Antibody Information

General Information of This Antibody
Antibody ID
ANI0BJQGX
Antibody Name
Labetuzumab
Brand Name
CEACIDE
Organization
Immunomedics, Inc.
Indication
Colorectal cancer
Synonyms
hMN14; CEA-CIDE; hMN 14; hMN-14
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-nd
Antigen Name
Carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5)
  Antigen Info 
ChEMBI ID
CHEMBL2108501
DrugBank ID
DB05097
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
EVQLVESGGGVVQPGRSLRLSCSASGFDFTTYWMSWVRQAPGKGLEWIGEIHPDSSTINY
APSLKDRFTISRDNAKNTLFLQMDSLRPEDTGVYFCASLYFGFPWFAYWGQGTPVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Light Chain Sequence
DIQLTQSPSSLSASVGDRVTITCKASQDVGTSVAWYQQKPGKAPKLLIYWTSTRHTGVPS
RFSGSGSGTDFTFTISSLQPEDIATYYCQQYSLYRSFGQGTKVEIKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Labetuzumab govitecan [Phase 2 (discontinued)]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Relapsed or refractory metastatic colorectal cancer (mCRC) who had received at least one prior irinotecan-containing regimen.
Administration Dosage
Once weekly at 8 and 10 mg/kg, or two times per week at 4 and 6 mg/km on weeks 1 and 2 of 3-week repeated cycles, intravenous.
Related Clinical Trial
NCT Number NCT01605318  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of once or twice weekly IMMU-130 (hMN-14-SN38, antibody-drug conjugate) in patients with colorectal cancer.
Primary Endpoint
The median PFS for all 86 patients was 3.60 months (95% CI,2.00 months to 4.00 months), with 16.8% (14 of 86) remaining progression free for at least 6 months, including three patients who maintained this status for at least 1 year. The median OS was 6.90 months (95% CI, 5.70 months to 7.80 months), with 24.41% (21 of 86) surviving for at least 1 year, including three patients who survived at least 2 years (one for 3 years).

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Other Endpoint
In the regorafenib subset (n = 23), the median PFS and OS were 3.90 and 6.70 months, respectively.
Experiment 2 Reporting the Activity Date of This ADC [3]
Patients Enrolled
Eligible participants must have metastatic colorectal adenocarcinoma (prior irinotecan-treated, ECOG 0-1, CEA >5 ng/mL, measurable disease) with adequate organ function. Exclusions include pregnancy, active CNS metastases, bulky disease (>10 cm), HIV/HBV/HCV positivity, significant cardiac/respiratory disease, or concurrent conditions impairing study compliance. Prior malignancies require ≥3-year disease-free interval (exceptions: non-melanoma skin/cervical cancers).

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Related Clinical Trial
NCT Number NCT01605318  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase I/II Study of Once or Twice Weekly IMMU-130 (hMN-14-SN38, Antibody-Drug Conjugate) in Patients With Colorectal Cancer
Primary Endpoint
The study assesses the percentage of participants experiencing adverse events (AEs), serious AEs (SAEs), and laboratory abnormalities from the first dose until approximately 2 years post-treatment or disease progression.
Other Endpoint
Key efficacy parameters include duration of response (DOR; time from PR/CR to PD/death), progression-free survival (PFS; treatment start to PD/death), time to progression (TTP), overall survival (OS; treatment start to death), and time-to-treatment failure (TTF). CEA serum level changes are monitored longitudinally.
Experiment 3 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Eligible patients must have metastatic colorectal adenocarcinoma (prior treatment failure, ECOG 0-1, CEA >5 ng/mL, measurable disease) and adequate organ function. Exclusions include pregnancy, active CNS metastases (unless stable post-treatment), CEA >1000 ng/mL (pre-MTD), grade 3 anorexia/vomiting, uncontrolled autoimmune disease (except stable conditions), HIV/HBV/HCV positivity, recent cardiac/respiratory events, or other conditions impairing study compliance. Prior malignancies require ≥3-year disease-free interval (exceptions: non-melanoma skin/cervical cancers).

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Administration Dosage
IMMU-130 will be administered intravenously every 2 weeks for up to 6 months or longer.
Related Clinical Trial
NCT Number NCT01270698  Clinical Status PHASE1
Clinical Description
A Phase I Study of IMMU-130 (hMN-14-SN38 Antibody Drug Conjugate) in Patients With Colorectal Cancer.
Primary Endpoint
The primary focus is on evaluating the safety profile of IMMU-130 across different dose levels, with adverse events and overall toxicity monitored during 6 months of treatment and up to 5 years of follow-up.
Other Endpoint
Secondary objectives include assessing pharmacokinetics, immunogenicity, and preliminary efficacy, with CT scans performed every 8-12 weeks during treatment, every 6 months in the 2nd year, and annually up to 5 years thereafter.
Experiment 4 Reporting the Activity Date of This ADC [5]
Patients Enrolled
Eligible patients include adults ≥18 with histologically confirmed metastatic colorectal adenocarcinoma, prior irinotecan treatment, ECOG 0-1, adequate organ function, and measurable disease. Exclusions cover pregnancy, uncontrolled comorbidities, active infections, recent malignancies, and conditions interfering with study compliance per investigator judgment.

