Drug intelligence / Profile preview

gemcitabine + tipifarnib

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

Overview

Gemcitabine + tipifarnib is a combination of two small molecule chemotherapeutic agents used in clinical trials for the treatment of advanced solid tumors and pancreatic cancer. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by being incorporated into DNA during replication and inhibiting ribonucleotide reductase, leading to masked chain termination and apoptosis of malignant cells. Tipifarnib (R115777) is an orally available farnesyltransferase inhibitor that blocks the post-translational modification (farnesylation) of proteins such as Ras, thereby interfering with signal transduction pathways involved in tumor growth. The combination has been evaluated for synergistic antitumor activity but did not show significant improvement in overall survival compared to single-agent gemcitabine in phase III trials for pancreatic cancer[2][3][5].

Brand names
GemzarZarnestra
Other names
gemcitabine hydrochlorideR115777R-115777R 115777tipifarnib
02

Targets

DNA polymerase familyRNR (Ribonucleotide reductase)FTase (Protein Farnesyltransferase)

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