Neratinib

Neratinib Brand Name– Nerlynx

What is Neratinib

Neratinib is a kinase inhibitor that irreversibly inhibits EGFR, HER2, and HER4.

It is indicated for the extended adjuvant treatment of adult patients with early-stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy.

It is also indicated for the treatment of metastatic HER2-positive breast cancer in patients who have received at least 2 prior anti-HER2 based regimens, in combination with capecitabine.

Most patients (95%) treated with neratinib develop diarrhea, which may be severe and was the most frequent reason for discontinuation of treatment.

Prophylaxis with loperamide is recommended for the first 2 months of treatment, and should be used as needed thereafter.

Liver function tests should also be monitored, as neratinib has been associated with hepatotoxicity

Indications

  • breast cancer

For the treatment of breast cancer

For the extended adjuvant treatment of early-stage HER2-positive breast cancer, after completion of adjuvant trastuzumab-based therapy, as monotherapy

Side Effects

  1. abdominal pain
  2. abdominal pain
  3. acneiform rash
  4. anorexia
  5. anorexia
  6. arthralgia
  7. asthenia
  8. back pain
  9. cheilitis
  10. constipation
  11. dehydration
  12. dehydration
  13. diarrhea
  14. diarrhea
  15. dizziness
  16. dyspepsia
  17. dyspepsia
  18. dysuria
  19. elevated hepatic enzymes
  20. elevated hepatic enzymes
  21. eosinophilia
  22. epistaxis
  23. fatigue
  24. fatigue
  25. fever
  26. glossitis
  27. hepatotoxicity
  28. hyperbilirubinemia
  29. hypotension
  30. infection
  31. infection
  32. influenza
  33. maculopapular rash
  34. malaise
  35. muscle cramps
  36. muscle cramps
  37. nail discoloration
  38. nausea
  39. nausea
  40. oral ulceration
  41. rash
  42. rash
  43. renal failure (unspecified)
  44. stomatitis
  45. stomatitis
  46. vomiting
  47. vomiting
  48. weight loss
  49. weight loss
  50. xerosis
  51. xerostomia

Monitoring Parameters

  • LFTs
  • pregnancy testing

Contraindications

  • breast-feeding
  • contraception requirements
  • diarrhea
  • geriatric
  • hepatic disease
  • hepatotoxicity
  • infertility
  • pregnancy
  • pregnancy testing
  • reproductive risk

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Afatinib
  • Aluminum Hydroxide
  • Aluminum Hydroxide; Magnesium Carbonate
  • Aluminum Hydroxide; Magnesium Hydroxide
  • Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
  • Aluminum Hydroxide; Magnesium Trisilicate
  • Amiodarone
  • Amobarbital
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Antacids
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Omeprazole
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Betrixaban
  • Bexarotene
  • Boceprevir
  • Bosentan
  • Butabarbital
  • Calcium Carbonate
  • Calcium Carbonate; Magnesium Hydroxide
  • Calcium Carbonate; Risedronate
  • Calcium Carbonate; Simethicone
  • Carbamazepine
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Cimetidine
  • Ciprofloxacin
  • Clarithromycin
  • Cobicistat
  • Colchicine
  • Colchicine; Probenecid
  • Conivaptan
  • Crizotinib
  • Cyclosporine
  • Dabigatran
  • Dabrafenib
  • Danazol
  • Dapagliflozin; Saxagliptin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deferasirox
  • Delavirdine
  • Dexamethasone
  • Dexlansoprazole
  • Digoxin
  • Diltiazem
  • Doravirine; Lamivudine; Tenofovir disoproxil fumarate
  • Doxorubicin
  • Dronedarone
  • Duvelisib
  • Edoxaban
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Emtricitabine; Tenofovir disoproxil fumarate
  • Enzalutamide
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Esomeprazole
  • Esomeprazole; Naproxen
  • Etravirine
  • Famotidine
  • Famotidine; Ibuprofen
  • Fedratinib
  • Fexofenadine
  • Fexofenadine; Pseudoephedrine
  • Fluconazole
  • Fluvoxamine
  • Fosamprenavir
  • Fosphenytoin
  • Glecaprevir; Pibrentasvir
  • grapefruit juice
  • H2-blockers
  • Idelalisib
  • Imatinib
  • Indinavir
  • Irinotecan
  • Irinotecan Liposomal
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lamivudine; Tenofovir Disoproxil Fumarate
  • Lansoprazole
  • Lansoprazole; Naproxen
  • Lapatinib
  • Lefamulin
  • Letermovir
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Magnesium Hydroxide
  • Maraviroc
  • Mephobarbital
  • Metformin; Saxagliptin
  • Methohexital
  • Mifepristone
  • Mitotane
  • Modafinil
  • Morphine
  • Morphine; Naltrexone
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Nicardipine
  • Nilotinib
  • Nizatidine
  • Octreotide
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole
  • Omeprazole; Amoxicillin; Rifabutin
  • Omeprazole; Sodium Bicarbonate
  • Pantoprazole
  • Pazopanib
  • Pentobarbital
  • Phenobarbital
  • Phenytoin
  • Posaconazole
  • Primidone
  • Proton pump inhibitors
  • Quinine
  • Rabeprazole
  • Ranitidine
  • Ranolazine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Rifaximin
  • Rimegepant
  • Ritonavir
  • Romidepsin
  • Saquinavir
  • Saxagliptin
  • Secobarbital
  • Simeprevir
  • Sirolimus
  • Sodium Bicarbonate
  • St. John’s Wort, Hypericum perforatum
  • Talazoparib
  • Telithromycin
  • Telotristat Ethyl
  • Temsirolimus
  • Tenofovir, PMPA
  • Thiopental
  • Tipranavir
  • Tolvaptan
  • Topotecan
  • Trandolapril; Verapamil
  • Tucatinib
  • Ubrogepant
  • Venetoclax
  • Verapamil
  • Vincristine
  • Vincristine Liposomal
  • Voriconazole
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