ALECENSA 150mg is indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC).
Alecensa 150mg belongs to second generation oral drug which selectively prohibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. It is part used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells. Prohibitions of ALK prevents phosphorylation and following downstream activation of STAT3 and AKT resulting in reduced tumour cell viability.
Mechanism of action
Alectinib belongs tyrosine kinase inhibitor whichaims ALK and RET. In nonclinical studies, Alectinibprohibits ALK phosphorylation and ALK-mediated activation of the downstream signalling proteins STAT3 and AKT, and reduced tumor cell viability in multiple cell lines harbouring ALK fusions, amplifications, or activating mutations.
Peak plasma concentration 4 hours and bioavailability of Alecensa 37%
Alectinib bound to human plasma proteins 99%
Metabolized by CYP3A4 to its major active metabolite M4, the main circulating moieties in plasma, total radioactivity 76% constituting.
In oral administration, radioactivity 98% was excreted in feces. 84% dose was excreted in the feces unchanged Alectinib.
Half-life is 33 hours
Non- Small Cell Lung Cancer :
The recommended dose is 600mg PO BID until disease progression or unacceptable Renal impairment patients dose is 450mg orally twice daily Alecensa is administrated with food
• Muscle pain
• Feeling tired
• Feeling less hungry than usual
• Dark urine
• Itchy skin
• Nausea or vomiting
• Abdominal Pain on the right side
• Bleeding or bruising more easily than normal.
• Trouble breathing
• Shortness of breath
Due to Alecensa administration, Symptomatic bradycardia may have observed; control heart rate and blood pressure regularly
Alecensa may causes Severe myalgia and elevated CPK resulted; advise patients to report any unexplained muscle pain, tenderness, or weakness;
Embryo-fetal toxicity: Based on data from animal studies and its mechanism of action, Alecensa can cause fetal harm when administered to pregnant women.
Renal impairment occurred during Alecensa treatment; incidence of Grade ≥3 renal impairment was 1.7%, of which 0.5% were fatal events.