Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00341
|
|||||
|---|---|---|---|---|---|---|
| PDC Name |
SN38-HKD/RGDR
|
|||||
| PDC Status |
Investigative
|
|||||
| Indication |
In total 1 Indication(s)
Triple-negative breast cancer
|
|||||
| Structure |
|
|||||
| Peptide Name |
CGVVQQ
|
Peptide Info | ||||
| Receptor Name |
Integrin alpha-V (ITGAV)
|
Receptor Info | ||||
| Drug Name |
7-Ethyl-10-hydroxycamptothecin
|
Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
|
Target Info | ||||
| Linker Name |
4-(Disulfanyl)butanoic acid
|
Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
|
|||||
| Modified Segment |
(OEG)4HKD/RGDR
|
|||||
| Ternimal Modification |
C-terminal modification
|
|||||
| Formula |
C88H131N23O31S2
|
|||||
| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 2071.28 | ||||
| Lipid-water partition coefficient (xlogp) | -7.0024 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 23 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 34 | |||||
| Rotatable Bond Count (rotbonds) | 69 | |||||
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 | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
74% (Day 14)
|
|||
| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+ T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
|
||||
| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
|
||||
| In Vivo Model | 4T1 tumor-bearing mice. | ||||
| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
75% (Day 18)
|
|||
| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
|
||||
| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
|
||||
| In Vivo Model | EMT6 tumor-bearing mice. | ||||
| In Vitro Model | Mammary gland malignant neoplasms | EMT6 cell | CVCL_1923 | ||
References