Drug intelligence / Profile preview

erlotinib + temozolomide + vorinostat

Development stage
Discontinued
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of three small molecule drugs—erlotinib, temozolomide, and vorinostat—investigated primarily for the treatment of recurrent glioblastoma multiforme (GBM) and anaplastic gliomas. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling to inhibit tumor cell proliferation. Temozolomide is an oral alkylating agent that induces DNA damage in cancer cells, leading to apoptosis. Vorinostat is a histone deacetylase (HDAC) inhibitor that alters chromatin structure and gene expression, promoting cancer cell death or growth arrest. The rationale for combining these agents lies in their complementary mechanisms targeting tumor growth pathways, DNA integrity, and epigenetic regulation[1][9]. This combination has been evaluated in early-phase clinical trials to determine safety, tolerability, maximum tolerated dose (MTD), and preliminary efficacy in patients with recurrent GBM.

Other names
erlotinib plus temozolomide plus vorinostaterlotinib and temozolomide and vorinostat
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)DNAHDAC1/6 (Histone deacetylase 1 and Histone deacetylase 6)

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