৳ 1,400/unit
Pack: ৳ 42,000
৳ 1,400/unit
Pack: ৳ 42,000
At a glance
Brigatinib is a tyrosine kinase inhibitor used in the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) in patients who have progressed on or are intolerant to crizotinib.
Indications
- Anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) - in patients who have progressed on or are intolerant to crizotinib
Pharmacology
Brigatinib is a tyrosine kinase inhibitor with in vitro activity at clinically achievable concentrations against multiple kinases, including ALK, ROS1, IGF-1R, FLT-3, and EGFR deletion and point mutations. It inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of downstream signaling proteins STAT3, AKT, ERK1/2, and S6.
Dosage
Adults (ALK-positive metastatic NSCLC):
First 7 days: 90 mg PO qDay (with or without food).
If 90 mg/day is tolerated: Increase dose to 180 mg PO qDay.
Continue until disease progression or unacceptable toxicity.
Hepatic impairment:
Mild or moderate (Child-Pugh A or B): No dose adjustment required.
Severe (Child-Pugh C): Reduce once daily dose by ~40% (e.g., 180 mg to 120 mg, 120 mg to 90 mg, or 90 mg to 60 mg).
Renal impairment:
Mild or moderate (CrCl 30-89 mL/min): No dose adjustment required.
Severe (CrCl 15-29 mL/min): Reduce dose by ~50% (e.g., 180 mg to 90 mg, or 90 mg to 60 mg).
Side effects
>10%: Increased AST (38%), Hyperglycemia (38%), Increased ALT (34%), Nausea (33%), Fatigue (29%), Headache (28%), Increased CPK (27%), Increased amylase (27%), Dyspnea (27%), Vomiting (24%), Anemia (23%), Decreased appetite (22%), Prolonged aPTT (22%), Increased lipase (21%), Diarrhea (19%), Constipation (19%), Lymphopenia (19%), Cough (18%), Abdominal pain (17%), Increased alkaline phosphatase (15%), Decreased phosphorous (15%), Rash (15%), Pyrexia (14%), Arthralgia (14%), Peripheral neuropathy (13%), Muscle spasms (12%), Hypertension (11%), Pain in extremity (11%), Insomnia (11%).
1-10%: Back pain (10%), Myalgia (9.2%), Visual disturbances (7.3%), Pneumonia (4.6%), Interstitial lung disease/pneumonitis (3.7%).
<1%: Hypoxia (0.9%).
Use in pregnancy
Can cause fetal harm based on mechanism of action and animal findings (skeletal anomalies, decreased fetal body weight, postimplantation loss). Females of reproductive potential should use effective non-hormonal contraception during treatment and for at least 4 months after the final dose. Males should use effective contraception during treatment and for at least 3 months after the last dose.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Precautions & warnings
- Interstitial lung disease (ILD)/pneumonitis: Risk exists; discontinue for Grade 3 or 4 ILD/pneumonitis or recurrence of Grade 1/2 ILD.
- Hypertension (HTN): Discontinue for Grade 4 HTN or recurrence of Grade 3 HTN.
- Bradycardia: Discontinue for life-threatening bradycardia; caution with antihypertensives causing bradycardia.
- Visual disturbances: Blurred vision, diplopia, reduced visual acuity; discontinue for Grade 4.
- CPK and pancreatic enzyme elevation: Withhold treatment for Grade 3 or 4 elevation.
- Hyperglycemia: Withhold treatment for inadequate glycemic control.
- Contraception: Females of reproductive potential should use effective non-hormonal contraception during treatment and for at least 4 months after the final dose; males should use effective contraception during treatment and for at least 3 months after the last dose.
- Do not use during pregnancy and lactation; not for use in children.
Overdose effects
Overdose symptoms: Nausea, vomiting, diarrhea, fatigue, headache. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store below 30°C. Keep away from light and moisture. Keep out of reach of children.