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cabozantinib

Brand and Other Names: CABOMETYX
Mechanism of Action:

Cabozantinib is a multi-kinase inhibitor targeting MET, VEGFR-1/2/3, AXL, RET, ROS1, and others—interfering with tumor growth, angiogenesis, and metastatic progression.

Indications:

CABOMETYX is indicated for:

Renal Cell Carcinoma (RCC)

    • As monotherapy for advanced RCC.

    • First-line treatment in combination with nivolumab.

Hepatocellular Carcinoma (HCC)

    • For patients previously treated with sorafenib.

Differentiated Thyroid Cancer (DTC)

    • For patients aged 12+ with locally advanced/metastatic DTC after VEGFR-targeted therapy and who are RAI-refractory or ineligible.

Neuroendocrine Tumors (NETs)

    • Pancreatic (pNET) and Extra-pancreatic (epNET), previously treated, unresectable, locally advanced, or metastatic.

    • Approved for adults and pediatric patients aged 12+.

Route: oral
Dose:

Monotherapy (RCC, HCC, DTC, NET) - 60 mg once daily

Combination (with nivolumab for RCC) - CABOMETYX 40 mg daily + nivolumab 240 mg q2w or 480 mg q4w

Pediatric (<40 kg) - 40 mg once daily

Adverse Reactions:

Monotherapy:

  • ≥20%: Diarrhea, fatigue, PPE, appetite loss, hypertension, nausea, vomiting.

With Nivolumab:

  • Added risk of: Hepatotoxicity, stomatitis, rash, hypothyroidism, musculoskeletal pain, URTIs.

Contraindication:

None

Warnings and Precautions:

CABOMETYX has a broad array of potential serious side effects, including:

  • Hemorrhage (discontinue if Grade 3 or 4)
  • GI perforations and fistulas
  • Thromboembolic events
  • Hypertension/hypertensive crisis
  • Diarrhea and Palmar-Plantar Erythrodysesthesia (PPE)
  • Hepatotoxicity (especially with nivolumab)
  • Adrenal insufficiency, thyroid dysfunction, hypocalcemia
  • Osteonecrosis of the jaw, impaired wound healing
  • Reversible Posterior Leukoencephalopathy Syndrome (RPLS)
See package insert for full prescribing information.