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OncoFAP-GlyPro-monomethyl auristatin E
- Development stage
- Preclinical
- Lead developer
- Philochem
- Modality
- Prodrugs/Conditional Activator Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
OncoFAP-GlyPro-monomethyl auristatin E is a Fibroblast Activation Protein (FAP)-targeted conjugate developed by Philochem for veterinary oncology applications. It utilizes the OncoFAP ligand, a high-affinity small molecule that selectively binds to FAP, which is overexpressed in the stroma of most solid tumors. The conjugate features a monomethyl auristatin E (MMAE) payload attached via a Glycine-Proline (GlyPro) dipeptide linker. This specific linker is designed to be cleaved by the enzymatic (dipeptidyl peptidase) activity of FAP itself, allowing for the targeted release of the cytotoxic MMAE within the tumor microenvironment. This approach aims to maximize anti-tumor efficacy while minimizing systemic side effects. The drug is currently in preclinical development and being evaluated in veterinary clinical trials for dogs with various solid tumors.
- Other names
- OncoFAP-GlyPro-monomethyl auristatin EOncoFAP-MMAEFAP-targeted MMAE conjugate
02
Targets
TUBB (Tubulin (alpha and beta subunits))FAP (Fibroblast activation protein alpha)
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