Neratinib Maleate; Dosage, Side Effect, Drug Interactions

Neratinib Maleate is an orally available tyrosine kinase receptor inhibitor that is used in the extended adjuvant therapy of early-stage breast cancer. Neratinib is associated with a low rate of transient elevations in serum aminotransferase levels during therapy but has not been convincingly linked to cases of clinically apparent liver injury with jaundice.

Neratinib Maleate is the maleate salt form of neratinib, an orally available, quinazoline-based, irreversible inhibitor of both the receptor tyrosine kinases (RTKs) human epidermal growth factor receptor 2 (HER2; ERBB2) and human epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, neratinib targets and covalently binds to the cysteine residue in the ATP-binding pockets of both HER2 and EGFR. This inhibits their activity and results in the inhibition of downstream signal transduction events, induces cell cycle arrest, apoptosis and ultimately decreases cellular proliferation in HER2- and EGFR-expressing tumor cells. EGFR and HER2, RTKs that are mutated or overactivated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.

Mechanism of Action of Neratinib Maleate

Neratinib Indications

Dosage of Neratinib Maleate

 Strengths: 40 mg

Breast Cancer – Adjuvant

• 240 mg orally once a day with food, continuously for 1 year

Side Effects of Neratinib Maleate

The Most Common

• Abdominal or stomach pain or tenderness
• diarrhea
• symptoms of heart problems (e.g., shortness of breath, swelling of the ankles or feet, chest pain, irregular heartbeat)
• symptoms of liver problems (e.g., nausea, vomiting, abdominal pain, yellowing of the skin and eyes, itchy skin, dark urine)
• symptoms of lung problems (e.g., shortness of breath or difficulty breathing, chest pain, cough)
• symptoms of a severe allergic reaction (e.g., hives; difficulty breathing; swelling of the face, mouth, tongue, or throat)
• signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort

More Common

• Acid or sour stomach
• back pain
• belching
• cracked lips
• diarrhea (mild)
• dry skin
• heartburn
• indigestion
• pain in the arms or legs
• redness, swelling, or painful skin
• scaling of the skin on the hands and feet
• sores, ulcers, or white spots on the lips, tongue, or the inside of the mouth

Rare

• Black, tarry stools
• body aches or pain
• burning, numbness, tingling, or painful sensations
• burning pain on urination
• chest pain
• chills
• cough
• difficult or labored breathing
• ear congestion
• fever
• headache
• loss of voice
• lower back or side pain
• nasal congestion
• painful or difficult urination
• pale skin
• red, swelling, or painful skin

Drug Indications of Neratinib Maleate

Neratinib may interact with following drugs, supplements & may change the efficacy of drugs

• calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
• carbamazepine
• carvedilol
• cetirizine
• corticosteroids (e.g., prednisone, dexamethasone)
• cyclosporine
• desipramine
• dexamethasone
• domperidone
• doxorubicin
• estrogens
• everolimus
• “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
• “glitazone” diabetes medications
• hydrocortisone
• loperamide
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• methadone
• methotrexate
• metronidazole
• mirabegron
• modafinil
• nadolol
• phenobarbital
• phenytoin
• prazosin
• progesterone
• propranolol
• protein kinase inhibitors (e.g.,  pazopanib, sunitinib)
• quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
• ranitidine
• repaglinide
• St. John’s Wort
• serotonin antagonists (anti-emetics; e.g., granisetron, ondansetron)
• sertraline
• sotalol
• “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
• tacrolimus

Pregnancy Category

US FDA Pregnancy Category: N(Not Assigned)

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Women who may become pregnant should use contraception and avoid becoming pregnant while they are taking this medication.

Lactation

It is not known if it passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should breastfeed. Breastfeeding while taking this medication is not recommended. The safety and effectiveness of using this medication have not been established for children.

References

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