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aripiprazole + temozolomide
- Development stage
- Unknown
- Lead developer
- VSPharmTech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
VS-101 + temozolomide is an investigational drug combination consisting of VS-101 (a low-dose repurposed formulation of the atypical antipsychotic aripiprazole) and the standard-of-care chemotherapeutic agent temozolomide. Developed by VS Pharmtech, VS-101 functions as an oral radiosensitizer that enhances the efficacy of radiation therapy. At the molecular level, VS-101 downregulates key DNA damage repair (DDR) proteins, including RAD51 and PARP, and suppresses inhibitor of apoptosis proteins (IAPs) while promoting reactive oxygen species (ROS) generation. Temozolomide is an oral cytotoxic alkylating agent that induces DNA double-strand breaks. By combining VS-101 with temozolomide and radiotherapy, the regimen aims to prevent cancer cells from repairing treatment-induced DNA damage, thereby promoting tumor cell death. The combination is currently in Phase 2 clinical development for the treatment of glioblastoma.
- Other names
- temozolomide + VS-101temozolomide + aripiprazoleVS-101 + temozolomide
02
Targets
HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2A (Serotonin receptor 5-HT2A)DNADRD2 (Dopamine D2 Receptor)
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