Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0HDIEW
ADC Name	CAC10-Gly5-MAY
Synonyms	Cac10 Gly5 May Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Acute lymphoblastic leukemia [ICD11:2B33] Investigative Non Hodgkin lymphoma [ICD11:2B33] Investigative
Drug-to-Antibody Ratio	3.4
	3D MOL	2D MOL
Antibody Name	Brentuximab		Antibody Info
Antigen Name	Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Gly5		Linker Info

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

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

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 100	%	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma
Tumor Growth Inhibition value (TGI)	≈ 100	%	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma

Revealed Based on the Cell Line Data

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

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	4.7	ng/mL	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 14)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 16)	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 10 mg/kg ADC preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm³.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.70 ng/mL	High CD30 expression (CD30+++)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

References

Ref 1	Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.