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Administration Dosage
This is a Phase II, open-label study of IMMU-130 administered every 14 days for a period of 24 weeks to patients with metastatic colorectal cancer who have been previously treated with at least one prior irinotecan-containing regimen.
Related Clinical Trial
NCT Number NCT01915472  Clinical Status PHASE2
Clinical Description
A Phase II Study of IMMU 130 (hMN-14-SN38 Antibody Drug Conjugate) in Patients With Metastatic Colorectal Cancer
Primary Endpoint
Safety is evaluated across 6 months of treatment and up to 5 years post-treatment, focusing on adverse events and toxicity levels with different doses of IMMU-130.
Other Endpoint
Secondary objectives include analyzing pharmacokinetics and immunogenicity, along with preliminary efficacy assessment via CT scans, measured every 8 weeks during treatment and every 3-6 months during follow-up for up to 5 years.
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.23 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.04 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate carcinoma DU145 cells CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
140 nM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate cancer MSKCC EF1 cells Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.32 uM
Method Description
The inhibitory activity of IMMU-130 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 4 days.
In Vitro Model Prostate small cell carcinoma NCI-H660 cells CVCL_1576
Labetuzumab-CL2E-SN-38 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Median survival time (MST)
63 Day
Low CEACAM5 expression (CEACAM5+)
Method Description
The intravenous WSU-FSCCL models were initiated by intravenous injection of 2.5 x 106 cells, in female severe combined immunodeficient (SCID) mice (Taconic). The dose was 0.30 mg/dose (4.8 g SN-38 equivalents).
In Vivo Model WSU-FSCCL CDX model
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Median survival time (MST)
76 Day
Low CEACAM5 expression (CEACAM5+)
Method Description
The intravenous WSU-FSCCL models were initiated by intravenous injection of 2.5 x 106 cells, in female severe combined immunodeficient (SCID) mice (Taconic). The dose was 0.15 mg/dose (2.4 g SN-38 equivalents).
In Vivo Model WSU-FSCCL CDX model
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 3 Reporting the Activity Date of This ADC [6]
Efficacy Data Median survival time (MST)
91 Day
Low CEACAM5 expression (CEACAM5+)
Method Description
The intravenous WSU-FSCCL models were initiated by intravenous injection of 2.5 x 106 cells, in female severe combined immunodeficient (SCID) mice (Taconic). The dose was 0.30 mg/dose (4.8 g SN-38 equivalents) plus Veltuzumab, 35 ug/dose.
In Vivo Model WSU-FSCCL CDX model
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 4 Reporting the Activity Date of This ADC [6]
Efficacy Data Median survival time (MST)
98 Day
Low CEACAM5 expression (CEACAM5+)
Method Description
The intravenous WSU-FSCCL models were initiated by intravenous injection of 2.5 x 106 cells, in female severe combined immunodeficient (SCID) mice (Taconic). The dose was 0.15 mg/dose (2.4 g SN-38 equivalents) plus Veltuzumab, 35 ug/dose.
In Vivo Model WSU-FSCCL CDX model
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.17 nM
Low CEACAM5 expression (CEACAM5+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.73 nM
Low CEACAM5 expression (CEACAM5+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 3 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50)
8.08 nM
Low CEACAM5 expression (CEACAM5+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
Experiment 4 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Negative CEACAM5 expression (CEACAM5-)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma MN-60 cells CVCL_1421
Experiment 5 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Negative CEACAM5 expression (CEACAM5-)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Adult B acute lymphoblastic leukemia RS4;11 cells CVCL_0093
Experiment 6 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Negative CEACAM5 expression (CEACAM5-)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Childhood B acute lymphoblastic leukemia 697 cells CVCL_0079
Experiment 7 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Negative CEACAM5 expression (CEACAM5-)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 8 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Low CEACAM5 expression (CEACAM5+)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Follicular lymphoma WSU-FSCCL cells CVCL_1903
Experiment 9 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 nM Negative CEACAM5 expression (CEACAM5-)
Method Description
Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Lmab-CL2A-SN38 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.7 nM
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model B acute lymphoblastic leukemia Reh cells CVCL_1650
Experiment 2 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.8 nM
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 3 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Effective Concentration (EC50)
5.1 nM
Method Description
In vitro cytotoxicity by MTS assay of SN-38 and specific ADC conjugates against several hematopoietic tumor cell lines. The effect of linkage stability on the cytotoxicity of antibody conjugates as determined by a 4-day MTS assay.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
References
Ref 1 Phase I/II Trial of Labetuzumab Govitecan (Anti-CEACAM5/SN-38 Antibody-Drug Conjugate) in Patients With Refractory or Relapsing Metastatic Colorectal Cancer. J Clin Oncol. 2017 Oct 10;35(29):3338-3346.
Ref 2 Regulation of CEACAM5 and Therapeutic Efficacy of an Anti-CEACAM5-SN38 Antibody-drug Conjugate in Neuroendocrine Prostate Cancer. Clin Cancer Res. 2021 Feb 1;27(3):759-774.
Ref 3 Study of Labetuzumab Govitecan in Participants With Metastatic Colorectal Cancer
Ref 4 Study of IMMU-130 in Patients With Relapsed/Refractory Colorectal Cancer
Ref 5 A Phase II Study of IMMU 130 in Patients With Metastatic Colorectal Cancer
Ref 6 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34. doi: 10.1158/1535-7163.MCT-11-0632. Epub 2011 Oct 28.
Ref 7 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34.