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.