(lorlatinib)

Prescribing Information
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2 DOSAGE AND ADMINISTRATION

2 DOSAGE AND ADMINISTRATION

     

2.1 Patient Selection

Select patients for the treatment of metastatic NSCLC with LORBRENA based on the presence of ALK positivity in tumor specimens [see Indications and Usage (1) and Clinical Studies (14)].

Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics.

2.2 Recommended Dosage

The recommended dosage of LORBRENA is 100 mg orally once daily, with or without food, until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3)].

Swallow tablets whole. Do not chew, crush or split tablets. Do not ingest if tablets are broken, cracked, or otherwise not intact.

Take LORBRENA at the same time each day. If a dose is missed, then take the missed dose unless the next dose is due within 4 hours. Do not take 2 doses at the same time to make up for a missed dose.

Do not take an additional dose if vomiting occurs after LORBRENA but continue with the next scheduled dose.

2.3 Dosage Modifications for Adverse Reactions

The recommended dose reductions are:

•
First dose reduction: LORBRENA 75 mg orally once daily
•
Second dose reduction: LORBRENA 50 mg orally once daily

Permanently discontinue LORBRENA in patients who are unable to tolerate 50 mg orally once daily.

Dosage modifications for adverse reactions of LORBRENA are provided in Table 1.

Table 1 Recommended LORBRENA Dosage Modifications for Adverse Reactions
Adverse Reaction*Dosage Modifications
Abbreviation: AV=atrioventricular; DBP=diastolic blood pressure; SBP=systolic blood pressure.
*
Grade based on National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.03.

Central Nervous System Effects [see Warnings and Precautions (5.2)]

Grade 1

Continue at the same dose or withhold the dose until recovery to baseline. Resume LORBRENA at the same dose or at a reduced dose.

Grade 2 OR Grade 3

Withhold dose until Grade 0 or 1. Resume LORBRENA at a reduced dose.

Grade 4

Permanently discontinue LORBRENA.

Hyperlipidemia [see Warnings and Precautions (5.3)]

Grade 4 hypercholesterolemia OR
Grade 4 hypertriglyceridemia

Withhold LORBRENA until recovery of hypercholesterolemia and/or hypertriglyceridemia to less than or equal to Grade 2. Resume LORBRENA at the same dose.

If severe hypercholesterolemia and/or hypertriglyceridemia recurs, resume LORBRENA at a reduced dose.

Atrioventricular (AV) Block [see Warnings and Precautions (5.4)]

Second-degree AV block

Withhold LORBRENA until PR interval is less than 200 ms. Resume LORBRENA at a reduced dose.

First occurrence of complete AV block

Withhold LORBRENA until

•
pacemaker placed OR
•
PR interval less than 200 ms.

If a pacemaker is placed, resume LORBRENA at the same dose.

If no pacemaker is placed, resume LORBRENA at a reduced dose.

Recurrent complete AV block

Place pacemaker or permanently discontinue LORBRENA.

Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.5)]

Any Grade treatment–related ILD/Pneumonitis

Permanently discontinue LORBRENA.

Hypertension [see Warnings and Precautions (5.6)]

Grade 3 (SBP greater than or equal to 160 mmHg or DBP greater than or equal to 100 mmHg; medical intervention indicated; more than one antihypertensive drug, or more intensive therapy than previously used indicated)

Withhold LORBRENA until hypertension has recovered to Grade 1 or less (SBP less than 140 mmHg and DBP less than 90 mmHg), then resume LORBRENA at the same dose.

If Grade 3 hypertension recurs, withhold LORBRENA until recovery to Grade 1 or less, and resume at a reduced dose.

If adequate hypertension control cannot be achieved with optimal medical management, permanently discontinue LORBRENA.

Grade 4 (life-threatening consequences, urgent intervention indicated)

Withhold LORBRENA until recovery to Grade 1 or less, and resume at a reduced dose or permanently discontinue LORBRENA.

If Grade 4 hypertension recurs, permanently discontinue LORBRENA.

Hyperglycemia [see Warnings and Precautions (5.7)]

Grade 3 (greater than 250 mg/dL) despite optimal anti-hyperglycemic therapy OR Grade 4

Withhold LORBRENA until hyperglycemia is adequately controlled, then resume LORBRENA at the next lower dosage.

If adequate hyperglycemic control cannot be achieved with optimal medical management, permanently discontinue LORBRENA.

Other Adverse Reactions

Grade 1 OR Grade 2

Continue LORBRENA at same dose or reduced dose.

Grade 3 OR Grade 4

Withhold LORBRENA until symptoms resolve to less than or equal to Grade 2 or baseline. Resume LORBRENA at reduced dose.

