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paclitaxel trevatide
- Development stage
- Discontinued
- Lead developer
- Angiochem
- Modality
- Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Recombinant Proteins and Enzymes
- Administration
- Intravenous
01
Overview
Paclitaxel trevatide is a peptide-drug conjugate, composed of three molecules of the chemotherapeutic agent paclitaxel covalently linked by a cleavable ester to the proprietary 19-amino-acid peptide Angiopep-2. The conjugation allows for receptor-mediated transport across the blood-brain barrier (BBB) via low-density lipoprotein receptor-related protein 1 (LRP1), which is upregulated in many CNS tumors, including high-grade glioma and brain metastases. Once inside the cell, intracellular esterases release paclitaxel, which stabilizes microtubule formation by binding to β-tubulin, thereby halting mitosis and inducing apoptosis. This design enables paclitaxel delivery to the CNS, overcoming P-glycoprotein and multidrug resistance protein efflux mechanisms that limit standard paclitaxel efficacy in brain tumors. Clinical trials have shown activity in breast cancer patients with leptomeningeal carcinomatosis, recurrent brain metastases, glioblastoma, and other CNS malignancies[1][2][4][7][8].
- Brand names
- Paclitaxel trevatide
- Other names
- Paclitaxel trevatideANG1005ANG-1005ANG 1005GRN1005GRN-1005GRN 1005NG1005NG-1005NG 1005
02
Targets
LRP1 (Prolow-density lipoprotein receptor-related protein 1)TUBB (Tubulin (alpha and beta subunits))
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