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Lorlatinib

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What is Lorlatinib?

Lorlatinib Structure.svg
Lorlatinib metabolism.svg

What are the uses of this medicine?

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

How does this medicine work?

  • An orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
  • Upon administration, lorlatinib binds to and inhibits both ALK and ROS1 kinases.
  • The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells.
  • In addition, PF-06463922 is able to cross the blood brain barrier.
  • ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors.
  • ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.

Who Should Not Use this medicine ?

This medcine cannot be used in patients who:

  • take certain other medicines called strong CYP3A inducers.

What drug interactions can this medicine cause?

  • 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.
  • Avoid concomitant use of moderate CYP3A inducers with LORBRENA. If concomitant use is unavoidable, increase the LORBRENA dose.
  • Avoid concomitant use of LORBRENA with a strong CYP3A inhibitor. If concomitant use cannot be avoided, reduce the LORBRENA dosage.
  • Avoid concomitant use of LORBRENA with fluconazole. If concomitant use cannot be avoided, reduce the LORBRENA dosage.
  • Avoid concomitant use with CYP3A substrates for which minimal concentration changes may lead to serious therapeutic failures.
  • Avoid concomitant use with P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures.

Is this medicine FDA approved?

  • It was approved for use in the United States in 2018.

How should this medicine be used?

  • Select patients for the treatment of metastatic NSCLC with LORBRENA based on the presence of ALK positivity in tumor specimens.

Recommended Dosage

  • The recommended dosage of LORBRENA is 100 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.

Administration

  • 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 close to the time of your next dose (within 4 hours), 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 dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

  • As Tablets: 25 mg or 100 mg.

This medicine is available in fallowing brand namesː

  • LORBRENA

What side effects can this medication cause?

The most common side effects of this medicine 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
  • high cholesterol and triglyceride levels in the blood
  • cough

LORBRENA may cause serious side effects, including:

  • Liver problems due to interactions with other medicines
  • Central nervous system (CNS) effects
  • Increases in the cholesterol and triglycerides (lipid) levels in your blood
  • Heart problems
  • Lung problems
  • High blood pressure (hypertension)
  • High blood sugar (hyperglycemia)

What special precautions should I follow?

  • Risk of Serious Hepatotoxicity with Concomitant Use of 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.
  • A broad spectrum of central nervous system (CNS) effects can occur in patients receiving LORBRENA. CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity.
  • Increases in serum cholesterol and triglycerides can occur in patients receiving LORBRENA. Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity.
  • PR interval prolongation and atrioventricular (AV) block can occur in patients receiving LORBRENA. Withhold and resume LORBRENA at same or reduced dose based on severity.
  • Severe or life-threatening pulmonary adverse reactions consistent with interstitial lung disease (ILD)/pneumonitis can occur with LORBRENA. Immediately withhold LORBRENA in patients with suspected ILD/pneumonitis. Permanently discontinue LORBRENA for treatment-related ILD/pneumonitis of any severity.
  • Hypertension can occur in patients receiving LORBRENA. Monitor blood pressure after 2 weeks and then at least monthly during treatment. For severe hypertension, withhold LORBRENA, then dose reduce or permanently discontinue.
  • Hyperglycemia can occur in patients receiving LORBRENA. Assess fasting serum glucose prior to starting LORBRENA and regularly during treatment. If not adequately controlled with optimal medical management, withhold LORBRENA, then consider dose reduction or permanently discontinue, based on severity.
  • LORBRENA Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus. Advise males and females of reproductive potential to use an effective non-hormonal method of contraception.

What to do in case of emergency/overdose?

  • In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

Can this medicine be used in pregnancy?

  • LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women.

Can this medicine be used in children?

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

What are the active and inactive ingredients in this medicine?

  • 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.

Who manufactures and distributes this medicine?

  • Packager: Pfizer Laboratories Div Pfizer Inc

What should I know about storage and disposal of this medication?

  • Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).

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External links

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