Alecensa150 mg

Alecensa is a targeted anticancer medicine (ALK tyrosine kinase inhibitor) approved for:

• Metastatic ALK-positive non-small cell lung cancer (NSCLC): Treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic NSCLC, as detected by an FDA-approved test. This is an established, FDA-approved indication used as first-line therapy or after progression on/intolerance to crizotinib.
• Adjuvant treatment after tumor resection: For adult patients with ALK-positive NSCLC (tumors ≥4 cm or node-positive) following complete tumor resection, to reduce the risk of recurrence. This is an established, FDA-approved indication, typically given for up to 2 years.

Alecensa also has demonstrated CNS-penetrant activity and is used, per guideline recommendations (e.g., NCCN), for patients with brain metastases from ALK-positive NSCLC. Alecensa must only be started after confirmation of ALK-positive status by a validated diagnostic test, and treatment should be initiated and supervised by a physician experienced in the use of anticancer therapies (oncologist).

Each capsule of Alectinib contains 150 mg of Alectinib (as Alectinib hydrochloride) as the active ingredient, along with pharmaceutically acceptable excipients.

Alecensa is a highly selective, second-generation, orally administered anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) used in the treatment of ALK-positive non-small cell lung cancer (NSCLC). It was developed to overcome resistance and limited central nervous system (CNS) penetration seen with first-generation ALK inhibitors such as crizotinib. Alecensa is supplied as oral capsules and is taken twice daily with food under oncology supervision.

Alecensa belongs to the therapeutic class of Antineoplastic Agents - Targeted Therapy, specifically the subclass of ALK (Anaplastic Lymphoma Kinase) Tyrosine Kinase Inhibitors. Alecensa is classified as a second-generation ALK inhibitor.

Alectinib is a potent and highly selective inhibitor of ALK and RET tyrosine kinases. In ALK-positive NSCLC, chromosomal rearrangements produce fusion oncoproteins (e.g., EML4-ALK) that drive constitutive ALK signaling, promoting uncontrolled cell proliferation and survival. Alectinib and its major active metabolite (M4) inhibit ALK phosphorylation and downstream signaling pathways (STAT3, AKT, ERK1/2), inducing cell cycle arrest and apoptosis in ALK-dependent tumor cells.

Alectinib is not a substrate of P-glycoprotein, which contributes to its ability to cross the blood-brain barrier and achieve clinically meaningful concentrations in the central nervous system, giving it activity against brain metastases. Alectinib is metabolized primarily by CYP3A4 to its active metabolite M4.

Alecensa capsules should be taken orally with food (a meal), swallowed whole with water. They should not be opened, crushed, or chewed. Doses should be taken approximately 12 hours apart at the same times each day for consistent drug levels.

Alecensa is primarily metabolized by CYP3A4, making it susceptible to clinically significant drug interactions:

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir): may increase Alecensa plasma concentrations, increasing risk of toxicity; avoid coadministration or monitor closely.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): may reduce Alecensa plasma concentrations, potentially reducing efficacy; avoid coadministration.
• Other bradycardia-causing agents (e.g., beta-blockers, non-dihydropyridine calcium channel blockers, digoxin, clonidine): concomitant use with Alecensa may increase the risk of symptomatic bradycardia; monitor heart rate and blood pressure closely (see Precautions and Warnings).

Common side effects (occurring in ≥20% of patients) associated with Alecensa include:

• Fatigue
• Constipation
• Edema (swelling)
• Myalgia (muscle pain) and elevated creatine kinase (CPK)
• Rash
• Cough
• Elevated liver enzymes (AST, ALT, bilirubin)
• Anemia

Less common but serious adverse effects include hepatotoxicity, interstitial lung disease/pneumonitis, bradycardia, severe myalgia with CPK elevation (rhabdomyolysis), hemolytic anemia, and gastrointestinal perforation. See Precautions and Warnings for details on monitoring for these serious effects.

Alecensa can cause fetal harm based on its mechanism of action and findings in animal reproduction studies. Alecensa should be used during pregnancy only if clearly needed and the potential benefit justifies the potential risk to the fetus; a physician must be consulted before use in pregnancy. Females of reproductive potential should use effective contraception during treatment with Alecensa and for at least 5 weeks after the final dose. Male patients with female partners of reproductive potential should also use effective contraception during treatment and for 3 months after the final dose.

