Linker Information
General Information of This Linker
| Linker ID |
LIN0GVDHS
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| Linker Name |
Fleximer polymer
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| Linker Type |
Polymer 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
ASN004 [Phase 1 (discontinued)]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 28.20% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 0.3 mg/kg single dose.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 54.30% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 0.3 mg/kg Q4D 4.
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| In Vivo Model | Lung cancer CDX model | ||||
| In Vitro Model | Lung cancer | Lung cancer cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 55.50% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 1 mg/kg Q4D 4.
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| In Vivo Model | Cervical advanced-stage cancer CDX model | ||||
| In Vitro Model | Cervical advanced-stage cancer | Cervical advanced-stage cancer cells | Homo sapiens | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.20% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 1 mg/kg single dose.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.30% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg single dose.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg Q4D 4.
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| In Vivo Model | Lung cancer CDX model | ||||
| In Vitro Model | Lung cancer | Lung cancer cells | Homo sapiens | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 1 mg/kg Q4D 4.
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| In Vivo Model | Lung cancer CDX model | ||||
| In Vitro Model | Lung cancer | Lung cancer cells | Homo sapiens | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Negative 5T4 expression (5T4-) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. A tumor xenograft model derived from the NCI-N87 human gastric tumor cell line [5T4-; 4, 400 binding sites per cell] and high expression of HER2. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg Q4D 3.
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| In Vivo Model | Gastric cancer CDX model | ||||
| In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Negative 5T4 expression (5T4-) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. A tumor xenograft model derived from the NCI-N87 human gastric tumor cell line [5T4-; 4, 400 binding sites per cell] and high expression of HER2. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg single dose.
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| In Vivo Model | Gastric cancer CDX model | ||||
| In Vitro Model | Gastric cancer | Gastric cancer cells | Homo sapiens | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | High 5T4 expression (5T4+++) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ubcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 10 mg/kg single dose.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells (5T4 overexpression) | CVCL_0062 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | High 5T4 expression (5T4+++) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 6mg/kg Q4D 4.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells (5T4 overexpression) | CVCL_0062 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | High 5T4 expression (5T4+++) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg Q4D 4.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells (5T4 overexpression) | CVCL_0062 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | High 5T4 expression (5T4+++) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 1 mg/kg Q4D 4.
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| In Vivo Model | Breast cancer CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells (5T4 overexpression) | CVCL_0062 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 10 mg/kg single dose.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 6mg/kg Q4D 4.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 3 mg/kg Q4D 4.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Low 5T4 expression (5T4+) | ||
| Method Description |
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was studied in a tumor xenograft model derived from the A431 (human cervical epidermoid,5T4+; 88, 000 binding sites per cell) tumor cell line. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of ASN004 was 1 mg/kg Q4D 4.
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| In Vivo Model | Cervical cancer CDX model | ||||
| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.07 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| 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) |
0.09 nM
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High 5T4 expression (5T4+++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder squamous cell carcinoma | SCaBER cells | CVCL_3599 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.09 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
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High 5T4 expression (5T4+++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Amelanotic melanoma | A-375 cells | CVCL_0132 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.12 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | 5637 cells | CVCL_0126 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.15 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.17 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Prostate carcinoma | DU145 cells | CVCL_0105 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.18 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cells | CVCL_0030 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.23 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.25 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.26 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.31 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | SW780 cells | CVCL_1728 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Glioblastoma | U-87MG cells | CVCL_0022 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.42 nM
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High 5T4 expression (5T4+++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells (5T4 overexpression) | CVCL_0062 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.42 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Prostate carcinoma | PC-3 cells | CVCL_0035 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.44 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Gestational choriocarcinoma | JEG-3 cells | CVCL_0363 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.56 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 18 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.57 nM
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Negative 5T4 expression (5T4-) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 19 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.62 nM
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Negative 5T4 expression (5T4-) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 20 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.66 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | TCCSUP cells | CVCL_1738 | ||
| Experiment 21 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.76 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Recurrent bladder carcinoma | HT-1197 cells | CVCL_1291 | ||
| Experiment 22 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.78 nM
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Negative 5T4 expression (5T4-) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | RT-4 cells | CVCL_0036 | ||
| Experiment 23 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.93 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | T24 cells | CVCL_0554 | ||
| Experiment 24 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.95 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Lung adenocarcinoma | NCI-H1975 cells | CVCL_1511 | ||
| Experiment 25 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.03 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Breast ductal carcinoma | HCC1937 cells | CVCL_0290 | ||
| Experiment 26 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.05 nM
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Low 5T4 expression (5T4+) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Lung large cell carcinoma | NCI-H1299 cells | CVCL_0060 | ||
| Experiment 27 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.06 nM
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High 5T4 expression (5T4+++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | HT-1376 cells | CVCL_1292 | ||
| Experiment 28 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.34 nM
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Negative 5T4 expression (5T4-) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Lung small cell carcinoma | DMS 114 cells | CVCL_1174 | ||
| Experiment 29 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.53 nM
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Negative 5T4 expression (5T4-) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | UM-UC-3 cells | CVCL_1783 | ||
| Experiment 30 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.28 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Bladder carcinoma | J82 cells | CVCL_0359 | ||
| Experiment 31 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.01 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Hepatoblastoma | Hep-G2 cells | CVCL_0027 | ||
| Experiment 32 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.03 nM
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Moderate 5T4 expression (5T4++) | ||
| Method Description |
The cytotoxic effect of ASN004 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing bladder,breast,cervical,colon,gastric,glioblastoma,liver,lung,melanoma,placenta,and prostate cancers.
