Alunib 90mg Tablet

Uses of Alunib 90

Treat a certain type of non-small cell lung cancer (NSCLC)

Side Effects of Alunib 90

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

How does Alunib 90 work?

Tyrosine Kinase Inhibitor (TKI):

• Demonstrates in vitro activity against multiple kinases, including:
  • ALK (Anaplastic Lymphoma Kinase)
  • ROS1
  • IGF-1R (Insulin-like Growth Factor-1 Receptor)
  • FLT-3
  • EGFR (Epidermal Growth Factor Receptor) deletion and point mutations.

Inhibition of ALK Signaling:

• Brigatinib inhibits autophosphorylation of ALK (Anaplastic Lymphoma Kinase).
• Inhibits ALK-mediated phosphorylation of downstream signaling proteins:
  • STAT3
  • AKT
  • ERK1/2
  • S6

Antitumor Activity:

• Exhibits in vivo antitumor activity against mutant forms of EML4-ALK, including G1202R and L1196M mutants.
• Effective against non-small cell lung cancer (NSCLC) tumors in patients who have progressed on crizotinib.

Activity Against ALK-Driven Tumors:

• Reduces tumor burden.
• Prolong survival in mice implanted intracranially with an ALK-driven tumor cell line.

Brigatinib's ability to inhibit key signaling pathways and its antitumor activity against various mutations, especially in the context of ALK-driven tumors, highlights its potential as a targeted therapy for certain types of cancer, particularly non-small cell lung cancer. These findings suggest a promising role for Brigatinib in the treatment of patients who have developed resistance to previous therapies, such as crizotinib.

Quick Suggestions:

• Limit sun exposure during Brigatinib treatment and for at least 5 days after the last dose. Brigatinib may increase sensitivity to sunlight, leading to a higher risk of sunburn.
• Protective Measures:
  • Wear a hat and protective clothing when in the sun.
  • Use a broad-spectrum sunscreen with SPF 30 or greater.
  • Apply lip balm with SPF protection.
• Refrain from consuming grapefruit or grapefruit juice while undergoing Brigatinib treatment. Grapefruit may impact Brigatinib levels in the blood, potentially affecting its efficacy or safety.

Indication of Alunib 90

Alunib 90 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

• Mechanism of Action: Brigatinib is a tyrosine kinase inhibitor with in vitro activity against multiple kinases, including ALK, ROS1, IGF-1R, FLT-3, EGFR, and more.
• Absorption: The median time to peak concentration (Tmax) ranges from 1 to 4 hours after single oral doses of Brigatinib.
• Distribution: Brigatinib is 66% bound to human plasma proteins, and 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, and the plasma elimination half-life is 25 hours.
• Metabolism: Primarily metabolized by CYP2C8 and CYP3A4, with N-demethylation and cysteine conjugation as major pathways.
• Excretion: About 65% of the administered dose is recovered in feces and 25% in urine, with unchanged Brigatinib being the major circulating component.

Dosage & Administration of Alunib 90

• Start with 90 mg orally once daily for the first 7 days.
• If tolerated, increase to 180 mg orally once daily.
• Safety and efficacy in pediatric patients not established.
• Administer until disease progression or unacceptable toxicity.
• If interrupted for 14 days or longer, resume at 90 mg once daily for 7 days before increasing.
• Tablets may be taken with or without food, swallowed whole, not crushed or chewed.

Interaction

• Increased Plasma Concentrations: Avoid strong CYP3A inhibitors.
• Decreased Plasma Concentrations: Avoid strong CYP3A inducers.
• Altered Plasma Concentrations: Induces CYP3A, and may decrease concentrations of CYP3A substrates.

Contraindications

Hypersensitivity to Brigatinib or any components.

Pregnancy & Lactation

• Pregnancy: Potential risk to the fetus.
• Lactation: Advised not to breastfeed during treatment.

Precautions & Warnings

• Interstitial Lung Disease (ILD)/Pneumonitis: Promptly evaluate new or worsening respiratory symptoms.
• Hypertension: Monitor blood pressure; withhold or discontinue for Grade 3 or 4 hypertension.
• Bradycardia: Monitor heart rate; caution with bradycardia-inducing agents.
• Visual Disturbance: Withhold, obtain an ophthalmologic evaluation for Grade 2 or greater severity.
• CPK Elevation: Monitor for muscle pain, tenderness, or weakness; withhold for Grade 3 or 4 CPK elevation.
• Pancreatic Enzyme Elevation: Monitor amylase and lipase; withhold for Grade 3 or 4 elevation.
• Hyperglycemia: Monitor serum glucose; adjust antihyperglycemic medications as needed.

Storage Conditions

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