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Iniparib + temozolomide

Development stage
Unknown
Lead developer
Sanofi
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

**Iniparib + temozolomide** is a combination therapy investigated primarily for the treatment of malignant gliomas, including glioblastoma multiforme and anaplastic astrocytoma. Iniparib is a prodrug that converts intracellularly to highly reactive cytotoxic metabolites. Initially thought to be a poly (ADP-ribose) polymerase (PARP) 1 inhibitor, further research revealed that at clinically relevant concentrations it does not directly inhibit PARP-1 but instead forms non-specific adducts with cysteine residues on various proteins—including those involved in redox regulation—leading to increased production of reactive oxygen species and disruption of cellular redox homeostasis[2][3]. Temozolomide is an oral alkylating agent that exerts its antitumor effect by methylating DNA at several sites (notably N7 guanine, N3 adenine, and O6 guanine), resulting in DNA damage and tumor cell death[1][6][8]. The combination has been studied as adjuvant therapy following radiation for newly diagnosed malignant gliomas[2][3].

Brand names
Temodar
Other names
4-iodo-3-nitrobenzamide
02

Targets

DNA

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