ADC ID	DRG0HPUIL
ADC Name	Farletuzumab ecteribulin
Synonyms	farletuzumab ecteribulin; MORAb-202; eribulin conjugated farletuzumab; farletuzumab-ecteribulin; BMS-986445; FZEC    Click to Show/Hide
Organization	Morphotek (Originator);Bristol-Myers Squibb (Top20 MNC) (No Rights)
Drug Status	Phase 2
Drug-to-Antibody Ratio	4
Structure
	3D MOL			2D MOL
Antibody Name	Farletuzumab					Antibody Info
Antigen Name	Folate receptor alpha (FOLR1)					Antigen Info
Payload Name	Eribulin					Payload Info
Therapeutic Target	Microtubule (MT)					Target Info
Linker Name	Mal-PEG2-Val-Cit-PABC					Linker Info
Conjugate Type	Random Cysteines
Combination Type	ecteribulin

Bystander Killing Effect	Description	Reference
yes	The effect of MORAb-202 was further characterized in an in vitro coculture system of the FRalpha- HL60 and FRalpha+ IGROV1 cell lines. A consistent in vitro effect of MORAb-202 was observed from 48 to 96 hours. Endpoint supernatant recovered from the coculture exhibited cell cytotoxicity in FRalpha- cells, suggesting that released eribulin is liable for the observed effect.    Click to Show/Hide	[1]
yes	This result demonstrated that eribulin conjugated to MORAb-202 was efficiently cleaved in NLG-IGROV-1 cells, and free eribulin released from the apoptotic NLR-IGROV-1 cells was cytotoxic to adjacent NLR-HL-60 cells, resulting in bystander killing.    Click to Show/Hide	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	7160	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	7800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6970	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	12300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	13400	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11500	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	18300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	19000	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17100	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17200	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 22, AUC0-t.	[3]

Standard Type	Value	Units	Description	Reference
Volume of Distribution (Vd)	2.47	L	Farletuzumab ecteribulin PK was well described by a 2-compartment model with linear elimination from the central compartment	[1], [2]
Area Under the Concentration-Time Curve (AUC)	7160	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	7800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6970	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	12300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	13400	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11500	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	18300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	19000	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17100	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17200	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 22, AUC0-t.	[3]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	7160	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	7800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6970	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	12300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	13400	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11500	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	18300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	19000	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 22, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17100	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17200	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 22, AUC0-t.	[3]

Standard Type	Value	Units	Description	Reference
Clearance (CL)	0.0162	L/h	Farletuzumab ecteribulin PK was well described by a 2-compartment model with linear elimination from the central compartment	[1], [2]
Area Under the Concentration-Time Curve (AUC)	7160	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	7800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Male, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	192	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Day 1, Male.	[3]
Elimination Half-Life (t1/2)	175	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Day 22, Male.	[3]
Area Under the Concentration-Time Curve (AUC)	6300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	6970	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Female, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	162	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Day 1, Female.	[3]
Elimination Half-Life (t1/2)	148	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 2 mg/kg, Day 22, Female.	[3]
Area Under the Concentration-Time Curve (AUC)	12300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	13400	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Male, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	192	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Day 1, Male.	[3]
Elimination Half-Life (t1/2)	164	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Day 22, Male.	[3]
Area Under the Concentration-Time Curve (AUC)	11500	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	11800	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Female, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	151	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Day 1, Female.	[3]
Elimination Half-Life (t1/2)	144	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 4 mg/kg, Day 22, Female.	[3]
Area Under the Concentration-Time Curve (AUC)	18300	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	19000	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Male, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	186	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Day 1, Male.	[3]
Elimination Half-Life (t1/2)	144	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Day 22, Male.	[3]
Area Under the Concentration-Time Curve (AUC)	17100	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 1, AUC0-t.	[3]
Area Under the Concentration-Time Curve (AUC)	17200	ug*h/mL	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Female, Day 22, AUC0-t.	[3]
Elimination Half-Life (t1/2)	147	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Day 1, Female.	[3]
Elimination Half-Life (t1/2)	152	h	MORAb-202 was administered Q3Wx2 (2, 4, and 6 mg/kg) to cynomolgus monkeys, 6 mg/kg, Day 22, Female.	[3]

