farletuzumab ecteribulin (MORAb-202) / Eisai - LARVOL DELTA

Open label, multicenter, phase 2 study of farletuzumab ecteribulin (FZEC), a folate receptor alpha (FRα)-targeting antibody-drug conjugate (ADC), alone and in combination with lenvatinib in platinum-resistant ovarian cancer (PROC) (AACR-NCI-EORTC 2025) - P1/2 | "Up to 3 prior lines of systemic therapy are allowed; up to 4 prior lines of therapy are permitted for patients who received prior mirvetuximab soravtansine. Previous bevacizumab maintenance therapy is permitted and is not counted as an independent line of therapy...Adverse events will be monitored and graded according to Common Terminology Criteria for Adverse Events (CTCAE) version 5.0; interstitial lung disease events will be carefully monitored and managed. This multinational study is actively recruiting."

Clinical • Combination therapy • Late-breaking abstract • P2 data • Platinum resistant • Fallopian Tube Cancer • High Grade Serous Ovarian Cancer • Oncology • Ovarian Cancer • Peritoneal Cancer • Solid Tumor • CTSB • FOLR1

CA116-001: A Study of MORAb-202 Versus Investigator's Choice Chemotherapy in Female Participants With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary Peritoneal, or Fallopian Tube Cancer (clinicaltrials.gov) - P2 | N=106 | Completed | Sponsor: Bristol-Myers Squibb | Active, not recruiting ➔ Completed | Trial completion date: Oct 2026 ➔ Sep 2025

Platinum resistant • Trial completion • Trial completion date • Fallopian Tube Cancer • Oncology • Ovarian Cancer • FOLR1

MORAb-202-G000-201: A Study to Evaluate the Safety, Tolerability, and Efficacy of MORAb-202 (Herein Referred to as Farletuzumab Ecteribulin), a Folate Receptor Alpha (FRα)-Targeting Antibody-drug Conjugate (ADC) in Participants With Selected Tumor Types (clinicaltrials.gov) - P1/2 | N=182 | Recruiting | Sponsor: Eisai Inc. | Trial completion date: Dec 2024 ➔ Aug 2030 | Trial primary completion date: Dec 2024 ➔ Aug 2030

Trial completion date • Trial primary completion date • Breast Cancer • Endometrial Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Ovarian Cancer • Solid Tumor • Triple Negative Breast Cancer • ALK • BRAF • ER • HER-2 • PGR • ROS1

A Study of MORAb-202 in Participants With Previously Treated Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) (clinicaltrials.gov) - P2 | N=31 | Terminated | Sponsor: Bristol-Myers Squibb | N=50 ➔ 31

Enrollment change • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Comprehensive assessments of pharmacokinetics and immunogenicity of farletuzumab ecteribulin, a novel antibody-drug conjugate against tumors expressing folate receptor α, in monkeys. (PubMed, J Pharm Biomed Anal) - "Following intravenous administration, the PK profiles of Tab and ADC were similar, while minimal levels of eribulin. No ADA against MORAb-202 was detected in postdose samples."

Journal • PK/PD data • Oncology • CTSB • FOLR1

Antitumor Effect of Farletuzumab ecteribulin in Molecular Subtypes of Endometrial Cancer Patient-Derived Xenograft Models. (PubMed, Mol Cancer Ther) - "Notably, intratumoral eribulin accumulation exhibited a stronger correlation with efficacy than with FRα expression alone. These findings support further clinical development of FZEC for EC treatment and highlight the complexity of the mechanisms of action of ADCs."

Journal • Preclinical • Endometrial Cancer • Oncology • Solid Tumor • FOLR1

Antitumor effect of farletuzumab ecteribulin in molecular subtypes of endometrial cancer patient-derived xenograft models (AACR 2025) - "FZEC demonstrated robust antitumor effect against the FRα high EC-PDX models. Importantly, significant antitumor effects were observed, even in FRα-low or negative models. Intratumoral eribulin accumulation exhibited a stronger correlation with efficacy than with FRα expression alone."

