Antibody Information

General Information of This Antibody
Antibody ID
ANI0NMRGS
Antibody Name
MAB802
Synonyms
Fyper-fucosylated Trastuzumab
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG
PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN
STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREE
MTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW
QQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Light Chain Sequence
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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The Activity Data of This Antibody
Antibody Activity Information 1 [1]
Dissociation Constant (Kd)
986
pM
Antibody Function Confirm the effect of the drug conjugation with the anti-HER2 Ab on binding activity to target.
Antibody Antigen Binding Assay Binding affinity of MRG002 and MAB802 to human HER2 as determined by SPR.
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
MRG-002 [Phase 3]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
34.70%
Patients Enrolled
Advanced/metastatic HER2-low expressing breast cancer that failed standard therapies.
Administration Dosage
MRG002 was administered intravenously once every 3 weeks at the dose of 2.60 mg/kg, until disease progression or unacceptable toxicity which ever occurred first.
Related Clinical Trial
NCT Number NCT04742153  Clinical Status Phase 2
Clinical Description
A multicenter, non-randomized, open-label phase 2 clinical study to evaluate the efficacy and safety of MRG002 in the treatment of patients with HER2-low locally advanced or metastatic breast cancer (BC).
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Objective Response Rate (ORR)
65.00%
Patients Enrolled
Histologically HER2-positive (IHC 2+ or 3+) UC pts confirmed by a central-laboratory, ECOG PS 0-1, prior received 1 standard treatment.
Administration Dosage
Receive MRG002 at a dose of 2.60 mg/kg or 2.20 mg/kg administered by intravenous infusion every 3 weeks.
Related Clinical Trial
NCT Number NCT04839510  Clinical Status Phase 2
Clinical Description
An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelium cancer.
Experiment 3 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT05754853  Clinical Status Phase 3
Clinical Description
An open-label, randomized, multi-center, phase 3 clinical study of MRG002 versus investigator's choice of chemotherapy in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelial cancer previously treated with platinum-based chemotherapy and PD-1/PD-L1 inhibitors.
Experiment 4 Reporting the Activity Date of This ADC [5]
Related Clinical Trial
NCT Number NCT04924699  Clinical Status Phase 2/3
Clinical Description
A study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic breast cancer.
Experiment 5 Reporting the Activity Date of This ADC [6]
Related Clinical Trial
NCT Number NCT05263869  Clinical Status Phase 2
Clinical Description
An open-label, multi-center, single-arm phase 2 clinical study to evaluate the efficacy and safety of MRG002 in advanced HER-2 positive breast cancer patients previously treated with trastuzumab and TKIs (Magic-009).
Experiment 6 Reporting the Activity Date of This ADC [7]
Related Clinical Trial
NCT Number NCT05141786  Clinical Status Phase 2
Clinical Description
An open-label, multi-center, non-randomized phase 2 clinical study to evaluate the efficacy and safety of MRG002 in patients With HER2-mutated unresectable/metastatic non-small cell lung cancer (NSCLC).
Experiment 7 Reporting the Activity Date of This ADC [8]
Related Clinical Trial
NCT Number NCT05141747  Clinical Status Phase 2
Clinical Description
An open-label, multi-center, phase 2 clinical study to evaluate the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive/HER2-low locally advanced or metastatic gastric/ gastroesophageal junction cancer.
Experiment 8 Reporting the Activity Date of This ADC [9]
Related Clinical Trial
NCT Number NCT04837508  Clinical Status Phase 2
Clinical Description
An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable, locally advanced or metastatic biliary tract cancer.
Experiment 9 Reporting the Activity Date of This ADC [10]
Related Clinical Trial
NCT Number NCT05338957  Clinical Status Phase 1/2
Clinical Description
An open-label, multi-center, phase 1/2 dose escalation and expansion study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of MRG002 in combination with HX008 in patients with HER2-expressed advanced malignant solid tumors.
Experiment 10 Reporting the Activity Date of This ADC [11]
Related Clinical Trial
NCT Number NCT04492488  Clinical Status Phase 1/2
Clinical Description
An open-label, multi-center phase 1/2 dose escalation and expansion study to assess the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive advanced solid tumors and locally advanced or metastatic gastric/gastroesophageal junction (GEJ) cancer.
