LORBRENA (lorlatinib) tablets for NSCLC

LORBRENA is a once-daily pill available as a prescription that is used to treat people with non-small cell lung cancer (NSCLC):

• that is caused by an ALK (abnormal anaplastic lymphoma kinase) gene and,

• that has spread to other parts of your body and,

• who have taken the medicine alectinib or ceritinib, or

• who have taken both crizotinib and at least 1 other medicine to treat NSCLC that is caused by the ALK gene, and their NSCLC is no longer working or responding to these treatments.

It is not known if LORBRENA is safe to use in children.

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

LORBRENA reduced the risk of cancer spreading or growing by 72% compared to crizotinib. After a median of 9.3 months, half of the crizotinib patients were living without their tumors spreading or growing, and half were not. More than half of LORBRENA patients were still living without their tumors progressing (based on the time of the clinical study conducted). Therefore, the median time point when half of the patients were living without their tumors progressing is not yet known for LORBRENA. More time is needed to determine whether or not LORBRENA helps patients live longer.

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

• are taking other medications

• have had episodes of depression or seizures

• have high levels of cholesterol or triglycerides in your blood

• have problems with your heartbeat

• have lung or breathing problems

• are pregnant or planning to become pregnant. LORBRENA can harm your unborn baby. Your doctor will do a pregnancy test before you start treatment with LORBRENA. Tell your doctor right away if you become pregnant or think you may be pregnant during treatment with LORBRENA.
  • Females who are able to become pregnant should use effective birth control during treatment with LORBRENA and for at least 6 months after the final dose of LORBRENA.
  • Males who have female partners who are able to become pregnant should use effective birth control during treatment with LORBRENA and for at least 3 months after the final dose of LORBRENA.

• are breastfeeding or planning to breastfeed. It is not known if LORBRENA can pass into your breast milk. Do not breastfeed during treatment with LORBRENA and for 7 days after the final dose.

• Tell your doctor about all the medicines you take, including prescription medicines, over-the-counter medicines, vitamins, and herbal supplements.

• Take LORBRENA exactly as your doctor tells you to take it.

• Your doctor may temporarily stop, change your dose, or permanently stop treatment with LORBRENA if you develop side effects.

• Swallow LORBRENA tablets whole. Do not crush, chew, or split LORBRENA tablets.

• Do not take LORBRENA tablets if they are cracked, broken, or not intact.

• Take LORBRENA at the same time each day.

• You may take the LORBRENA tablet with or without food.

• If you miss a dose, take it as soon as possible. However, if it is close to the time of your next dose (within 4 hours), just take your next dose at your regular time.

• If you vomit after taking a LORBRENA tablet, do not take an extra dose. Take your next dose at your regular time.

The recommended dosage is 100 mg orally once daily.

Tablets: 25 mg or 100 mg.

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)
• difficulty thinking or confusion
• difficulty breathing
• tiredness (fatigue)
• weight gain
• pain in your joints
• changes in mood, feeling sad or anxious
• diarrhea
• LORBRENA may cause decreased fertility in males. In males, this could affect your ability to father a child. Talk to your healthcare provider if you have concerns about fertility.

LORBRENA may cause serious side effects, including:

• Liver problems due to interactions with other medicines: It is important to know what medicines should not be taken with LORBRENA.

• Problems with brain (central nervous system [CNS]) function: Many patients experienced problems with brain function including problems with thinking, mood, speech, seeing or hearing things that are not real, and seizures during treatment with LORBRENA. In some patients, these problems are severe and your doctor may need to have you stop taking LORBRENA.

• Increases in the cholesterol and triglycerides (lipid) levels in your blood: Most patients will have an increase in the lipid levels in their blood during treatment with LORBRENA. If you have an increase in the lipid levels in your blood during treatment with LORBRENA, your doctor may need you to start on a medicine to lower the levels. If you are already taking a medicine to lower the lipid levels in your blood, your doctor may need to increase your dose of that medicine. Your doctor should do blood tests to check the lipid levels in your blood before starting treatment, 1 to 2 months after starting treatment, and during treatment with LORBRENA.

• Heart problems: LORBRENA may cause very abnormal or slow heartbeats. Your doctor should check your heart rhythm before starting and during treatment with LORBRENA. Tell your doctor right away if you feel dizzy, fainting, or have abnormal heartbeats. In some patients, these problems are severe and your doctor may need to have you stop taking LORBRENA or have a pacemaker placed.

• Lung problems: LORBRENA may cause severe swelling of the lungs during treatment that can lead to death. These symptoms may be similar to those of lung cancer. Tell your doctor right away if you have any new or worsening symptoms of lung problems, including shortness of breath, trouble breathing, cough, or fever.

• Infertility: LORBRENA may transiently impair fertility in men.

CYP3A Inducers, CYP3A Inhibitors, and CYP3A Substrates can interact with LORBRENA.

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

Active ingredient: lorlatinib
Inactive ingredients: microcrystalline cellulose, sodium starch glycolate, dibasic calcium phosphate anhydrous, and magnesium stearate. Film-coating contains lactose monohydrate, hydroxypropyl methylcellulose (HPMC) 2910/hypromellose, triacetin, macrogol/polyethylene glycol (PEG) 3350, titanium dioxide, ferrosoferric oxide/black iron oxide, and iron oxide red.