General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0CRYVT
ADC Name
DP-303c
Synonyms
DP 303c; DP303c
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Organization
CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.; CSPC Pharmaceutical Group Ltd.
Drug Status
Phase 3
Indication
In total 5 Indication(s)
HER2(+) breast cancer [ICD11:2C60-2C65]
Phase 3
Gastric cancer [ICD11:2B72]
Phase 2
Ovarian cancer [ICD11:2C73]
Phase 2
HER2(+) solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 1
Salivary gland tumor [ICD11:2E91]
Phase 1
Drug-to-Antibody Ratio
2
Antibody Name
DP001
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
PEG2-Val-Cit-PABC
 Linker Info 
Conjugate Type
Site-specific conjugation through the glutamine 295 by an engineered transglutaminase (mTgase).
Drugbank ID
DB17212
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Undisclosed  NCT05334810
Phase 2
A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Undisclosed  NCT04828616
Phase 2
An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Undisclosed  NCT04826107
Phase 2
An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Undisclosed  NCT04146610
Phase 1
A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 34 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 7.6
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 16.2
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 28.47
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 33.6
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 39
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 45.26
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 54.4
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 82.1
%
SK-BR-3 cells
Breast adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 83.94
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 90.48
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 91.6
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94.1
%
SK-BR-3 cells
Breast adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94.16
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 94.3
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.1
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.5
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.5
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.8
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.8
%
SK-BR-3 cells
Breast adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.8
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 98.5
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 98.54
%
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 98.8
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.1
%
HCC1954 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.9
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
JIMT-1 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
JIMT-1 cells
Breast ductal carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.07
nM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.07
nM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.08
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.08
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.15
nM
HCC1954 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.15
nM
HCC1954 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.22
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.22
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.23
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.23
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.39
nM
JIMT-1 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.39
nM
JIMT-1 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 50
nM
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 1000
nM
MDA-MB-468 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Related Clinical Trial
NCT Number NCT05334810  Clinical Status Phase 2
Clinical Description A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT04828616  Clinical Status Phase 2
Clinical Description An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT04826107  Clinical Status Phase 2
Clinical Description An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Experiment 4 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT04146610  Clinical Status Phase 1
Clinical Description A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 34 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 7.60% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP001 (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 16.20% (Day 32) Moderate HER2 expression (HER2++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 28.47% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP001 (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.60% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP001 (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 39.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (0.3 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.26% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (1 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 54.40% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.94% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (3 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.48% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP001 (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.60% (Day 25) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (2.5 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (5 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.10% (Day 18) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.16% (Day 18) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 17 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.30% (Day 21) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 18 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 19 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 20 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (3 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 21 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

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In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 23 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 24 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 25 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 18) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 26 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 27 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 28 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.54% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 29 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.80% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 30 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.

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In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 31 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.90% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 32 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (1 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 33 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 34 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (3 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.07 nM Moderate HER2 expression (HER2++; HER2 MFI=157,231)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.07 nM High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.08 nM High HER2 expression (HER2+++; HER2 MFI=987,353)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.08 nM Negative HER2 expression (HER2-; HER2 MFI=256)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.15 nM High HER2 expression (HER2+++)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.15 nM High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.22 nM Negative HER2 expression (HER2-)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.22 nM High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.23 nM High HER2 expression (HER2+++; HER2 MFI=804,573)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.23 nM High HER2 expression (HER2+++; HER2 MFI=892,333)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.39 nM High HER2 expression (HER2+++)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.39 nM Moderate HER2 expression (HER2++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50.00 nM High HER2 expression (HER2+++; HER2 MFI=1,106,494)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM High HER2 expression (HER2+++; HER2 MFI=765,629)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 A Multi-center, Open-lable, Single-arm Phase II Study to Evaluate the Efficacy and Safety of DP303c in Patients With HER2-positive Unresectable Locally Advanced, Relapsed, or Metastatic Breast Cancer, NCT05334810
Ref 2 An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With HER2-expressing Advanced Ovarian Cancer, NCT04828616
Ref 3 An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Gastric Cancer With HER2 Expression, NCT04826107
Ref 4 A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors, NCT04146610
Ref 5 An Innovative Site-Specific Anti-HER2 Antibody-Drug Conjugate with High Homogeneity and Improved Therapeutic Index. Onco Targets Ther. 2022 Apr 8;15:331-343.

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