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Alectinib - Uses, Dosage, Side Effects, and Mechanism of Action

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Alectinib is a drug for treating non-small-cell lung cancer. Read this article to know more about the drug in detail.

Medically reviewed by

Dr. Abdul Aziz Khan

Published At May 15, 2023
Reviewed AtJuly 11, 2023

Overview

Alectinib is a drug prescribed explicitly for treating non-small-cell lung cancer, positive for anaplastic lymphoma kinase. The anaplastic lymphoma kinase enzyme is related to nervous system development and its dysregulation associated with tumors. It is a second-generation drug that inhibits the ALK (anaplastic lymphoma kinase) tyrosine kinase enzyme. The enzyme inhibition prevents the activation of the tumor cells and reduces their viability. The Food and Drug Administration (FDA) approved it in 2015 for treating non-small-cell lung cancer patients who cannot tolerate Crizotinib.

How Does Alectinib Work?

Alectinib works by blocking the proteins signaling the cancer cells to replicate. This slows down the multiplication and distribution of the cancer cells.

Uses:

Alectinib treats non-small-cell lung cancer, positive for anaplastic lymphoma kinase. It is prescribed for patients who are intolerant to Crizotinib.

Dosage:

  • The recommended dose of Alectinib is 600 mg.

  • It can be taken orally and twice daily.

  • Dose reduction based on disease progression is made. The first dose reduction is 450 mg twice daily, and the second is 300 mg twice daily.

  • The drug is discontinued if the patient cannot tolerate 300 mg of Alectinib.

Warnings:

  • Hepatotoxicity.

  • Pneumonitis.

  • Renal impairment.

  • Bradycardia.

  • Myalgia and creatine phosphokinase elevation.

  • Embryo-fetal toxicity.

For Patients

What Is Non-small-Cell Lung Cancer?

Lung cancer is classified into small-cell and non-small-cell lung cancer. Non-small-cell lung cancer is a common type, and it progresses slowly. Therefore, it is usually identified later after spreading to other body parts. The types of non-small-cell lung cancer are adenocarcinoma, undifferentiated carcinoma, and squamous cell carcinoma. The most common symptoms include chest pain, difficulty breathing, wheezing, coughing up blood, hoarseness of voice, weight loss, loss of appetite, and swelling in the face or neck.

Learn More About Alectinib-

When and How Often to Take Alectinib?

  • Take Alectinib twice daily with food.

  • A person taking Alectinib can have sunburns when exposed to sunlight. Hence they are recommended to apply sunscreen or avoid going out during the treatment.

How Effective Is Alectinib?

Clinical studies have shown that Alectinib is effective against non-small-cell lung cancer and can increase survival within 35 months.

Things to Inform the Doctor Before They Prescribe Alectinib-

The doctor must be informed about the following history before prescribing Alectinib.

  • Liver problems.

  • Respiratory issues.

  • Pregnancy.

  • Breastfeeding.

  • Medications and supplements.

Starting Alectinib-

How to Take Alectinib?

  • Take Alectinib as prescribed by the physician.

  • Swallow the whole capsule.

  • Take the drug twice daily with food.

  • Do not take another dose of Alectinib if one vomits after taking the drug. Take the next dose regularly.

  • Do not stop or overdose on the drug without a physician’s consent.

Things to Do After Taking Alectinib-

Look Out for Side Effects:

An individual must report common side effects to the doctor if they persist for a long time are:

  • Headache.

  • Weight gain.

  • Rash.

  • Diarrhea.

  • Constipation.

  • Swelling in the hands, face, and eyelids.

The side effects individuals must report immediately to the doctor are

  • Shortness of breath.

  • Chest pain.

  • Fever.

  • Vision problems.

  • Muscle pain.

  • Weakness.

  • Back pain.

  • Itchy skin.

  • Loss of appetite.

  • Change in urine color.

  • Yellowing of the skin.

  • Vomiting.

  • Bleeding more easily.

Dietary Alterations-

Intake of grapefruit juice with Alectinib can disrupt the metabolism and increase the serum concentration of the drug. In contrast, St. John’s wort (a herb) can reduce the serum concentration of the drug. Therefore, avoid taking grapefruit juice and St. John’s wort with Alectinib.

