Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0WOUMV
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| ADC Name |
RG7841
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| Synonyms |
RG7841; DLYE5953A
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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 |
4
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| Structure |
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| Antibody Name |
MLYE4489A
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Antibody Info | ||||
| Antigen Name |
Lymphocyte antigen 6E (LY6E)
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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 | ||
|---|---|---|---|---|---|---|---|---|---|
| Unspecific solid tumor |
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) | 3.45 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.2 mg/kg.
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[1] |
| Maximum Observed Concentration (Cmax) | 7.74 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.4 mg/kg.
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| Maximum Observed Concentration (Cmax) | 16.1 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.8 mg/kg.
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| Maximum Observed Concentration (Cmax) | 36.9 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 1.6 mg/kg.
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| Maximum Observed Concentration (Cmax) | 44.1 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg.
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| Maximum Observed Concentration (Cmax) | 47 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg MBC.
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| Maximum Observed Concentration (Cmax) | 46.4 | ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg NSCLC.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 13.6 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.2 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 29.8 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 89.7 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.8 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 141 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 1.6 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 219 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 258 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg MBC.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 253 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg NSCLC.
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[1] |
Distribution
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 13.6 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.2 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 29.8 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 89.7 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.8 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 141 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 1.6 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 219 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 258 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg MBC.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 253 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg NSCLC.
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[1] |
| Volume of Distribution (Vd) | 126 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.2 mg/kg.
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| Volume of Distribution (Vd) | 109 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.4 mg/kg.
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[1] |
| Volume of Distribution (Vd) | 129 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.8 mg/kg.
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[1] |
| Volume of Distribution (Vd) | 71.6 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 1.6 mg/kg.
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[1] |
| Volume of Distribution (Vd) | 90.5 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg.
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[1] |
| Volume of Distribution (Vd) | 88 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg MBC.
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[1] |
| Volume of Distribution (Vd) | 87.4 | mL/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg NSCLC.
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[1] |
Metabolism
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 13.6 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.2 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 29.8 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 89.7 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.8 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 141 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 1.6 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 219 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 258 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg MBC.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 253 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg NSCLC.
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[1] |
Excretion
| Standard Type | Value | Units | Description | Reference |
|---|---|---|---|---|
| Area Under the Concentration-Time Curve (AUC) | 13.6 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.2 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 29.8 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 89.7 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 0.8 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 141 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 1.6 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 219 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 258 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg MBC.
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[1] |
| Area Under the Concentration-Time Curve (AUC) | 253 | day*ug/mL |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, AUC0-inf, 2.4 mg/kg NSCLC.
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| Elimination Half-Life (t1/2) | 7.05 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.2 mg/kg.
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| Elimination Half-Life (t1/2) | 8.38 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.4 mg/kg.
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| Elimination Half-Life (t1/2) | 13.3 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.8 mg/kg.
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| Elimination Half-Life (t1/2) | 4.97 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 1.6 mg/kg.
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| Elimination Half-Life (t1/2) | 7.6 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg.
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| Elimination Half-Life (t1/2) | 7.02 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg MBC.
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| Elimination Half-Life (t1/2) | 7.27 | day |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg NSCLC.
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| Clearance (CL) | 16.6 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.2 mg/kg.
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| Clearance (CL) | 13.6 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.4 mg/kg.
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| Clearance (CL) | 10.1 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 0.8 mg/kg.
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| Clearance (CL) | 12 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 1.6 mg/kg.
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| Clearance (CL) | 11.9 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg.
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| Clearance (CL) | 10 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg MBC.
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| Clearance (CL) | 10.9 | mL/day/kg |
Selected mean (SD) pharmacokinetic parameters for total antibody after DLYE5953A treatment at cycle 1, 2.4 mg/kg NSCLC.
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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 | [2] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
17.76%
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| Patients Enrolled |
Eastern Cooperative Oncology Group (ECOG) performance status of 0-1, histologically or cytologically documented advanced or metastatic breast, ovarian, pancreatic, NSCLC, head and neck squamous cell carcinoma, or gastric cancer in dose escalation, adequate hematologic and end organ function, and measurable disease per RECIST v1.1.
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| Administration Dosage |
Intravenously at doses of 0.20, 0.40, 0.80, 1.60, or 2.40 mg/kg once every 3 weeks (Q3W).
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| Related Clinical Trial | |||||
| NCT Number | NCT02092792 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1, open-label study evaluating the safety and tolerability of escalating doses of DLYE5953A in patients with refractory solid tumors. | ||||
| Primary Endpoint |
The confirmed overall objective response rate was 17.76%. All responders (8/68 patients) had PR,and all had received the RP2D dose of 2.40 mg/kg. This included three patients with MBC, and five patients in the NSCLC expansion cohort (5/25; 20%).
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| Other Endpoint |
The recommended phase II dose (RP2D) was 2.40 mg/kg Q3W. No dose-limiting toxicities were identified during dose escalation (0.20-2.40 mg/kg; n = 20).
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| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Patients Enrolled |
Eligible participants (≥18 years, ECOG 0-1) must have measurable advanced/metastatic solid tumors with no effective standard therapies. Exclusions: recent anticancer treatments (chemotherapy/radiation within 4 weeks; oral kinase inhibitors within 2 weeks unless toxicity resolves).
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| Administration Dosage |
.
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| Related Clinical Trial | |||||
| NCT Number | NCT02092792 | Clinical Status | PHASE1 | ||
| Clinical Description | A PHASE I, OPEN-LABEL STUDY EVALUATING THE SAFETY AND TOLERABILITY OF ESCALATING DOSES OF DLYE5953A IN PATIENTS WITH REFRACTORY SOLID TUMORS | ||||
| Primary Endpoint |
The study evaluates safety through dose-limiting toxicities (Days 1-21) and adverse events (up to 32 months) in patients with advanced solid tumors, while also assessing efficacy and drug exposure.
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| Other Endpoint |
Key outcomes include total drug exposure (AUC), immunogenicity (anti-DLYE5953A antibodies), and efficacy measures like objective response (RECIST v1.1), duration of response, and progression-free survival (all tracked up to 32 months).
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References