Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00257
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| PDC Name |
P-(A5G27scrm)-PTX
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Metastatic Tumor
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| Structure |
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| Peptide Name |
P-(A5G27scrm)-FITC
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Peptide Info | ||||
| Receptor Name |
CD44 antigen (CD44)
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Receptor Info | ||||
| Drug Name |
Paclitaxel
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Drug Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
4-(2-(glycylglycyl)hydrazineylidene)pentanoic acid
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Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
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| Modified Segment |
N-(2-hydroxypropyl)methacrylamide
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| Formula |
C187H254N34O46S
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 3746.348 | ||||
| Lipid-water partition coefficient (xlogp) | 2.8128 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 38 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 50 | |||||
| Rotatable Bond Count (rotbonds) | 103 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Median overall survival (mOS) |
40.5 days
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| Administration Dosage | 15 mg/kg PTX equivalent dose | ||||
| Description |
The median survival of mice in the P-(A5G27)-PTX treatment group was longer than in P-(A5G27scrm)-PTX, P-(A5G27), and free PTX-treated groups (48.50 vs 40.5, 43, and 45.5, respectively); however, differences were nonsignificant (Figure 6B).
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| In Vivo Model | 4T1 tumor-bearing mice. | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.221 ± 0.055 µM
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| Administration Time | 72 h | ||||
| Description |
P-(A5G27)-PTX was ˜4-fold more toxic than the nontargeted P-(A5G27scrm)-PTX copolymer, suggesting a faster (receptor-mediated) internalization (Figure 4).
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| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
References