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Inlyta (Axitinib)
Axitinib inhibits VEGFR-1, VEGFR-2, and VEGFR-3 to block pathologic angiogenesis and tumor growth.
Axitinib is a receptor tyrosine kinase inhibitor indicated for first-line treatment of advanced RCC in combination with avelumab or pembrolizumab, and as monotherapy for second-line advanced RCC. The drug demonstrates selective inhibition of VEGFR-1, VEGFR-2, and VEGFR-3 with a half-life of 2.5-6.1 hours and 58% oral bioavailability. Primary risks include significant drug interactions with CYP3A4/5 inhibitors and inducers requiring dose adjustments or avoidance. Axitinib represents an important treatment option for advanced RCC with established efficacy in combination immunotherapy regimens.
At a glance
| Generic name | Axitinib |
|---|---|
| Sponsor | Pfizer |
| Drug class | Receptor tyrosine kinase inhibitor |
| Target | Vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, VEGFR-3 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2012 |
Mechanism of action
Axitinib is a receptor tyrosine kinase inhibitor that selectively targets VEGFR-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression. VEGF-mediated endothelial cell proliferation and survival were inhibited by axitinib in vitro and in mouse models. Axitinib was shown to inhibit tumor growth and phosphorylation of VEGFR-2 in tumor xenograft mouse models.
Approved indications
- Renal cell carcinoma
Common side effects
- Diarrhoea
- Hypertension
- Fatigue
- Nausea
- Hypothyroidism
- Palmar-plantar erythrodysaesthesia syndrome
- Decreased appetite
- Dysphonia
- Cough
- Arthralgia
- Alanine aminotransferase increased
- Aspartate aminotransferase increased
Drug interactions
- Strong CYP3A4/5 inhibitors (e.g., ketoconazole)
- Grapefruit or grapefruit juice
- Strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarbital, St. John's wort)
- Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin)
- Antacids
Key clinical trials
- Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
- A Study to Evaluate the Bioavailability of Pembrolizumab (MK-3475) Via Subcutaneous (SC) Injection of Pembrolizumab Formulated With Berahyaluronidase Alfa (MK-5180) [MK-3475A] In Advanced Solid Tumors (MK-3475A-C18) (PHASE1)
- A Study of Sasanlimab, Palbociclib and Axitinib in Metastatic Renal Cell Carcinoma (PHASE2)
- Drug Screening Using Novel IMD in Renal Cell Carcinoma (PHASE1)
- Neoadjuvant of Axitinib Plus PD-1 to Improve Disease Free Survival of Patients With Renal Cell Carcinoma (PHASE3)
- A Study to Evaluate the Efficacy and Safety of OTX-TKI (Axitinib Implant) in Participants With Non-Proliferative Diabetic Retinopathy (PHASE3)
- Talazoparib and Palbociclib, Axitinib, or Crizotinib for the Treatment of Advanced or Metastatic Solid Tumors, TalaCom Trial (PHASE1)
- An Open-label, Randomized Phase 2 Clinical Trial to Evaluate the Efficacy and Safety of the Combination Therapy of SLC-3010 and Axitinib Compared to Axitinib Monotherapy as a Second-line Treatment for Locally Advanced or Metastatic Clear Cell Renal Cell Carcinoma (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |