(lorlatinib)

Prescribing Information
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8 USE IN SPECIFIC POPULATIONS

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Risk Summary

Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1)], LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of 100 mg once daily based on AUC (see Data). Advise a pregnant woman of the potential risk to a fetus.

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively.

Data

Animal Data

Preliminary embryo-fetal development studies investigating the administration of lorlatinib during the period of organogenesis were conducted in rats and rabbits. In rabbits, lorlatinib administration resulted in abortion and total loss of pregnancy at doses of 15 mg/kg (approximately 3 times the human exposure at the recommended dose of 100 mg) or greater. At a dose of 4 mg/kg (approximately 0.6 times the human exposure at the recommended dose of 100 mg) toxicities included increased post-implantation loss and malformations including rotated limbs, malformed kidneys, domed head, high arched palate, and dilation of the cerebral ventricles. In rats, administration of lorlatinib resulted in total loss of pregnancy at doses of 4 mg/kg (approximately 5 times the human exposure at the recommended dose of 100 mg) or greater. At a dose of 1 mg/kg (approximately equal to the human exposure at the recommended dose of 100 mg) there was increased post-implantation loss, decreased fetal body weight, and malformations including gastroschisis, rotated limbs, supernumerary digits, and vessel abnormalities.

8.2 Lactation

Risk Summary

There are no data on the presence of lorlatinib or its metabolites in either human or animal milk or its effects on the breastfed infant or on milk production. Because of the potential for serious adverse reactions in breastfed infants, instruct women not to breastfeed during treatment with LORBRENA and for 7 days after the final dose.

8.3 Females and Males of Reproductive Potential

Pregnancy Testing

Verify pregnancy status in females of reproductive potential prior to initiating LORBRENA [see Use in Specific Populations (8.1)].

Contraception

LORBRENA can cause embryo-fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1)].

Females

Advise female patients of reproductive potential to use effective non-hormonal contraception during treatment with LORBRENA and for at least 6 months after the final dose. Advise females of reproductive potential to use a non-hormonal method of contraception, because LORBRENA can render hormonal contraceptives ineffective [see Drug Interactions (7.2)].

Males

Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment with LORBRENA and for at least 3 months after the final dose [see Nonclinical Toxicology (13.1)].

Infertility

Males

Based on findings from animal studies, LORBRENA may transiently impair male fertility [see Nonclinical Toxicology (13.1)].

8.4 Pediatric Use

The safety and effectiveness of LORBRENA in pediatric patients have not been established.

8.5 Geriatric Use

Of the patients in Study B7461001 (N=295) and Study B7461006 (N=149) who received 100 mg LORBRENA orally once daily, 18% and 40% of patients, respectively, were aged 65 years or older. No clinically important differences in safety or efficacy were observed between patients aged 65 years or older and younger patients.

8.6 Hepatic Impairment

In patients with severe hepatic impairment (Child-Pugh C), the recommended dosage of LORBRENA is 50 mg orally once daily [see Dosage and Administration (2.5) and Clinical Pharmacology (12.3)].

No dose adjustment is recommended for patients with mild (total bilirubin ≤ ULN with AST > ULN or total bilirubin >1 to 1.5 × ULN with any AST) to moderate (Child-Pugh B) hepatic impairment [see Clinical Pharmacology (12.3)].

8.7 Renal Impairment

In patients with CLcr 15 to <30 mL/min (estimated by Cockcroft‑Gault), the recommended dosage of LORBRENA is 75 mg orally once daily [see Dosage and Administration (2.6) and Clinical Pharmacology (12.3)].

No dose adjustment is recommended for patients with CLcr 30 to 89 mL/min (estimated by Cockcroft‑Gault) [see 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:

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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.”
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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:
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problems with thinking, such as forgetfulness or confusion
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changes in mood, such as depression and thoughts about suicide or dying
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psychotic effects, such as seeing or hearing things that are not real (hallucinations)
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seizures
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changes in speech
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changes in sleep
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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.
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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.
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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.
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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.
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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.
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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:
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feeling very thirsty
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needing to urinate more than usual
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feeling very hungry
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feeling sick to your stomach
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feeling weak or tired
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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
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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:

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have kidney problems
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have liver problems
•
have had episodes of depression or seizures
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have high levels of cholesterol or triglycerides in your blood
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have problems with your heart beat
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have lung or breathing problems
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have high blood pressure
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have diabetes or high blood sugar
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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?

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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.
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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.
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Take LORBRENA 1 time a day, at the same time each day.
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You may take LORBRENA with or without food.
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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.
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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:

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

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Store LORBRENA at room temperature between 68°F to 77°F (20°C to 25°C).
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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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