What Should Be Done When a Dose Is Missed?

Overdose of Alectinib must be avoided when a dose is missed. Instead, take the next dose according to the schedule.

What Should Be Done to Treat Alectinib Overdose?

No reported cases of Alectinib overdose have been identified yet. Hence no antidote was identified. If an individual experiences symptoms of difficulty breathing, seizures, or being unresponsive, immediately call the physician for further management.

How to Store Alectinib?

Store Alectinib capsules in the original container and at room temperature below 30 degrees Celsius. Keep the container away from light and out of the reach of pets and children.

How to Dispose of Alectinib?

Unused or expired medicines must be disposed of in a special way such that it is away from pets and children. For example, the drug should not be flushed in the toilet. Instead, a local recycling or garbage department has to be contacted to dispose of the drug.

Avoid Self-Medication

Avoid taking the drug for a condition not prescribed. In addition, do not recommend the medication to a person with similar symptoms.

Staying On Alectinib-

Tips to Stay On Track:

Take the drug as per the physician’s advice and take the drug at a fixed time to avoid missing the dose. In addition, schedule regular appointments with the physician to monitor the disease's progress.

For Doctors

Indication:

Alectinib is an inhibitor of ALK (anaplastic lymphoma kinase) enzyme and treats metastatic non-small-cell lung cancer, positive for anaplastic lymphoma kinase. It is prescribed for patients who are intolerant to Crizotinib.

Pharmacology-

Mechanism of Action: Alectinib is prescribed for treating non-small-cell lung cancer, expressing an ALK-EML4 (anaplastic lymphoma kinase - echinoderm microtubule-associated protein-like 4) protein that proliferates the cancer cells. This is because it inhibits the activity of the ALK enzyme and reduces tumor cell viability. The drug and its active metabolite M4 have a similar mechanism of action.

Pharmacodynamics-

Cardiac Electrophysiology: A clinical study to assess the ability of Alectinib to prolong the QT interval (electrical activity of the heart) showed that the drug did not significantly prolong the QT interval.

Chemical Taxonomy:

Chemical Taxonomy

Ingredients-

Active Ingredient: Alectinib.

Inactive Ingredients: The inactive ingredients include lactose monohydrate, sodium lauryl sulfate, magnesium stearate, hydroxypropyl cellulose, and carboxymethyl cellulose calcium. The capsule coating contains potassium chloride, hypromellose, carrageenan, corn starch, carnauba wax, and carrageenan. The ink printed on the capsule contains yellow iron oxide, red iron oxide, carnauba wax, aluminum lake, glyceryl monooleate, and white shellac.

Absorption: Alectinib, when administered 600 mg twice daily, can reach maximum concentration at four hours. The bioavailability of the drug is 37 % in a fed state.

Distribution: The volume of distribution is 4016 liters, and 99 % of the drug metabolites bind to human plasma proteins.

Metabolism: Cytochrome-P3A4 can metabolize Alectinib to its active metabolite M4, which can further metabolize by the same enzyme.

Elimination: On administration of radioactively labeled Alectinib, 98 % was found in feces, in which 6 % were identified as M4 (the active metabolite), and 84 % remained unchanged. In addition, 0.5 % was found in urine. Furthermore, the half-life of the drug is 33 hours, and its active metabolite is 31 hours.

Toxicity:

  • The carcinogenic potential of Alectinib has not yet been studied.

  • General toxicology studies showed no adverse effects of Alectinib on male and female reproductive organs.

  • No studies have been conducted to assess the effects of Alectinib on fertility in humans. However, the studies on rats indicate embryo-fetal toxicity.

Warning and Precaution-

  • Hepatotoxicity: Alectinib is discontinued, withheld, or reduced if the bilirubin, alanine transaminase, and aspartate transaminase levels are high. Hence liver tests must be conducted every two weeks during the treatment course, especially during the first three months.

