Lorbrena (Lorlatinib)
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Fact Table
| Fact Table | |
|---|---|
| Formula | C21H19FN6O2 |
| License | FDA approved (first U.S. approval: November 2, 2018; regular approval expanded in 2021) |
| Bioavailability | Mean absolute bioavailability 81% |
| Legal status | Prescription only (Rx) |
| Chemical Name | (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile |
| Elimination half-life | Approximately 24 hours |
| Dosage (Strength) | 25 mg and 100 mg oral tablets; usual dosage 100 mg orally once daily |
| Pregnancy | Can cause embryo-fetal harm; avoid use in pregnancy and verify pregnancy status before starting therapy |
| Brands | Lorbrena |
| Protein binding | 66% |
| PubChem CID | 71731823 |
| MedlinePlus | a619005 |
| ChEBI | 143117 |
| ATC code | L01ED05 |
| DrugBank | DB12130 |
| KEGG | D11012 |
| Routes of administration | By mouth (oral tablets) |
Lorbrena (lorlatinib) is a kinase inhibitor used to treat ALK-positive metastatic non-small cell lung cancer. It works by blocking abnormal proteins that cause cancer cells to grow and spread throughout the body. The medication is taken orally in tablet form.
Directions
Lorbrena is taken by mouth as a tablet once daily, with or without food. The recommended starting dose is typically 100 mg. The dosage may be reduced to 50 mg once daily in people with severe liver problems or 75 mg once daily in people with kidney problems.
The medication is taken until the cancer progresses or side effects become unmanageable. If certain side effects occur, healthcare providers may temporarily pause treatment, reduce the dosage, or discontinue the medication entirely.
It's important not to skip doses or stop taking Lorbrena without consulting a doctor. If a dose is missed and it's more than 4 hours until the next scheduled dose, take the missed dose immediately. However, if the next dose is less than 4 hours away, skip the missed dose and resume the regular schedule. Never take two doses at the same time to make up for a missed one.
Ingredients
The active ingredient in Lorbrena is lorlatinib.
Cautions
Before using this medication, you may want to consult a healthcare provider about the following:
- Any existing health conditions
- Any allergies
- A list of all medications currently being taken
Lorbrena should not be taken with strong CYP3A inducers (such as rifampin) because this combination can cause severe liver injury. Your healthcare provider will review your medications before starting treatment.
Changes in thinking, mood, or behavior may occur. Some people taking Lorbrena experience effects on the brain and nervous system, including memory problems, mood changes, speech issues, sleep disturbances, or seizures.
Cholesterol and triglycerides may increase. Lorbrena can increase blood cholesterol and triglyceride levels, sometimes within a few weeks of starting treatment. Your healthcare provider may check your lipid levels and prescribe medication to control them.
Heart rhythm changes are possible. The medication can affect electrical signals in the heart and may cause a condition called atrioventricular (AV) block. Your healthcare provider may monitor your heart rhythm with an ECG during treatment.
Serious lung inflammation can occur. Rarely, Lorbrena may cause interstitial lung disease or pneumonitis. Contact your healthcare provider if you develop new or worsening cough, shortness of breath, or fever.
Some people develop high blood pressure while taking Lorbrena. Blood pressure should be monitored regularly during treatment.
Lorbrena can cause high blood sugar (hyperglycemia), so your healthcare provider may monitor your glucose levels during treatment.
Lorbrena may harm an unborn baby. Women who can become pregnant should use effective non-hormonal birth control during treatment and for several months afterward.
Contraindications
Avoid taking or using this medication if any of the following apply:
- Currently taking strong CYP3A inducers such as rifampin, carbamazepine, phenytoin, or St. John's wort
- Unable to stop strong CYP3A inducers for the required period before treatment begins
- Known hypersensitivity to lorlatinib or any other ingredients in the formulation
Side Effects
Common side effects of Lorbrena include:
- Swelling in the arms, legs, hands, or feet
- Tiredness or fatigue
- Diarrhea
- Joint or leg pain
Some people may also experience numbness or tingling in the arms or legs, cough, weight gain, or difficulty breathing. Changes in mood, such as irritability or depression, and problems with thinking or memory may also occur. Blood tests may show increased cholesterol or triglyceride levels during treatment.
More serious side effects are less common but possible. Lorbrena can cause central nervous system effects such as confusion, hallucinations, seizures, or severe mood changes. It may also lead to heart rhythm problems, lung inflammation, high blood pressure, high blood sugar, or liver problems related to drug interactions. Contact a healthcare provider immediately if you develop trouble breathing, chest pain, severe dizziness, confusion, or signs of high blood sugar.
Frequently Asked Questions about Lorbrena (Lorlatinib)
What is Lorbrena (lorlatinib) used for?
Lorbrena is a prescription cancer medicine used to treat adults with metastatic non-small cell lung cancer whose tumor is ALK-positive. Patients are usually tested first to confirm that the cancer has the ALK abnormality.
How does Lorbrena work?
Lorlatinib is a kinase inhibitor. It blocks abnormal ALK signaling that helps cancer cells grow and spread, which can slow or stop tumor growth.
How is Lorbrena usually taken?
The usual dose is 100 mg by mouth once daily, with or without food. Tablets should be swallowed whole and not chewed, crushed, or split.
What are the common side effects of Lorbrena?
Important and fairly common side effects include high cholesterol, high triglycerides, central nervous system effects such as changes in thinking, mood, speech, sleep, or behavior, swelling, weight gain, high blood pressure, and high blood sugar. Some people also develop fatigue or nerve-related symptoms.
Why are cholesterol and triglycerides monitored so closely with Lorbrena?
Lorlatinib commonly raises blood cholesterol and triglyceride levels, often early in treatment. The label recommends checking these before starting treatment, again at 1 and 2 months, and periodically after that, because many patients need lipid-lowering medicine while taking Lorbrena.
Can Lorbrena affect the brain or mood?
Yes. Lorbrena can cause central nervous system effects, including changes in memory, concentration, mood, speech, mental status, sleep, and in some cases seizures or psychotic effects. These symptoms should be reported promptly because the dose may need to be held, reduced, or stopped depending on severity.
Are there important heart or lung warnings with Lorbrena?
Yes. Lorlatinib can cause PR prolongation and atrioventricular block, so ECG monitoring is recommended before treatment and periodically during therapy. It can also rarely cause interstitial lung disease or pneumonitis, which can show up as new or worsening cough, shortness of breath, or fever.
Are there important drug interactions with Lorbrena?
Yes. Lorbrena should not be taken with strong CYP3A inducers because of the risk of serious liver toxicity, and other CYP3A interactions can also require dose changes or avoidance. The current label also specifically advises avoiding fluconazole if possible, or reducing the lorlatinib dose if the combination cannot be avoided.
What should patients know about pregnancy and birth control while taking Lorbrena?
Lorbrena can harm an unborn baby. It can also make hormonal birth control less effective, so females who can become pregnant are advised to use effective non-hormonal contraception during treatment and for 6 months after the last dose, and males with partners of reproductive potential should use effective contraception during treatment and for 3 months after the last dose.
Who should use Lorbrena especially carefully?
Extra caution is needed in people with a history of depression, seizures, heart rhythm or conduction problems, lung disease, high cholesterol or triglycerides, diabetes, high blood pressure, liver problems, or kidney problems. These issues do not always prevent treatment, but they often require closer monitoring during therapy.
