Linker Information

Linker Information

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)

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Each Antibody-drug Conjugate Related to This Linker

Full Information of The Activity Data of The ADC(s) Related to This Linker

FOLR1-ADC 15 [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 6 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.60% (Day 95)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 0.7 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.27% (Day 95)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 1.4 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)
Experiment 3 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 0.7 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)
Experiment 4 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 1.4 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)
Experiment 5 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 2.7 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)
Experiment 6 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 95)	Low FOLR1 expression (FOLR1+)
Method Description	SCID mice bearing OV90 subcutaneous ovarian xenografts, which express folate receptor alpha heterogeneously, at a very low level (H-Score 40)16 were treated with ADC 15 (DAR 3.2).as treatment with a single i.v. dose of 2.7 mg/kg.
In Vivo Model	Ovarian cancer PDX model (PDX: OV90)

References

Ref 1	Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs). ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.

Linker Name

Adipic acid-Val-CIt-PABC

Linker Type

Cathepsin-cleavable linker

Antibody-Linker Relation