Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0RGMND
ADC Name	Epratuzumab-CL2E-SN-38
Synonyms	Emab-CL2E-SN-38 Click to Show/Hide
Drug Status	Investigative
Indication	In total 3 Indication(s) B-cell lymphoma [ICD11:2A86] Investigative Burkitt lymphoma [ICD11:2A85] Investigative Mantle cell lymphoma [ICD11:2A85] Investigative
Drug-to-Antibody Ratio	6
	3D MOL	2D MOL
Antibody Name	Epratuzumab		Antibody Info
Antigen Name	B-cell receptor CD22 (CD22)		Antigen Info
Payload Name	Active metabolite of irinotecan SN38		Payload Info
Therapeutic Target	DNA topoisomerase 1 (TOP1)		Target Info
Linker Name	CL2E		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 4 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Median survival time (MST)	42	Day	WSU-FSCCL cells	Follicular lymphoma
Median survival time (MST)	63	Day	WSU-FSCCL cells	Follicular lymphoma
Median survival time (MST)	140	Day	WSU-FSCCL cells	Follicular lymphoma
Median survival time (MST)	> 161	Day	WSU-FSCCL cells	Follicular lymphoma

Revealed Based on the Cell Line Data

Click To Hide/Show 37 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Effective Concentration (EC50)	0.06	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.19	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.2	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.34	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.38	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.41	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.46	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.46	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.5	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.51	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.52	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.68	nM	WSU-FSCCL cells	Follicular lymphoma
Half Maximal Effective Concentration (EC50)	0.73	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	0.81	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	0.83	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	0.84	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	1.16	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	1.16	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	1.22	nM	Reh cells	B acute lymphoblastic leukemia
Half Maximal Effective Concentration (EC50)	1.5	nM	Daudi cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	1.66	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	1.68	nM	RS4 11 cells	Adult B acute lymphoblastic leukemia
Half Maximal Effective Concentration (EC50)	1.72	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	1.77	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	1.84	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	. 2.1	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	2.21	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	2.25	nM	JeKo-1 cells	Mantle cell lymphoma
Half Maximal Effective Concentration (EC50)	2.29	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	2.45	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	2.67	nM	697 cells	Childhood B acute lymphoblastic leukemia
Half Maximal Effective Concentration (EC50)	2.88	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	2.92	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	3.65	nM	MN-60 cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	135.8	nM	Raji cells	EBV-related Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	152.3	nM	Ramos cells	Burkitt lymphoma
Half Maximal Effective Concentration (EC50)	271	nM	Ramos cells	Burkitt lymphoma

Full List of Activity Data of This Antibody-drug Conjugate

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					[1]
Efficacy Data	Median survival time (MST)	42 Day	Low CD22 expression (CD22+)
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 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	63 Day	Low CD22 expression (CD22+)
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 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	140 Day	Low CD22 expression (CD22+)
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
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	> 161 Day	Low CD22 expression (CD22+)
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

Revealed Based on the Cell Line Data

Click To Hide/Show 37 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.06 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.20 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.34 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.38 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with SN38 and increasing concentrations of Emab-SN-38.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.41 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.46 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.46 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.50 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with SN38 and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 10 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.51 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 11 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.52 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 12 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.68 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Follicular lymphoma	WSU-FSCCL cells		CVCL_1903
Experiment 13 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.73 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 14 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.81 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 15 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.83 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 16 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.84 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 17 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.16 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 18 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.16 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with veltuzumab (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 19 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.22 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	B acute lymphoblastic leukemia	Reh cells		CVCL_1650
Experiment 20 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.50 nM	High CD22 expression (CD22+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 21 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.66 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 22 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.68 nM	Moderate CD22 expression (CD22++)
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 23 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.72 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with SN38 and increasing concentrations of Emab-SN-38.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 24 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.77 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with SN38 and increasing concentrations of Emab-SN-38.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 25 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.84 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with SN38 and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 26 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	. 2.10 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 27 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.21 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 28 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.25 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 29 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.29 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 30 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.45 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (1.33 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 31 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.67 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Childhood B acute lymphoblastic leukemia	697 cells		CVCL_0079
Experiment 32 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.88 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay. Cells were co-incubated with hRS7 (133 nmol/L) and increasing concentrations of Emab-SN-38.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 33 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.92 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 34 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.65 nM	Low CD22 expression (CD22+)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Burkitt lymphoma	MN-60 cells		CVCL_1421
Experiment 35 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	135.80 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 36 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	152.30 nM	Moderate CD22 expression (CD22++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 37 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	271 nM	High CD20 expression (CD20+++)
Method Description	Cytotoxicity was determined using the MTS dye reduction assay.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

References

Ref 1	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.

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Antibody-drug Conjugate Information

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)