Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0JQHJW
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| ADC Name |
AGX101
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| Synonyms |
susitabart ponetansine; AGX101
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| Organization |
Angiex (Originator)
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| Drug Status |
Phase 1
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| Drug-to-Antibody Ratio |
2
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| Structure |
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| Antibody Name |
Anti-TM4SF1 antibody
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Antibody Info | ||||
| Antigen Name |
Transmembrane 4 L6 family member 1 (TM4SF1)
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Antigen Info | ||||
| Payload Name |
Maytansine derivative
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
A non-cleavable linker
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Linker Info | ||||
| Conjugate Type |
Reactive 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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| Unspecific solid tumor |
1 Trials
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| Sarcoma |
1 Trials
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| Colorectal cancer |
1 Trials
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| Pancreatic cancer |
1 Trials
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| Liver cancer |
1 Trials
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| Breast cancer |
1 Trials
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| Prostate cancer |
1 Trials
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General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
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] | ||||
| Patients Enrolled |
Eligible patients have histologically confirmed advanced/metastatic solid tumors refractory to standard therapy, ECOG 0-1, adequate organ function, and effective contraception. Exclusions include untreated CNS metastases, uncontrolled infections, unresolved Grade ≥2 AEs (except neuropathy/endocrine irAEs), major recent surgery/radiotherapy, life-threatening comorbidities, active infections, pregnancy, or recent use of CYP3A modulators. Colorectal cancer/NSCLC with squamous histology requires sponsor approval.
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| Administration Dosage |
Experimental: Dose Escalation Phase AGX-101, initial 90-minute IV infusion, second 60-minute IV infusion and 30 minute subsequent IV infusions on Day 1 of every 3, 6 or 9-week cycle in Dose Escalation Phase. Dose escalation will be carried out in sequential cohorts of escalating doses, with an expansion cohort in advanced angiosarcoma.
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| Related Clinical Trial | |||||
| NCT Number | NCT06440005 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase 1, Open-Label, Dose-Escalation and Expansion Study of AGX101, a TM4SF1 Directed Antibody Drug Conjugate in Patients with Unresectable, Locally Advanced, or Metastatic Solid Tumors | ||||
| Primary Endpoint |
The study evaluates the maximum tolerated dose (MTD) of AGX101 and dose-limiting toxicities (DLTs) over 21 days post-dose (Day 1-Day 21). Adverse events will be assessed for incidence, severity, and duration from screening through treatment end (approx. 6 months up to 3 years).
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| Other Endpoint |
Pharmacokinetic parameters include terminal elimination half-life, AUC, and Cmax over 22 days (Day 1-Day 22). ADA levels will be measured for approx. 6 months up to 3 years. Efficacy assessments involve ORR, DoR, DCR, PFS, treatment duration, and overall survival per RECIST v1.1.
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Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.60% | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
Mice bearingeither MIA PaCa-2 tumors were treated with either vehiclecontrol or AGX101 at 12 mg/kg g7dx2.
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| In Vivo Model | Pancreatic cancer CDX model | ||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | MIA PaCa-2 cells | CVCL_0428 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.40% | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
Mice bearingeither MIA PaCa-2 tumors were treated with either vehiclecontrol or AGX101 at 12 mg/kg g7dx2.
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| In Vivo Model | Pancreatic cancer CDX model | ||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | MIA PaCa-2 cells | CVCL_0428 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.50% | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
Mice bearingeither HCC1954 tumors were treated with either vehiclecontrol or AGX101 at 12 mg/kg g7dx2.
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| In Vivo Model | Breast ductal cancer CDX model | ||||
| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.60% | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
Mice bearingeither HCC1954 tumors were treated with either vehiclecontrol or AGX101 at 12 mg/kg g7dx2.
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| In Vivo Model | Breast ductal cancer CDX model | ||||
| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.10% | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
Mice bearingeither CALU-3 tumors were treated with either vehiclecontrol or AGX101 at 12 mg/kg g7dx2.
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| In Vivo Model | Lung adenocarcinoma CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | Calu-3 cells | CVCL_0609 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.02 nM | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
The inhibitory activity of AGX101 exerted a potent cytotoxic effect against TM4SF1+ solid tumor cell lines.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | MIA PaCa-2 cells | CVCL_0428 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.02 nM | High TM4SF1 expression (TM4SF1+++) | ||
| Method Description |
The inhibitory activity of AGX101 exerted a potent cytotoxic effect against TM4SF1+ cell lines.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
References