Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0BGJNX
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| ADC Name |
Plozalizumab plevistinag
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| Synonyms |
TAK-500; plozalizumab plevistinag
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| Organization |
Takeda Pharmaceuticals (Top20 MNC) (Originator)
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| Drug Status |
Phase 1/2 (discontinued)
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
Plozalizumab
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Antibody Info | ||||
| Antigen Name |
C-C chemokine receptor type 2 (CCR2)
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Antigen Info | ||||
| Payload Name |
dazostinag (TAK-676)
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Payload Info | ||||
| Therapeutic Target |
Stimulator of interferon genes protein (STING1)
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Target Info | ||||
| Linker Name |
Maleimido-caproyl-PEG8-Val-Ala-PABC
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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The indication landscape of This ADC(2027 Update)
The clinical trial pipeline of This ADC(2027 Update)
| Indication | Phase 1 | Phase 1/2 | Phase 2 | Phase 2/3 | Phase 3 | New Drug Application | Approved | ||
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| Breast cancer |
1 Trials
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| Gastric cancer |
1 Trials
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| Head and neck cancer |
1 Trials
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| Kidney cancer |
1 Trials
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| Liver cancer |
1 Trials
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| Lung cancer |
1 Trials
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| Nasopharyngeal cancer |
1 Trials
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| Oesophageal cancer |
1 Trials
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| Pancreatic cancer |
1 Trials
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| Pleura mesothelioma |
1 Trials
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
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|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4770 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 35800 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 644 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 12700 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 2310 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13500 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 175 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1760 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 39300 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, AUC from time 0 to infinity, calculated using the observed value of the last quantifiable concentration.
Click to Show/Hide
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4770 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 35800 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 644 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 12700 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 2310 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13500 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 175 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1760 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 39300 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, AUC from time 0 to infinity, calculated using the observed value of the last quantifiable concentration.
Click to Show/Hide
|
[1] |
| Volume of Distribution (Vd) | 82.4 | mL/kg |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4770 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 35800 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 644 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 12700 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 2310 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13500 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 175 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1760 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 39300 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, AUC from time 0 to infinity, calculated using the observed value of the last quantifiable concentration.
Click to Show/Hide
|
[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 4770 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 35800 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 644 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 12700 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from the start of dose administration to the time of the last observation.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 272 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 2 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 2310 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 13500 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 175 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 10 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 1760 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Tumor, area under the concentration-time curve from time 0 to 24 hours.
Click to Show/Hide
|
[1] |
| Area Under the Concentration-Time Curve (AUC) | 39300 | ng*h/mL |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma, AUC from time 0 to infinity, calculated using the observed value of the last quantifiable concentration.
Click to Show/Hide
|
[1] |
| Clearance (CL) | 1.27 | mL/h/kg |
Pharmacokinetic Parameters of ADC in Female C57BL/6 Mice Bearing MC38 Tumors After Intravenous Administration of mTAK-500, 50 ug/kg, Matrix Plasma.
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[1] |
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical 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 | [2] | ||||
| Patients Enrolled |
Eligible participants (ECOG 0-1) have advanced solid tumors (e.g., NSCLC, pancreatic adenocarcinoma, RCC) refractory to prior therapies, with specific requirements per cohort (e.g., 2L NSCLC: anti-PD- (L)1 progression; 3L RCC: prior VEGFR TKI + immunotherapy). Key exclusions: cardiac/pulmonary dysfunction (NYHA III-IV, pneumonitis), uncontrolled hepatitis, recent immunosuppressants/radiotherapy, or hypersensitivity to study drugs. Lab thresholds include ANC ≥1000/uL, creatinine clearance ≥30 mL/min, and LVEF >50%. HCC requires Child-Pugh ≤7.
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| Administration Dosage |
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| Related Clinical Trial | |||||
| NCT Number | NCT05070247 | Clinical Status | PHASE1|||PHASE2 | ||
| Clinical Description | An Open-label, Dose Escalation and Expansion, Phase 1/2 Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Antitumor Activity of TAK-500, a Novel Stimulator of Interferon Genes Agonist, as a Single Agent and in Combination With Pembrolizumab in Adult Patients With Select Locally Advanced or Metastatic Solid Tumors | ||||
| Primary Endpoint |
The study evaluates safety endpoints including Grade ≥3 TEAEs, SAEs, DLTs (Cycle 1, per NCI CTCAE v5.0), and treatment modifications/discontinuations over ~50 months. Efficacy in dose expansion focuses on ORR (confirmed PR/CR per RECIST 1.1), DCR (CR+PR+SD >6 weeks), DOR, TTR, PFS, and OS, with RECIST-defined tumor assessments.
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| Other Endpoint |
Pharmacokinetics of TAK-500 (single/multi-dose) include Cmax, Tmax, AUCt, AUCinf, t1/2, CL, and Vss, measured during Cycles 1-4. Biomarkers assess intratumoral immune cell changes (IHC/ISH) and ADA immunogenicity. Tumor response metrics (ORR/DCR/DOR/TTR in escalation/expansion) follow RECIST 1.1, while survival endpoints (PFS/OS) track progression/death over ~50 months.
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| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04879849 | Clinical Status | Phase 1 | ||
| Clinical Description | An open-label, phase 1, dose-escalation study to evaluate the safety and preliminary antitumor activity of TAK-676 with pembrolizumab following radiation therapy in the treatment of non-small-cell lung cancer, triple-negative breast cancer, or squamous-cell carcinoma of the head and neck that has progressed on checkpoint inhibitors. | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [4] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04420884 | Clinical Status | Phase 1 | ||
| Clinical Description | An open-label, dose escalation, phase 1 study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-676 as a single agent and in combination with pembrolizumab in adult patients with advanced or metastatic solid tumors. | ||||
References