Afatinib

DEA Class; Rx

Common Brand Names; Gilotrif

• Antineoplastics, Tyrosine Kinase Inhibitor; 
• Antineoplastics, EGFR Inhibitor

Non-Small Cell Lung Cancer

Metastatic Non-Small Cell Lung Cancer

• Indicated for first-line treatment in metastatic non-small cell lung cancer (NSCLC) whose tumors have nonresistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test

Metastatic Squamous Non-Small Cell Lung Cancer

• Indicated for metastatic squamous NSCLC progressing after platinum-based chemotherapy

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All grades included unless otherwise noted

• Diarrhea (75-96%)
• Rash/dermatitis acneiform (70-90%)
• Stomatitis (30-71%)
• Paronychia (11-58%)
• Increased ALT (10-54%)
• Decreased creatinine clearance (49%)
• Increase alkaline phosphate (34-51%)
• Increased AST (7-46%)
• Decreased lymphocytes (38%)
• Dry skin (31%)
• Decreased potassium (11-30%)
• Decreased appetite (25%)
• Pruritus (21%)
• Nausea (21%)
• Epistaxis (17%)
• Decreased weight (17%)
• Rash/dermatitis acneiform, Grade 3 or 4 (7-16%)
• Increased bilirubin (3-16%)
• Diarrhea, Grade 3 or 4 (11-15%)
• Vomiting (13%)
• Cystitis (13%)
• Decreased WBC (12%)
• Cheilitis (12%)
• Rhinorrhea (11%)
• Paronychia, Grade 3 or 4 (1-11%)
• Stomatitis, Grade 3 or 4 (9%)
• Decreased lymphocytes, Grade 3 or 4 (9%)
• Decreased potassium, Grade 3 or 4 (1-8%)
• Stomatitis, Grade 3 or 4 (4%)
• Decreased appetite, Grade 3 or 4 (3%)
• Increased AST, Grade 3 or 4 (1-3%)
• Increase alkaline phosphate, Grade 3 or 4 (2-3%)
• Decreased creatinine clearance (2%)
• Nausea, Grade 3 or 4 (2%)
• Increased ALT, Grade 3 or 4 (1-2%)
• Decreased WBC, Grade 3 or 4 (1%)
• Vomiting, Grade 3 or 4 (1%)
• Cystitis, Grade 3 or 4 (1%)
• Decreased weight, Grade 3 or 4 (1%)
• Increased bilirubin, Grade 3 or 4 (1%)

May cause diarrhea that results in dehydration with or without renal impairment; some reported cases were fatal; withhold therapy for severe and prolonged diarrhea not responsive to antidiarrheal agents (see Dosage Modifications)

Postmarketing cases consistent with toxic epidermal necrolysis (TEN), including bullous and exfoliative skin disorders, and Stevens Johnson syndrome (SJS) reported; discontinue if life-threatening bullous, blistering, or exfoliating lesions occur; withhold therapy for severe and prolonged cutaneous reactions (see Dosage Modifications)

May increase risk for sunburn/phototoxicity; may worsen rash or acne; caution patients to limit sun exposure and where sunscreen and protective clothing

Interstitial lung disease (ILD) or ILD-like adverse reactions reported (eg, lung infiltration, pneumonitis, acute respiratory distress syndrome, alveolitis allergy) occurred in 1%, of these, 0.4% were fatal; discontinue therapy if ILD diagnosed (see Dosage Modifications)

Hepatotoxicity reported; monitor with periodic liver testing; withhold or discontinue therapy for severe or worsening liver tests

Keratitis, characterized as acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye occurred in 0.8%; withhold or discontinue therapy for confirmed ulcerative keratitis

Gastrointestinal perforation, including fatal cases, reported; patients receiving concomitant corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs) or anti-angiogenic agents, or patients with increasing age or who have an underlying history of gastrointestinal ulceration, underlying diverticular disease or bowel metastases may be at increased risk of perforation; permanently discontinue therapy in patients who develop gastrointestinal perforation

Based on findings from animal studies and mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; there are no available data on use in pregnant women

There are no data on presence of afatinib in human milk or effects on breastfed infant or on milk production

Afatinib 

tablet

• 20mg
• 30mg
• 40mg