Drug intelligence / Profile preview

S-1 + osimertinib

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

S-1 + osimertinib is a combination therapy under investigation for the treatment of non-small cell lung cancer (NSCLC). Osimertinib is an oral, third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that selectively targets both EGFR-sensitizing and T790M-resistance mutations. It works by blocking the action of abnormal EGFR proteins that drive cancer cell proliferation, thereby slowing or stopping tumor growth[2][5][6]. Osimertinib also exhibits inhibitory activity against other kinases such as HER2, HER3, HER4, ACK1, and BLK[5]. S-1 is an oral fluoropyrimidine-based chemotherapy agent composed of tegafur (a prodrug of 5-fluorouracil), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase), and oteracil potassium (which reduces gastrointestinal toxicity). The combination aims to leverage the targeted inhibition provided by osimertinib with the cytotoxic effects of S-1 to enhance antitumor efficacy in NSCLC.

Other names
osimertinib mesylate
02

Targets

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