Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00047
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| PDC Name |
99mTc-HYNIC-CLB-c(NGR)
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Melanoma
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| Structure |
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| Peptide Name |
Cyclic NGR
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Peptide Info | ||||
| Drug Name |
Chlorambucil
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
Amide bond
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Linker Info | ||||
| Peptide Modified Type |
Cyclization modification
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| Modified Segment |
Head-to-tail cyclization
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| Formula |
C59H90Cl2N20O16S2Tc+4
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 1569.439255 | ||||
| Lipid-water partition coefficient (xlogp) | -3.05413 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 15 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 25 | |||||
| Rotatable Bond Count (rotbonds) | 36 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Melanoma | ||||
| Efficacy Data | Growth inhibition rate |
30%
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| Administration Time | 48 h | ||||
| Administration Dosage | 1 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The exposure of cells to PDC resulted in significant growth inhibition at all the concentrations as compared to the drug or the peptide alone. It was observed that nearly 25-fold excess concentration of the drug is required to achieve similar cytotoxicity as obtained on exposure to PDC. The RGD peptide-CLB conjugate has also been reported to show higher growth inhibition in B16F10 cells as compared to the drug or peptide alone.24 The enhanced cytotoxic effect of PDC even at lower levels indicates clear advantage in reducing the systemic exposure and side effects of the drug.
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| In Vitro Model | Mouse melanoma | B16-F10 cell | CVCL_0159 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Melanoma | ||||
| Efficacy Data | Growth inhibition rate |
33%
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| Administration Time | 48 h | ||||
| Administration Dosage | 5 µM | ||||
| Evaluation Method | MTT assay | ||||
| MOA of PDC |
Although RNT with 177Lu-DOTATATE/PSMA is known as a novel and effective therapy option for cancer that significantly improves the quality of life and survival of patients, it may have acute or chronic side effects. Therefore, any method that can ameliorate these side effects is useful in the RNT process. For this purpose, a few clinical studies have reported that antioxidants as free radical scavengers such as amifostine and vitamins C and E can reduce radioiodine-related side effects, particularly in salivary glands in thyroid cancer patients.
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| Description |
The exposure of cells to PDC resulted in significant growth inhibition at all the concentrations as compared to the drug or the peptide alone. It was observed that nearly 25-fold excess concentration of the drug is required to achieve similar cytotoxicity as obtained on exposure to PDC. The RGD peptide-CLB conjugate has also been reported to show higher growth inhibition in B16F10 cells as compared to the drug or peptide alone.24 The enhanced cytotoxic effect of PDC even at lower levels indicates clear advantage in reducing the systemic exposure and side effects of the drug.
Click to Show/Hide
|
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| In Vitro Model | Mouse melanoma | B16-F10 cell | CVCL_0159 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Melanoma | ||||
| Efficacy Data | Growth inhibition rate |
40%
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| Administration Time | 48 h | ||||
| Administration Dosage | 10 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The exposure of cells to PDC resulted in significant growth inhibition at all the concentrations as compared to the drug or the peptide alone. It was observed that nearly 25-fold excess concentration of the drug is required to achieve similar cytotoxicity as obtained on exposure to PDC. The RGD peptide-CLB conjugate has also been reported to show higher growth inhibition in B16F10 cells as compared to the drug or peptide alone.24 The enhanced cytotoxic effect of PDC even at lower levels indicates clear advantage in reducing the systemic exposure and side effects of the drug.
Click to Show/Hide
|
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| In Vitro Model | Mouse melanoma | B16-F10 cell | CVCL_0159 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Melanoma | ||||
| Efficacy Data | Growth inhibition rate |
55%
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| Administration Time | 48 h | ||||
| Administration Dosage | 25 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The exposure of cells to PDC resulted in significant growth inhibition at all the concentrations as compared to the drug or the peptide alone. It was observed that nearly 25-fold excess concentration of the drug is required to achieve similar cytotoxicity as obtained on exposure to PDC. The RGD peptide-CLB conjugate has also been reported to show higher growth inhibition in B16F10 cells as compared to the drug or peptide alone.24 The enhanced cytotoxic effect of PDC even at lower levels indicates clear advantage in reducing the systemic exposure and side effects of the drug.
Click to Show/Hide
|
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| In Vitro Model | Mouse melanoma | B16-F10 cell | CVCL_0159 | ||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Melanoma | ||||
| Efficacy Data | Growth inhibition rate |
75%
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| Administration Time | 48 h | ||||
| Administration Dosage | 50 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The exposure of cells to PDC resulted in significant growth inhibition at all the concentrations as compared to the drug or the peptide alone. It was observed that nearly 25-fold excess concentration of the drug is required to achieve similar cytotoxicity as obtained on exposure to PDC. The RGD peptide-CLB conjugate has also been reported to show higher growth inhibition in B16F10 cells as compared to the drug or peptide alone.24 The enhanced cytotoxic effect of PDC even at lower levels indicates clear advantage in reducing the systemic exposure and side effects of the drug.
Click to Show/Hide
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| In Vitro Model | Mouse melanoma | B16-F10 cell | CVCL_0159 | ||
References