Warnings and Precautions (5.6) ] Embryo-Fetal Toxicity [see Warnings and Precautions (5.
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.