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT05577715	PHASE2	A Phase 2, Open-label, Randomized Study of MORAb-202 (Farletuzumab Ecteribulin), a Folate Receptor Alpha-targeting Antibody-Drug Conjugate, in Participants With Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) After Progression on Prior Therapies    Click to Show/Hide
Undisclosed	NCT05613088	PHASE2	A Phase 2 Open-label Randomized Study of Farletuzumab Ecteribulin (MORAb-202), a Folate Receptor Alpha-targeting Antibody-drug Conjugate, Versus Investigator's Choice Chemotherapy in Women With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary Peritoneal, or Fallopian Tube Cancer    Click to Show/Hide
Undisclosed	NCT03386942	PHASE1	A Phase 1 Study of MORAb-202 in Subjects With Solid Tumors
Undisclosed	NCT04300556	PHASE1|||PHASE2	A Multicenter, Open-Label Phase 1/2 Trial Evaluating the Safety, Tolerability, and Efficacy of MORAb-202, a Folate Receptor Alpha (FRalpha)-Targeting Antibody-drug Conjugate (ADC) in Subjects With Selected Tumor Types    Click to Show/Hide

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 2.1	%	Breast cancer PDX model (PDX: OD-BRE-0631)
Tumor Growth Inhibition value (TGI)	≈ 65.7	%	Breast cancer PDX model (PDX: OD-BRE-0631)
Tumor Growth Inhibition value (TGI)	≈ 98.3	%	Breast cancer PDX model (PDX: IM-BRE-563)

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.01	pM	IGROV-1 cells	Ovarian endometrioid adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.74	pM	NCI-H2110 cells	Lung non-small cell carcinoma
Half Maximal Inhibitory Concentration (IC50)	> 1	pM	SJSA-1 cells	Osteosarcoma
Half Maximal Inhibitory Concentration (IC50)	23	pM	A431-A3 cells	Skin squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50)	0.02	nM	IGROV-1 cells	Ovarian endometrioid adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.42	nM	NCI-H2110 cells	Lung non-small cell carcinoma
Half Maximal Inhibitory Concentration (IC50)	0.43	nM	Caov-3 cells	Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.75	nM	OVCAR-3 cells	Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	1.03	nM	HEC-59 cells	Endometrial adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	1.42	nM	HCC1954 cells	Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50)	1.76	nM	MKN74 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	1.81	nM	HEC-1-A cells	Endometrial adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	2.17	nM	MKN7 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	4.42	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	13.15	nM	HEC-251 cells	Endometrial carcinoma
Half Maximal Inhibitory Concentration (IC50)	24.58	nM	NUGC-3 cells	Gastric carcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	A431 cells	Skin squamous cell carcinoma