2.4 Dosage Modifications for Drug Interactions

Strong CYP3A Inducers

LORBRENA is contraindicated in patients taking strong CYP3A inducers. Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA [see Contraindications (4), Warnings and Precautions (5.1), Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Moderate CYP3A Inducers

Avoid concomitant use of moderate CYP3A inducers with LORBRENA. If concomitant use with moderate CYP3A inducers is unavoidable, increase the LORBRENA dose to 125 mg once daily [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Strong CYP3A Inhibitors

Avoid concomitant use of LORBRENA with strong CYP3A inhibitors. If concomitant use with a strong CYP3A inhibitor is unavoidable, reduce the starting dose of LORBRENA from 100 mg orally once daily to 75 mg orally once daily.

In patients who have had a dose reduction to 75 mg orally once daily due to adverse reactions and who initiate a strong CYP3A inhibitor, reduce the LORBRENA dose to 50 mg orally once daily.

If concomitant use of a strong CYP3A inhibitor is discontinued, increase the LORBRENA dose (after 3 plasma half-lives of the strong CYP3A inhibitor) to the dose that was used before starting the strong inhibitor [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

Fluconazole

Avoid concomitant use of LORBRENA with fluconazole [see Clinical Pharmacology (12.3)]. If concomitant use is unavoidable, reduce the starting dose of LORBRENA from 100 mg orally once daily to 75 mg orally once daily [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].

2.5 Recommended Dosage for Severe Hepatic Impairment

The recommended dosage of LORBRENA for patients with severe hepatic impairment (Child-Pugh C) is 50 mg orally once daily [see Use in Specific Populations (8.6), Clinical Pharmacology (12.3)].

2.6 Recommended Dosage for Renal Impairment

The recommended dosage of LORBRENA for patients with creatinine clearance [CLcr] 15 to < 30 mL/min (estimated by Cockcroft‑Gault) is 75 mg orally once daily [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3)].

Medication Guide

MEDICATION GUIDE

PATIENT INFORMATION
LORBRENA (lor-BREN-ah)
(lorlatinib)
tablets
This Patient Information has been approved by the U.S. Food and Drug Administration.     Revised: January 2026

What is the most important information I should know about LORBRENA?

LORBRENA can cause serious side effects, including:

•
Liver problems due to interactions with other medicines. Liver problems can be severe. It is important to know what medicines not to take during treatment with LORBRENA. See “Tell your healthcare provider about all the medicines you take, including.”
•
Central nervous system (CNS) effects. CNS effects can be severe. Tell your healthcare provider if you get any new or worsening symptoms of CNS effects, including:
o
problems with thinking, such as forgetfulness or confusion
o
changes in mood, such as depression and thoughts about suicide or dying
o
psychotic effects, such as seeing or hearing things that are not real (hallucinations)
o
seizures
o
changes in speech
o
changes in sleep
•
Increases in the cholesterol and triglycerides (lipid) levels in your blood. Most people will get an increase in the lipid levels in their blood during treatment with LORBRENA.
o
If you get increases in the lipid levels in your blood, your healthcare provider may start you on a new medicine or increase your dose if you are already taking a medicine to lower the lipid levels in your blood.
o
Your healthcare provider will do blood tests to check the lipid levels in your blood before starting treatment, 1 and 2 months after starting treatment, and during treatment with LORBRENA.
•
Heart problems. LORBRENA can cause very slow or abnormal heartbeats. Your healthcare provider will check your heart rhythm (electrocardiogram or EKG) before starting and during treatment with LORBRENA. In some people, these problems are severe, and you may need to get a pacemaker. Tell your healthcare provider right away if you feel dizzy or faint or have abnormal heartbeats.
•
Lung problems. LORBRENA can cause severe or life-threatening swelling (inflammation) of the lungs during treatment that can lead to death. Symptoms may be like those from lung cancer. Tell your healthcare provider right away if you get any new or worsening symptoms of lung problems, including trouble breathing, shortness of breath, cough, or fever.
•
High blood pressure (hypertension). Your healthcare provider will check your blood pressure before starting treatment, 2 weeks after starting treatment, and then at least every month during treatment with LORBRENA. Your healthcare provider may start or change your blood pressure medicine if you get high blood pressure. Tell your healthcare provider right away if you get signs or symptoms of high blood pressure, including: headaches, dizziness, blurred vision, chest pain or shortness of breath.
•
High blood sugar (hyperglycemia). LORBRENA can cause new or worsening increases in your blood sugar levels. Your healthcare provider will do blood tests to check your blood sugar levels before starting and during treatment with LORBRENA. Your healthcare provider may start or change your blood sugar medicine if you get high blood sugar. Tell your healthcare provider right away if you get any signs and symptoms of high blood sugar, including:
o
feeling very thirsty
o
needing to urinate more than usual
o
feeling very hungry
o
feeling sick to your stomach
o
feeling weak or tired
o
feeling confused

If you get serious side effects during treatment, your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with LORBRENA.
See "What are possible side effects of LORBRENA?" for more information about side effects.

