Lorlagen 100

Indications

Lorlatinib is a targeted cancer medicine used in adults with advanced or metastatic non-small cell lung cancer (NSCLC) that is ALK-positive, meaning the cancer cells have an abnormal ALK gene. It can be used as a first treatment or after other ALK inhibitors, and it is able to reach cancer that has spread to the brain.

How It Works

Lorlatinib is a third-generation ALK (and ROS1) tyrosine kinase inhibitor. It blocks the faulty ALK protein that drives the cancer to grow, including many resistant forms of ALK that no longer respond to earlier medicines. Because it crosses into the brain well, it also acts on brain metastases.

Dosage and Administration

The dose is set by your cancer specialist, as prescribed, and is usually taken once a day, at about the same time each day, with or without food. Swallow tablets whole. If you vomit after a dose, do not take another; take the next dose at the usual time. The dose may be paused or reduced if side effects occur, so do not change it yourself.

Interactions

• Strong CYP3A inducers such as Rifampicin, Carbamazepine, Phenytoin, Enzalutamide and St John's Wort: must not be used together, because of serious liver toxicity.
• Strong CYP3A inhibitors (Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, grapefruit juice): raise Lorlatinib levels; avoid or reduce the dose as advised.
• Medicines broken down by CYP3A (such as some hormonal contraceptives, Midazolam, Tacrolimus, Cyclosporine): Lorlatinib may make them less effective.
• Medicines that slow the heart or affect heart conduction: more risk of heart block.

Contraindications

• Allergy to Lorlatinib or any ingredient.
• Use with strong CYP3A inducers.

Side Effects

Very common effects include high cholesterol and triglycerides, swelling of the legs or other areas, weight gain, numbness or tingling (peripheral neuropathy), changes in thinking, memory, mood, speech or sleep, tiredness, joint or muscle pain and diarrhoea. It can also raise blood sugar and blood pressure and slow the heart.

Get urgent medical help if you have new or worsening cough, breathlessness or chest pain (possible lung inflammation), fainting, dizziness or a very slow heartbeat, sudden confusion, hallucinations, severe mood changes or thoughts of suicide, very high blood sugar with thirst and frequent urination, or signs of a severe allergic reaction.

Pregnancy and Lactation

Lorlatinib may harm an unborn baby. Women should use effective non-hormonal contraception (because Lorlatinib makes hormonal methods less reliable) during treatment and for at least 6 months after the last dose, and men with female partners should use condoms for at least 3 months after the last dose. Do not breastfeed during treatment and for 7 days after the last dose.

Precautions and Warnings

Cholesterol, triglycerides, blood sugar, blood pressure, liver tests and heart rhythm (ECG) are checked regularly, and cholesterol-lowering medicines are often needed. Tell your doctor about any heart, liver, lung or mental health problems. Family members should watch for changes in mood or behaviour. Be careful when driving if you feel confused or dizzy.

Overdose

Overdose may increase side effects such as confusion, mood changes, high lipids and slow heart rate. Contact a doctor or go to hospital at once.

Therapeutic Class

Antineoplastic, ALK and ROS1 tyrosine kinase inhibitor (targeted therapy).

Storage

Store below 30°C in a dry place, away from light and out of the reach of children. Keep in the original pack.