Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0RIGUP
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| ADC Name |
RG7598
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| Synonyms |
RG7598; DFRF4539A; DFRF-4539A
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| Organization |
Genentech (Top20 MNC) (Originator)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
MFRF3266A
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Antibody Info | ||||
| Antigen Name |
Fc receptor-like protein 5 (FCRL5)
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Antigen Info | ||||
| Payload Name |
MMAE
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Random Cysteines
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| Combination Type |
vedotin
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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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| Multiple myeloma |
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 |
|---|---|---|---|---|
| Maximum Observed Concentration (Cmax) | 55.1 | ug/mL |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg.
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| Area Under the Concentration-Time Curve (AUC) | 291 | day*ug/mL |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg, AUCinf.
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Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 291 | day*ug/mL |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg, AUCinf.
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Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 291 | day*ug/mL |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg, AUCinf.
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Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 291 | day*ug/mL |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg, AUCinf.
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| Clearance (CL) | 9.6 | mL/day/kg |
Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg.
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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 | [1] | ||||
| Patients Enrolled |
Eligibility requires adults (≥18) with ECOG 0-2, relapsed/refractory myeloma (prior proteasome inhibitor/immunomodulatory therapy), and measurable disease. Exclusions: recent mAb/chemotherapy (≤4/2 weeks), unresolved toxicities (except neuropathy), recent transplants, antibody allergies, active infections, or hepatitis/HIV. Pregnancy is prohibited.
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| Administration Dosage |
multiple ascending doses
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| Related Clinical Trial | |||||
| NCT Number | NCT01432353 | Clinical Status | PHASE1 | ||
| Clinical Description | An Open-label, Multicenter, Phase I Trial of the Safety and Pharmacokinetics of Escalating Doses of DFRF4539A in Patients With Relapsed or Refractory Multiple Myeloma | ||||
| Primary Endpoint |
The study evaluates safety outcomes including AE incidence over 3.5 years, MTD/DLT determination within 1.5 years, and establishes the RP2D for DFRF4539A administered every 3 weeks or weekly.
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| Other Endpoint |
Immunogenicity (serum ATA levels) and PK (AUC) are monitored over 3.5 years. Efficacy is assessed via IMWG/EBMT criteria for objective response, DoR (time to progression/death), and PFS (from treatment initiation to progression/death within 30 days post-treatment).
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References