Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0JCWGF
ADC Name
TRPH-222
Synonyms
TRPH-222; CAT-02-106; CD22-4AP
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Organization
Catalent (Top20 MNC) (Originator);Triphase Accelerator
Drug Status
Phase 1 (discontinued)
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Anti-CD20 antibody
  Antibody Info 
Antigen Name
B-cell receptor CD22 (CD22)
  Antigen Info 
Payload Name
DM1
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
HIPS-4AP
  Linker Info 
Conjugate Type
Enzymatic Catalysis
Combination Type
RED-106
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
Follicular lymphoma
1 Trials
Trial ID
NCT03682796
Diffuse large b-cell lymphoma
1 Trials
Trial ID
NCT03682796
Mantle cell lymphoma
1 Trials
Trial ID
NCT03682796
Unspecific non-hodgkin lymphoma
1 Trials
Trial ID
NCT03682796
ADC-specific functional property(2027 Update)
Bystander Killing Effect
Click To Hide/Show 1 ADC-specific functional property Data
Bystander Killing Effect Description Reference
no
Furthermore, an anti-HER2-based ADC conjugated to RED-106 did not mediate bystander killing of antigen-negative cells in coculture with antigen-positive cells (Supplementary Fig. S6), implying that the active metabolite of CAT-02-106-which would be the same as that of the anti-HER2 RED-106 conjugate-would also not mediate bystander killing.

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[1]
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 21 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106, AUCinf.
 [1]
Maximum Observed Concentration (Cmax) 74.4 ug/mL
Summary of PK parameters of ADC in Mouse, 5 mg/kg.
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Maximum Observed Concentration (Cmax) 136 ug/mL
Summary of PK parameters of ADC in Mouse, 10 mg/kg.
 [1]
Area Under the Concentration-Time Curve (AUC) 1500 day*ug/mL
Summary of PK parameters of ADC in Mouse, 5 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2530 day*ug/mL
Summary of PK parameters of ADC in Mouse, 10 mg/kg, AUCinf.
 [1]
Maximum Observed Concentration (Cmax) 83.9 ug/mL
Summary of PK parameters of ADC in Rat (single dose), 3 mg/kg.
 [1]
Maximum Observed Concentration (Cmax) 110 ug/mL
Summary of PK parameters of ADC in Rat (single dose), 6 mg/kg.
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Maximum Observed Concentration (Cmax) 382 ug/mL
Summary of PK parameters of ADC in Rat (single dose), 20 mg/kg.
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Maximum Observed Concentration (Cmax) 687 ug/mL
Summary of PK parameters of ADC in Rat (single dose), 40 mg/kg.
 [1]
Maximum Observed Concentration (Cmax) 1020 ug/mL
Summary of PK parameters of ADC in Rat (single dose), 60 mg/kg.
 [1]
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 3 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 660 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 6 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2280 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 20 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 3740 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 40 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 5201 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 60 mg/kg, AUCinf.
 [1]
Maximum Observed Concentration (Cmax) 318 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 10 mg/kg.
 [1]
Maximum Observed Concentration (Cmax) 1030 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 30 mg/kg.
 [1]
Maximum Observed Concentration (Cmax) 1630 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 60 mg/kg.
 [1]
Area Under the Concentration-Time Curve (AUC) 1360 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 4200 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 30 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 6140 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 60 mg/kg, AUCinf.
 [1]
Distribution
Click To Hide/Show 12 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106, AUCinf.
 [1]
Volume of Distribution (Vd) 36.7 mL/kg
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106.
 [1]
Area Under the Concentration-Time Curve (AUC) 1500 day*ug/mL
Summary of PK parameters of ADC in Mouse, 5 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2530 day*ug/mL
Summary of PK parameters of ADC in Mouse, 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 3 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 660 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 6 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2280 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 20 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 3740 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 40 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 5201 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 60 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 1360 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 4200 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 30 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 6140 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 60 mg/kg, AUCinf.