What is LORBRENA?

LORBRENA is a prescription medicine used to treat adults with non-small cell lung cancer (NSCLC):

•
that is caused by an abnormal anaplastic lymphoma kinase (ALK) gene, and
•
that has spread to other parts of your body (metastatic).

Your healthcare provider will perform a test to make sure that LORBRENA is right for you.
It is not known if LORBRENA is safe and effective in children.

Do not take LORBRENA if you take certain other medicines called strong CYP3A inducers. Ask your healthcare provider for a list of these medicines if you are not sure.

Before taking LORBRENA, tell your healthcare provider about all of your medical conditions, including if you:

•
have kidney problems
•
have liver problems
•
have had episodes of depression or seizures
•
have high levels of cholesterol or triglycerides in your blood
•
have problems with your heart beat
•
have lung or breathing problems
•
have high blood pressure
•
have diabetes or high blood sugar
•
are pregnant or plan to become pregnant. LORBRENA can harm your unborn baby.
 
Females who are able to become pregnant:
o
Your healthcare provider will do a pregnancy test before you start treatment with LORBRENA.
o
Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with LORBRENA.
o
Use effective non-hormonal birth control during treatment and for at least 6 months after the final dose of LORBRENA.
o
Birth control pills (oral contraceptives) and other hormonal forms of birth control may not be effective if used during treatment with LORBRENA. Talk to your healthcare provider about birth control choices that are right for you during this time.
 
Males with female partners who are able to become pregnant:
o
Use effective birth control during treatment and for at least 3 months after the final dose of LORBRENA.
•
are breastfeeding or plan to breastfeed. It is not known if LORBRENA passes into your breast milk. Do not breastfeed during treatment and for 7 days after the final dose of LORBRENA. Talk to your healthcare provider about the best way to feed your baby during this time.

Tell your healthcare provider about all the medicines you take, including prescription medicines, over-the-counter medicines, vitamins, and herbal supplements. Taking LORBRENA with certain other medicines may increase your risk of side effects and may affect the way LORBRENA or the other medicines work.
Know the medicines you take. Keep a list of them to show to your healthcare provider and pharmacist when you get a new medicine.

How should I take LORBRENA?

•
Take LORBRENA exactly as your healthcare provider tells you to take it. Do not change your dose or stop taking LORBRENA unless your healthcare provider tells you to.
•
Swallow LORBRENA tablets whole. Do not chew, crush, or split LORBRENA tablets. Do not take LORBRENA tablets if they are broken, cracked, or not intact.
•
Take LORBRENA 1 time a day, at the same time each day.
•
You may take LORBRENA with or without food.
•
If you miss a dose, take it as soon as you remember. However, if it is within 4 hours of the time to take your next dose, just take your next dose at your regular time. Do not take 2 doses of LORBRENA at the same time to make up for the missed dose.
•
If you vomit after taking a dose of LORBRENA, do not take an extra dose. Take your next dose at your regular time.

What are the possible side effects of LORBRENA?

•
See "What is the most important information I should know about LORBRENA?"

The most common side effects of LORBRENA include:

•
swelling in your arms, legs, hands and feet (edema)
•
numbness and tingling feeling in your joints or arms and legs (peripheral neuropathy)
•
weight gain
•
problems with thinking, such as forgetfulness or confusion
•
tiredness (fatigue)
•
difficulty breathing
•
pain in your joints
•
diarrhea
•
changes in mood, such as depression and irritability
•
increased cholesterol and triglyceride levels in the blood
•
cough

LORBRENA may cause decreased fertility in males, which may affect your ability to have children. Talk to your healthcare provider if you have concerns about fertility.

These are not all of the possible side effects of LORBRENA.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1‑800‑FDA‑1088.

How should I store LORBRENA?

•
Store LORBRENA at room temperature between 68°F to 77°F (20°C to 25°C).
•
LORBRENA comes in a bottle that contains a child resistant cap.

Keep LORBRENA and all medicines out of the reach of children.

General information about the safe and effective use of LORBRENA.

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use LORBRENA for a condition for which it was not prescribed. Do not give LORBRENA to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for more information about LORBRENA that is written for health professionals.

What are the ingredients in LORBRENA?

Active ingredient: lorlatinib

Inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate.

Film-coating contains: hydroxypropyl methylcellulose (HPMC) 2910/hypromellose, lactose monohydrate, macrogol/polyethylene glycol (PEG) 3350, triacetin, titanium dioxide, ferrosoferric oxide/black iron oxide, and iron oxide red.

For more information, go to www.Pfizer.com.

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