General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ZUUMS
ADC Name
TE-1146
Synonyms
TE-1146
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Organization
Immunwork, Inc.; Institute of Biomedical Sciences.
Drug Status
Investigative
Drug-to-Antibody Ratio
6
Antibody Name
alpha-CD38 mAb
 Antibody Info 
Antigen Name
ADP-ribosyl cyclase/cyclic ADP-ribose hydrolase 1 (CD38)
 Antigen Info 
Payload Name
Lenalidomide
 Payload Info 
Linker Name
Undisclosed
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The ADMET Data Related to This ADC(2027 Update)
Excretion
Click To Hide/Show 1 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Elimination Half-Life (t1/2) 6-7 day
We assessed the stability of TE-1146 compared to that of daratumumab or unconjugated alpha-CD38. All three molecules were dissolved in 90% human plasma, incubated at 37 °C for 28 days, and analyzed by ELISA. Daratumumab, alpha-CD38 mAb, and TE-1146 exhibited similar half-lives (T1/2) of 6-7 days in human plasma over the 28 days.

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[1]
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 (lC50) 
0.45
uM
CVCL_1600
Multiple myeloma, Plasma cell myeloma
Half Maximal inhibitory Concentration (lC50) 
0.45
uM
CVCL_8792
Plasma cell myeloma, Multiple myeloma
Half Maximal inhibitory Concentration (lC50) 
> 10000
uM
Undisclosed
Multiple myeloma, Plasma cell myeloma
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 (lC50) 0.45 uM High CD38 expression (CD38 +++)
Method Description
To evaluate the cytotoxic effects of various drugs, H929, U266-CD38-, MM.1S, and Daudi cells were seeded at 5000 cells per well in 96-well plates and cocultured with fresh medium containing different drug concentrations for varying durations (5 h, 1 day, 3 or 5 days) at 37 °C. Cell viability was determined using the alamarBlue cell viability reagent (Thermo Fisher Scientific). About 10 uL alamarBlue cell viability reagent was added to achieve a final concentration of 10% v/v and incubated at 37 °C for 1.5 h. The fluorescence was measured on a microplate reader in arbitrary fluorescent units following excitation at 560 nm and emission at 590 nm.

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In Vitro Model Multiple myeloma, Plasma cell myeloma H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.45 uM High CD38 expression (CD38 +++)
Method Description
To evaluate the cytotoxic effects of various drugs, H929, U266-CD38-, MM.1S, and Daudi cells were seeded at 5000 cells per well in 96-well plates and cocultured with fresh medium containing different drug concentrations for varying durations (5 h, 1 day, 3 or 5 days) at 37 °C. Cell viability was determined using the alamarBlue cell viability reagent (Thermo Fisher Scientific). About 10 uL alamarBlue cell viability reagent was added to achieve a final concentration of 10% v/v and incubated at 37 °C for 1.5 h. The fluorescence was measured on a microplate reader in arbitrary fluorescent units following excitation at 560 nm and emission at 590 nm.

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In Vitro Model Plasma cell myeloma, Multiple myeloma MM.1S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 10000 uM Negative CD38 expression (CD38-)
Method Description
To evaluate the cytotoxic effects of various drugs, H929, U266-CD38-, MM.1S, and Daudi cells were seeded at 5000 cells per well in 96-well plates and cocultured with fresh medium containing different drug concentrations for varying durations (5 h, 1 day, 3 or 5 days) at 37 °C. Cell viability was determined using the alamarBlue cell viability reagent (Thermo Fisher Scientific). About 10 uL alamarBlue cell viability reagent was added to achieve a final concentration of 10% v/v and incubated at 37 °C for 1.5 h. The fluorescence was measured on a microplate reader in arbitrary fluorescent units following excitation at 560 nm and emission at 590 nm.

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In Vitro Model Multiple myeloma, Plasma cell myeloma U266 (CD38-) cells Homo sapiens
References
Ref 1 An Antibody-Drug Conjugate for Multiple Myeloma Prepared by Multi-Arm Linkers