Evaluation of CNS and peripheral antitumor activity of ANG1005 in patients with brain metastases from breast tumors and other advanced solid tumors.

2523 Background: ANG1005 consists of 3 paclitaxel molecules covalently linked to a proprietary 19 AA peptide that targets the LRP1 receptor. This receptor is highly expressed on endothelial cells of the blood-brain barrier, where it mediates transcytosis, and on multiple tumor cells, where it mediates endocytosis. Thus, ANG1005 is both brain-penetrant and tumor-penetrant due to the LRP1-targeting peptide moiety. Methods: Ph I: Patients with advanced solid tumors and brain metastases received ANG1005 by IV infusion q3w at escalating doses of 30-700 mg/m2 (n=56), including 20 patients at 650 mg/m2 (MTD). Study objectives included safety/tolerability and overall tumor response (CNS and peripheral). Ph II: Patients with breast cancer brain metastases received ANG1005 by IV infusion q3w at a starting dose of 650 mg/m2 (n=13) or 550 mg/m2 (n=67). Study objectives included independent CNS and peripheral tumor response evaluations as per RECIST 1.1. Results: Safety and tolerability of ANG1005 were consistent with...