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cytarabine + osimertinib + temozolomide

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intrathecal, Subcutaneous
01

Overview

This is a combination regimen consisting of three small molecule chemotherapeutic agents: cytarabine, osimertinib, and temozolomide. Cytarabine is an antimetabolite that inhibits DNA synthesis by acting as a cytosine analog, primarily used in the treatment of leukemias. Osimertinib is an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that irreversibly binds to mutant forms of EGFR, including T790M mutation, and is approved for non-small cell lung cancer with specific EGFR mutations. Temozolomide is an oral alkylating agent that methylates DNA at the O6 and N7 positions of guanine residues, leading to DNA damage and apoptosis; it crosses the blood-brain barrier and is primarily used for brain tumors such as glioblastoma multiforme[1][3][5]. This combination may be considered in investigational or off-label settings for aggressive or refractory cancers where multiple mechanisms are targeted simultaneously.

Other names
TemodalAra-C
02

Targets

DNA polymerase familyN7-G (DNA guanine-N7 adduct)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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