Evaluation of the efficacy of axitinib/axitinib in the treatment of renal cancer

Axitinib/Axitinib (Axitinib) is a targeted therapy drug specifically for renal cell carcinoma. Its main mechanism is to exert anti-tumor effects by inhibiting tyrosine kinases such as vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor-α (PDGFR-α) and c-kit. The results of the clinical phase I study showed that the recommended starting dose was 5 mg twice daily, and significant efficacy was observed in patients with renal cell carcinoma. This finding was further confirmed in the subsequent phase II trial.

In the international randomized phase III clinical trial AXIS, the therapeutic effects of axitinib and sorafenib were compared. The study involved 723 patients with metastatic kidney cancer who were randomly assigned to axitinib or sorafenib. The results showed that the median progression-free survival time in the axitinib group was 6.7 months, while that in the sorafenib group was 4.7 months (P<.0001). Axitinib showed clinical benefit regardless of prior treatment, although no significant improvement in overall survival was observed.

In terms of tolerability, axitinib showed good safety and had no significant impact on patients' quality of life. Common Grade 3 adverse reactions included hypertension (16%), diarrhea (11%), and fatigue (11%). Other side effects include anorexia, nausea, hand-foot syndrome and rash. The study also found that median overall survival and overall response rate with axitinib were significantly longer in patients with diastolic blood pressure above 90 mmHg. Therefore, if a patient's blood pressure does not rise significantly during treatment, the manufacturer recommends that the twice-daily dose may be increased to 7 mg or 10 mg to improve tolerability.

In terms of pharmacokinetics, axitinib reaches peak plasma concentrations 2 to 6 hours after dosing and reaches steady state after 15 days. The study noted that the median plasma exposure of the drug was higher in the fasting state, so patients were advised to take 5 mg orally twice daily in the fasting state. In a phase I evaluation, 2 of 6 patients with renal cell carcinoma achieved objective partial responses, further demonstrating the activity of axitinib in the treatment of renal cell carcinoma.

Reference materials:https://pmc.ncbi.nlm.nih.gov/articles/PMC4334173/