Experiment 1 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Eligibility requires histologically confirmed metastatic NSCLC adenocarcinoma (IASLC 8th ed.), measurable disease (RECIST 1.1), and ECOG PS 0-1. Exclusions include non-adenocarcinoma NSCLC histologies, uncontrolled third-space fluid accumulation, prior pneumonectomy (<12 months), recent chest radiotherapy (<6 months), and protocol-specified criteria affecting safety or study integrity.    Click to Show/Hide
Administration Dosage	Specified dose on specified days
Related Clinical Trial
NCT Number	NCT05577715	Clinical Status	PHASE2
Clinical Description	A Phase 2, Open-label, Randomized Study of MORAb-202 (Farletuzumab Ecteribulin), a Folate Receptor Alpha-targeting Antibody-Drug Conjugate, in Participants With Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) After Progression on Prior Therapies
Primary Endpoint	Primary endpoints assess treatment-related adverse events (TRAEs) leading to discontinuation and objective response rate (ORR) by RECIST 1.1, both evaluated over a 2-year timeframe through investigator assessment to determine safety and efficacy profiles.
Other Endpoint	Safety monitoring tracks adverse events (AEs), serious AEs (SAEs), treatment-related AEs/SAEs, AEs of special interest (AESIs), deaths, and lab abnormalities over 2 years. Key efficacy measures include progression-free survival (PFS), disease control rate (DCR), and duration of response (DoR), all assessed via RECIST 1.1 by investigators during the same 2-year period.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[5]
Patients Enrolled	Eligible participants must have confirmed high-grade serous ovarian/peritoneal/fallopian tube cancer with platinum-resistant disease (1-3 prior lines) and measurable progression per RECIST v1.1. Key exclusions include non-HGS histologies, platinum-refractory status, significant pulmonary/ILD issues, uncontrolled effusions, hypersensitivity to study drugs, and protocol-specified lab/clinical abnormalities that may compromise safety or interpretation.    Click to Show/Hide
Administration Dosage	Specified dose on specified days
Related Clinical Trial
NCT Number	NCT05613088	Clinical Status	PHASE2
Clinical Description	A Phase 2 Open-label Randomized Study of Farletuzumab Ecteribulin (MORAb-202), a Folate Receptor Alpha-targeting Antibody-drug Conjugate, Versus Investigator's Choice Chemotherapy in Women With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary Peritoneal, or Fallopian Tube Cancer
Primary Endpoint	The primary endpoints evaluate efficacy and tolerability, measuring objective response rate (ORR) by RECIST v1.1 and treatment-related adverse events (TRAEs) causing study discontinuation, both assessed over a 2-year period to determine the treatment's clinical benefit and safety profile.
Other Endpoint	Secondary outcomes include comprehensive safety monitoring of adverse events (AEs), serious AEs (SAEs), AE-related discontinuations, and laboratory abnormalities, along with efficacy assessments of disease control rate (DCR), duration of response (DoR), and progression-free survival (PFS) by RECIST v1.1 - all tracked for 2 years to characterize the treatment's overall risk-benefit profile.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Eligible participants (&ge;20 years, ECOG 0-1) require FRA-positive solid tumors (Part 1) or specific ovarian/NSCLC histologies (Part 2) with adequate organ function. Key exclusions: uncontrolled cardiovascular disease, active infections, ILD, brain metastases, prior FRalpha/eribulin intolerance, or concurrent malignancies. Reproductive-age participants must use contraception, and prior anticancer therapies require appropriate washout periods (2-4 weeks depending on treatment type).    Click to Show/Hide
Administration Dosage	Part 1: farletuzumab ecteribulin intravenous (IV) infusion administered every 3 weeks starting at a 0.3 mg/kg dose and successively increasing doses until DLT. Part 2: farletuzumab ecteribulin administered IV every 3 weeks at a dose determined in Part 1 until any of the criteria for discontinuation are met.
Related Clinical Trial
NCT Number	NCT03386942	Clinical Status	PHASE1
Clinical Description	A Phase 1 Study of MORAb-202 in Subjects With Solid Tumors
Primary Endpoint	The study evaluates safety through dose-limiting toxicities (DLTs) in Cycle 1 (21 days), including severe hematologic events (grade 4 neutropenia/thrombocytopenia/anemia) and clinically significant grade 3-4 non-hematologic toxicities. Additional safety assessments over 50 months monitor AEs, SAEs, lab abnormalities, vital signs, ECOG PS changes, and immunogenicity via ADA titers to characterize the treatment's long-term safety profile.    Click to Show/Hide
Other Endpoint	Pharmacokinetics analysis measures maximum serum concentration (Cmax) of farletuzumab ecteribulin, total antibody, and free eribulin to establish the maximum tolerated dose (MTD) and recommended dose (RD) based on DLT rates (target 25%). Efficacy outcomes over 50 months include RECIST v1.1-based responses (ORR, DCR, CBR, BOR), with Part 2 specifically tracking survival metrics (PFS, OS) and duration of response (DOR) in defined cohorts.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[7]
Patients Enrolled	Eligible participants (&ge;18 years, ECOG 0-1) include platinum-resistant ovarian, TNBC, NSCLC adenocarcinoma, or endometrial cancer patients with measurable disease and adequate organ function. Key exclusions: prior FRalpha/eribulin therapy, uncontrolled cardiovascular/autoimmune conditions, active infections (HIV/hepatitis), untreated brain metastases, pregnancy, or ILD risk factors (e.g., abnormal PFTs, chest radiotherapy <2 years). Contraception is mandated for reproductive-age participants, with washout periods (2-4 weeks) required for prior therapies.    Click to Show/Hide
Administration Dosage	The initial cohort has enrolled 7 patients at a MORAb-202 25 mg/m2 IV Q3W dose and is ongoing; further enrollment of patients at 25 mg/m2 and 33 mg/m2 will occur following ILD safety evaluation. 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.
Related Clinical Trial
NCT Number	NCT04300556	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Multicenter, Open-Label Phase 1/2 Trial Evaluating the Safety, Tolerability, and Efficacy of MORAb-202, a Folate Receptor Alpha (FRalpha)-Targeting Antibody-drug Conjugate (ADC) in Subjects With Selected Tumor Types
Primary Endpoint	The study assesses safety through dose-limiting toxicities (DLTs) in Cycle 1 (21 days), including severe hematologic and non-hematologic events (grade 3-4 per NCI CTCAE v5.0). Long-term safety (up to ~4 years 8 months) monitors SAEs, AEs leading to discontinuation, AEIs (e.g., ILD), lab/vital sign abnormalities, and immunogenicity via ADA titers. Efficacy endpoints include ORR (RECIST v1.1, up to ~24 weeks) and dose-finding for the RP2D.    Click to Show/Hide
Other Endpoint	Secondary outcomes evaluate pharmacokinetics (Cmax, AUC, t½) of farletuzumab ecteribulin and its components, alongside RECIST v1.1-based efficacy measures (DOR, DCR, CBR, PFS, OS) over ~4.8 years. Exploratory analyses correlate tumor FRA expression with clinical outcomes (ORR, PFS). Additional metrics include ECOG PS changes, SpO2 levels, and cardiac/laboratory parameters to comprehensively assess treatment impact.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.10%	Moderate FOLR1 expression (FOLR1++)
Method Description	The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 2.5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
In Vivo Model	Breast cancer PDX model (PDX: OD-BRE-0631)
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.70%	Moderate FOLR1 expression (FOLR1++)
Method Description	The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
In Vivo Model	Breast cancer PDX model (PDX: OD-BRE-0631)
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.30%	High FOLR1 expression (FOLR1+++)
Method Description	The each group was randomized to be a similar mean volume of 100-250 mm3.The treatment schedule was as follows: a single IV injection of vehicle at day 0, and a single IV injection of MORAb-202 at 5 mg/kg at day 0 ((Q1Dx1) or every 11 days (Q11Dx2)).
In Vivo Model	Breast cancer PDX model (PDX: IM-BRE-563)