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| In Vitro Model | Prostate carcinoma | LNCaP cells | CVCL_0395 | ||
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Patients Enrolled |
Eligible patients must have histologically confirmed advanced solid tumors (dose expansion limited to 5T4-expressing cancers like colorectal, breast, and ovarian) with progression after standard therapy or no standard options. Key exclusions include untreated brain metastases (>1 cm or symptomatic), LVEF <50%, and hematologic malignancies. All patients require measurable disease (exceptions per Medical Monitor), ECOG 0-1, adequate organ function, and compliance with contraception (3 months post-treatment). Archival/fresh tumor tissue (mandatory for 5T4 confirmation in some cohorts) must be provided.
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| Administration Dosage |
Patients will receive escalating doses of ASN004 to identify the best dose for further study.
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| Related Clinical Trial | |||||
| NCT Number | NCT04410224 | Clinical Status | PHASE1 | ||
| Clinical Description |
An Open Label, Multicenter, Dose-Finding Clinical Phase 1 Study of ASN004 to Evaluate Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Preliminary Efficacy in Patients With Advanced Malignant Solid Tumors
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| Primary Endpoint |
The study will determine the Maximum Tolerated Dose (MTD) of ASN004 by assessing treatment-related adverse events (AEs) and dose-limiting toxicities (DLTs) within the first 21 days (for Q3W dosing) or 28 days (for Q4W dosing) of treatment. The MTD will define the highest dose with acceptable safety for future studies.
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| Other Endpoint |
Pharmacokinetic (PK) parameters will be evaluated over the first 63 days, including plasma concentration (AUC), maximum steady-state concentration (Cmax), and terminal elimination rate. Tumor response will be tracked for one year using RECIST v1.1 criteria, measuring changes in lesion size, resolution of non-measurable lesions, and appearance of new lesions.
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XMT-1522 [Phase 1 (discontinued)]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
XMT-1522 (3 mg/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of JIMT-1 cells with HER2 expression with high expression.
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| In Vivo Model | JIMT-1 CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Disease control rate (DCR) |
83%
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| Patients Enrolled |
Eligible patients have HER2+ breast, gastric, or NSCLC (IHC 2+/3+), ECOG 0-1, adequate organ function, and progression after standard therapies. Exclusions include active infections, significant cardiac disease, recent anticancer therapy (<28 days), brain metastases, prior cardiotoxic anthracyclines, or additional malignancies within 5 years.
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| Administration Dosage |
XMT-1522 treatment will administered in groups of patients who will receive doses that increase over time. Once the maximum tolerated dose or recommended Phase 2 dose is achieved, new groups of patients will receive XMT-1522 at this fixed dose.
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| Related Clinical Trial | |||||
| NCT Number | NCT02952729 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1b, First-in-Human, Dose Escalation and Expansion Study of XMT-1522 in Patients With Advanced Breast Cancer and Other Advanced Tumors Expressing HER2
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| Primary Endpoint |
The study evaluates the maximum tolerated dose (MTD) or recommended Phase 2 dose (RP2D) of XMT-1522 over 14 weeks through monitoring adverse events, dose-limiting toxicities (DLTs), and concomitant medication use.
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| Other Endpoint |
Pharmacokinetic parameters (Tmax, Cmax, AUC) of XMT-1522 are measured frequently after dosing. Tumor response is assessed via RECIST every 6 weeks up to 12 months, while immunogenicity (anti-drug antibodies) is monitored periodically over ~100 days.
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References