Drug intelligence / Profile preview

adozelesin

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Adozelesin is an experimental antitumor small molecule belonging to the duocarmycin class of antibiotics. It is a synthetic cyclopropylpyrroloindole (CPI) analog of CC-1065 that acts as a potent DNA alkylating agent. The drug binds covalently to the minor groove of double-stranded DNA, specifically at A-T-rich sequences, which results in the inhibition of DNA replication and transcription. Developed primarily by Upjohn (now Pfizer), adozelesin was evaluated in Phase 1 and Phase 2 clinical trials for various cancers, including melanoma, sarcoma, and lung carcinoma, but development was ultimately discontinued. Additionally, it has been researched for potential anti-malarial properties due to its high affinity for A-T-rich DNA sequences characteristic of the Plasmodium genome.

Other names
adolezesin
02

Targets

Double-stranded DNA minor groove at AT-rich sequences

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