Axitinib is an oral small molecule tyrosine kinase inhibitor primarily used as second-line therapy for advanced renal cell carcinoma, blocking tumor angiogenesis by specifically inhibiting the vascular endothelial growth factor receptor (VEGFR). It has precise targeting and significant anti-tumor effects, suitable for personalized treatment of specific populations.

1. Basic information of the drug

Axitinib was developed by Pfizer and approved for market by the FDA in January 2012 under the trade name Inlyta. As a second-generation VEGFR inhibitor, its molecular weight is smaller than that of the first generation drugs, and it has stronger target selectivity and inhibitory efficacy.

2. Mechanism of action

Selective inhibition of VEGFR-1/2/3 tyrosine kinase activity, blocking VEGF mediated angiogenesis signaling pathway. By reducing the microvascular density of tumor tissue, it effectively inhibits the proliferation and metastasis of cancer cells.

3 Indications Scope

(1) Monotherapy: Used for advanced renal cell carcinoma that has previously failed to receive sunitinib or cytokine therapy; (2) Combination therapy: extended to first-line treatment with PD-1 inhibitors, significantly improving the objective remission rate to over 55%.

4 Pharmacokinetic characteristics

The oral bioavailability is about 58%, and the peak time of blood drug concentration is 2-6 hours. Metabolized by CYP3A4/5 in the liver, with a half-life of 2-5 hours. A high-fat diet can reduce AUC by 19%, and it is recommended to take it on an empty stomach.

5 Usage and Dosage Standards

The initial dose is 5mg twice a day, taken on an empty stomach. According to tolerance, the dosage can be gradually increased to 10mg or decreased to 3mg. For patients with liver dysfunction, a 50% reduction is required without adjusting the dosage for elderly patients.

6 Adverse Reaction Management

Common symptoms include hypertension (40%), diarrhea (55%), and fatigue (39%). Regular monitoring of blood pressure is required. In case of grade 3 toxicity, medication should be suspended until it returns to ≤ grade 1.