farletuzumab ecteribulin (MORAb-202)

FRα-targeting ADCs, including MIRV, demonstrated definite efficacy and good safety as novel choices for second-line and beyond treatment of advanced or recurrent ovarian cancer. Patients with high FRα expression showed ORR and PFS benefits similar to those in the overall cohort.

P2, N=50, Terminated, Bristol-Myers Squibb | Trial completion date: Feb 2026 --> Aug 2024 | Recruiting --> Terminated | Trial primary completion date: Mar 2024 --> Aug 2024; Business objectives have changed

P1/2, N=142, Recruiting, Eisai Inc. | Trial completion date: Mar 2025 --> Oct 2024 | Trial primary completion date: Mar 2025 --> Oct 2024

P1/2, N=142, Recruiting, Eisai Inc. | N=66 --> 142

Intratumoral imaging analysis using tumors on day 21st showed an association between the antitumor effect and intratumoral accumulation of eribulin. Conclusions These results suggest that FZEC may be a promising treatment for FRα-expressing EC of all four molecular subtypes.

P2, N=50, Recruiting, Bristol-Myers Squibb | N=100 --> 50

P2, N=90, Recruiting, Bristol-Myers Squibb | N=150 --> 90

Background: MORAb-202 (farletuzumab ecteribulin) is an antibody-drug conjugate (ADC) comprised of the humanized antifolate receptor-alpha (FRα) monoclonal antibody, farletuzumab, and the cytotoxic microtubule inhibitor, eribulin, conjugated by a cathepsin B-cleavable linker. Tumor assessments will be conducted by investigators using RECIST v1.1 at screening, every 6 weeks for 24 weeks, then every 12 weeks or as needed. Assessments of computed tomography scans for ILD will be conducted by a central expert review board.

Measures to enhance early detection of ILD have been introduced and steps to potentially reduce the occurrence of severe ILD include implementation of BSA–based dosing, lung-specific eligibility criteria, revised and stringent ILD management criteria, and ILD training for relevant study personnel. *Formerly MORAb-202.

P1, N=82, Completed, Eisai Inc. | Active, not recruiting --> Completed | N=120 --> 82

Introduction/Background: MORAb-202 (farletuzumab ecteribulin) is an antibody-drug conjugate (ADC) comprised of the humanised antifolate receptor-alpha (FRα) monoclonal antibody, farletuzumab, and the cytotoxic microtubule inhibitor, eribulin, conjugated by a cathepsin B-cleavable linker. TIP

P1, N=120, Active, not recruiting, Eisai Inc. | Trial completion date: Dec 2022 --> Oct 2022 | Trial primary completion date: Dec 2022 --> Oct 2022

P1/2, N=55, Recruiting, Eisai Inc. | Active, not recruiting --> Recruiting | N=196 --> 55 | Trial completion date: Nov 2023 --> Mar 2025 | Trial primary completion date: Apr 2023 --> Mar 2025

P1, N=120, Active, not recruiting, Eisai Inc. | Trial completion date: Dec 2021 --> Dec 2022 | Trial primary completion date: Dec 2021 --> Dec 2022

P1/2, N=196, Active, not recruiting, Eisai Inc. | Recruiting --> Active, not recruiting | Trial completion date: Aug 2025 --> Nov 2023 | Trial primary completion date: Aug 2022 --> Apr 2023

Background MORAb-202 is an ADC consisting of a FRα-targeting antibody (farletuzumab) paired with a cathepsin B-cleavable linker and an eribulin payload. The major toxicity observed with MORAb-202 treatment was hematologic toxicity. Conclusion These findings suggest MORAb-202 may be a promising ADC for TNBC and warrants further clinical investigation in this setting.

P1, N=120, Active, not recruiting, Eisai Inc. | Recruiting --> Active, not recruiting

The ADC could be a more reasonable choice than mAb as a targeting agent for the FOLRα-expressing tumor.

The antibody-drug conjugate (ADC) MORAb-202, consisting of farletuzumab paired with a cathepsin B-cleavable linker and eribulin, targets folate receptor alpha (FRA), which is frequently overexpressed in various tumor types. Toxicology studies (Q3Wx2) in non-human primates suggested that the major observed toxicity of MORAb-202 is hematologic toxicity. Overall, these findings support the concept that MORAb-202 represents a promising investigational ADC for the treatment of TNBC patients.

In orthotopic xenograft mouse models, FOLR1-expressing T47D tumors and non-FOLR1-expressing MCF7 tumors were suppressed upon MORAb-202 administration. The novel anti-FOLR1 antibody-eribulin conjugate MORAb-202 has potential antitumor effects in breast cancer.

P1/2, N=196, Recruiting, Eisai Inc. | Not yet recruiting --> Recruiting | Trial completion date: Oct 2022 --> Aug 2025 | Initiation date: Feb 2020 --> Aug 2020

P1, N=120, Recruiting, Eisai Inc. | N=80 --> 120

P1/2, N=196, Not yet recruiting, Eisai Inc.