 [1]
Metabolism
Click To Hide/Show 11 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 1500 day*ug/mL
Summary of PK parameters of ADC in Mouse, 5 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2530 day*ug/mL
Summary of PK parameters of ADC in Mouse, 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 3 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 660 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 6 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2280 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 20 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 3740 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 40 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 5201 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 60 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 1360 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 4200 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 30 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 6140 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 60 mg/kg, AUCinf.
 [1]
Excretion
Click To Hide/Show 13 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106, AUCinf.
 [1]
Clearance (CL) 13.8 mL/day/kg
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106.
 [1]
Elimination Half-Life (t1/2) 6.13 day
Summary of pharmacokinetic findings in rats dosed at 3 mg/kg with CAT-02-106.
 [1]
Area Under the Concentration-Time Curve (AUC) 1500 day*ug/mL
Summary of PK parameters of ADC in Mouse, 5 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2530 day*ug/mL
Summary of PK parameters of ADC in Mouse, 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 218 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 3 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 660 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 6 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 2280 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 20 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 3740 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 40 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 5201 day*ug/mL
Summary of PK parameters of ADC in Rat (single dose), 60 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 1360 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 10 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 4200 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 30 mg/kg, AUCinf.
 [1]
Area Under the Concentration-Time Curve (AUC) 6140 ug/mL
Summary of PK parameters of ADC in Cynomolgus monkey (q3w 2), 60 mg/kg, AUCinf.
 [1]
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Objective Response Rate (ORR)  NCT03682796
PHASE1
Phase 1, Multicenter, Open-Label Study of the Antibody-Drug Conjugate TRPH-222 in Subjects With Relapsed and/or Refractory B-Cell Lymphoma
Complete Response Rate (CRR)  NCT03682796
PHASE1
Phase 1, Multicenter, Open-Label Study of the Antibody-Drug Conjugate TRPH-222 in Subjects With Relapsed and/or Refractory B-Cell Lymphoma
Objective Response Rate (ORR)  NCT03682796
Phase 1
Phase 1, multicenter, open-label study of the antibody-drug conjugate TRPH-222 in subjects with relapsed and/or refractory B-cell lymphoma.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 51
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 87
%
Granta-519 cells
Mantle cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 91
%
SU-DHL-2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
SU-DHL-4 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
46%
Patients Enrolled
Eligible participants must be ≥18 with histologically confirmed relapsed/refractory B-cell NHL (DLBCL, FL, MZL, or MCL), ECOG 0-2. Key exclusions include leukemic lymphoma, double-/triple-hit DLBCL, prior organ transplants, significant neuropathy, cardiovascular disease, or other high-risk comorbidities per investigator assessment.
Administration Dosage
TRPH-222-100 is an open-label, multicenter study comprised of dose-escalation and dose-expansion stages. TRPH-222 was administered IV once every 3 weeks. 22 patients were enrolled in dose-escalating cohorts of TRPH-222 (0.6 mg/kg to 10 mg/kg) from DLBCL, FL, TFL, MCL and MZL histologies, and 10 patients in a dose-expansion cohort (7.5 mg/kg) focusing on DLBCL and FL histologies.

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Related Clinical Trial
NCT Number NCT03682796  Clinical Status PHASE1
Clinical Description Phase 1, Multicenter, Open-Label Study of the Antibody-Drug Conjugate TRPH-222 in Subjects With Relapsed and/or Refractory B-Cell Lymphoma
Primary Endpoint
The study aims to determine the maximum tolerated dose (MTD) of TRPH-222 over a 21-day timeframe while evaluating safety through adverse events (AEs), serious AEs (SAEs), and treatment-related AEs leading to discontinuation or death.
Other Endpoint
Tumor activity will be assessed via objective response rate (ORR), progression-free survival (PFS), overall survival (OS), and duration of response (DOR) using Lugano criteria in NHL subtypes. Pharmacokinetic analysis (Cmax, AUC, CL, Vd, t½) will be conducted over multiple cycles, alongside anti-drug antibody (ADA) incidence monitoring.
