Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0BFNMH
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
GQ1001
|
|||||
| Synonyms |
GQ1001
Click to Show/Hide
|
|||||
| Organization |
GeneQuantum Healthcare (Originator)
|
|||||
| Drug Status |
Phase 1/2
|
|||||
| Drug-to-Antibody Ratio |
2
|
|||||
| Structure |
|
|||||
|
|
||||||
| Antibody Name |
Trastuzumab variant
|
Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (HER2 ECD2); Receptor tyrosine-protein kinase erbB-2 (HER2 ECD4)
|
Antigen Info | ||||
| Payload Name |
DM1
|
Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
K'-MCC'
|
Linker Info | ||||
| Conjugate Type |
Enzymatic Catalysis
|
|||||
| Combination Type |
K'-MCC'-DM1
|
|||||
The indication landscape of This ADC(2027 Update)
The clinical trial pipeline of This ADC(2027 Update)
| Indication | Phase 1 | Phase 1/2 | Phase 2 | Phase 2/3 | Phase 3 | New Drug Application | Approved | ||
|---|---|---|---|---|---|---|---|---|---|
| Biliary tract cancer |
1 Trials
|
||||||||
| Breast cancer |
1 Trials
|
||||||||
| Gastric cancer |
1 Trials
|
||||||||
| Gastroesophageal junction adenocarcinoma |
1 Trials
|
||||||||
| Oral cavity cancer |
1 Trials
|
||||||||
| Unspecific solid tumor |
1 Trials
|
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 34505 | ng/mL |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1760000 | ng*h/mL |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1760000 | ng*h/mL |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
| Volume of Distribution (Vd) | 44.4 | mL/kg |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1760000 | ng*h/mL |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 1760000 | ng*h/mL |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
| Elimination Half-Life (t1/2) | 49.01 | h |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
| Clearance (CL) | 0.629 | mL/h/kg |
Blood samples for pharmacokinetics analysis were available from all 32 enrolled patients at the first cycle, the dose of adc is 1.2 mg/kg.
|
[1] |
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Partial Response (PR) |
40%
|
|||
| Patients Enrolled |
HER2-positive advanced solid tumors.
|
||||
| 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.
|
||||
| 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. | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| 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. | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [4] | ||||
| 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.
|
||||
| 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.
|
||||
| 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) | ||||
| 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.
|
||||
| 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.
|
||||
| Experiment 4 Reporting the Activity Date of This ADC | [5] | ||||
| 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.
Click to Show/Hide
|
||||
| Administration Dosage |
GQ1001 will be administered intravenously every 21 days. Dose Escalation will be guided by a modified 3+3 design.
|
||||
| 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 | ||||
| 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.
|
||||
| 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.
|
||||
References