Drug intelligence / Profile preview

USP24-i-101 + astemizole

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

USP24-i-101 + astemizole is an experimental drug combination investigated for overcoming drug resistance in cancer, especially lung cancer. **USP24-i-101** is a small molecule inhibitor of the deubiquitinase USP24, which modulates autophagy, genomic instability, and immune evasion in drug-resistant cancer cells by increasing PD-L1 protein degradation and stabilizing the genome in an autophagy-dependent manner. **Astemizole** is a second-generation, long-acting, non-sedating antihistamine that functions primarily as a histamine H1 receptor antagonist, previously used for allergy symptoms but withdrawn due to cardiac toxicity (QT prolongation via hERG blockade). Recent studies have shown that, in combination, USP24-i-101 and astemizole synergistically re-sensitize drug-resistant lung cancer cells to therapies such as Taxol and Gefitinib, enhancing cytotoxicity and inhibiting drug resistance[1][3][9].

Brand names
Hismanal
Other names
USP24-i-101USP-24-i-101USP 24-i-101R43512R-43512R 43512
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)USP24 (Ubiquitin carboxyl-terminal hydrolase 24)HRH1 (Histamine H1 Receptor)

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