Preclinical • Endometrial Cancer • Oncology • Solid Tumor • FOLR1

Farletuzumab ecteribulin and MORAb-109, folate receptor alpha and mesothelin targeting antibody-drug conjugates, show activity in poor prognosis gynaecological cancer models. (PubMed, Clin Transl Med) - No abstract available

Journal • Preclinical • Gynecologic Cancers • Oncology • FOLR1 • MSLN

The Efficacy And Safety Of Folate Receptor a-Targeted Antibody-Drug Conjugate Therapy In Patients With High-Grade Epithelial Ovarian, Primary Peritoneal, Or Fallopian Tube Cancers: A Systematic Review And Meta-Analysis (ESGO 2025) - "The protocol was registered with PROSPERO (CRD42023491151).Results Ten studies with a total of 940 patients (859 treated with mirvetuximab soravtansine-gynx (MIRV), 45 with farletuzumab ecteribulin (MORAb-202), and 36 with luveltamab tazevibulin (STRO-002)) were included in this meta-analysis. The incidence of grade ≥3 adverse events was 27% (95% CI: 0.19–0.36).Conclusion 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."

Retrospective data • Review • Fallopian Tube Cancer • Oncology • Ovarian Cancer • Solid Tumor • FOLR1

Preclinical evaluation of farletuzumab ecteribulin (FZEC) and MORAb-109, antibody-drug conjugates (ADCs) targeting folate receptor alpha and mesothelin, in high-risk gynaecological cancers. (LCC 2025) - " Eribulin demonstrated activity in 11 out of 15 gynaecological cancer models, outperforming the standard anti-microtubule agent, paclitaxel, despite 80% of models being resistant to cisplatin. The 15 aggressive gynaecological cancer PDX models showed remarkable responses to FZEC and MORAb-109 when FRA and/or MSLN expression was positive and ABCB1 expression was low. Given the limited treatment options for advanced gynaecological cancer, our findings underscore the urgent need to include these cancers in eribulin ADC trials early in the disease course."

Preclinical • Carcinosarcoma • Clear Cell Carcinoma • Endometrial Serous Adenocarcinoma • Gynecologic Cancers • High Grade Serous Ovarian Cancer • Oncology • Ovarian Cancer • Sarcoma • Solid Tumor • Uterine Cancer • ABCB1 • FOLR1 • MSLN

Pharmacokinetic and Exposure-Response Modeling Support Body Surface Area-Based Dosing of Farletuzumab Ecteribulin in Japanese Patients with Solid Tumors. (PubMed, J Clin Pharmacol) - "Dosing simulations showed that BSA-based dosing (33 mg/m2) yielded similar tumor responses to BW-based dosing (0.9 mg/kg) and decreased ILD rates. This study showed that BW-based dosing resulted in higher risks of ILD events for patients with a high BW versus low BW, whereas BSA-based dosing is predicted to reduce this risk while maintaining clinical efficacy."

Journal • PK/PD data • Interstitial Lung Disease • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Pneumonia • Pulmonary Disease • Respiratory Diseases • Solid Tumor

The Efficacy and Safety of Folate Receptor α-Targeted Antibody-Drug Conjugate Therapy in Patients With High-Grade Epithelial Ovarian, Primary Peritoneal, or Fallopian Tube Cancers: A Systematic Review and Meta-Analysis. (PubMed, Cancer Med) - "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."

Clinical • Journal • Retrospective data • Review • Fallopian Tube Cancer • Oncology • Ovarian Cancer • Solid Tumor • FOLR1

CA116-001: A Study of MORAb-202 Versus Investigator's Choice Chemotherapy in Female Participants With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary Peritoneal, or Fallopian Tube Cancer (clinicaltrials.gov) - P2 | N=90 | Active, not recruiting | Sponsor: Bristol-Myers Squibb | Recruiting ➔ Active, not recruiting

