Drug intelligence / Profile preview

duocarmycin SA

Development stage
Unknown
Lead developer
Byondis
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

Duocarmycin SA is a highly potent antitumor antibiotic, originally isolated from Streptomyces bacteria. It belongs to the duocarmycin class of DNA minor groove-binding alkylating agents. It exerts its cytotoxic effects by sequence-selectively and irreversibly alkylating adenine at the N3 position within the minor groove of DNA. This action disrupts DNA architecture, inhibits replication and transcription, and ultimately leads to cell death, often through apoptosis. Known for its extreme cytotoxicity with picomolar IC50 values, duocarmycin SA is a powerful antineoplastic compound. Its exceptional potency makes it a valuable payload in antibody-drug conjugates (ADCs) for targeted cancer therapies, aiming to deliver the cytotoxic agent directly to cancer cells while minimizing systemic toxicity. It has also been investigated for its ability to sensitize glioblastoma multiforme (GBM) cells to proton radiation.

Other names
DSA
02

Targets

Adenine-Thymine-rich duplex DNA

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