Drug intelligence / Profile preview

2-methoxyestradiol + temozolomide

Development stage
Unknown
Lead developer
Cancer Research UK
Modality
Small Molecules
Administration
Oral
01

Overview

**2-methoxyestradiol + temozolomide** is a combination therapy investigated primarily for the treatment of recurrent glioblastoma multiforme (GBM). 2-methoxyestradiol (2ME2) is a natural estradiol metabolite with antineoplastic properties, functioning mainly through inhibition of hypoxia-inducible factor 1-alpha (HIF1α), microtubule disruption, and antiangiogenic activity, leading to cell cycle arrest and apoptosis[1][4][5]. Temozolomide is an oral alkylating agent that induces DNA damage causing tumor cell death[6]. The combination has been evaluated in Phase II clinical trials for recurrent GBM, aiming to leverage synergistic inhibition of tumor proliferation, angiogenesis, and enhancement of apoptosis through complementary mechanisms of both agents[5][4]. 2ME2’s clinical efficacy is suggested to be modulated by PTEN-PI3K pathway status, and temozolomide remains a cornerstone chemotherapeutic for gliomas[1][3][5]. This combination is not approved for any indication but represents a research therapeutic approach in oncology, especially for high-grade gliomas.

Brand names
Panzem Nanocrystal Colloidal Dispersion + Temozolomide
Other names
2ME2 + TMZ
02

Targets

DNA

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