Drug intelligence / Profile preview

KRT-232 + decitabine

Development stage
Discontinued
Lead developer
Kartos Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

KRT-232 + decitabine is an investigational pharmaceutical combination being studied for the treatment of acute myeloid leukemia (AML), especially in relapsed/refractory or newly diagnosed patients not eligible for intensive chemotherapy. KRT-232, also known as navtemadlin or AMG-232, is a small molecule inhibitor of MDM2, a negative regulator of p53 tumor suppressor. By inhibiting MDM2, KRT-232 reactivates p53, promoting apoptosis in cancer cells with wild-type TP53. Decitabine is a hypomethylating agent (nucleoside analog) that inhibits DNA methyltransferase and is used to induce DNA hypomethylation and promote differentiation or apoptosis of abnormal hematopoietic cells. The combination aims to synergistically induce cancer cell death through epigenetic modulation (decitabine) and p53 pathway reactivation (KRT-232).

02

Targets

DNMT (DNA methyltransferase)MDM2 (Mouse double minute 2 homolog)DNA

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