Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0AQITP
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| ADC Name |
RG7636
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| Synonyms |
RG7636; DEDN6526A
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| Organization |
Roche (Top20 MNC) (Originator)
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| Drug Status |
Phase 1 (discontinued)
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| Drug-to-Antibody Ratio |
3 to 4
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| Structure |
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| Antibody Name |
MEDN6000A
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Antibody Info | Antigen Name | |||
| 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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| Melanoma |
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) | 45000 | ng/mL |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg, AUCinf
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[1] |
| Maximum Observed Concentration (Cmax) | 45000 | ng/mL |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg, AUCinf.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg, AUCinf
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[1] |
| Volume of Distribution (Vd) | 70.6 | mL/kg |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg, AUCinf.
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[1] |
| Volume of Distribution (Vd) | 70.6 | mL/kg |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg, AUCinf
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg, AUCinf.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg, AUCinf
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[1] |
| Elimination Half-Life (t1/2) | 3.92 | day |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Clearance (CL) | 20.9 | mL/kg/day |
Mean (%CV) of the key pharmacokinetic parameters for ADC analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 128000 | ng*day/mL |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg, AUCinf.
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[1] |
| Elimination Half-Life (t1/2) | 3.92 | day |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 mg/kg
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[1] |
| Clearance (CL) | 20.9 | mL/kg/day |
Mean (%CV) of the key pharmacokinetic parameters for total antibody analytes in Cycle 1 at 2.4 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 | [2] | ||||
| Patients Enrolled |
Eligible patients were adults with advanced melanoma (Stage III/IV) resistant to prior therapies, adequate organ function, and measurable disease. Exclusions included recent anticancer treatments (21 days for cytotoxic/antibody therapies), active infections, CNS metastases, prior MMAE-ADC treatment, or significant comorbidities.
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| Administration Dosage |
DEDN6526A (0.3-2.8 mg/kg) was given intravenously every 3 weeks (q3w) to pts with metastatic or unresectable cutaneous, mucosal, or ocular (uveal) melanoma in a 3+3 design to determine the maximum-tolerated dose, followed by cohort expansion at the recommended phase II dose (RP2D).
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| Related Clinical Trial | |||||
| NCT Number | NCT01522664 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DEDN6526A in Patients With Metastatic or Unresectable Melanoma | ||||
| Primary Endpoint |
Safety evaluation included ongoing monitoring of adverse events (up to 90 days post-treatment), determination of maximum tolerated dose/dose-limiting toxicities, and establishment of recommended Phase II dose over approximately 2 years.
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| Other Endpoint |
Pharmacokinetic assessments covered concentration-time curve analysis and anti-therapeutic antibody monitoring during treatment cycles, with tumor response evaluated via RECIST criteria for approximately 1 year.
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| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Patients Enrolled |
Eligibility requires adult Stage III/IV melanoma patients (ECOG 0-1, failed ≥1 prior therapies) with adequate organ function. Key exclusions include recent anticancer treatments (21-day washout), active CNS metastases, Grade ≥2 toxicities, MMAE-ADC exposure, or uncontrolled comorbidities. Contraception is mandated for 6 months post-treatment.
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| Administration Dosage |
DEDN6526A (0.3-2.8 mg/kg) was given intravenously every 3 weeks (q3w) to pts with metastatic or unresectable cutaneous, mucosal, or ocular (uveal) melanoma in a 3+3 design to determine the maximum-tolerated dose, followed by cohort expansion at the recommended phase II dose (RP2D).
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| Related Clinical Trial | |||||
| NCT Number | NCT01522664 | Clinical Status | PHASE1 | ||
| Clinical Description | A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DEDN6526A in Patients With Metastatic or Unresectable Melanoma | ||||
| Primary Endpoint |
Safety will be continuously monitored for adverse events through 90 days post-treatment, while dose-limiting toxicities and MTD will be evaluated over one year to establish the recommended Phase II dose within approximately two years.
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| Other Endpoint |
PK parameters including AUC will be assessed through serial sampling (pre/post-dose during Cycles 1-5), alongside ATA monitoring and tumor response evaluations per RECIST criteria for approximately one year.
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References