Lorbrena contains the active ingredient lorlatinib, which is in an anhydrous form and acts as a kinase inhibitor. It is supplied as tablets in strengths of 25 mg and 100 mg for oral administration. Key inactive ingredients include microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate. Lorbrena is intended to function as a kinase inhibitor but further therapeutic uses are not specified in the description.

How should I use this medication?

Take this medication by mouth. Take it as directed on the prescription label at the same time every day. Do not cut, crush, or chew this medication. Swallow the tablets whole. You can take it with or without food. If it upsets your stomach, take it with food. Keep taking it unless your care team tells you to stop.

Do not take this medication with grapefruit juice.

Talk to your care team about the use of this medication in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can unless it is less than 4 hours before the next dose. If it is less than 4 hours before the next dose, skip the missed dose. Take the next dose at the normal time.

Where should I keep my medication?

Keep out of the reach of children and pets.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Get rid of any unused medication after the expiration date.

To get rid of medications that are no longer needed or have expired:

• Take the medication to a medication take-back program. Check with your pharmacy or law enforcement to find a location.
• If you cannot return the medication, check the label or package insert to see if the medication should be thrown out in the garbage or flushed down the toilet. If you are not sure, ask your care team. If it is safe to put it in the trash, take the medication out of the container. Mix the medication with cat litter, dirt, coffee grounds, or other unwanted substance. Seal the mixture in a bag or container. Put it in the trash.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

What side effects may I notice from receiving this medication?

Side effects that you should report to your care team as soon as possible:

• Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or throat
• Dry cough, shortness of breath or trouble breathing
• Heart rhythm changes—fast or irregular heartbeat, dizziness, feeling faint or lightheaded, chest pain, trouble breathing
• High blood sugar (hyperglycemia)—increased thirst or amount of urine, unusual weakness or fatigue, blurry vision
• Increase in blood pressure
• Mood and behavior changes—anxiety, nervousness, confusion, hallucinations, irritability, hostility, thoughts of suicide or self-harm, worsening mood, feelings of depression
• Pain, tingling, or numbness in the hands or feet, muscle weakness, change in vision, confusion or trouble speaking, loss of balance or coordination, trouble walking, seizures

Side effects that usually do not require medical attention (report these to your care team if they continue or are bothersome):

• Diarrhea
• Fatigue
• Joint pain
• Swelling of the ankles, hands, or feet
• Weight gain

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What should I tell my care team before I take this medication?

They need to know if you have any of these conditions:

• Diabetes
• High blood pressure
• High cholesterol
• Irregular heartbeat or rhythm
• Kidney disease
• Lung disease
• Mental health condition
• Scarring or thickening of the lungs
• Seizures
• Suicidal thoughts, plans, or attempt by you or a family member
• An unusual or allergic reaction to lorlatinib, other medications, foods, dyes, or preservatives
• Pregnant or trying to get pregnant
• Breast-feeding

What may interact with this medication?

Do not take this medication with any of the following:

• Apalutamide
• Certain medications for seizures, such as carbamazepine, phenytoin, mephobarbital, phenobarbital, primidone
• Enzalutamide
• Lumacaftor; ivacaftor
• Mitotane
• Ranolazine
• Rifampin
• Rifapentine
• St. John's wort

This medication may also interact with the following:

• Bosentan
• Certain antibiotics, such as clarithromycin or troleandomycin
• Certain antivirals for hepatitis, such as boceprevir or telaprevir
• Certain antivirals for HIV, such as cobicistat, indinavir, lopinavir, ritonavir, saquinavir, tipranavir, efavirenz, etravirine
• Certain medications for fungal infections, such as fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole
• Conivaptan
• Estrogen or progestin hormones
• Grapefruit juice
• Midazolam
• Modafinil

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medication?

Visit your care team for regular checks on your progress. It may be some time before you see the benefit from this medication.

This medication may make you feel generally unwell. This is not uncommon as chemotherapy can affect healthy cells as well as cancer cells. Report any side effects. Continue your course of treatment even though you feel ill unless your care team tells you to stop.

Talk to your care team if you wish to become pregnant or think you might be pregnant. This medication can cause serious birth defects if taken during pregnancy or for 6 months after the last dose. A negative pregnancy test is required before starting this medication. Estrogen and progestin hormones may not work as well while you are taking this medication. A barrier contraceptive, such as condom or diaphragm, is recommended. Talk to your care team about reliable forms of contraception. Do not father a child while taking this medication and for 3 months after the last dose. Use a condom when having sex during this time period.

Do not breast-feed while taking this medication and for 7 days after the last dose.

This medication may cause infertility. It is usually temporary. Talk to your care team if you are concerned about your fertility.

Avoid taking medications that contain aspirin, acetaminophen, ibuprofen, naproxen, or ketoprofen unless instructed by your care team. These medications may hide a fever.

Be careful brushing or flossing your teeth or using a toothpick because you may get an infection or bleed more easily. If you have any dental work done, tell your dentist you are receiving this medication.

This medication may increase your risk of getting an infection. Call your care team for advice if you get a fever, chills, sore throat, or other symptoms of a cold or flu. Do not treat yourself. Try to avoid being around people who are sick.

This medication can increase bad cholesterol and fats (such as LDL, triglycerides) and decrease good cholesterol (HDL) in your blood. You may need blood tests to check your cholesterol. Ask your care team what you can do to lower your risk of high cholesterol while taking this medication.

This medication may increase blood sugar. The risk may be higher in patients who already have diabetes. Ask your care team what you can do to lower your risk of diabetes while taking this medication.

This medication may cause thoughts of suicide or depression. This includes sudden changes in mood, behaviors, or thoughts. These changes can happen at any time but are more common in the beginning of treatment or after a change in dose. Call your care team right away if you experience these thoughts or worsening depression.