Drug intelligence / Profile preview

Apatinib + S-1

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Apatinib + S-1 is a combination therapy used primarily in the treatment of advanced or metastatic cancers, especially gastric cancer and metastatic colorectal cancer. Apatinib is an oral small molecule tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptor 2 (VEGFR2), thereby blocking angiogenesis and reducing tumor blood supply. S-1 is an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-fluorouracil), gimeracil, and oteracil potassium; it acts as a cytotoxic antimetabolite interfering with DNA synthesis in rapidly dividing cells. The combination has shown promising efficacy and manageable toxicity as second-line or later therapy for advanced gastric cancer (AGC) and refractory metastatic colorectal cancer (mCRC), particularly in patients who have failed prior lines of chemotherapy[1][2][3][4][5]. Clinical studies indicate improved disease control rates, progression-free survival, and overall survival compared to monotherapy with either agent[1][3][4]. The regimen is under investigation in various clinical settings.

Brand names
YN968D1 (for apatinib)None (S-1 is generally referred to by this name)
Other names
None
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)

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