Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ZIJNR
ADC Name
hLL1-DOX
Synonyms
CD-74-DOX; IMMU-110; Milatuzumab doxorubicin; Milatuzumab-DOX; Milatuzumab-doxorubicin conjugate; hCD74-DOX; hLL1-DOX; hLL1-DOX, IMMU-115; hLL1-doxorubicin
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Organization
Immunomedics, Inc.; Gilead Sciences, Inc.
Drug Status
Phase 1/2 (Terminated)
Indication
In total 3 Indication(s)
Chronic lymphocytic leukemia
Phase 2
Clinical Trial
Multiple myeloma
Phase 2
Clinical Trial
Unspecific non-hodgkin lymphoma
Phase 2
Clinical Trial
Drug-to-Antibody Ratio
6 to 8
Structure
Antibody Name
Milatuzumab
  Antibody Info 
Antigen Name
HLA class II histocompatibility antigen gamma chain (CD74)
  Antigen Info 
Payload Name
Doxorubicin
  Payload Info 
Therapeutic Target
DNA topoisomerase 2-alpha (TOP2A)
  Target Info 
Linker Name
Mcc-hydrazide
  Linker Info 
Conjugate Type
Random Cysteines
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.8
uM
Raji cells
EBV-related Burkitt lymphoma
Half Maximal Inhibitory Concentration (IC50) 
0.9
uM
MC/CAR cells
Normal
Half Maximal Inhibitory Concentration (IC50) 
1.5
uM
Daudi cells
Burkitt lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.80 uM Positive CD74 expression (CD74+++/++)
Method Description
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).

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In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.90 uM Positive CD74 expression (CD74+++/++)
Method Description
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).

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In Vitro Model Normal MC/CAR cells CVCL_1397
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.50 uM Positive CD74 expression (CD74+++/++)
Method Description
Briefly, cells were placed in 96-well plates (2 x105 per well) and subsequently incubated with serial dilutions of IMMU-110,naked hLL1,nonspecific negative control mAb-drug conjugate (hRS7-doxorubicin),or nonspecific mAb (hRS7) on ice for 1.5 hours. 4-hour IC50 values of IMMU-110,hRS7-doxorubicin,and free doxorubicin against the multiple myeloma cell line (MC/CAR) and other CD74-positive non-Hodgkin's lymphoma cell lines (Daudi and Raji).

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In Vitro Model Burkitt lymphoma Daudi cells CVCL_0008
References
Ref 1 Anti-CD74 antibody-doxorubicin conjugate, IMMU-110, in a human multiple myeloma xenograft and in monkeys. Clin Cancer Res. 2005 Jul 15;11(14):5257-64.