General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0JYNCF
ADC Name
CX-2029
Synonyms
CX-2029; ABBV-2029; ABBV-CX-2029
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Organization
CytomX Therapeutics (Originator);AbbVie (Top20 MNC) (No Rights)
Drug Status
Phase 1/2 (discontinued)
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Anti-CD71 CX-151 probody
 Antibody Info 
Antigen Name
Transferrin receptor protein 1 (TFRC)
 Antigen Info 
Payload Name
MMAE
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random Cysteines
Combination Type
vedotin
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
Diffuse large b-cell lymphoma
1 Trials
Trial ID
NCT03543813; EudraCT2018-001456-34
Head and neck cancer
1 Trials
Trial ID
NCT03543813; EudraCT2018-001456-34
Lung cancer
1 Trials
Trial ID
NCT03543813; EudraCT2018-001456-34
Oesophageal cancer
1 Trials
Trial ID
NCT03543813; EudraCT2018-001456-34
ADC-specific functional property(2027 Update)
Binding Affinity
Click To Hide/Show 1 ADC-specific functional property Data
Dissocation Constant (Kd) Binding Target Description Reference
2.58 nM
CD-71
The binding activity of anti-CD71 PDC (CX-2029) was comparable with that of the unconjugated Probody therapeutic (CX-151).
[2]
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 6 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Maximum Observed Concentration (Cmax) 409 nM
Pk parameter following single intravenous bolus injection of 2 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Maximum Observed Concentration (Cmax) 1008 nM
Pk parameter following single intravenous bolus injection of 6 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Maximum Observed Concentration (Cmax) 2045 nM
Pk parameter following single intravenous bolus injection of 12 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 1670 day*nmol/L
Pk parameter following single intravenous bolus injection of 2 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 4355 day*nmol/L
Pk parameter following single intravenous bolus injection of 6 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 8580 day*nmol/L
Pk parameter following single intravenous bolus injection of 12 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Distribution
Click To Hide/Show 4 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Volume of Distribution (Vd) 3.2-10.6 L
Following 0.25-5.0 mg/kg, CX-2029 circulates predominantly as intact CX-2029 (>90%).
[1]
Area Under the Concentration-Time Curve (AUC) 1670 day*nmol/L
Pk parameter following single intravenous bolus injection of 2 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 4355 day*nmol/L
Pk parameter following single intravenous bolus injection of 6 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 8580 day*nmol/L
Pk parameter following single intravenous bolus injection of 12 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Metabolism
Click To Hide/Show 3 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 1670 day*nmol/L
Pk parameter following single intravenous bolus injection of 2 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 4355 day*nmol/L
Pk parameter following single intravenous bolus injection of 6 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 8580 day*nmol/L
Pk parameter following single intravenous bolus injection of 12 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Excretion
Click To Hide/Show 6 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Clearance (CL) 0.55-2.7 L/day
Following 0.25-5.0 mg/kg, CX-2029 circulates predominantly as intact CX-2029 (>90%).
[1]
Elimination Half-Life (t1/2) 2.3-9.8 day
Following 0.25-5.0 mg/kg, CX-2029 circulates predominantly as intact CX-2029 (>90%).
[1]
Area Under the Concentration-Time Curve (AUC) 1670 day*nmol/L
Pk parameter following single intravenous bolus injection of 2 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 4355 day*nmol/L
Pk parameter following single intravenous bolus injection of 6 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Area Under the Concentration-Time Curve (AUC) 8580 day*nmol/L
Pk parameter following single intravenous bolus injection of 12 mg/kg CX-2029 in cynomolgus monkeys.
[2]
Elimination Half-Life (t1/2) 2.3-5.8 day
Following 0.25 to 5.0 mg/kg, CX-2029 circulated predominantly as intact CX-2029 (>90%), whereas free MMAE circulated at no greater than 4.3% of total CX-2029. The median terminal half-life spanned 2.3 to 5.8 days.

