Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0BSQPI
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| ADC Name |
Sacituzumab tirumotecan
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| Brand Name |
Jiatailai
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| Synonyms |
A-264; KL-A264; MK-2870; MK2870; SKB 264; SKB-264; SKB264; TROP-2-targeted antibody-drug conjugate; sacituzumab tirumotecan(MK-2870)
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| Organization |
Sichuan Kelun Pharmaceutical Co., Ltd.; KLUS Pharma, Inc.; Merck & Co., Inc.
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| Drug Status |
Approved (FDA): Apr 22, 2020
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| Indication |
In total 13 Indication(s)
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| Drug-to-Antibody Ratio |
7 to 8
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| Structure |
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| Antibody Name |
Sacituzumab
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TROP2)
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Antigen Info | ||||
| Payload Name |
KL610023
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Pyrimidine-CL2A-carbonate
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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| Combination Type |
tirumotecan
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| Special Approval(s) |
Breakthrough therapy(NMPA)
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General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Discovered Using Patient-derived Xenograft Model
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line 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 | [1] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05347134 | Clinical Status | Phase 3 | ||
| Clinical Description | A randomized, controlled, open-label, multi-center phase 3 clinical trial of SKB264 for injection versus investigator selected regimens in patients with unresectable locally advanced, recurrent or metastatic triple-negative breast cancer who have failed second-line or above prior standard of care. | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05642780 | Clinical Status | Phase 2 | ||
| Clinical Description | Amulticenter, open-label, phase 2, basket study to evaluate the efficacy and safety of SKB264 in combination with pembrolizumab in subjects with selected solid tumors. | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05631262 | Clinical Status | Phase 2 | ||
| Clinical Description | A multicenter, open-label, phase 2 study to evaluate the efficacy and safety of SKB264 monotherapy in selected subjects with advanced solid tumors. | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [4] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05445908 | Clinical Status | Phase 2 | ||
| Clinical Description | A phase 2 clinical study of SKB264 with/without KL-A167 in patients with unresectable locally advanced, recurrent or metastatic triple-negative breast cancer (TNBC) who have not received prior systemic therapy. | ||||
| Experiment 5 Reporting the Activity Date of This ADC | [5] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05351788 | Clinical Status | Phase 2 | ||
| Clinical Description | A phase 2 clinical study of combination therapy of SKB264 in patients with advanced or metastatic non-small cell lung cancer. | ||||
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | < 30.00% (Day 21) | Negative TROP2 expression (TROP2-) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | < 30.00% (Day 21) | Negative TROP2 expression (TROP2-) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 38.40% (Day 21) | Moderate TROP2 expression (TROP2++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 42.90% (Day 21) | Low TROP2 expression (TROP2+) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 0501116) | ||||
| Experiment 5 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 44.00% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 0.5 mg/kg for BR1282 PDX models twice a week for six times.
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| In Vivo Model | Breast cancer PDX model (PDX: BR1282) | ||||
| Experiment 6 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | < 50.00% (Day 21) | Negative TROP2 expression (TROP2-) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 7 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.70% (Day 21) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 406022) | ||||
| Experiment 8 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 92.60% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 1.5 mg/kg for BR1282 PDX models twice a week for six times.
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| In Vivo Model | Breast cancer PDX model (PDX: BR1282) | ||||
| Experiment 9 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 406022) | ||||
| Experiment 10 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | Moderate TROP2 expression (TROP2++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 11 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | Low TROP2 expression (TROP2+) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 10 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 0501116) | ||||
| Experiment 12 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 406022) | ||||
| Experiment 13 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | Moderate TROP2 expression (TROP2++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX model (PDX: A11068) | ||||
| Experiment 14 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 21) | Low TROP2 expression (TROP2+) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 3 mg/kg for gastric cancer PDX models twice a week for six times.
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| In Vivo Model | Gastric cancer PDX models (PDX: 0501116) | ||||
| Experiment 15 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
The tumor-bearing mice were treated with SKB264 via i.v. injection at doses of 5 mg/kg for BR1282 PDX models twice a week for six times.
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| In Vivo Model | Breast cancer PDX model (PDX: BR1282) | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 51.20% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 3 mg/kg in the NCI-N87.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 75.60% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 1 mg/kg in the HCC1806.
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| In Vitro Model | Breast squamous cell carcinoma | HCC1806 cells | CVCL_1258 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 78.40% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 0.3 mg/kg in the NCI-N87.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 98.50% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 3 mg/kg in the HCC1806.
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| In Vitro Model | Breast squamous cell carcinoma | HCC1806 cells | CVCL_1258 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 10 mg/kg in the HCC1806.
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| In Vitro Model | Breast squamous cell carcinoma | HCC1806 cells | CVCL_1258 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 100.00% (Day 24) | High TROP2 expression (TROP2+++) | ||
| Method Description |
When the average tumor volume reached about 120 mm3, mice were randomized into five groups (n = 8) and subsequently administered by intravenous (i.v.) injection with the testing item twice a week for six times. SKB264 treatments were performed at doses of 1 mg/kg in the NCI-N87.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1.28 nM | High TROP2 expression (TROP2+++) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations:Calu-3 (8,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2.24 nM | High TROP2 expression (TROP2+++) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations: NCI-N87 (5,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 3.41 nM | High TROP2 expression (TROP2+++) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations: NCI-H23 (TROP2+, 3,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Lung adenocarcinoma | NCI-H23 cells | CVCL_1547 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 5.70 nM | High TROP2 expression (TROP2+++) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations: HCC1806 (3,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Breast squamous cell carcinoma | HCC1806 cells | CVCL_1258 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 11.03 nM | High TROP2 expression (TROP2+++) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations: BxPC-3 (2,000 cells per well),After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [6] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 18.83 nM | Negative TROP2 expression (TROP2-) | ||
| Method Description |
Tumor cells were seeded on 96-well plates at the following concentrations: NCIH23 (parental, 3,000 cells per well).After overnight incubation,the diluted testing items were added respectively. After 72 h, cell viability was evaluated using a CellTiter-Glo Luminescent Cell Viability Assay.
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| In Vitro Model | Lung adenocarcinoma | NCI-H23 cells | CVCL_1547 | ||
References