Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0AQHSO
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| ADC Name |
EGFR-ADC 13a
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| Synonyms |
EGFR ADC 13a
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Squamous cell cancer [ICD11:2D60-2D61]
Investigative
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| Drug-to-Antibody Ratio |
3.4
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| Antibody Name |
Anti-EGFR mAb
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Antibody Info | ||||
| Antigen Name |
Epidermal growth factor receptor (EGFR)
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Antigen Info | ||||
| Payload Name |
PBD dimer 14a
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Payload Info | ||||
| Therapeutic Target |
Human Deoxyribonucleic acid (hDNA)
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Target Info | ||||
| Linker Name |
Adipic acid-Val-Ala-PABC
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Linker Info | ||||
| Conjugate Type |
Random conjugation through nucleophilic lysines.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | High EGFR expression (EGFR+++) | ||
| Method Description |
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC 14a at a single i.v. dose of 3.7 mg/kg.
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | High EGFR expression (EGFR+++) | ||
| Method Description |
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 14.9 mg/kg.
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | High EGFR expression (EGFR+++) | ||
| Method Description |
Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 7.4 mg/kg.
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| In Vitro Model | Hypopharyngeal squamous cell carcinoma | FaDu cells | CVCL_1218 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.30 nM | Positive EGFR expression (EGFR+++/++) | ||
| Method Description |
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
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| In Vitro Model | Oral cavity squamous cell carcinoma | HSC-2 cells | CVCL_1287 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.00 nM | Positive EGFR expression (EGFR+++/++) | ||
| Method Description |
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
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| In Vitro Model | Human papillomavirus-related endocervical adenocarcinoma | KB cells | CVCL_0372 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 3.00 nM | Negative EGFR expression (EGFR-) | ||
| Method Description |
Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
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| In Vitro Model | Lung non-small cell carcinoma | NCI-H2110 cells | CVCL_1530 | ||
References
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