Posted on December 4th, 2008 by

Class: Biologic therapy

Generic Name: Lapatinib (luh-PA-ti-nib)
Trade Name: Tykerb®

For what conditions is this drug used? Lapatinib is FDA approved for the treatment of patients with advanced breast cancer that is human epidermal growth factor receptor 2 (HER2)- positive and has progressed following therapy with chemotherapy agents known as taxanes and anthracyclines and the targeted therapy agent Herceptin® (trastuzumab). Lapatinib is to be used in combination with the chemotherapy agent Xeloda® (capecitabine). If your doctor has prescribed this drug for a different condition, keep in mind that doctors have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA; you should discuss this issue with your doctor.

What is the mechanism of action? Lapatinib is classified as a targeted agent. The epidermal growth factor receptor and HER2 are both involved in regulating growth and replication of a cell. In many cancer cells, these pathways are abnormal and provide continual growth stimulation of a cell. Lapatinib blocks part of the epidermal growth factor receptor pathway and HER2 so that the cellular growth signals are inhibited.

How is lapatinib given (administered)? Lapatinib is given in the form of a pill and is taken orally. It should be taken one hour prior to a meal or one hour following a meal.

How are patients monitored? Patients will usually have scheduled meetings with their healthcare provider while being treated with lapatinib. Physical examinations, scans, or other measures may be performed to assess side effects and response to therapy. Blood may be drawn to monitor functions of some organs, such as the liver. In addition, patients will have their heart monitored, as rare but serious side effects affecting the heart may occur.

What are the common (occur in 30% or more of patients) side effects of treatment with lapatinib?

  • Diarrhea
  • Nausea
  • Irritation, redness, pain of the palms of the hands and soles of the feet

What are the less common (occur in 10% to 29% of patients) side effects of treatment with lapatinib?

  • Rash
  • Vomiting
  • Difficulty in breathing
  • Inflammation of the mucosal membranes
  • Upset stomach
  • Dry skin
  • Inflammation of the lining of the mouth
  • Pain
  • Difficulty sleeping

What can patients do to help alleviate or prevent discomfort and side effects?

  • Patients should inform their doctors of any side effects.
  • Wear sunscreen and protective clothing; try to minimize sun exposure.
  • Drink plenty of fluid. Patients should ask their physician about the amount of liquid to consume during a day.
  • Maintain adequate rest and nutrition.
  • Eat small meals frequently to help alleviate nausea.

Are there any special precautions patients should be aware of before starting treatment?

  • Patients should tell their physician if they are pregnant, breastfeeding, or planning a family in the near future. This drug may cause birth defects. It is important to use some kind of birth control while undergoing treatment. Also, patients may want to talk to their physician if they are considering having children in the future since some drugs may cause fertility problems.
  • It is important that patients inform their physician of any pre-existing conditions (chicken pox, heart disease, kidney stones, liver disease, lung disease, etc.) as they may worsen with this drug.
  • Patients should let their physician know of any other medication they are taking (whether prescription or over the counter, including vitamins, herbs, etc.) as they may interfere with treatment.
  • If an oral dose is missed, do not double up on doses. Patients should contact their doctor in this event.
  • Keep tablets out of reach of children and return to the pharmacy for safe disposal if treatment is terminated.

When should patients notify their physician?

  • Sudden onset of shortness of breath, cough, and/or fever
  • Persistent or extreme diarrhea
  • Persistent or extreme nausea and vomiting
  • Changes in heart rhythm or rate
  • Pain or inflammation of the lining of the mouth, soles of the feet, or the palms of the hands.

What is a package insert?
A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers. A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics, and metabolism of the specific drug. By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.

Copyright © 2016 CancerConnect Last updated 07/10.

Important Limitations of Use

The information provided above on the drug you have selected is provided for your information only and is not a substitute for consultation with an appropriate medical doctor. We are providing this information solely as a courtesy and, as such, it is in no way a recommendation as to the safety, efficacy or appropriateness of any particular drug, regimen, dosing schedule for any particular cancer, condition or patient nor is it in any way to be considered medical advice. Patients should discuss the appropriateness of a particular drug or chemotherapy regimen with their physician.

As with any printed reference, the use of particular drugs, regimens and drug dosages may become out-of-date over time, since new information may have been published and become generally accepted after the latest update to this printed information. Please keep in mind that health care professionals are fully responsible for practicing within current standards, avoiding use of outdated regimens, employing good clinical judgment in selecting drugs and/or regimens, in calculating doses for individual patients, and verifying all dosage calculations.



The prescribing physician is solely responsible for making all decisions relating to appropriate patient care including, but not limited to, drugs, regimens, dose, schedule, and any supportive care.

Tags: Biological Therapy, Drug Dictionary, T

You must be logged-in to the site to post a comment.