৳ 300/unit
Pack: ৳ 3,000
৳ 300/unit
Pack: ৳ 3,000
At a glance
Dacomitinib is an irreversible kinase inhibitor used for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletion or exon 21 L858R substitution mutations.
Indications
- Metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletion or exon 21 L858R substitution mutations
Pharmacology
Dacomitinib is an irreversible inhibitor of the kinase activity of the human EGFR family (EGFR/HER1, HER2, and HER4) and certain EGFR activating mutations (exon 19 deletion or the exon 21 L858R substitution mutation). In vitro dacomitinib also inhibited the activity of DDR1, EPHA6, LCK, DDR2, and MNK1 at clinically relevant concentrations. Dacomitinib demonstrated dose-dependent inhibition of EGFR and HER2 autophosphorylation and tumor growth in mice bearing subcutaneously implanted human tumor xenografts driven by HER family targets including mutated EGFR.
Dosage
Adult: 45 mg orally once daily, continue until disease progression or unacceptable toxicity occurs.
First dose reduction: 30 mg (once daily)
Second dose reduction: 15 mg (once daily)
Side effects
Common Side Effects (Incidence >20%):
- Diarrhea (87%)
- Rash (69%)
- Paronychia (64%)
- Stomatitis (45%)
- Anemia (44%)
- Hypoalbuminemia (44%)
- Lymphopenia (42%)
- Increased ALT (40%)
- Hyperglycemia (36%)
- Increased AST (35%)
- Hypocalcemia (33%)
- Decreased appetite (31%)
- Dry skin (30%)
- Hypokalemia (29%)
- Decreased weight (26%)
- Hyponatremia (26%)
- Increased creatinine (24%)
- Alopecia (23%)
- Increased alkaline phosphatase (22%)
- Hypomagnesemia (22%)
- Pruritus (21%)
- Cough (21%)
- Nasal mucosal disorder (19%)
- Conjunctivitis (19%)
- Nausea (19%)
- Hyperbilirubinemia (16%)
- Palmar-plantar erythrodysesthesia syndrome (15%)
- Pain in extremity (14%)
- Dyspnea (13%)
- Constipation (13%)
- Asthenia (13%)
- Mouth ulceration (12%)
- Musculoskeletal pain (12%)
- Upper respiratory tract infection (12%)
- Dermatitis (11%)
- Insomnia (11%)
Serious Side Effects:
- Interstitial Lung Disease (ILD)/Pneumonitis
- Severe diarrhea
Use in pregnancy
Pregnancy Category D. Based on animal studies and its mechanism of action, fetal harm may occur when administered to a pregnant woman. Advise females of reproductive potential to use effective contraception during treatment and for at least 17 days after final dose.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Precautions & warnings
- Severe and fatal ILD/pneumonitis occurred; monitor for pulmonary symptoms indicative of ILD/pneumonitis. Permanently discontinue if ILD is confirmed.
- Severe and fatal diarrhea occurred; promptly initiate antidiarrheal treatment.
- Withhold and reduce dose based on severity of diarrhea and dermatologic reactions.
- Advise females of reproductive potential to use effective contraception.
Overdose effects
No adequate information on overdose is available. Overdose may lead to diarrhea, skin reactions, and other toxic effects. Seek medical attention.
Storage conditions
Do not store above 30°C. Keep away from light and out of reach of children.