Enrollment closed • Fallopian Tube Cancer • Oncology • Ovarian Cancer • FOLR1

A Study of MORAb-202 in Participants With Previously Treated Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) (clinicaltrials.gov) - P2 | N=50 | Terminated | Sponsor: Bristol-Myers Squibb | Trial completion date: Feb 2026 ➔ Aug 2024 | Recruiting ➔ Terminated | Trial primary completion date: Mar 2024 ➔ Aug 2024; Business objectives have changed

Metastases • Trial completion date • Trial primary completion date • Trial termination • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

MORAb-202-G000-201: A Study to Evaluate the Safety, Tolerability, and Efficacy of MORAb-202 (Herein Referred to as Farletuzumab Ecteribulin), a Folate Receptor Alpha (FRα)-Targeting Antibody-drug Conjugate (ADC) in Participants With Selected Tumor Types (clinicaltrials.gov) - P1/2 | N=142 | Recruiting | Sponsor: Eisai Inc. | Trial completion date: Mar 2025 ➔ Oct 2024 | Trial primary completion date: Mar 2025 ➔ Oct 2024

Trial completion date • Trial primary completion date • Breast Cancer • Endometrial Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • Triple Negative Breast Cancer • ALK • BRAF • ER • HER-2 • PGR • ROS1

IKS012, a novel ADC design with favorable efficacy and safety for treatment of Folate Receptor Alpha-positive cancers (EORTC-NCI-AACR 2024) - "In the IGROV-1 model, IKS012 showed improved efficacy over MORAb-202, an eribulin ADC with a cathepsin cleavable linker...In the OVCAR-3 model, a single dose of 5 mg/kg IKS012 induced 75% TGI on day 35 in comparison to 42% and 68% TGI for the Elahere analogue and MORAb-202, respectively... The IKS012 ADC design with stable PermaLink® conjugation and the selective glucuronide trigger confers a favorable preclinical anti-tumor activity and safety profile. Our findings support the clinical development of IKS012 for the treatment of FRα-positive solid cancers."

Clinical • Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CTSB • CTSC • FOLR1

EISAI ANNOUNCES MOVE TO SOLO DEVELOPMENT AND COMMERCIALIZATION OF FARLETUZUMAB ECTERIBULIN (FZEC) ANTIBODY DRUG CONJUGATE (ADC) (Eisai Press Release) - "Eisai Co., Ltd...announced today that it has agreed to end its global strategic collaboration with Bristol Myers Squibb for the co-development and co-commercialization of farletuzumab ecteribulin (FZEC)...due to ongoing portfolio prioritization efforts within Bristol Myers Squibb. Based on the agreement, Eisai now owns all rights to FZEC and will solely conduct the global development and commercialization of the agent...Eisai plans to refund a part of the unused portion of the $200 million payment it received towards research and development expenses from Bristol Myers Squibb under the collaboration agreement and record the remaining as other income."

Licensing / partnership • Oncology

Taiyao’s new production capacity is put into operation + sales of breast cancer injections are launched, and the growth trend next year is clear [Google translation] (stock.yahoo) - "In addition, the breast cancer injection Eribulin Injectable is expected to be launched in the European and American markets next year....It has successively completed licensing agreements in North America and the Asia-Pacific region. Among them, the US drug license results are expected to be released in July next year. If everything goes well, it is expected to be released next year. When Four Seasons is launched, it will also be the first batch of generic drugs to be launched. In addition, the licensing contract for the European market will be completed in the near future, and the licensing contract for the Turkish market will also be signed....In the Taiwan market, Eribulin Injectable has successively obtained drug certificates and health insurance prices this year, and is expected to start sales and contribute revenue next year."

Commercial • Generic launch • Breast Cancer • Oncology • Solid Tumor

MORAb-202-G000-201: A Study to Evaluate the Safety, Tolerability, and Efficacy of MORAb-202 (Herein Referred to as Farletuzumab Ecteribulin), a Folate Receptor Alpha (FRα)-Targeting Antibody-drug Conjugate (ADC) in Participants With Selected Tumor Types (clinicaltrials.gov) - P1/2 | N=142 | Recruiting | Sponsor: Eisai Inc. | N=66 ➔ 142

Enrollment change • Breast Cancer • Endometrial Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • Triple Negative Breast Cancer • ALK • BRAF • ER • FOLR1 • HER-2 • PGR • ROS1

Antitumor activity of farletuzumab ecteribulin in a panel of endometrial cancer patient-derived xenografts with four different molecular subtypes (ESMO 2023) - "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."

