Drug intelligence / Profile preview

rubitecan + gemcitabine

Development stage
Unknown
Lead developer
Supergene
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Combination of **rubitecan** (an oral camptothecin derivative, specifically a topoisomerase I inhibitor) and **gemcitabine** (a nucleoside analog) developed as combination chemotherapy for advanced solid tumors, particularly pancreatic cancer. Rubitecan inhibits topoisomerase I, causing single-strand DNA breaks, and is oral; gemcitabine interferes with DNA synthesis and repair as a pyrimidine antimetabolite, administered intravenously. This combination has shown activity in pancreatic and other solid tumors and has undergone Phase I–II testing, with established doses and some evidence for disease stabilization and response in gemcitabine-refractory cancers[1][2][3][4][5].

Other names
9-nitrocamptothecin9NCRFS 2000RFS2000RFS-2000deoxycytidine (for gemcitabine)
02

Targets

DNA polymerase familyTOP1 (DNA Topoisomerase I)RRM1

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