It is not known whether Alecensa passes into human breast milk. Because of the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with Alecensa and for at least 1 week after the final dose. Consult a physician before breastfeeding.

Alecensa requires close specialist oncology monitoring. Key precautions include:

• Hepatotoxicity: Liver function tests (AST, ALT, bilirubin) should be monitored every 2 weeks during the first 3 months of treatment with Alecensa, then periodically, with dose interruption, reduction, or discontinuation as needed.
• Interstitial lung disease (ILD)/pneumonitis: Severe, life-threatening, or fatal ILD/pneumonitis has been reported. Monitor for new or worsening respiratory symptoms (dyspnea, cough, fever); withhold Alecensa if ILD/pneumonitis is suspected and discontinue permanently if confirmed.
• Bradycardia: Monitor heart rate and blood pressure regularly, particularly when Alecensa is used with other bradycardia-causing drugs; dose adjustment or discontinuation may be required for symptomatic bradycardia.
• Severe myalgia and CPK elevation: Monitor creatine kinase levels every 2 weeks during the first month of Alecensa therapy and as clinically indicated thereafter.
• Photosensitivity: Patients taking Alecensa should avoid prolonged sun exposure and use sun protection (sunscreen, protective clothing) during treatment and for 7 days after discontinuation.
• Gastrointestinal perforation: Rare cases have been reported; monitor for symptoms of GI perforation and manage appropriately.
• Renal impairment/hemolytic anemia: Rare, sometimes serious, cases have been reported; monitor renal function and hemoglobin/hemolysis parameters as clinically indicated.
• Embryo-fetal toxicity: See Pregnancy and Lactation for contraception requirements.

Alecensa should only be prescribed by, and treatment supervised by, a physician experienced in the use of anticancer therapies, after confirmation of ALK-positive tumor status using a validated test. This is not a medication for general/self-administration or initiation outside specialist oncology care.

There is limited clinical experience with overdose of Alecensa. In case of a suspected overdose of Alecensa, seek immediate medical attention or contact a poison control center/emergency services. Management should include general supportive measures and close monitoring of vital signs and organ function (particularly liver, heart rhythm, and pulmonary status) as clinically indicated; there is no specific antidote for Alecensa overdose.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Hepatic impairment: No dose adjustment is needed for mild or moderate hepatic impairment. For severe hepatic impairment (Child-Pugh C), the recommended dose of Alecensa is reduced to 450 mg twice daily with food.

Renal impairment: No dose adjustment is required for mild to moderate renal impairment. Alecensa has not been studied in patients with severe renal impairment or end-stage renal disease; use with caution and monitor renal function.

Elderly patients: No overall differences in safety or efficacy of Alecensa have been observed between elderly and younger patients; no dose adjustment is required based on age alone, but elderly patients should be monitored closely.

Pediatric patients: Safety and efficacy of Alecensa in pediatric patients have not been established.

For metastatic ALK-positive NSCLC, treatment with Alecensa is continued as long as clinical benefit is observed, until disease progression or unacceptable toxicity occurs. For adjuvant treatment after tumor resection, Alecensa is typically given for a total duration of 2 years, or until disease recurrence or unacceptable toxicity, whichever occurs first. Duration should always be determined by the treating oncologist.

Alectinib is classified as an antineoplastic agent, specifically a second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI).

Alectinib works by selectively binding to and inhibiting the ALK tyrosine kinase enzyme, blocking abnormal ALK fusion protein signaling (such as EML4-ALK) that drives tumor cell growth in ALK-positive NSCLC. By inhibiting ALK autophosphorylation and downstream signaling pathways (STAT3, PI3K/AKT, MAPK/ERK), Alectinib induces cell cycle arrest and apoptosis in ALK-dependent cancer cells, thereby slowing or halting tumor growth. Alectinib also has activity against RET rearrangements and achieves therapeutic concentrations in the central nervous system.

The safety and effectiveness of Alecensa in pediatric patients (below 18 years) have not been established. Alecensa is not recommended for use in children and adolescents outside of a clinical trial setting.