General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TIZRJ
ADC Name
B4-SPP-DC4
Synonyms
B4 SPP DC4
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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
Antibody Name
Anti-CD19 mAb B4
 Antibody Info 
Antigen Name
B-lymphocyte antigen CD19 (CD19)
 Antigen Info 
Payload Name
Phosphate prodrugs 40 (DC4)
 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-DC4
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) 
≈ 84
%
Ramos cells
Burkitt lymphoma
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
11
pM
Ramos cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.74
nM
Ramos cells
Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
> 1.5
nM
HL-60 cells
Adult acute myeloid leukemia
Half Maximal Inhibitory Concentration (IC50) 
> 3
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) ≈ 84.00% (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.

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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 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 11.00 pM Positive CD19 expression (CD19+++/++)
Method Description
Cytotoxicity of B4-SPP-DCx Conjugates (without 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) 0.74 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 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1.50 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
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 3.00 nM Negative CD19 expression(CD19-)
Method Description
Cytotoxicity of B4-SPP-DCx Conjugates (without 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.

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