Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00181
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| Peptide Name |
LDC10B
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| Structure |
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| Sequence |
KDD-2-(4-(aminomethyl)phenyl)acetic acid-Urea-K-Urea-E
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| Peptide Type |
Linear
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| Receptor Name |
Glutamate carboxypeptidase 2 (FOLH1)
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Receptor Info | ||||
| PDC Transmembrane Types | Cell targeting peptides (CTPs) | |||||
| Formula |
C45H70N12O18S
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| Isosmiles |
NCCCC[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)Cc1ccc(CNC(=O)NCCCC[C@H](NC(=O)N[C@@H](CCC(=O)O)C(=O)O)C(=O)O)cc1)C(N)=O
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| InChI |
InChI=1S/C45H70N12O18S/c46-16-4-1-7-26(37(48)65)52-41(69)32(23-76)55-38(66)27(8-2-5-17-47)53-40(68)31(21-36(63)64)54-39(67)30(20-35(61)62)51-33(58)19-24-10-12-25(13-11-24)22-50-44(74)49-18-6-3-9-28(42(70)71)56-45(75)57-29(43(72)73)14-15-34(59)60/h10-13,26-32,76H,1-9,14-23,46-47H2,(H2,48,65)(H,51,58)(H,52,69)(H,53,68)(H,54,67)(H,55,66)(H,59,60)(H,61,62)(H,63,64)(H,70,71)(H,72,73)(H2,49,50,74)(H2,56,57,75)/t26-,27-,28-,29-,30-,31-,32-/m0/s1
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| InChIKey |
BODYDEMPLJEKCD-YYGRSCHNSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1099.188
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Polar area
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509.39
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Complexity
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1098.465174
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xlogp Value
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-3.6845
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Heavy Count
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76
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Rot Bonds
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39
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Hbond acc
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16
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Hbond Donor
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18
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Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
CBP-1018 [Phase 1]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | WBC decrease |
40%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
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| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
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| Half life period | 0.54-1.15 h | ||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Stable disease (SD) |
29.40%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
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| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
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| Half life period | 0.54-1.15 h | ||||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Non-progressive disease (Non-PD) |
41.10%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
||||
| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
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| Half life period | 0.54-1.15 h | ||||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Neutrophil decrease |
50%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
||||
| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
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| Half life period | 0.54-1.15 h | ||||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Hypokalemia |
10%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
|
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
||||
| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
||||
| Half life period | 0.54-1.15 h | ||||
| Experiment 6 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Hypertriglyceridaemia |
10%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
|
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
||||
| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
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| Half life period | 0.54-1.15 h | ||||
| Experiment 7 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Solid tumor | ||||
| Efficacy Data | Grade ≥3 treatment-emergent adverse event rate |
75%
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| Patients Enrolled |
20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma).
|
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| Administration Time | 4 week | ||||
| Administration Dosage | 0.03 mg/kg | ||||
| MOA of PDC |
Prostate-specific membrane antigen (PSMA) is highly expressed on prostate cancer and folate receptor α (FRα) overexpressed in various malignant tissues which both related to tumor invasiveness. CBP-1018 is a first-in-class bi-ligand-drug conjugate targeting both PSMA and FRα with monomethyl auristatin E (MMAE) as payload.
|
||||
| Description |
As of 27 April 2023, 20 patients (18 mCRPC, 1 bladder cancer and 1 ureteral carcinoma) were enrolled at 6 dose levels (DLs). No DLTs or drug-related deaths were observed. For 15 patients (75%) experienced treatment-related adverse events (TRAEs) ≥ grade 3, most common were neutrophil decrease (50%), WBC decrease (40%), hypokalemia (10%) and hypertriglyceridaemia (10%). Among 17 evaluable mCRPC patients, 5 SD and 7 Non-PD were observed with 9 patients delayed administration and 6 patients dropped for Covid-19. Prostate-specific antigen (PSA) 50% decrease was detected in 2 patients. The median PFS was 9.2 months (95%CI, 1.7-9.2) in mCRPC patients. For PK profile of CBP-1018 and free MMAE, t1/2z was ranged 0.54-1.15 h and 38.27-57.27 h, respectively, no accumulation of both substances after multiple doses.
Click to Show/Hide
|
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| Half life period | 0.54-1.15 h | ||||
References