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Complete Response Rate (CRR)
31%
Patients Enrolled
Eligible participants must be ≥18 with histologically confirmed relapsed/refractory B-cell NHL (DLBCL, FL, MZL, or MCL), ECOG 0-2. Key exclusions include leukemic lymphoma, double-/triple-hit DLBCL, prior organ transplants, significant neuropathy, cardiovascular disease, or other high-risk comorbidities per investigator assessment.
Administration Dosage
TRPH-222-100 is an open-label, multicenter study comprised of dose-escalation and dose-expansion stages. TRPH-222 was administered IV once every 3 weeks. 22 patients were enrolled in dose-escalating cohorts of TRPH-222 (0.6 mg/kg to 10 mg/kg) from DLBCL, FL, TFL, MCL and MZL histologies, and 10 patients in a dose-expansion cohort (7.5 mg/kg) focusing on DLBCL and FL histologies.

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Related Clinical Trial
NCT Number NCT03682796  Clinical Status PHASE1
Clinical Description Phase 1, Multicenter, Open-Label Study of the Antibody-Drug Conjugate TRPH-222 in Subjects With Relapsed and/or Refractory B-Cell Lymphoma
Primary Endpoint
The study aims to determine the maximum tolerated dose (MTD) of TRPH-222 over a 21-day timeframe while evaluating safety through adverse events (AEs), serious AEs (SAEs), and treatment-related AEs leading to discontinuation or death.
Other Endpoint
Tumor activity will be assessed via objective response rate (ORR), progression-free survival (PFS), overall survival (OS), and duration of response (DOR) using Lugano criteria in NHL subtypes. Pharmacokinetic analysis (Cmax, AUC, CL, Vd, t½) will be conducted over multiple cycles, alongside anti-drug antibody (ADA) incidence monitoring.
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Objective Response Rate (ORR)
22.70%
Patients Enrolled
Patients with diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), and marginal zone lymphoma (MZL) were enrolled. Patients had received a median of 4 prior systemic therapy.
Administration Dosage
TRPH-222 was administered IV 0.60 to 5.60 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number NCT03682796  Clinical Status Phase 1
Clinical Description Phase 1, multicenter, open-label study of the antibody-drug conjugate TRPH-222 in subjects with relapsed and/or refractory B-cell lymphoma.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 51% Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 1 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87% Positive CD22 expression (CD22+++/++)
Method Description
In Granta-519 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Mantle cell lymphoma CDX model
In Vitro Model Mantle cell lymphoma Granta-519 cells CVCL_1818
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91% Positive CD22 expression (CD22+++/++)
Method Description
In SU-DHL-2 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Diffuse large B cell lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-2 cells CVCL_9550
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive CD22 expression (CD22+++/++)
Method Description
In SU-DHL-4 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Diffuse large B cell lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-4 cells CVCL_0539
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once every three-week intravenous (IV) dosing with 10 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 10 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 3 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
References
Ref 1 CAT-02-106, a Site-Specifically Conjugated Anti-CD22 Antibody Bearing an MDR1-Resistant Maytansine Payload Yields Excellent Efficacy and Safety in Preclinical Models
Ref 2 Study of TRPH-222 in Patients With Relapsed and/or Refractory B-Cell Lymphoma
Ref 3 First-in-Human Phase I Study of ABBV-085, an Antibody-Drug Conjugate Targeting LRRC15, in Sarcomas and Other Advanced Solid Tumors. Clin Cancer Res. 2021 Jul 1;27(13):3556-3566. doi: 10.1158/1078-0432.CCR-20-4513.
Ref 4 Trph-222, a Novel Anti-CD22 Antibody Drug Conjugate (ADC), Has Signficant Anti-Tumor Activity in NHL Xenografts and Is Well Tolerated in Non-Human Primates. Blood. 2017 Dec 8;130 (Suppl_1) : 4105.
Ref 5 TRPH-222, a novel anti-CD22 antibody drug conjugate (ADC), has significant anti-tumor activity in NHL xenografts and reduces B cells in monkeys.