  • Pneumonitis: Alectinib is withheld in pneumonitis patients and is permanently discontinued in patients with pneumonitis where no other cause is identified other than the drug’s effects. Hence the patients must be monitored for symptoms of pneumonitis like cough, dyspnea, and fever.

  • Renal Impairment: Patients with renal impairment can reduce the dose or permanently discontinue the drug.

  • Bradycardia: Alectinib can be reduced or permanently discontinued in patients with bradycardia. Therefore, monitor the blood pressure regularly.

  • Myalgia and Creatine Phosphokinase Elevation: The creatinine phosphokinase levels should be monitored every two weeks during the treatment course, especially for patients with muscle tenderness, pain, and weakness. The drug can be discontinued, reduced, or withheld in elevated conditions.

  • Embryo-Fetal Toxicity: Alectinib is expected to affect the fetus. Hence women should be advised to use contraceptives.

Dosage and Administration-

  • Alectinib are available in capsule form.

  • The recommended dosage is 600 mg twice daily.

  • The dose can be reduced to 450 mg and 300 mg based on disease progression or adverse effects.

  • Patients who are intolerant to 300 mg of Alectinib must not be allowed to continue the drug.

Contraindications-

Alectinib is contraindicated in the following conditions.

  • Pregnancy.

  • Breastfeeding.

  • Hemolytic anemia.

  • Acute kidney failure.

  • Abnormal liver function tests.

  • Muscle pain.

  • Respiratory disorders.

Clinical Studies for Alectinib:

1) A clinical study was conducted comparing the efficacy of Alectinib and Crizotinib for treating metastatic, advanced non-small-cell lung cancer, positive for anaplastic lymphoma kinase protein. It was started in 2014 and is still in progress, and is expected to end in 2026.

Dosage of the Drugs: Alectinib 600 mg and Crizotinib 250 mg twice daily were administered.

The drugs were administered until they noticed disease progress, intolerable side effects, or even death.

Until now, a few side effects are evident from both drugs. Accordingly, the drug is stopped or reduced.

2) A clinical study was conducted to study the efficacy of Alectinib in patients with non-small-cell lung cancer who have not yet received systemic therapy for metastatic disease. Neurologically stable patients with brain metastasis were selected for the study. However, patients who had neurological symptoms were also included after brain radiation therapy.

The efficacy of Alectinib was established by comparing it with Crizotinib in progressing the survival rate. Although certain patients experienced adverse events, a great response was observed with Alectinib than with Crizotinib.

Drug Interactions:

  • No significant effects were observed when Alectinib was administered with Posaconazole, Esomeprazole, and Rifampin.

  • No clinical effects were observed when administering Alectinib followed by Repaglinide or Midazolam.

  • The coadministration of Acalabrutinib and Alectinib can decrease the metabolism of Alectinib. In contrast, the coadministration of Alectinib and Acetaminophen can increase the metabolism of Alectinib.

  • Abalaparatide can decrease the therapeutic efficacy of Alectinib.

Other Specifications-

Alectinib in Pregnant Women: The use of Alectinib in pregnant humans is not yet established. But animal studies indicate that Alectinib can cause fetal harm. Therefore, to be cautious, Alectinib is not administered to pregnant women.

Alectinib in Lactating Women: No significant data on the presence of Alectinib in breast milk has been identified. But significant adverse effects in lactating women have been reported. Therefore, lactating women must not take Alectinib while breastfeeding or must not breastfeed one week after the dose.

Alectinib in Pediatric Patients: The effectiveness and safety of Alectinib for pediatric populations have not yet been reported.

Alectinib in Geriatric Patients: No significant data for the difference in effects of Alectinib among geriatric populations has been reported yet.

Alectinib in Renal Impairment Patients: No dose adjustment is recommended for mild to moderate renal impairment patients. However, the effect of Alectinib in severe renal impairment patients has not yet been established.

Alectinib in Hepatic Impairment Patients: No dose adjustment is recommended for mild to moderate hepatic impairment. However, the dose is reduced to 450 mg twice daily for patients with severe hepatic impairment because of their increased exposure to Alectinib.

Dr. Abdul Aziz Khan
Dr. Abdul Aziz Khan

Medical oncology

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