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
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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]
Identified from the Human Clinical Data
Click To Hide/Show 1 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.
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)
140.00 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]
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 [3]
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 [3]
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 [3]
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 [3]
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 [3]
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 [3]
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 [3]
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 [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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 7 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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 8 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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 9 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50.00 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
Lmab-CL2A-SN38 [Investigative]
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 [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.70 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 [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.80 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 [4]
Efficacy Data Half Maximal Effective Concentration (EC50)
5.10 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 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 4 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34.

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