Drug intelligence / Profile preview

ZE50-0134 + itraconazole

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

Overview

ZE50-0134 + itraconazole is a combination of two drugs used experimentally, primarily in hematologic malignancies. ZE50-0134 (also known as eiletoclax) is a novel, highly selective small molecule inhibitor of BCL2, a key anti-apoptotic protein overexpressed in several cancers. ZE50-0134 has shown greater selectivity for BCL2 over BCL-xL compared to venetoclax, leading to less immunosuppression and improved safety in preclinical models. It binds to the P2 pocket of BCL2, inducing apoptosis in malignant cells. Itraconazole is a well-established antifungal agent and a strong CYP3A inhibitor, occasionally co-administered to study pharmacokinetic interactions because many BCL2 inhibitors (like venetoclax) are metabolized by CYP3A enzymes. The combination may be used clinically to assess safety and pharmacokinetic modulation or for managing fungal infections during anti-leukemic therapy[1][4].

Other names
eiletoclax + itraconazole
02

Targets

BCL-2 (BCL-2 family)CYP51A1 (Sterol 14α-demethylase)CYP3A (CYP3A family)

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