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tamoxifen + temozolomide
- Development stage
- Unknown
- Lead developer
- Rutgers Robert Wood Johnson Medical School
- Modality
- DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Tamoxifen + temozolomide is an investigational combination therapy consisting of tamoxifen, a selective estrogen receptor modulator with additional protein kinase C (PKC) inhibitory activity, and temozolomide, an oral alkylating agent. This combination has been studied primarily in the treatment of high-grade gliomas such as glioblastoma multiforme (GBM), particularly in recurrent or resistant cases. Tamoxifen may enhance the antitumor effect of temozolomide by inhibiting PKC-mediated pathways that contribute to tumor proliferation and chemoresistance. Preclinical studies have shown synergistic antiproliferative and pro-apoptotic effects when both drugs are used together. Clinical trials suggest this regimen is generally well tolerated but may increase risk for thromboembolic events[1][2][3][5][6].
- Other names
- tamoxifen and temozolomideTMX + TMZ
02
Targets
ND1 (Mitochondrial electron transport chain complex I)O6-G (DNA guanine O6 position)ESR1 (ERα)PKC (Protein kinase C family)
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