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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
- For use as an extended adjuvant treatment in adult patients with early-stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy [FDA Label].
- Neratinib 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.
- For the extended adjuvant treatment of adult patients with early-stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy.
- Nerlynx is indicated for the extended adjuvant treatment of adult patients with early-stage hormone receptor-positive HER2-overexpressed/amplified breast cancer and who are less than one year from the completion of prior adjuvant trastuzumab-based therapy.
Neratinib Contraindications
- Severe infection
- insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">Diabetes
- Anemia
- Decreased Blood Platelets
- Severely Decreased Platelets
- Decreased Neutrophils a Type of White Blood Cell
- Peripheral pain, numbness, tingling, or weakness. সহজ বাংলা: স্নায়ুর ক্ষতি/সমস্যা।" data-rx-term="neuropathy" data-rx-definition="Neuropathy means nerve damage or irritation causing pain, numbness, tingling, or weakness. সহজ বাংলা: স্নায়ুর ক্ষতি/সমস্যা।">neuropathy
- Disease of Inadequate Blood Flow to the Heart Muscle
- Abnormal heart rhythm
- Heart Disease
- Liver problems
- Severe liver disease
- High Amount of jaundice. সহজ বাংলা: জন্ডিসে বাড়তে পারে এমন হলুদ রঞ্জক।" data-rx-term="bilirubin" data-rx-definition="Bilirubin is a yellow pigment that can build up in jaundice. সহজ বাংলা: জন্ডিসে বাড়তে পারে এমন হলুদ রঞ্জক।">Bilirubin in the Blood
- Abnormal liver function tests
- Pregnancy
- A mother who is producing milk and breastfeeding
- Severely Decreased Levels of Neutrophils in the Blood
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
- pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">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
