Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0HCGBQ
ADC Name	CAC10-Gly5-PNU
Synonyms	Cac10 Gly5 PNU 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	3.7-3.9
	3D MOL	2D MOL
Antibody Name	Brentuximab		Antibody Info
Antigen Name	Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)		Antigen Info
Payload Name	PNU-159682		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		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 2 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	1.8	ng/mL	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma
Half Maximal Inhibitory Concentration (IC50)	4.8	ng/mL	Reh cells	B acute lymphoblastic leukemia

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 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 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 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

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)	1.80 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
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.80 ng/mL	Negative 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	B acute lymphoblastic leukemia	Reh cells		CVCL_1650

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.