ANG1005, a peptide conjugated to paclitaxel was granted ODD by the FDA for the treatment of breast cancer patients with brain metastases. ANG1005 is an Angiopep-2 paclitaxel conjugate that is under development by Angiochem, a biotechnology company based in Montreal, Canada. The Angiopep-2 peptide in ANG1005 can bind to low-density lipoprotein receptor-related protein-1 (LRP-1), a receptor expressed on the blood brain barrier (BBB). Via LRP-1-mediated transcytosis, ANG1005 crosses BBB and achieves brain penetration. Once inside the brain, ANG1005 enters tumor cells using the same receptor-mediated pathway through LRP-1, which is upregulated in various cancer cells and kills cancer cells via its paclitaxel moiety. Two Phase I trials have been conducted in patients with malignant glioma and in patients with advanced solid tumors with brain metastasis respectively. Currently, Phase II trials are ongoing for patients with brain metastasis from breast cancer and high grade glioma.