Clinical • Endometrial Cancer • Microsatellite Instability • Oncology • Solid Tumor • FOLR1 • MSI • POLE

EISAI TO PRESENT RESEARCH FROM ONCOLOGY PORTFOLIO AND PIPELINE AT ESMO CONGRESS 2023 (Eisai Press Release) - "Eisai...announced today the presentation of research across various types of cancer from its oncology portfolio and pipeline during the European Society for Medical Oncology (ESMO) Congress 2023....Research from Eisai’s pipeline will be featured in a poster presentation of findings from the dose-expansion portion of a Phase 1 study evaluating E7389-LF, a liposomal formulation of eribulin, as a potential first-line chemotherapy treatment option for patients with metastatic/advanced HER2-negative breast cancer (Presentation: #405P). Additionally, insights from preclinical research on farletuzumab ecteribulin (FZEC, formerly known as MORAb-202), a folate receptor alpha (FRα)-targeting antibody drug conjugate (ADC), in endometrial cancer will be presented (Presentation: #786P)."

P1 data • Preclinical • Endometrial Cancer • HER2 Negative Breast Cancer

Phase I biomarker analysis of farletuzumab ecteribulin (FZEC), formerly MORAb-202, effects on cancer responses in patients with platinum resistant ovarian cancer. (AACR-NCI-EORTC 2023) - No abstract available

Biomarker • Clinical • P1 data • Oncology • Ovarian Cancer • Solid Tumor

Preclinical testing of farletuzumab ecteribulin (FZEC [MORAb-202]) and MORAb-109, folate receptor α and mesothelin targeting antibody-drug conjugates (ADCs), in rare gynecologic cancers. (ASCO 2023) - "The anti-microtubule agent (AMA) paclitaxel is used in first-line treatment of most gynecologic cancers; however, the AMA eribulin is known to have additional anticancer properties (Goto et al...Despite most (80%) models being cisplatin refractory, 11/15 responded to eribulin with the 4 non-responders having high MDR1 expression and being from previously treated patients... Responses to FZEC and MORAb-109 correlated with FRA and MSLN expression, with equivalent or better activity compared to eribulin in target-positive PDX models of HGSOC, USC and OCCA. >* Models tested for FRA and MSLN expression (not all were tested for ADC activity). ** FZEC response in FRA+ PDXs."

Preclinical • Endometrial Serous Adenocarcinoma • Gynecologic Cancers • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Sarcoma • Uterine Cancer • ABCB1 • FOLR1 • MSLN

Eisai Delivers New Data and Highlights Continued Progress of Oncology Portfolio and Pipeline at ASCO 2023 (PRNewswire) - "Additional data from Eisai's pipeline include a poster presentation of findings from a Phase 1b study of E7386, a CREB-binding protein (CBP) / β-catenin interaction inhibitor, in combination with lenvatinib in patients with advanced HCC...and the small cell lung cancer cohort of a Phase 1b/2 trial evaluating E7389-LF, a new liposomal formulation of eribulin, in combination with nivolumab...Insights from preclinical testing of farletuzumab ecteribulin (FZEC), formerly known as MORAb-202, and MORAb-109, antibody drug conjugates (ADC), in rare gynecologic cancers will also be published online."

P1 data • P1/2 data • Preclinical • Gastrointestinal Cancer • Gynecologic Cancers • Hepatocellular Cancer • Liver Cancer • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor

A Study of MORAb-202 in Participants With Previously Treated Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) (clinicaltrials.gov) - P2 | N=50 | Recruiting | Sponsor: Bristol-Myers Squibb | N=100 ➔ 50

Enrollment change • Metastases • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor