ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system.
ANG1005 shows significantly improved delivery to brain and brain metastases of breast cancer compared to free paclitaxel [1].
References:
[1]. Thomas FC, et al. Uptake of ANG1005, a novel paclitaxel derivative, through the blood-brain barrier into brain and experimental brain metastases of breast cancer. Pharm Res. 2009 Nov;26(11):2486-94.
[2]. Li F, et al. Targeting metastatic breast cancer with ANG1005, a novel peptide-paclitaxel conjugate that crosses the blood-brain-barrier (BBB). Genes Dis. 2017 Feb 10;4(1):1-3.
[3]. Kumthekar P, et al. ANG1005, a Brain-Penetrating Peptide-Drug Conjugate, Shows Activity in Patients with Breast Cancer with Leptomeningeal Carcinomatosis and Recurrent Brain Metastases. Clin Cancer Res. 2020 Jun 15;26(12):2789-2799.