Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0CMIZW
ADC Name	B4-SPP-DC44
Synonyms	B4 SPP DC44 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Acute promyelocytic leukemia [ICD11:2A60] Investigative Burkitt lymphoma [ICD11:2A85] Investigative
Drug-to-Antibody Ratio	3.5-5
Structure
	3D MOL	2D MOL
Antibody Name	Anti-CD19 mAb B4		Antibody Info
Antigen Name	B-lymphocyte antigen CD19 (CD19)		Antigen Info
Payload Name	DC44		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	N-succinimidyl 4-(2-pyridyldithio) pentanoate (SPP)		Linker Info
Conjugate Type	Lysine residue on the antibody is conjugated via an amide bond to the linker-payload moiety.
Combination Type	SPP-DC44

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 64	%	Ramos cells	Burkitt lymphoma

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.4	nM	Ramos cells	Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50)	> 1.8	nM	HL-60 cells	Adult acute myeloid leukemia

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.00% (Day 9)	Positive CD19 expression (CD19+++/++)
Method Description	Animals with established subcutaneous xenograft Ramos tumors were treated with either huB4-SPP-DC4 (DC4 dose of 75 ug/kg, qdx5), or huB4-SPP-DC44 (DC44 dose of 75 ug/kg, qdx5), unconjugated DC4 (75 ug/kg, qdx5), unconjugated DC44 (75 ug/kg, qdx5), or with phosphate-buffered saline vehicle (control), administered intravenously, and the tumor growth was monitored. Click to Show/Hide
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive CD19 expression (CD19+++/++)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1.80 nM	Negative CD19 expression(CD19-)
Method Description	Cytotoxicity of B4-SPP-DCx Conjugates (with acid phosphatase treatment) against Ramos (Ag+) and HL60/s (Ag-) Cells.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

References

Ref 1	Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer. J Med Chem. 2012 Jan 26;55(2):766-82. doi: 10.1021/jm201284m.