Gefitinib Brand Name– Iressa
What is Gefitinib
Gefitinib is an oral, selective epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI).
EGRF is expressed, overexpressed, or dysregulated in many cancers including breast, ovarian, non-small cell (NSCLC), mesothelioma, colorectal, and head and neck cancers.
Clinically, EGFR expression has been associated with poor prognosis, development of metastasis, and resistance to chemotherapy, hormonal therapy, and radiation therapy.
Gefitinib was originally approved by the FDA in 2002 for the third-line treatment of advanced NSCLC.
However, in 2005 the indication was modified to only include patients who benefited from either current or past gefitinib treatment, due to a large clinical trial in patients with refractory NSCLC showing no survival benefit, as well as the early termination of another clinical trial after an interim analysis due to a lack of survival at in advanced NSCLC following chemotherapy and radiation.
Of note, the impact of EGFR status on efficacy was unknown at that time. In 2015, the FDA approved gefitinib for the first-line treatment of metastatic NSCLC in patients with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations based on a small, single-arm, open-label study.
Serious adverse reactions include interstitial lung disease, liver damage, gastrointestinal perforation, severe diarrhea, bullous and exfoliative skin disorders, and ocular disorders; the most common side effects are diarrhea and skin reactions. Periodically monitor liver function tests during therapy.
Indications
- head and neck cancer
- non-small cell lung cancer (NSCLC)
For the first-line treatment of metastatic non-small cell lung cancer (NSCLC) in patients whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test
Side Effects
- acne vulgaris
- acneiform rash
- acute respiratory distress syndrome (ARDS)
- alopecia
- angioedema
- anorexia
- anorexia
- asthenia
- bleeding
- blepharitis
- bullous rash
- cheilitis
- conjunctivitis
- corneal erosion
- cough
- cystitis
- dehydration
- diarrhea
- diarrhea
- dyspnea
- elevated hepatic enzymes
- elevated hepatic enzymes
- epistaxis
- erythema
- erythema multiforme
- exfoliative dermatitis
- fever
- folliculitis
- GI perforation
- hematuria
- hemorrhagic cystitis
- hepatotoxicity
- hyperbilirubinemia
- hyperbilirubinemia
- keratitis
- maculopapular rash
- nausea
- ocular inflammation
- ocular irritation
- ocular pruritus
- onycholysis
- oral ulceration
- pancreatitis
- pneumonitis
- pneumonitis
- proteinuria
- proteinuria
- pruritus
- pulmonary embolism
- pulmonary fibrosis
- rash
- Stevens-Johnson syndrome
- stomatitis
- stomatitis
- toxic epidermal necrolysis
- urticaria
- vasculitis
- vesicular rash
- visual impairment
- vomiting
- vomiting
- xerophthalmia
- xerosis
- xerostomia
Monitoring Parameters
- LFTs
Contraindications
- breast-feeding
- chronic lung disease (CLD)
- contraception requirements
- diarrhea
- GI perforation
- hepatic disease
- infertility
- keratitis
- ocular disease
- pneumonitis
- pregnancy
- pulmonary disease
- pulmonary fibrosis
- reproductive risk
- serious rash
Interactions
- Abiraterone
- Acetaminophen; Oxycodone
- Aluminum Hydroxide
- Aluminum Hydroxide; Magnesium Carbonate
- Aluminum Hydroxide; Magnesium Hydroxide
- Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
- Aluminum Hydroxide; Magnesium Trisilicate
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Antacids
- Apalutamide
- Aripiprazole
- Aspirin, ASA; Citric Acid; Sodium Bicarbonate
- Aspirin, ASA; Omeprazole
- Aspirin, ASA; Oxycodone
- Atazanavir
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Bupropion
- Bupropion; Naltrexone
- Calcium Carbonate
- Calcium Carbonate; Magnesium Hydroxide
- Calcium Carbonate; Risedronate
- Calcium Carbonate; Simethicone
- Carbamazepine
- Ceritinib
- Chloramphenicol
- Cimetidine
- Cinacalcet
- Clarithromycin
- Cobicistat
- Conivaptan
- Dacomitinib
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Delavirdine
- Dexamethasone
- Dexlansoprazole
- Dextromethorphan; Quinidine
- Dronedarone
- Duloxetine
- Eliglustat
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Enzalutamide
- Escitalopram
- Esomeprazole
- Esomeprazole; Naproxen
- Famotidine
- Famotidine; Ibuprofen
- Fedratinib
- Fluoxetine
- Fluoxetine; Olanzapine
- Fosamprenavir
- Fosphenytoin
- grapefruit juice
- Halofantrine
- Ibuprofen; Oxycodone
- Idelalisib
- Indinavir
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ketoconazole
- Lansoprazole
- Lansoprazole; Naproxen
- Letermovir
- Lopinavir; Ritonavir
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Magnesium Hydroxide
- Mephobarbital
- Mifepristone
- Mirabegron
- Mitotane
- Nefazodone
- Nelfinavir
- Nizatidine
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole
- Omeprazole; Amoxicillin; Rifabutin
- Omeprazole; Sodium Bicarbonate
- Oxycodone
- Panobinostat
- Pantoprazole
- Paroxetine
- Pentosan
- Phenobarbital
- Phentermine; Topiramate
- Phenytoin
- Pimozide
- Posaconazole
- Primidone
- Propafenone
- Quinidine
- Quinine
- Rabeprazole
- Ranitidine
- Ranolazine
- Ribociclib
- Ribociclib; Letrozole
- Rifampin
- Ritonavir
- Rolapitant
- Saquinavir
- Sodium Bicarbonate
- St. John’s Wort, Hypericum perforatum
- Telithromycin
- Terbinafine
- Thioridazine
- Tipranavir
- Topiramate
- Tucatinib
- Voriconazole
- Warfarin
