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S-1 + nal-IRI
- Development stage
- Unknown
- Lead developer
- Ipsen
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Oral, Intravenous
01
Overview
S-1 + nal-IRI is a combination therapy consisting of two agents: - **S-1** is an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-fluorouracil), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (which reduces gastrointestinal toxicity). It acts as an antimetabolite by inhibiting DNA synthesis in rapidly dividing cancer cells. - **nal-IRI** (liposomal irinotecan) is a liposome-formulated version of irinotecan, a topoisomerase I inhibitor. The liposomal formulation enhances delivery to tumor tissue and prolongs systemic exposure. This combination has been investigated primarily for the treatment of advanced or metastatic pancreatic adenocarcinoma, particularly as second-line therapy after progression on gemcitabine-based regimens. The mechanism involves dual cytotoxic effects via inhibition of DNA synthesis and topoisomerase I activity. Clinical trials have evaluated its safety and efficacy compared to other regimens such as nal-IRI plus 5-FU/leucovorin[5].
- Brand names
- OnivydeTeysuno
- Other names
- liposomal irinotecan + S-1nanoliposomal irinotecan + S-1
02
Targets
TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)
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