Farletuzumab ecteribulin (MORAb-202) is a highly cytotoxic antibody-drug conjugate (ADC) targeting human folate receptor alpha (FRA). This ADC comprises the humanized Farletuzumab antibody linked to Mal-PEG2-Val-Cit-PAB-eribulin through reduced interchain disulfide bonds, with an agent-to-antibody ratio of 4.0, demonstrating potent antitumor activity against FRA-positive cells in vitro.

Farletuzumab ecteribulin (MORAb-202; 5.1 pM-10 μM; 5 days) demonstrates potent in vitro cytotoxicity against FRA-positive cells (IGROV-1: IC50=1 nM, NCI-H2110: IC50=74 nM, A431-A3: IC50=2.3 μM) [1].

Farletuzumab ecteribulin (MORAb-202; intravenous administration; a single injection of 1, 5 mg/kg on Day 0; or injections of 5 mg/kg every 11 days for a total of 2 doses; 60 days) demonstrated significant antitumor activity at one or two doses of 5 mg/kg [1]. With a dosage of 2 mg/kg intravenously, the half-life (T1/2) of farletuzumab ecteribulin on Day 1 was 192 hours in male and 162 hours in female cynomolgus monkeys, with corresponding AUC (0-t) values of 7160 and 6300 µg·h/mL, respectively [1].

Human

Monoclonal