Linker Information
General Information of This Linker
| Linker ID |
LIN0SZZUJ
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| Linker Name |
K'-MCC'
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| Antibody-Linker Relation |
Uncleavable
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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
GQ1001 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Partial Response (PR) |
40%
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| Patients Enrolled |
HER2-positive advanced solid tumors.
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| Administration Dosage |
Administered intravenously as a monotherapy on Day 1 of 21-day cycles. The starting dose was 1.20 mg/kg, followed by 2.40, 3.60, 4.80, 6.00, 7.20 and 8.40 mg/kg.
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| Related Clinical Trial | |||||
| NCT Number | NCT04450732 | Clinical Status | Phase 1 | ||
| Clinical Description |
A phase 1, first-in-human, multicenter, open-label, study of GQ1001, a HER2 targeted antibody-drug conjugate, administered intravenously, in adult patients with HER2-positive advanced solid tumors.
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| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05575804 | Clinical Status | Phase 1/2 | ||
| Clinical Description |
Phase 1b/2 study of GQ1001 and pyrotinib in HER2 positive metastatic breast cancer patients who had failed previous anti-HER2 treatment GRACE.
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| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Patients Enrolled |
Eligible patients are HER2+ metastatic breast cancer patients (IHC3+/ISH+, ECOG 0-1, LVEF≥50%) with ≥1 prior trastuzumab-based therapy, measurable lesions, and adequate organ function, excluding those with active CNS metastases, prior DM1-ADC/pyrotinib use (exceptions apply), significant cardiac/ILD history, or uncontrolled infections.
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| Administration Dosage |
Patients will receive the recommended phase 2 dose of GQ1001 determined in phase I. GQ1001 infusions on day 1 of each 21-day cycle combinate with pyrotinib 320mg orally once daily until disease progression or unacceptable toxicity.
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| Related Clinical Trial | |||||
| NCT Number | NCT05575804 | Clinical Status | PHASE1|||PHASE2 | ||
| Clinical Description |
Phase Ib/II Study of GQ1001 and Pyrotinib in HER2 Positive Metastatic Breast Cancer Patients Who Had Failed Previous Anti-HER2 Treatment(GRACE)
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| Primary Endpoint |
The study evaluates dose-limiting toxicities (DLTs) and maximum tolerated dose (MTD) in Phase I (21-day cycles), along with treatment-related adverse events (CTCAE v5.0) and objective response rate (ORR, RECIST 1.1) over 24 months.
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| Other Endpoint |
Pharmacokinetic parameters (Cmax, Ctrough, AUC) for GQ1001, DM1, pyrotinib, and anti-HER2 antibody are assessed in Phase I, while efficacy outcomes (ORR, DoR, DCR, PFS per RECIST 1.1) are tracked across both phases for 24 months.
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| Experiment 4 Reporting the Activity Date of This ADC | [4] | ||||
| Patients Enrolled |
Eligible patients are adults (≥18) with HER2+ advanced/metastatic solid tumors (breast, gastric/GEJ, or other) refractory to standard therapy, ECOG 0-1, LVEF≥50%, and adequate organ function, excluding those with active brain metastases, significant cardiac/pulmonary disease, unresolved toxicities (>Grade 1), uncontrolled infections, or prior cumulative anthracycline dose >360mg/m2 doxorubicin-equivalent.
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| Administration Dosage |
GQ1001 will be administered intravenously every 21 days. Dose Escalation will be guided by a modified 3+3 design.
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| Related Clinical Trial | |||||
| NCT Number | NCT04450732 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1, First-In-Human, Multicenter, Open-Label, Study of GQ1001, a HER2 Targeted Antibody-Drug Conjugate, Administered Intravenously, in Adult Patients With HER2-Positive Advanced Solid Tumors
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| Primary Endpoint |
The study evaluates dose-limiting toxicities (DLTs) and determines maximum tolerated dose (MTD) or recommended expansion dose (DRDE) during the first 21-day cycle, with adverse events assessed per NCI CTCAE v5.0 criteria.
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| Other Endpoint |
Safety assessments include AE monitoring, lab abnormalities, and pharmacokinetic parameters (AUC, Cmax, Tmax, T1/2, MRT, Vd) of GQ1001, along with efficacy outcomes (ORR, DCR, DoR, PFS per RECIST 1.1) and immunogenicity (anti-drug antibodies) over approximately 1 year.
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References