Linker Information
General Information of This Linker
| Linker ID |
LIN0KETHD
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| Linker Name |
A cleavable peptide linker
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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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
DXC006 [Phase 1]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.0046-0.061 nM
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Positive CD56 expression (CD56+++/++) | ||
| Method Description |
Cytotoxicity of ADC to CD56 positive IMR-32 cells
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.0046-0.061 nM
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Positive CD56 expression (CD56+++/++) | ||
| Method Description |
Cytotoxicity of ADC to CD56 NCI-H526 positive cells
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.0046-0.061 nM
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Positive CD56 expression (CD56+++/++) | ||
| Method Description |
Cytotoxicity of ADC to CD56 positive NCI-H929 cells
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 675 nM | |||
| Method Description |
Cytotoxicity of ADC to human NK cells
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| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Patients Enrolled |
Eligible patients (≥18 years, ECOG 0-2) must consent, have ≥3-month life expectancy, and show target protein expression. Exclusions encompass recent transplants, uncontrolled CVD (QTcF≥470ms, NYHA III-IV), active HBV/HCV/HIV/syphilis, pregnancy, major surgery within 28 days, bleeding disorders, or live vaccinations within 28 days. Organ function thresholds vary by disease status.
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| Administration Dosage |
Dose escalation period: DXC006 is administered intravenously every two weeks (Q2W) at the dose corresponding to the enrolled dose cohort.Dose expansion period: DXC006 is administered intravenously Q2W at the corresponding dose.
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| Related Clinical Trial | |||||
| NCT Number | NCT06224855 | Clinical Status | PHASE1 | ||
| Clinical Description |
An Open-label Dose Escalation and Cohort Expansion Phase I Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and and Efficacy of DXC006 in Patients With Advanced Solid Tumors and Hematologic Malignancies
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| Primary Endpoint |
The study will quantify dose-limiting toxicities (DLTs) within 28 days to establish maximum tolerated dose, while monitoring adverse events (CTCAE v5.0) for approximately 1 year post-treatment.
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| Other Endpoint |
Pharmacokinetic analysis includes Cmax, Tmax, Vd, Vss, t½, AUC0-t/0-inf, and CL measurements over 1 year. Immunogenicity (ADA titers), ORR (RECIST 1.1), DOR, PFS, and OS will be evaluated for 1 year post-enrollment.
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LY4052031 [Phase 1 (discontinued)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Patients Enrolled |
Eligible participants include those with specific solid tumors (separate cohort requirements apply), ECOG 0-1, and adequate tumor tissue availability. Major exclusions include uncontrolled CNS metastases, cardiovascular disease, severe prior toxicities, QTcF ≥470 ms, and active corneal/pulmonary conditions, with additional enfortumab vedotin-related restrictions for certain cohorts.
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| Related Clinical Trial | |||||
| NCT Number | NCT06465069 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1a/1b Study of LY4052031, an Antibody-Drug Conjugate Targeting Nectin-4, in Participants With Advanced or Metastatic Urothelial Carcinoma or Other Solid Tumors
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| Primary Endpoint |
Phase 1a aims to determine the Recommended Phase 2 Dose (RP2D) of LY4052031 by evaluating dose-limiting toxicities (DLTs) within Cycle 1 (21 days). Phase 1b assesses antitumor activity through Overall Response Rate (ORR) per RECIST 1.1 over approximately 48 months.
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| Other Endpoint |
Key evaluations include pharmacokinetics (PK) parameters (Cmin, AUC) during Cycle 1 and antitumor activity metrics (ORR, DOR, TTR, PFS, DCR, OS) per RECIST 1.1 tracked over 48 months to comprehensively characterize LY4052031's clinical profile.
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References