Linker Information
General Information of This Linker
| Linker ID |
LIN0KCPHV
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| Linker Name |
PEG3-Val-Cit-PABC
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C29H49N5O9
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| Isosmiles |
CCOCCOCCOCCOCCC(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1)C(C)C
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| 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)
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| InChIKey |
NPMZKNGOTDXYHJ-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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611.737
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Polar area
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199.57
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Complexity
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43
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xlogp Value
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0.6679
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Heavy Count
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43
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Rot Bonds
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24
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Hbond acc
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9
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Hbond Donor
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6
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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
SYSA1801 [Phase 1 (discontinued)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Inclusion criteria for Parts A/B: histologically confirmed pancreatic/gastric/esophagogastric junction cancer with ≥50% tumor cells showing moderate-to-strong claudin 18.2 staining (IHC 2+/3+), archived/fresh tumor tissue, adequate organ function, life expectancy >12 weeks, age ≥18, ECOG PS 0/1, informed consent, and negative pregnancy test for reproductive-potential females within 48h prior to enrollment.
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| Administration Dosage |
Part A will follow the standard 3+3 dose-escalation design and will be enrolled at dose levels of CPO102 at (0.5, 1, 1.8, 2.5, 3.5, 4.5, 5.5 mg/kg).
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| Related Clinical Trial | |||||
| NCT Number | NCT05043987 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1, Multicenter, Dose Escalation and Dose Expansion Study to Evaluate Safety of CPO102, an Anti-claudin 18.2 Antibody-MMAE Drug Conjugate Administered Intravenously in Patients With Advanced Pancreatic and Gastric Cancers
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| Primary Endpoint |
The study will assess the number of participants with dose-limiting toxicities (DLTs) during the DLT evaluation period (first 21-day cycle) to determine the maximum tolerated dose (MTD) and/or recommended phase 2 dose (RP2D), with data collected over an average of 3 years.
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| Other Endpoint |
Safety evaluations include treatment-emergent adverse events (TEAEs) graded by NCI-CTCAE v5.0 (Grade ≥3, serious, or fatal TEAEs with causality assessment), clinically significant changes in vital signs and lab tests, and CPO102 pharmacokinetics (AUC, Cmax, Tmax, t½, CL). Efficacy is measured by objective response rate (ORR per RECIST v1.1), while immunogenicity tracks anti-drug-antibody (ADA) incidence, all monitored over ~3 years.
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| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
47.10
33.30 40.00 100.00 20.00 38.10 % |
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| 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.
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| Administration Dosage |
0.50 up to 3.00 mg/kg on day 1, administered once every 3 weeks.
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| 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.
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References