Experiment 11 Reporting the Activity Date of This ADC [12]
Related Clinical Trial
NCT Number NCT04941339  Clinical Status Phase 1
Clinical Description
A phase 1, open-label, multi-center, first in human, dose escalation and expansion study to assess the safety, tolerability, efficacy and pharmacokinetics of MRG002 in patients with HER2 positive advanced solid tumors.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 16 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
0.00% (Day 21)
Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#151)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
10.00% (Day 21)
Low HER2 expression (HER2+; IHC 1+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#395)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
17.00% (Day 21)
High HER2 expression (HER2+++; IHC 3+)
In Vivo Model HER2-positive breast cancer PDX model (PDX: BC#239)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
19.00% (Day 21)
Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#053)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
41.00% (Day 21)
Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#240)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 55.10% (Day 63) High HER2 expression (HER2+++; IHC 3+)
In Vivo Model HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.00% (Day 56) Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.40% (Day 35) High HER2 expression (HER2+++; IHC 3+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 78.90% (Day 24)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
84.00% (Day 21)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.90% (Day 70)
In Vivo Model HER2-positive breast cancer PDX model (PDX: BC#197)
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
90.00% (Day 21)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#069)
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 63)
In Vivo Model HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.10% (Day 56)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 70) High HER2 expression (HER2+++; IHC 3+)
In Vivo Model HER2-positive breast cancer PDX model (PDX: BC#197)
Experiment 16 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) Low HER2 expression (HER2+; IHC 1+)
In Vivo Model HER2-positive gastric cancer PDX model (PDX: STO#410)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 60.70% (Day 36) Moderate HER2 expression (HER2++)
In Vivo Model HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 66.20% (Day 36) High HER2 expression (HER2+++)
Method Description
MRG-002 induces efficient tumor cell killing in PDX models of breast cancer or gastric cancer tissues with HER2 expression,administered with vehicle,MRG002,HX008 or MRG002 + HX008 combo intravenously.
In Vivo Model HER2-positive breast cancer BT-474 CDX model
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.00% (Day 36) Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive breast cancer BT-474 CDX model
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.00% (Day 36) Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model HER2-positive breast cancer BT-474 CDX model
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.00% (Day 36) High HER2 expression (HER2+++)
In Vivo Model HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.00% (Day 36) High HER2 expression (HER2+++)
In Vivo Model HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM
Method Description
The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Method Description
The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.15 nM
Method Description
The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.40 nM
Method Description
The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
References
Ref 1 Preclinical evaluation of MRG002, a novel HER2-targeting antibody-drug conjugate with potent antitumor activity against HER2-positive solid tumors. Antib Ther. 2021 Aug 28;4(3):175-184.
Ref 2 A multiple center, open-label, single-arm, phase II clinical trial of MRG002, an HER2-targeted antibody-drug conjugate, in patients with HER2-low expressing advanced or metastatic breast cancer. J Clin Oncol. 2022 40:16_suppl, 1102-1102.
Ref 3 MRG002-006: A multicenter phase II clinical trial of MRG002-ADC for unresectable locally advanced or metastatic urothelial cancer. J Clin Oncol. 2022 40:16_suppl, 4570-4570.
Ref 4 An Open-label, Randomized, Multi-center, Phase III Clinical Study of MRG002 Versus Investigator's Choice of Chemotherapy in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelial Cancer Previously Treated With Platinum-based Chemotherapy and PD-1/PD-L1 Inhibitors, NCT05754853
Ref 5 A Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer, NCT04924699
Ref 6 An Open-label, Multi-center, Single-arm Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in Advanced HER-2 Positive Breast Cancer Patients Previously Treated With Trastuzumab and TKIs (Magic-009), NCT05263869
Ref 7 An Open-label, Multi-center, Non-randomized Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in Patients With HER2-mutated Unresectable/Metastatic Non-small Cell Lung Cancer (NSCLC). NCT05141786
Ref 8 An Open-label, Multi-center, Phase II Clinical Study to Evaluate the Safety, Efficacy and Pharmacokinetics of MRG002 in Patients With HER2-positive/HER2-low Locally Advanced or Metastatic Gastric/ Gastroesophageal Junction Cancer. NCT05141747
Ref 9 An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable, Locally Advanced or Metastatic Biliary Tract Cancer, NCT04837508
Ref 10 An Open-label, Multi-center, Phase I/II Dose Escalation and Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of MRG002 in Combination With HX008 in Patients With HER2-expressed Advanced Malignant Solid Tumors. NCT05338957
Ref 11 An Open-Label, Multi-center Phase I/II Dose Escalation and Expansion Study to Assess the Safety, Efficacy and Pharmacokinetics of MRG002 in Patients With HER2-Positive Advanced Solid Tumors and Locally Advanced or Metastatic Gastric/Gastroesophageal Junction (GEJ) Cancer, NCT04492488
Ref 12 A Phase I, Open-label, Multi-center, First in Human, Dose Escalation and Expansion Study to Assess the Safety, Tolerability, Efficacy and Pharmacokinetics of MRG002 in Patients With HER2 Positive Advanced Solid Tumors, NCT04941339

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