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Tykerb 250mg Tablet
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Indications & Clinical Uses
- Tykerb (lapatinib) 250 mg is a tyrosine kinase inhibitor (TKI) that blocks HER2 and EGFR signaling in cancer cells.
- It is approved for HER2-positive advanced or metastatic breast cancer in combination with capecitabine in patients who have received prior therapy with anthracyclines, taxanes, and trastuzumab (Herceptin).
- Lapatinib is also used alone for HER2-positive advanced breast cancer in postmenopausal women with hormone receptor-positive tumors, in combination with letrozole.
- It is indicated for ErbB2-overexpressing breast cancer.
- Tykerb is an oral therapy taken daily as a tablet.
- It represents an important option for patients with HER2-positive breast cancer, particularly those who have developed resistance or intolerance to trastuzumab.
Side Effects
- Diarrhea is very common, occurring in more than half of patients and sometimes severe enough to require dose reduction; antidiarrheal medications are frequently needed.
- Hand-foot skin reaction (palmar-plantar erythrodysesthesia) causes painful redness and peeling of palms and soles.
- Nausea, vomiting, and decreased appetite occur frequently.
- Fatigue and weakness are common, affecting quality of life.
- Rash and alopecia (hair loss) may develop.
- Hepatotoxicity with elevation of liver enzymes is important to monitor.
- Serious adverse reactions include left ventricular ejection fraction (LVEF) decrease or heart failure, severe diarrhea with dehydration, QT prolongation with potential arrhythmias, and severe hepatic impairment.
- Some patients experience CNS effects including headache and dizziness.
Precautions & Warnings
- Monitor LVEF (heart function) before starting treatment and periodically during therapy; lapatinib can cause heart failure in susceptible patients, especially those with prior anthracycline exposure.
- Monitor liver function tests regularly as hepatotoxicity can develop.
- QT interval monitoring may be needed in patients at risk of arrhythmias.
- Lapatinib is contraindicated in patients with decreased LVEF or symptomatic heart failure.
- Use with extreme caution in patients with baseline hepatic impairment; dose reduction is often needed.
- Avoid in patients with severe renal impairment.
- Lapatinib causes fetal harm; women of reproductive potential must use effective contraception and pregnancy tests.
- Breastfeeding is contraindicated.
- Monitor for severe diarrhea and provide aggressive supportive care; dose interruption or reduction may be necessary.
Avoid Interactions
- Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) increase lapatinib levels significantly, increasing toxicity risk; dose reduction is recommended.
- CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital) decrease lapatinib levels, reducing effectiveness; dose increase may be needed.
- Lapatinib is a CYP3A4 substrate and CYP2D6 inhibitor; it can increase levels of drugs metabolized by these enzymes, including certain beta-blockers and antiarrhythmics.
- H2-blockers and proton pump inhibitors reduce lapatinib absorption; separate administration by 12 hours or use antacids instead.
- Grapefruit and grapefruit juice inhibit CYP3A4 and must be avoided.
- QT-prolonging drugs (antiarrhythmics, some antipsychotics, fluoroquinolones) increase arrhythmia risk.
- Capecitabine and letrozole (common combination partners) require careful monitoring for enhanced toxicity.
References
Frequently Asked Questions
Tykerb (lapatinib) is a cancer drug used to treat HER2-positive breast cancer that has spread or is advanced. It works by blocking growth signals in cancer cells. Tykerb is usually combined with chemotherapy (capecitabine) or hormone therapy (letrozole) depending on your situation. It is taken as a tablet once daily.
Tykerb 250 mg tablets are taken once daily by mouth on an empty stomach, 1 hour before or 2 hours after a meal. Swallow tablets whole; do not crush, chew, or split them. Your doctor will determine the exact dose based on your individual situation. Take it at the same time each day.
Severe diarrhea is the most common side effect, affecting more than half of patients and sometimes requiring dose reduction or discontinuation. Hand and foot redness and peeling (painful), nausea, vomiting, fatigue, and hair loss also occur commonly. Heart function can decrease, especially in patients previously treated with certain chemotherapy drugs.
Avoid grapefruit and grapefruit juice as they increase Tykerb levels dangerously. Certain seizure and tuberculosis medications reduce effectiveness. Some antacids and acid-reducing medications reduce absorption. Ketoconazole and other antifungals increase toxicity. Tell your doctor all medications, supplements, and recent chemotherapy treatments.
Regular heart function tests (echocardiogram or MUGA scan) are required before starting and periodically during treatment, as lapatinib can weaken the heart. Liver function tests are monitored regularly. Blood counts and electrolytes are checked. This monitoring helps detect problems early and guide treatment adjustments.
Tykerb causes fetal harm and must not be taken during pregnancy. Women of reproductive age must use effective contraception during and after treatment. Pregnancy tests are performed before starting therapy. Breastfeeding is not recommended as lapatinib passes into breast milk and could harm a nursing infant.
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