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AVA3996
- Development stage
- Preclinical
- Lead developer
- Avacta
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
01
Overview
AVA3996 is a tumor-targeted proteasome inhibitor prodrug being developed by Avacta Group plc using their proprietary pre|CISION™ technology. The drug consists of a proteasome inhibitor warhead, AVA2727D, covalently bonded to a peptide substrate containing a D-Ala-L-Pro cleaving sequence. This sequence is specifically recognized and cleaved by Fibroblast Activation Protein (FAP), an enzyme highly overexpressed in the tumor microenvironment of over 90% of malignant epithelial cancers. Designed as a FAP-activated analogue of bortezomib (Velcade), AVA3996 aims to reduce the systemic toxicities associated with traditional proteasome inhibitors while maintaining anti-cancer efficacy. It is currently in pre-clinical development for the treatment of multiple myeloma and solid tumors, such as pancreatic cancer.
- Other names
- Pro-Velcade
02
Targets
26S proteasomeFAP (Fibroblast activation protein alpha)
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