Table 1.

Analyses of farletuzumab ADCs

Cytotoxicity analysis (IC50, nmol/L)
PayloadConjugation chemistrySpacerCleavage chemistryIGROV1NCI-H2110A431SJSA1
EribulinMaleimidePEG2Val-cit-pAB0.103.7>100>100
EribulinMaleimidePEG8Val-cit-pAB0.127.186n.t.
EribulinMaleimideCaproylVal-cit-pAB0.113.9>100n.t.
EribulinMaleimidePEG2Ala-ala-asn-pAB0.0803.832n.t.
EribulinMaleimidePEG4-triazole-PEG3Disulfidyl-dimethyl-pAB0.270.857.0n.t.
EribulinMaleimidePEG4-triazole-PEG3Sulfonamide0.370.696.8n.t.
EribulinMaleimidePEG2None0.3338>100n.t.
EribulinMaleimidePEG4None0.2822>100n.t.
EribulinSuccinamide/SPAACPEG4Val-cit-pAB0.0384.3>100n.t.
EribulinSuccinamide/SPAACPEG3Disylfidyl-dimethyl-pAB0.550.909.7n.t.
EribulinSuccinamide/SPAACPEG3Sulfonamide1.81.725n.t.
EribulinSuccinamide/SPAACPEG2None4.338>100n.t.
EribulinSuccinamide/SPAACPEG4None1.346>100n.t.
CryptophycinMaleimidePEG2Val-cit-pAB0.030n.t.n.t.>100
MMAEMaleimideCaproylVal-cit-pAB0.20n.t.n.t.>100
MMAFMaleimideCaproylVal-cit-pAB1.0n.t.n.t.>100
Eribulinn/an/an/a0.320.200.652.9
  • NOTE: IC50 values represent averages of at least two independent assays.

  • Abbreviations: n/a, not applicable; n.t., not tested.