Farletuzumab ecteribulin (MORAb-202) is an antibody-drug conjugate (ADC), consisting of the humanized anti-human folate receptor alpha (FRA) antibody Farletuzumab conjugated via reduced interchain disulfide bonds to Mal-PEG2-Val-Cit-PAB-eribulin. Farletuzumab ecteribulin has a agent-to-antibody ratio of 4.0. Farletuzumab ecteribulin is highly cytotoxic to FRA-positive cells in vitro. Farletuzumab ecteribulin has potent antitumor activity.
Farletuzumab ecteribulin (MORAb-202; 5.1 pM-10 μM; 5 days) is highly cytotoxic to FRA-positive cells in vitro (IGROV-1: IC50=1 nM, NCI-H2110: IC50=74 nM, A431-A3: IC50=2.3 μM)[1].
Farletuzumab ecteribulin (MORAb-202; IV; single injection 1, 5 mg/kg at day 0 or 5 mg/kg every 11 days; 60 days) has a significant antitumor activity with once or twice 5 mg/kg[1]. Farletuzumab ecteribulin (2mg/kg; IV) has a T1/2s of 192 and 162 hours and AUC(0-t)s of 7160 and 6300 ug·h/mL for male and female cynomolgus monkeys on Day 1[1].
References:
[1]. Keiji Furuuchi, et al. Antibody-drug conjugate MORAb-202 exhibits long-lasting antitumor efficacy in TNBC PDx models. Cancer Sci. 2021 Jun;112(6):2467-2480.
[2]. Xin Cheng, et al. MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FRα Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018 Dec;17(12):2665-2675.