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[3]
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Partial Response (PR)  NCT03543813
Phase 1
A phase 1-2, first-in-human study of CX-2029 in adults with metastatic or locally advanced unresectable solid tumors or diffuse large B-cell lymphomas (PROCLAIM-CX-2029).
Undisclosed  NCT03543813
PHASE1|||PHASE2
A Phase 1-2, First-in-Human Study of CX-2029 in Adults With Metastatic or Locally Advanced Unresectable Solid Tumors or Diffuse Large B-cell Lymphomas (PROCLAIM-CX-2029)
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 17 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 74.1
%
Pancreatic cancer PDX model (PDX: PA6237)
Tumor Growth Inhibition value (TGI) 
≈ 80.8
%
CTG-820 PDX model
Tumor Growth Inhibition value (TGI) 
≈ 97.6
%
Non-small cell lung cancer PDX model (PDX: CTG-0860)
Tumor Growth Inhibition value (TGI) 
≈ 98
%
CTG-820 PDX model
Tumor Growth Inhibition value (TGI) 
≈ 98
%
CTG-820 PDX model
Tumor Growth Inhibition value (TGI) 
≈ 99.4
%
Gastric cancer PDX models (PDX: GA6881)
Tumor Growth Inhibition value (TGI) 
≈ 99.8
%
Breast cancer PDX model (PDX: CTG-0708)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Esophageal caner PDX model (PDX: ES0136)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Gastric cancer PDX models (PDX: GA6881)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Breast cancer PDX model (PDX: CTG-0708)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Head and neck squamous cell carcinoma PDX model (PDX: CTG-820)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Pancreatic cancer PDX model (PDX: PA6237)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Esophageal cancer PDX model (PDX: ES0136)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Gastric cancer PDX model (PDX: GA6881)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Pancreatic cancer PDX model (PDX: PA6237)
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
1.2
nM
NCI-H520 cells
Lung squamous cell carcinoma
Half Maximal Effective Concentration (EC50) 
1.3
nM
HT29 cells
Colon cancer
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Partial Response (PR) 20.00, 50.00 % High CD71 expression (CD71+++)
Patients Enrolled
Metastatic or locally advanced unresectable solid tumors without approved life-prolonging treatment options.
Administration Dosage
CX-2029 (0.10, 0.25, 0.50, 1, 2, 3, 4, or 5 mg/kg) i.v. over 90 minutes [later increased to 180 minutes to mitigate infusion-related reactions (IRR)] every 3 weeks.
Related Clinical Trial
NCT Number NCT03543813  Clinical Status Phase 1
Clinical Description A phase 1-2, first-in-human study of CX-2029 in adults with metastatic or locally advanced unresectable solid tumors or diffuse large B-cell lymphomas (PROCLAIM-CX-2029).
Primary Endpoint
For the dose of 3 mg/kg, confirmed partial response rate=20.00% (n=2, 95% CI=2.50-55.60). For the dose of 5 mg/kg, confirmed partial response rate=50.00% (n=1, 95% CI=1.30-98.70).
Other Endpoint
For the dose of 0.5 mg/kg, Disease controla rate=50.00% (n=3, 95% CI=11.80-82.20). For the dose of 2 mg/kg, Disease controla rate=28.60% (n=2, 95% CI=3.7-71.0). For the dose of 3 mg/kg, Disease controla rate=50.00% (n=5, 95% CI 18.70-81.30). For the dose of 5 mg/kg, Disease controla rate=50.00% (n=1, 95% CI 1.30-98.70).
Experiment 2 Reporting the Activity Date of This ADC [6]
Patients Enrolled
Eligible patients include adults (≥18) with metastatic/locally advanced unresectable tumors (specific histologies required for Arms B/C) progressing after standard therapies, who can provide tumor samples. Key exclusions include Grade 1+ neuropathy, active infections, cardiac/metabolic disorders, CNS conditions, anticoagulation use, hepatic impairment (Child-Pugh B/C), or recent major surgery. Additional criteria may apply.

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Administration Dosage
.
Related Clinical Trial
NCT Number NCT03543813  Clinical Status PHASE1|||PHASE2
Clinical Description A Phase 1-2, First-in-Human Study of CX-2029 in Adults With Metastatic or Locally Advanced Unresectable Solid Tumors or Diffuse Large B-cell Lymphomas (PROCLAIM-CX-2029)
Primary Endpoint
The study evaluates dose-limiting toxicities (DLTs) of CX-2029 monotherapy across various dose levels during the initial 21-day observation period.
Other Endpoint
Anti-tumor activity is assessed by objective response rate (ORR) at different dose levels over a 2-year timeframe following CX-2029 monotherapy administration.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 17 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 74.10% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Pancreatic cancer PDX model (PDX: PA6237)
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.80% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 9. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model CTG-820 PDX model
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.60% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 13. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model CTG-820 PDX model
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 10. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model CTG-820 PDX model
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.40% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Gastric cancer PDX models (PDX: GA6881)
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.80% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Breast cancer PDX model (PDX: CTG-0708)
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Esophageal caner PDX model (PDX: ES0136)
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Gastric cancer PDX models (PDX: GA6881)
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Breast cancer PDX model (PDX: CTG-0708)
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Head and neck squamous cell carcinoma PDX model (PDX: CTG-820)
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model Pancreatic cancer PDX model (PDX: PA6237)
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 12. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model Esophageal cancer PDX model (PDX: ES0136)
Experiment 15 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 11. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model Gastric cancer PDX model (PDX: GA6881)
Experiment 16 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 8. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 17 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD71 expression (CD71+++)
Method Description
Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.

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In Vivo Model Pancreatic cancer PDX model (PDX: PA6237)
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.2 nM
Method Description
Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50) 1.3 nM High CD71 expression (CD71+++)
Method Description
Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
References
Ref 1 CX-2029, a PROBODY Drug Conjugate Targeting CD71 (Transferrin Receptor): Results From a First in-Human study (PROCLAIM-CX-2029) in Patients With Advanced Cance
Ref 2 Nonclinical Efficacy and Safety of CX-2029, an Anti-CD71 Probody-Drug Conjugate
Ref 3 Phase I, First-in-Human Study of the Probody Therapeutic CX-2029 in Adults with Advanced Solid Tumor Malignancies
Ref 4 Phase I, First-in-Human Study of the Probody Therapeutic CX-2029 in Adults with Advanced Solid Tumor Malignancies. Clin Cancer Res. 2021 Aug 15;27(16):4521-4530.
Ref 5 Nonclinical Efficacy and Safety of CX-2029, an Anti-CD71 Probody-Drug Conjugate. Mol Cancer Ther. 2022 Aug 2;21(8):1326-1336.
Ref 6 PROCLAIM-CX-2029: A Trial to Find Safe and Active Doses of an Investigational Drug CX-2029 for Patients With Solid Tumors or DLBCL