← AtlasFarletuzumab ecteribulin
InvestigationalMORAb-202; FZEC; ER-001159569; VCP-Eribulin; eribulin/farletuzumab ADC
Sponsor
Eisai (Morphotek); Bristol Myers Squibb
Indication
FOLR1+ platinum-resistant ovarian cancer
Target family
GPI-anchored
RP2D dose
0.9 mg/kgQ3WRP2D
01Multi-organ toxicity
Fingerprint & organ drill-down
Also reported
3 adverse-event terms
Ocular
sagittal schematic · Unknown
↳Tissues shaded by reported adverse-event rate.
Reported ocular events
Eye disorders (SOC, PT not specified)9%
02Construct
Molecular anatomy
Linker structureC29H42N6O9
[H]OC([H])([H])c1c([H])c([H])c(N(C(=O)C([H])(N([H])C(=O)C([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])N2C(=O)C([H])=C([H])C2=O)C([H])(C([H])([H])[H])C([H])([H])[H])C(=O)N([H])[H])c([H])c1[H]
Payload structureC40H59NO11
C[C@@H]1C[C@@H]2CC[C@H]3C(=C)C[C@@H](O3)CC[C@]45C[C@@H]6[C@H](O4)[C@H]7[C@@H](O6)[C@@H](O5)[C@@H]8[C@@H](O7)CC[C@@H](O8)CC(=O)C[C@H]9[C@H](C[C@H](C1=C)O2)O[C@@H]([C@@H]9OC)C[C@@H](CN)O
03Antibody
Antibody & Fc engineering
Linker
Mal-PEG2-Val-Cit-PAB
Attachment
Cysteine (interchain)
Conjugation
Conventional interchain Cys (maleimide; reduced disulfides; ADCdb 'Random Cysteines')
DAR homogeneity
Heterogeneous
Cleavage trigger
Cathepsin B (Val-Cit)
Release control
Conditional
Hydrophilicity mask
Discrete-PEG-spacer
Mechanism
Tubulin inhibitor
Released catabolite
Eribulin (free base)
Mechanistic subtype
Tubulin-other
Stereochem / salt
Conjugated as eribulin mesylate; releases free-base eribulin (single stereoisomer, 19 chiral centres)
Bioactivity note
ADCdb reports ADC cytotoxicity IC50: IGROV-1 (ovarian) 0.01 pM / 0.02 nM; NCI-H2110 (lung) 0.74 pM / 0.42 nM; Caov-3 (ovarian) 0.43 nM; OVCAR-3 (ovarian) 0.75 nM (FOLR1-dependent, sub-nM to pM potency).
07Ocular & expression
Ocular profile & eye-tissue target expression
Target profile →Target expression in eye tissues (HCA detection · HPA bulk)
Cross-trial comparability · source-verified
Ascertainment: Symptom-driven reportingScale: CTCAE v4Denominator: RP2D⚠ OAE rate not directly comparable across trials
08Identity & registry
Identifiers, registry & notes
ADC id
farletuzumab-ecteribulin
Approval status
Investigational
Primary source
Shimizu CCR 2021;27(14):3905 (FIH Ph1, n=22); Yonemori IJGO 2026, doi 10.1002/ijgo.70676 (PROC expansion, n=45)
Aliases & development codes
MORAb-202; FZEC; ER-001159569; VCP-Eribulin; eribulin/farletuzumab ADC
Notes
NEW conjugate row, distinct from the existing naked-Ab row 'farletuzumab' (MORAb-003). MORAb-202 = humanized anti-FRalpha IgG1/kappa farletuzumab + cathepsin-B-cleavable Mal-PEG2-Val-Cit-PAB linker + eribulin (DAR 4, random interchain-Cys/maleimide). 'RP2D'-tagged toxicity rows = the FIH Ph1 pooled cohort (Shimizu CCR 2021, n=22, 0.3-1.2 mg/kg Q3W, NCT03386942) — the primary/qualifying OAE cohort: eye disorders 2/22 (9%), all grade 1, markedly lower than the FRalpha comparator mirvetuximab (blurred vision ~42-48%, keratopathy ~33-36%). Recommended expansion doses were 0.9 & 1.2 mg/kg (Yonemori IJGO 2026 PROC expansion, Cohort 1 n=24 + Cohort 2 n=21); in the expansion the ONLY ocular PT reported was cataract (8.3% at 0.9, 14.3% at 1.2 mg/kg) — a lens finding likely age/steroid-confounded in this PROC population, not an ocular-surface ADC signal; hence ocular_surface_subtype/dominant_ae_tissue = Unknown. Key AE of interest = ILD/pneumonitis (FIH 23% G1-2; expansion 37.5% at 0.9 mg/kg, 66.7% at 1.2 mg/kg incl. 1 G3). NOTE neutropenia discrepancy by cohort: FIH 45% (10/22; escalation incl. higher doses) vs expansion 4.4% (2/45) at recommended doses. Later PK/E-R modelling (Hayato JCP 2025) supports 33 mg/m2 BSA-based Q3W. Eribulin released as membrane-permeable free base -> strong bystander (>140-fold). Thrombocytopenia and infusion-reaction rates NOT reported in available sources (left blank, not zero). FOLR1 not corneal/conjunctival-expressed (HCA ~0.02-0.19%), consistent with the low ocular-surface signal. Cross-refs: adcdb_adc_id DRG0HPUIL, linker LIN0KCWDR (PubChem CID 155889591), payload eribulin PAY0JAEKD/PubChem CID 11354606, ChEMBL4802212.