Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0WPYAS
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| ADC Name |
OBI-992
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| Synonyms |
OBI-992; BSI-992
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| Organization |
Biosion (Originator);OBI Pharma
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| Drug Status |
Phase 1/2
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
R4702
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Antibody Info | ||||
| Antigen Name |
Tumor-associated calcium signal transducer 2 (TACSTD2); Programmed cell death 1 ligand 1 (PD-L1)
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Antigen Info | ||||
| Payload Name |
Exatecan
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Mal-PEG24-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 | ||
|---|---|---|---|---|---|---|---|---|---|
| Gastric cancer |
1 Trials
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| Lung cancer |
1 Trials
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| Unspecific solid tumor |
1 Trials
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ADC-specific functional property(2027 Update)
Bystander Killing Effect
| Bystander Killing Effect | Description | Reference |
|---|---|---|
| yes |
OBI-992 demonstrated a killing effect as OBI-992 was able to kill TROP2-negative xenografts in the presence of nearby TROP2-positive cells.
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[2]
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General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 3.5 | ug/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 184 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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| Maximum Observed Concentration (Cmax) | 13.4 | ug/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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| Area Under the Concentration-Time Curve (AUC) | 1064 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Maximum Observed Concentration (Cmax) | 42 | ug/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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| Area Under the Concentration-Time Curve (AUC) | 3858 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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| Maximum Observed Concentration (Cmax) | 154.4 | ug/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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| Area Under the Concentration-Time Curve (AUC) | 16978 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 184 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1064 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 3858 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 16978 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 184 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1064 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 3858 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 16978 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 184 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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| Clearance (CL) | 1.61 | mL/h/kg |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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| Elimination Half-Life (t1/2) | 54 | h |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 0.3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 1064 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Clearance (CL) | 0.93 | mL/h/kg |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 81 | h |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 1 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 3858 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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| Clearance (CL) | 0.76 | mL/h/kg |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 93 | h |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 3 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 16978 | ug*h/mL |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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[1] |
| Clearance (CL) | 0.54 | mL/h/kg |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/kg.
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[1] |
| Elimination Half-Life (t1/2) | 145 | h |
Mean Pharmacokinetic Parameters of Serum ADC in NCI-H1975 Tumor-Bearing Mice, 10 mg/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 | [3] | ||||
| Patients Enrolled |
Eligible subjects must be ≥18yo with metastatic/advanced solid tumors (measurable per RECIST v1.1, ECOG 0-1) refractory to standard therapy, with adequate organ function (ALT/AST ≤3×ULN [≤5×ULN with liver mets], bilirubin ≤1.5×ULN, CrCl >50mL/min, ANC ≥1500/uL). Special populations: HIV+ (CD4≥350 cells/uL, VL<200 copies/mL), HBV (suppressed VL), HCV (curative treatment with undetectable VL). Part B requires NSCLC/SCLC histology. All subjects must provide pretreatment tumor biopsy (archival acceptable) and comply with contraception requirements (120 days post-treatment).
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| Administration Dosage |
OBI-992 at dose level 1, 2, 3, 4, 6, 8, 10 mg/kg, Q3W
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| Related Clinical Trial | |||||
| NCT Number | NCT06480240 | Clinical Status | PHASE1|||PHASE2 | ||
| Clinical Description | A Phase 1/2, Open-Label, Dose-Escalation and Cohort-Expansion Study Evaluating the Safety, Pharmacokinetics, and Therapeutic Activity of OBI-992 in Subjects With Advanced Solid Tumors | ||||
| Primary Endpoint |
Primary objectives include assessing OBI-992 safety/tolerability (AEs/SAEs/lab abnormalities per NCI CTCAE v5.0), determining MTD/RP2D, and evaluating preliminary efficacy (ORR, CBR, DOR, DCR, PFS per RECIST v1.1) over a study duration of up to 2 years and 2 months.
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| Other Endpoint |
Secondary objectives involve characterizing OBI-992 immunogenicity (ADA incidence) and serum PK parameters (Cmax, AUC, T1/2, CL, Vdss) for both OBI-992 and active metabolite exatecan throughout the study period.
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References