Drug intelligence / Profile preview

AVA6000

Development stage
Phase 1
Lead developer
Avacta
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

AVA6000 is a peptide drug conjugate and a prodrug of doxorubicin, developed using Avacta's proprietary pre|CISION technology. It is designed to be selectively activated in the tumor microenvironment by fibroblast activation protein alpha (FAP), which is upregulated in most solid tumors but not in healthy tissues. The drug consists of a doxorubicin molecule covalently bonded to a dipeptide linker that is specifically cleaved by FAP, releasing active doxorubicin at the tumor site while minimizing systemic exposure and toxicity. This targeted approach aims to reduce the dose-limiting toxicities associated with conventional doxorubicin therapy, such as myelosuppression and cardiotoxicity, while maintaining or enhancing antitumor efficacy. The primary mechanism of action after activation involves DNA intercalation and inhibition of type II DNA topoisomerase, leading to apoptotic cell death in cancer cells[3][5][6][9]. AVA6000 has shown promising results in early clinical trials for several solid tumors—particularly salivary gland cancers—with meaningful tumor shrinkage and improved safety profile compared to standard chemotherapy[4][6][8][10]. The FDA has granted orphan drug designation for soft tissue sarcoma[5][7].

Brand names
FAP-Dox
Other names
AVA6000 pro-DoxorubicinAVA-6000 pro-DoxorubicinAVA 6000 pro-Doxorubicin
02

Targets

TOP2A (DNA topoisomerase II)FAP (Fibroblast activation protein alpha)

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