Drug intelligence / Profile preview

NTX-301 + temozolomide

Development stage
Unknown
Lead developer
PinotBio
Modality
Small Molecules
Administration
Oral
01

Overview

**NTX-301 + temozolomide** is an investigational combination regimen under clinical evaluation for the treatment of certain advanced cancers, including high-grade glioma. **NTX-301** is a novel, oral hypomethylating agent (HMA), chemically known as 5-aza-4′-thio-2′-deoxycytidine, which acts as a DNA methyltransferase 1 (DNMT1) inhibitor, reactivating tumor suppressor genes by inducing DNA hypomethylation and leading to cell cycle arrest, apoptosis, and differentiation. **Temozolomide** is an alkylating agent that induces DNA damage and cytotoxicity in tumor cells. The combination is being tested particularly in IDH1-mutant high-grade glioma, as an adjuvant therapy following chemoradiation, intended to replace standard temozolomide maintenance therapy, and the aim is to improve efficacy through combined epigenetic modulation and direct cytotoxicity[1][9].

02

Targets

DNMT3A (DNA methyltransferase 3 alpha)DNMT1 (DNA (cytosine-5)-methyltransferase 1)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)

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