Brigatinib

Brigatinib, sold as Alunbrig, is a tyrosine kinase inhibitor indicated for the treatment of anaplastic lymphoma kinase (ALK) positive metastatic non-small cell lung cancer (NSCLC). Brigatinib is active against ALK and epidermal growth factor receptor (EGFR) mutations, being effective against crizotinib-resistant ALK mutants. Brigatinib is an oral drug and can result in severe side effects including lung disease, vision disturbances, and hypertension. It is a highly effective inhibitor with an acceptable benefit-risk profile and is therefore a useful choice in patients with the correct genetic markers. There is a need for regular monitoring to manage side effects and to maximize treatment effect.

Active Ingredient: Brigatinib

Chemical Formula: C29H39ClN7O2P

Molecular Weight: 584.1 g/mol

Excipients: May include microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, and lactose monohydrate. Specific formulations may vary.

Brigatinib has undergone several clinical trials to establish its safety and efficacy. Notable trials include:

ALTA-1L (NCT02737501): Phase 3 trial comparing Brigatinib to Crizotinib in ALK-positive NSCLC patients.

ALTA Trial (NCT02094573): Phase 2 trial assessing Brigatinib in patients with advanced ALK-positive NSCLC who had progressed on Crizotinib.

Long-term Follow-up Studies: Continuing to monitor patients for overall survival (OS) and progression-free survival (PFS).

Recommended Dosage: Initial dose of 90 mg once daily for 7 days, followed by 180 mg once daily.

Administration: Oral, with or without food.

Dose Adjustments: Based on tolerability and side effects.

Monitoring: Regular liver function tests and monitoring for pulmonary symptoms are recommended.

Indications:

Treatment of ALK-positive metastatic NSCLC.

Contraindications:

Known hypersensitivity to Brigatinib or any excipients.

Severe hepatic impairment.

History of severe interstitial lung disease or pneumonitis.

Common Side Effects:

Nausea, diarrhea, fatigue, headache, hypertension.

Serious Side Effects:

Pulmonary toxicity, hypertension, hyperglycemia, bradycardia.

Drug Interactions:

Avoid concurrent use with strong CYP3A inhibitors or inducers.

Caution with other drugs affecting heart rate or blood pressure.

Dosage Forms: Available as oral tablets in strengths of 30 mg, 90 mg, and 180 mg.

Packaging: Typically supplied in blister packs or bottles containing 30 or 60 tablets.

Store at room temperature between 20°C to 25°C (68°F to 77°F).

Protect from moisture and light.

Keep in the original container and tightly closed.

Brigatinib has undergone several clinical trials to establish its safety and efficacy. Notable trials include:

ALTA-1L (NCT02737501): Phase 3 trial comparing Brigatinib to Crizotinib in ALK-positive NSCLC patients.

ALTA Trial (NCT02094573): Phase 2 trial assessing Brigatinib in patients with advanced ALK-positive NSCLC who had progressed on Crizotinib.

Long-term Follow-up Studies: Continuing to monitor patients for overall survival (OS) and progression-free survival (PFS).

FDA Approval: Granted in 2017 for metastatic ALK-positive NSCLC.

EMA Approval: Approved in the European Union.

Other Approvals: Available in various countries under local regulatory bodies.

Brand Name: Alunbrig

Manufacturer: Takeda Pharmaceutical Company Limited.

• Clinical trial results and prescribing information are available through public health agency websites like FDA, EMA, and clinical trial registries.
• Accessible in most major hospitals and cancer treatment centers.

Manufacturers provide regular updates on safety, efficacy, and label modifications.

Self-certificates may include compliance with Good Manufacturing Practices (GMP) and other regulatory standards.

Updated data may be accessed through the official manufacturer website or relevant health authorities.