Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GYCJG
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| ADC Name |
Samatatug zovodotin
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| Synonyms |
ICON-2; XB002
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| Organization |
Zymeworks (Originator) (No Rights);Exelixis;Iconic Therapeutics (No Rights)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
3.3
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| Structure |
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| Antibody Name |
Samatatug
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Antibody Info | ||||
| Antigen Name |
Tissue factor (F3)
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Antigen Info | ||||
| Payload Name |
ZD02044
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-PEG3-Val-Cit
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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| Combination Type |
zovodotin
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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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| Cervical cancer |
1 Trials
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| Endometrial cancer |
1 Trials
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| Head and neck cancer |
1 Trials
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| Lung cancer |
1 Trials
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| Oesophageal cancer |
1 Trials
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| Ovarian cancer |
1 Trials
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| Pancreatic cancer |
1 Trials
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| Prostate cancer |
1 Trials
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| Unspecific solid tumor |
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 |
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| Maximum Observed Concentration (Cmax) | 68.1 | ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 214 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Maximum Observed Concentration (Cmax) | 165 | ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 511 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 214 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 511 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 214 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 511 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 214 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 1.9 | day |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 511 | day*ug/mL |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 2.2 | day |
Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.
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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 |
Inclusion Criteria: Adults with inoperable/metastatic solid tumors (specific histologies for each cohort) who exhausted standard therapies. Required: measurable disease (RECIST 1.1), ECOG 0-1, adequate organ function, archived/fresh tumor tissue (≤3 years old), and controlled AEs (CTCAE v5 ≤G1). Exclusion Criteria: Prior disqualifying therapies, untreated brain metastases (unless stable ≥4 weeks post-treatment), major surgery (within 4 weeks), QTcF >480 ms, pregnancy/lactation, hypersensitivity to study drugs, or active malignancies (except cured non-melanoma skin cancers/localized tumors).
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| Administration Dosage |
Dose-escalation followed by cohort-expansion in tumor-specific expansion cohorts
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| Related Clinical Trial | |||||
| NCT Number | NCT04925284 | Clinical Status | PHASE1 | ||
| Clinical Description | A Dose-Escalation and Expansion Study of the Safety and Pharmacokinetics of XB002 as Single-Agent and Combination Therapy in Subjects With Inoperable Locally Advanced or Metastatic Solid Tumors | ||||
| Primary Endpoint |
The study's Dose-Escalation Stage aimed to determine the MTD/recommended dose (RD) of IV XB002 alone or in combination over 18 months. The Cohort-Expansion Stage assessed preliminary efficacy through ORR using RECIST 1.1 (or RANO/PCWG3 criteria) over 12 months.
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| Other Endpoint |
Safety and tolerability were evaluated via AEs/SAEs, treatment duration, and dose intensity over 30 months. Pharmacokinetics (Cmax, Ctrough) and immunogenicity (ADA) of XB002, total antibody, and free payload were analyzed. Anti-tumor activity was measured by ORR, DOR, and PFS (RECIST 1.1/RANO/PCWG3) through investigator/BIRC assessments. Overall survival was tracked in expansion cohorts for 12 months.
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References