Drug intelligence / Profile preview

temozolomide + tipifarnib

Development stage
Unknown
Lead developer
Kura Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Temozolomide + tipifarnib is an investigational combination therapy consisting of two small molecule drugs used primarily in the treatment of glioblastoma and other high-grade gliomas. Temozolomide is an oral alkylating agent that induces DNA damage, leading to tumor cell death. Tipifarnib is a selective farnesyltransferase inhibitor that blocks the post-translational modification of proteins such as RAS, thereby inhibiting signaling pathways essential for tumor cell growth and survival. The combination has been studied in clinical trials alongside radiation therapy to assess safety, tolerability, and efficacy in newly diagnosed glioblastoma patients[6][1][2][3]. Both agents act through distinct mechanisms—temozolomide by direct cytotoxicity via DNA methylation and tipifarnib by targeting oncogenic signaling pathways.

Brand names
Zarnestra (for tipifarnib)Temodal (for temozolomide)Temodar (for temozolomide)Temomedac (for temozolomide)
Other names
tipifarnib + temozolomide
02

Targets

DNAFTase (Protein Farnesyltransferase)

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