lorlatinib at a glance
Medicine class
ALK and ROS1 tyrosine kinase inhibitor
Licensed use
Advanced ALK-positive non-small-cell lung cancer in adults
Food
May be taken with or without food; avoid grapefruit products
Tablet handling
Swallow intact; do not chew, crush, split or take a damaged tablet
What is lorlatinib used for?
Licensed uses include:
Used alone in adults with advanced ALK-positive non-small-cell lung cancer not previously treated with an ALK inhibitor.
Used alone when advanced ALK-positive non-small-cell lung cancer has progressed after treatment with an ALK inhibitor.
An appropriate validated test must confirm ALK-positive disease before treatment.
How does lorlatinib work?
Lorlatinib blocks the ATP-binding sites of ALK and ROS1 tyrosine kinases. In ALK-positive cancer, this interrupts signals that promote cancer-cell growth and survival. It was designed to enter the central nervous system and can inhibit several clinically relevant altered forms of ALK.
lorlatinib preparations and strengths
Tablet
Route: Oral
Strengths: 25 mg, 100 mg
How to take lorlatinib
Follow the oncology team's instructions and use the tablets only as supplied.
Take with or without food.
Swallow tablets whole with water.
Do not chew, crush or split them.
Do not take a tablet that is broken, cracked or otherwise damaged.
Avoid grapefruit and grapefruit juice.
lorlatinib side effects
Common or expected effects
- Raised cholesterol or triglycerides
- Swelling, particularly of the limbs
- Tingling, numbness, burning sensations or weakness
- Tiredness, weight gain or dizziness
- Joint or muscle pain
- Memory, concentration, mood or sleep changes
- Breathlessness or cough
- Diarrhoea, nausea, constipation or vomiting
- Headache, visual changes or rash
- Changes in liver or pancreatic-enzyme blood tests
Get urgent medical advice
- New or worsening cough, fever or breathlessness suggesting pneumonitis
- Seizure, hallucinations, severe confusion, suicidal thoughts or major mood or behaviour change
- Fainting, marked dizziness or symptoms of heart block
- Severe or persistent abdominal pain suggesting pancreatitis
- Severe hypertension or hyperglycaemia symptoms
- New or worsening severe visual disturbance
lorlatinib in pregnancy
Lorlatinib may harm an unborn baby and is not recommended during pregnancy. People who could become pregnant should use highly effective non-hormonal contraception during treatment and for at least 35 days afterwards because lorlatinib may make hormonal contraception less effective. Male patients should use effective contraception, including condoms, during treatment and for at least 14 weeks afterwards. Discuss pregnancy, fertility preservation or contraception with the specialist team.
lorlatinib while breastfeeding
Breastfeeding is not recommended because transfer into human milk is unknown and harm to an infant cannot be excluded. It should remain stopped during treatment and for 7 days after the final tablet; seek specialist advice before restarting.
lorlatinib interactions
The oncology and pharmacy teams should review prescription medicines, non-prescription products and herbal remedies before treatment and whenever these change.
Strong CYP3A inducers, including rifampicin, carbamazepine, phenytoin and St John's wort
These can markedly reduce lorlatinib exposure and increase liver-injury risk; combined use is contraindicated.
Strong CYP3A inhibitors, including itraconazole, voriconazole, posaconazole, ritonavir and cobicistat
These may increase lorlatinib exposure and toxicity, so alternatives are preferred and specialist management is required.
Grapefruit and grapefruit juice
These may increase lorlatinib concentrations and should be avoided.
Common questions about lorlatinib
Answers are fully visible for fast scanning and source review.
What is lorlatinib used for?
It is used alone for adults with advanced ALK-positive non-small-cell lung cancer, including disease not previously treated with an ALK inhibitor or disease that has progressed after one.
How does lorlatinib work?
It blocks ALK signalling that helps ALK-positive cancer cells grow and survive; it also inhibits ROS1 in laboratory models.
Can lorlatinib reach cancer in the brain?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.