Biganib 90mg Tablet

Pharmacology:

• Mechanism of Action: Brigatinib is a tyrosine kinase inhibitor with in vitro activity against multiple kinases, including ALK, ROS1, IGF-1R, FLT-3, EGFR deletion, and point mutations.
• Inhibition: It inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of downstream signaling proteins such as STAT3, AKT, ERK1/2, and S6 in vitro and in vivo assays.
• Proliferation Inhibition: Demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice.
• Metabolism: Primarily metabolized by CYP2C8 and CYP3A4 in vitro. The major metabolite, AP26123, has lower potency against ALK compared to Brigatinib.
• Excretion: Excreted mainly through feces (65%) and urine (25%).

Dosage & Administration:

• Recommended Dosing: Start with 90 mg orally once daily for the first 7 days.
• Dose Increase: If 90 mg is tolerated, increase the dose to 180 mg orally once daily.
• Continuation: Administer until disease progression or unacceptable toxicity.
• Interrupted Treatment: If interrupted for 14 days or longer for reasons other than adverse reactions, resume at 90 mg once daily for 7 days before increasing to the tolerated dose.
• Administration: This can be taken with or without food. Swallow tablets whole; do not crush or chew.

Pediatric Use:

The safety and efficacy of Brigatinib in pediatric patients have not been established.

Interaction:

• Inhibitors: Avoid strong CYP3A inhibitors; if unavoidable, reduce the Biganib dose by approximately 50%.
• Inducers: Strong CYP3A inducers should be avoided as they may decrease Brigatinib efficacy.

Contraindications:

Hypersensitivity: Contraindicated in patients with known hypersensitivity to Brigatinib or any other components.

Side Effects:

• Interstitial Lung Disease (ILD)/Pneumonitis
• Hypertension
• Bradycardia
• Visual Disturbance
• Creatine Phosphokinase (CPK) Elevation
• Pancreatic Enzyme Elevation
• Hyperglycemia

Pregnancy & Lactation:

• Pregnancy: Potential risk to the fetus; advise pregnant women accordingly.
• Lactation: Unknown if distributed in human breast milk; advise lactating women not to breastfeed during treatment and for 1 week following the final dose.

Reproductive Potential:

• Females: Use effective nonhormonal contraception during treatment and for at least 4 months after the final dose.
• Males: Use effective contraception during treatment and for at least 3 months after the final dose.

Infertility:

• Males: Brigatinib may cause reduced fertility.

Therapeutic Class:

• Cytotoxic Chemotherapy

Precautions & Warnings:

• ILD/Pneumonitis: Severe reactions observed; evaluate promptly for ILD/pneumonitis.
• Hypertension: Monitor blood pressure; withhold for Grade 3 hypertension.
• Bradycardia: Monitor heart rate; use caution with concomitant bradycardia-inducing agents.
• Visual Disturbance: Withhold for Grade 2 or greater severity; permanently discontinue for Grade 4.
• CPK Elevation: Monitor for muscle pain; withhold for Grade 3 or 4 CPK elevation.
• Pancreatic Enzyme Elevation: Monitor amylase and lipase; withhold for Grade 3 or 4 elevation.
• Hyperglycemia: Monitor glucose levels; adjust antihyperglycemic medications as needed.

Storage Conditions

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Disposal:

Disposal of medications is crucial to prevent accidental ingestion by pets, children, or others and to avoid environmental contamination.