Afatinib Brand Name– GILOTRIF
What is Afatinib
Afatinib is an oral, selective epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) with non-resistant EGFR mutations and in platinum-resistant metastatic NSCLC (not selected for EGFR). Clinically, EGFR expression has been associated with poor prognosis, development of metastasis, and resistance to chemotherapy, hormonal therapy, and radiation therapy.
First-line treatment with afatinib was associated with a significant improvement in progression-free survival (PFS) compared with combination cisplatin and pemetrexed in patients with advanced NSCLC and non-resistant EGFR mutations.
Treatment with afatinib also significantly improved overall survival and PFS compared with erlotinib in patients with platinum-resistant, metastatic NSCLC who were not selected for EGFR mutations in a separate randomized, open-label clinical trial.
Indications
- non-small cell lung cancer (NSCLC)
Side Effects
- acne vulgaris
- acneiform rash
- acute respiratory distress syndrome (ARDS)
- anemia
- blurred vision
- bullous rash
- cheilitis
- conjunctivitis
- constipation
- cough
- cystitis
- dehydration
- diarrhea
- dyspnea
- elevated hepatic enzymes
- epistaxis
- fatigue
- fever
- GI perforation
- heart failure
- hepatic failure
- hyperbilirubinemia
- hypokalemia
- infection
- keratitis
- lacrimation
- leukopenia
- maculopapular rash
- nausea
- neutropenia
- ocular inflammation
- ocular pain
- oral ulceration
- palmar-plantar erythrodysesthesia (hand and foot syndrome)
- pancreatitis
- photosensitivity
- pneumonitis
- pruritus
- rash
- renal failure (unspecified)
- rhinorrhea
- Stevens-Johnson syndrome
- stomatitis
- toxic epidermal necrolysis
- vomiting
- weight loss
- xerosis
Monitoring Parameters
- CBC with differential
- LFTs
- serum creatinine
Contraindications
- Asian patients
- breast cancer
- breast-feeding
- contact lenses
- contraception requirements
- corticosteroid therapy
- dehydration
- diarrhea
- diverticulitis
- geriatric
- hepatic disease
- hepatotoxicity
- infertility
- inflammation
- keratitis
- ocular disease
- peptic ulcer disease
- pneumonitis
- pregnancy
- pulmonary disease
- renal failure
- renal impairment
- reproductive risk
- respiratory distress syndrome
- serious rash
- skin disease
- visual disturbance
Interactions
- Amiodarone
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Brigatinib
- Cabozantinib
- Capmatinib
- Carbamazepine
- Carvedilol
- Clarithromycin
- Cobicistat
- Conivaptan
- Cyclosporine
- Daclatasvir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Dextromethorphan; Quinidine
- Dronedarone
- Elexacaftor; tezacaftor; ivacaftor
- Eliglustat
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Erythromycin
- Erythromycin; Sulfisoxazole
- Etravirine
- Flibanserin
- Fosamprenavir
- Fosphenytoin
- Fostamatinib
- Glecaprevir; Pibrentasvir
- grapefruit juice
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Istradefylline
- Itraconazole
- Ivacaftor
- Ketoconazole
- Lapatinib
- Ledipasvir; Sofosbuvir
- Lomitapide
- Lopinavir; Ritonavir
- Lorlatinib
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Mefloquine
- Mephobarbital
- Mifepristone
- Nelfinavir
- Neratinib
- Ombitasvir; Paritaprevir; Ritonavir
- Osimertinib
- Phenobarbital
- Phenytoin
- Ponatinib
- Posaconazole
- Primidone
- Propafenone
- Quinidine
- Ranolazine
- Rifampin
- Ritonavir
- Rolapitant
- Sapropterin
- Saquinavir
- Sarecycline
- Simeprevir
- Sofosbuvir; Velpatasvir
- Sofosbuvir; Velpatasvir; Voxilaprevir
- Sorafenib
- St. John’s Wort, Hypericum perforatum
- Tacrolimus
- Tedizolid
- Telaprevir
- Temsirolimus
- Tezacaftor; Ivacaftor
- Tipranavir
- Trandolapril; Verapamil
- Tucatinib
- Vemurafenib
- Venetoclax
- Verapamil
- Zonisamide
