Bigatab 90mg Tablet

✔️ Uses of Bigatab 90mg Tablet

Non-Small Cell Lung Cancer

✔️ How does Bigatab 90mg Tablet work?

It acts by inhibiting ALK phosphorylation and the activation of downstream signaling proteins.7

✔️ Side Effects of Bigatab 90mg Tablet

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

✔️ Quick Suggestions:

• Avoid grapefruit and grapefruit juice while taking brigatinib.
• Skip the missed dose and continue the regular schedule.
• If brigatinib is not taken for 14 days or longer, consult with your doctor before restarting.

✔️ Indication of Bigatab 90mg Tablet

Bigatab is indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic Non-Small Cell Lung Cancer (NSCLC) who have progressed on or are intolerant to Crizotinib.

✔️ Pharmacology

• 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.
• Inhibits autophosphorylation of ALK and downstream signaling proteins.
• Demonstrated antitumor activity against EML4-ALK-positive NSCLC xenografts in mice.

Absorption:

• Median time to peak concentration (Tmax) ranged from 1 to 4 hours after single oral doses of Brigatinib (30 to 240 mg).

Distribution:

• Brigatinib is 66% bound to human plasma proteins.
• The mean apparent volume of distribution (Vz/F) at steady-state is 153 L.

Elimination:

• The mean apparent oral clearance (CL/F) at steady-state is 12.7 L/h.
• The mean plasma elimination half-life is 25 hours.

Metabolism:

• Primarily metabolized by CYP2C8 and CYP3A4.
• N-demethylation and cysteine conjugation are major metabolic pathways.

Excretion:

• 65% of the administered dose is excreted in feces, and 25% in urine.
• Unchanged Brigatinib represented a significant portion of total radioactivity in feces and urine.

✔️ Dosage & Administration of Bigatab 90mg Tablet

• Recommended dosing regimen:
  • 90 mg orally once daily for the first 7 days.
  • If tolerated, increase to 180 mg orally once daily.
• Administer until disease progression or unacceptable toxicity.
• 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.
• May be taken with or without food.
• Tablets should be swallowed whole, not crushed or chewed.
• If a dose is missed or vomiting occurs after taking a dose, do not administer an additional dose.

✔️ Interaction

Drugs that may Increase Bigatab Plasma Concentrations:

• Strong CYP3A inhibitors: Avoid concomitant use; if unavoidable, reduce Bigatab dose by approximately 50%.

Drugs that may Decrease Bigatab Plasma Concentrations:

• Strong CYP3A inducers: Avoid concomitant use.

Drugs that may have their Plasma Concentrations altered by Bigatab:

• CYP3A substrates: Bigatab induces CYP3A in vitro, may decrease concentrations of CYP3A substrates.

✔️ Contraindications

Hypersensitivity to Brigatinib or any other components.

✔️ Pregnancy & Lactation

• Pregnancy: Contraindicated. Potential risk to a fetus.
• Lactation: Advised not to breastfeed during treatment and for 1 week following the final dose.

✔️ Precaution & Warnings:

Interstitial Lung Disease (ILD)/Pneumonitis:

• Promptly evaluate for ILD/pneumonitis with new or worsening respiratory symptoms.
• Discontinue permanently for Grade 3 or 4 ILD/pneumonitis.

Hypertension:

• Control blood pressure before treatment.
• Monitor regularly; withhold for Grade 3 hypertension; consider discontinuation for Grade 4 or recurrent Grade 3.

Bradycardia:

• Monitor heart rate and blood pressure; consider more frequent monitoring with concomitant use of bradycardia-inducing drugs.

Visual Disturbance:

• Withhold and obtain an ophthalmologic evaluation for Grade 2 or greater severity; resume at a reduced dose upon recovery.

CPK Elevation:

• Monitor for unexplained muscle pain, tenderness, or weakness.
• Withhold for Grade 3 or 4 CPK elevation.

Pancreatic Enzyme Elevation:

• Monitor lipase and amylase during treatment.
• Withhold for Grade 3 or 4 pancreatic enzyme elevation.

Hyperglycemia:

• Monitor fasting serum glucose; initiate or optimize antihyperglycemic medications.
• Withhold for inadequate hyperglycemic control; consider dose reduction.

✔️ Storage Conditions

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