Drug intelligence / Profile preview

venetoclax + artemisinin

Development stage
Preclinical
Lead developer
Shenyang Pharmaceutical University
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
01

Overview

Venetoclax + artemisinin refers to a series of novel chemical conjugates (such as A19, A20, and A21-A23) that link the Bcl-2 inhibitor venetoclax with dihydroartemisinin (DHA), a derivative of artemisinin. These conjugates are designed to overcome resistance in acute myeloid leukemia (AML) by simultaneously inhibiting Bcl-2 and promoting the NOXA-mediated degradation of Mcl-1. Developed by researchers at Shenyang Pharmaceutical University and the Samuel Waxman Institute for Aging and Cancer, these next-generation derivatives utilize optimized linkers, including polyethylene glycol (PEG) units and nitrogen-containing polar groups, to improve water solubility and bioavailability compared to earlier versions. Preclinical studies have demonstrated that these conjugates exhibit potent antileukemic effects, including inhibition of colony formation and significant tumor growth suppression in vivo.

Other names
venetoclax-artemisinin conjugatesvenetoclax-dihydroartemisinin conjugates
02

Targets

BCL2L1 (B-cell lymphoma-extra large protein)MYC (MYC proto-oncogene protein)MCL1 (Myeloid cell leukemia sequence 1)

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