Linker Information

General Information of This Linker

Linker ID	LIN0KCPHV
Linker Name	PEG3-Val-Cit-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
Structure	3D MOL		2D MOL
Formula	C29H49N5O9
Isosmiles	CCOCCOCCOCCOCCC(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1)C(C)C
InChI	InChI=1S/C29H49N5O9/c1-4-40-14-15-42-18-19-43-17-16-41-13-11-25(36)34-26(21(2)3)28(38)33-24(6-5-12-31-29(30)39)27(37)32-23-9-7-22(20-35)8-10-23/h7-10,21,24,26,35H,4-6,11-20H2,1-3H3,(H,32,37)(H,33,38)(H,34,36)(H3,30,31,39)
InChIKey	NPMZKNGOTDXYHJ-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	611.737	Polar area	199.57
	Complexity	43	xlogp Value	0.6679
	Heavy Count	43	Rot Bonds	24
	Hbond acc	9	Hbond Donor	6

Each Antibody-drug Conjugate Related to This Linker

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

SYSA-1801 [Phase 1]

ADC Info

Identified from the Human Clinical Data

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

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Objective Response Rate (ORR)	47.10% (gastric cancer) 33.30% (1.00 mg/kg) 40.00% (2.00 mg/kg) 100.00% (2.50 mg/kg) 20.00% (3.00 mg/kg) 38.10% (all)
Patients Enrolled	Patients with resistant/refractory solid tumors that express CLDN18.2 who progressed on or were intolerant to standard treatment, or had no standard treatment were recruited.. ECOG score of 0-2.
Administration Dosage	0.50 up to 3.00 mg/kg on day 1, administered once every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT05009966	Clinical Status	Phase 1
Clinical Description	A phase 1 trial to evaluate safety, tolerability, pharmacokinetics, immunogenicity and initial efficacy of SYSA1801 in the treatment of CLDN 18.2 positive advanced malignant solid tumor.

References

Ref 1	Phase I, first-in-human study of AbGn-107, a novel antibody-drug conjugate (ADC), in patients with gastric, colorectal, pancreatic or biliary cancers. J Clin Oncol. 2020 38:15_suppl, e16771-e16771.