Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00361
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| PDC Name |
CBX-12
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| PDC Status |
Phase 2
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| Indication |
In total 1 Indication(s)
Tumor
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| Structure |
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| Peptide Name |
Unique variant of pHLIP
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Peptide Info | ||||
| Receptor Name |
DNA topoisomerase 1 (TOP1)
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Receptor Info | ||||
| Drug Name |
Exatecan
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Disulfide bond
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Linker Info | ||||
| Formula |
C187H262FN39O49S2
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 3923.509 | ||||
| Lipid-water partition coefficient (xlogp) | -0.52178 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 43 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 50 | |||||
| Rotatable Bond Count (rotbonds) | 113 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Survival rate |
60 mm3
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| Administration Time | 45 days | ||||
| Administration Dosage | 5 mg/kg | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | HCT-116 xenografts | ||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Survival rate |
75 mm3
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| Administration Time | 42 days | ||||
| Administration Dosage | 10 mg/kg | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | MDA-MB-231 xenografts | ||||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Survival rate |
100 mm3
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| Administration Time | 42 days | ||||
| Administration Dosage | 10 mg/kg with ceralasertib 25 mg/kg | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | MDA-MB-231 xenografts | ||||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Survival rate |
100 mm3
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| Administration Time | 45 days | ||||
| Administration Dosage | 5 mg/kg with ceralasertib 25 mg/kg | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | HCT-116 xenografts | ||||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
58.10%
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| Administration Time | 23 days | ||||
| Administration Dosage | 5 mg/kg | ||||
| Evaluation Method | Tumor volume detection | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | HCT-116 xenografts | ||||
| Experiment 6 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
76.50%
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| Administration Time | 35 days | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | MDA-MB-231 xenografts | ||||
| Experiment 7 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
81.40%
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| Administration Time | 23 days | ||||
| Administration Dosage | 5 mg/kg with ceralasertib 25 mg/kg | ||||
| Evaluation Method | Tumor volume detection | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | HCT-116 xenografts | ||||
| Experiment 8 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
95%
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| Administration Time | 35 days | ||||
| Administration Dosage | 10 mg/kg with ceralasertib 25 mg/kg | ||||
| Evaluation Method | Tumor volume detection | ||||
| Description |
Combination treatment significantly inhibited tumor growth without significant toxicity in both mouse xenografts compared with CBX-12 and ceralasertib monotherapy without significant toxicity.
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| In Vivo Model | MDA-MB-231 xenografts | ||||
References