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 pM	High FOLR1 expression (FOLR1+++)
Method Description	Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 pM	High FOLR1 expression (FOLR1+++)
Method Description	Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.    Click to Show/Hide
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1 pM	Negative FOLR1 expression (FOLR1-)
Method Description	Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.    Click to Show/Hide
In Vitro Model	Osteosarcoma	SJSA-1 cells		CVCL_1697
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23 pM	Moderate FOLR1 expression (FOLR1++)
Method Description	Threefold serial dilutions of MORAb-202 (5.1x1012 - 1.0x107 mol/L) were added to the cell lines, and the cells were cultured for 5 days. Cells were stained with 0.2% crystal violet solution, a triarylmethane dye which accumulates in the nucleus of viable cells, washed with water, and solubilized with 1% sodium dodecyl sulfate. The viable cell number was determined by measuring the optical density (OD 570 nm) of the resulting lysate.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431-A3 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High FOLR1 expression(FOLR1+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 6 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.42 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530
Experiment 7 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 9 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.03 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Endometrial adenocarcinoma	HEC-59 cells		CVCL_2930
Experiment 10 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.42 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.76 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Gastric tubular adenocarcinoma	MKN74 cells		CVCL_2791
Experiment 12 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.81 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Endometrial adenocarcinoma	HEC-1-A cells		CVCL_0293
Experiment 13 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.17 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Gastric tubular adenocarcinoma	MKN7 cells		CVCL_1417
Experiment 14 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.42 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.15 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Endometrial carcinoma	HEC-251 cells		CVCL_2927
Experiment 16 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.58 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Gastric carcinoma	NUGC-3 cells		CVCL_1612
Experiment 17 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative FOLR1 expression(FOLR1-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Ref 1	Pharmacokinetic and Exposure-Response Modeling Support Body Surface Area-Based Dosing of Farletuzumab Ecteribulin in Japanese Patients with Solid Tumors
Ref 2	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
Ref 3	Assessment of quality of life in cardiovascular therapy
Ref 4	A Study of MORAb-202 in Participants With Previously Treated Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC)
Ref 5	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
Ref 6	A Study of MORAb-202 (Herein Referred to as Farletuzumab Ecteribulin) in Participants With Solid Tumors
Ref 7	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
Ref 8	Antibody-drug conjugate MORAb-202 exhibits long-lasting antitumor efficacy in TNBC PDx models. Cancer Sci. 2021 Jun;112(6):2467-2480.
Ref 9	MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FR Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018 Dec;17(12):2665-2675. doi: 10.1158/1535-7163.MCT-17-1215. Epub 2018 Sep 27.