Cabozantinib (CAS No.: 849217-68-1) 

1. Basic Information

• Chemical Name: N-(4-(6,7-Dimethoxyquinolin-4-yloxy)phenyl)-N’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
• Molecular Formula: C₂₈H₂₄FN₃O₅
• Molecular Weight: 501.51 g/mol
• Appearance: White to off-white crystalline powder
• Solubility: Slightly soluble in water, soluble in organic solvents (e.g., DMSO, ethanol)

2. Mechanism of Action

Cabozantinib is a multi-targeted tyrosine kinase inhibitor (TKI) that primarily inhibits:

• MET
• VEGFR2 (Vascular Endothelial Growth Factor Receptor 2)
• RET
• AXL
• ROS1

By blocking these signaling pathways, cabozantinib suppresses tumor cell proliferation, angiogenesis, and metastasis.

3. Indications

• Medullary Thyroid Cancer (FDA-approved, 2012)
• Advanced Renal Cell Carcinoma (RCC) (FDA-approved, 2016)
• Hepatocellular Carcinoma (HCC) (FDA-approved, 2019)
• Other Solid Tumors (e.g., prostate cancer, bone metastases; investigational uses in clinical trials)

4. Dosage Forms & Strengths

• Tablets: 20 mg, 40 mg, 60 mg (Brand names: Cometriq®, Cabometyx®)
• Recommended Dosage: Typically 60 mg once daily (taken on an empty stomach).

5. Adverse Effects

Common side effects include:

• Diarrhea, decreased appetite
• Palmar-plantar erythrodysesthesia (hand-foot syndrome)
• Hypertension, fatigue
• Elevated liver enzymes

6. Precautions & Warnings

• Monitoring Required: Blood pressure, liver function, and thyroid function tests.
• Drug Interactions: Strong CYP3A4 inhibitors or inducers may alter plasma concentrations.
• Contraindications: Pregnancy (embryotoxic potential).

7. Research & Market Status

• Originator: Exelixis (USA)
• Patent Status: Some patents have expired, leading to generic versions in certain markets.

8. Storage Conditions

• Store in a tightly sealed container, protected from light, at ≤25°C。

 

Property	Details
Chemical Name	N-(4-(6,7-Dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Molecular Formula	C28H24FN3O5
Molecular Weight	501.506 g/mol
Density	1.4 ± 0.1 g/cm³
Boiling Point	758.1 ± 60.0 °C at 760 mmHg
Solubility	Practically insoluble in water; soluble in DMSO
Storage Conditions	Sealed in dry, room temperature

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