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exisulind + gemcitabine
- Development stage
- Unknown
- Lead developer
- Cell Pathways
- 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
- Administration
- Oral, Intravenous
01
Overview
Exisulind is a selective apoptotic antineoplastic drug, also known as sulindac sulfone, which induces apoptosis in tumor cells. Gemcitabine is a nucleoside analog chemotherapy agent that inhibits DNA synthesis. The combination of exisulind and gemcitabine has been studied as second-line therapy for advanced non-small cell lung cancer (NSCLC) after progression on first-line chemotherapy. The regimen was generally well tolerated, with fatigue and constipation being the main dose-limiting toxicities. Response rates were modest, with median time to progression around 4 months and median overall survival about 9 months[1][2][3].
- Other names
- exisulind and gemcitabinegemcitabine and exisulind
02
Targets
DCK (Deoxycytidine kinase)RNR (Ribonucleotide reductase)ENT1 (Solute carrier family 29 member 1)DNA polymerase familyPDE6 (Phosphodiesterase 6)
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