Farletuzumab ecteribulin

Farletuzumab ecteribulin is an antibody-drug conjugate (ADC) consisting of the humanized antibody farletuzumab, which targets the folate receptor alpha (FRA), with an antibody-to-drug ratio of 4.0. In vitro, farletuzumab ecteribulin exhibits cytotoxic and antitumor activity against FRA-positive cells.

IGROV1 cells:1 nM, A431-A3 cells:2.3 μM, NCI-H2110 cells:74 nM

Methods: FRA-positive tumor cells were treated with farletuzumab ecteribulin (5.1 pM–10 μM) for 5 consecutive days.
Results: Farletuzumab ecteribulin showed potent cytotoxicity against FRA-positive cells, with an IC₅₀ of 1 nM in IGROV‑1 cells, 74 nM in NCI‑H2110 cells, and 2.3 μM in A431‑A3 cells [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