Drug intelligence / Profile preview

E7449 + temozolomide

Development stage
Unknown
Lead developer
Allarity Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

E7449 + temozolomide is a **combination therapy** under clinical investigation for cancer treatment, comprising E7449—a small molecule dual inhibitor of poly(ADP-ribose) polymerase 1/2 (PARP1/2) and tankyrase 1/2 (TNKS1/2), and temozolomide, an oral alkylating chemotherapy agent. E7449 inhibits DNA repair mechanisms and disrupts Wnt/β-catenin signaling, thereby enhancing the cytotoxicity of DNA-damaging agents like temozolomide. The combination synergistically potentiates antitumor activity, demonstrated in preclinical melanoma models and evaluated in Phase 1/2 studies for advanced solid tumors and melanoma[3][5]. E7449 is developed by Eisai; temozolomide is off-patent and produced by multiple manufacturers.

Brand names
None
Other names
TMZE7449 + TMZ
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)DNATNKS (Poly(ADP-ribose) Polymerase 5a)TNKS2 (Tankyrase 2)

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