drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
Antibody–drug conjugate of farletuzumab linked to eribulin; targets FRα on tumor cells to deliver eribulin intracellularly, disrupting microtubules and inducing apoptosis.
nci_thesaurus_concept_id
C173946
nci_thesaurus_preferred_term
Farletuzumab Ecteribulin
nci_thesaurus_definition
An antibody drug conjugate (ADC) composed of farletuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the folate receptor alpha (FRA; FolRa; FOLR1), and conjugated, via a cathepsin B-cleavable linker, to the microtubule-targeting agent (MTA) eribulin, a derivative of the macrocyclic polyether natural product halichondrin B, with potential antineoplastic activity. Upon administration of farletuzumab ecteribulin, the farletuzumab moiety targets and binds to FRA expressed on certain tumor cells. Upon binding, internalization, and enzymatic cleavage, eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and the induction of tumor cell death in FRA-expressing cells. FRA is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.
drug_mesh_term
MORAb-202
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
FRα-targeted ADC: farletuzumab binds folate receptor‑α on tumor cells and is internalized; a cathepsin B–cleavable linker releases eribulin intracellularly, which binds the vinca domain of tubulin to inhibit microtubule polymerization, causing G2/M mitotic arrest and apoptosis (with potential bystander effect).
drug_name
MORAb-202
nct_id_drug_ref
NCT05613088