General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00042
PDC Name
68Ga-PSMA HBED-CC
PDC Status
Investigative
Indication
In total 1 Indication(s)
Metastatic castration-resistant prostate cancer
Structure
Peptide Name
PSMA-617
 Peptide Info 
Receptor Name
Glutamate carboxypeptidase 2 (FOLH1)
 Receptor Info 
Drug Name
Gallium-68
 Drug Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Aminocaproic acid
 Linker Info 
Distribution
DTX-P7 can be detected in the plasma in the first 24 h post treatments with higher area under curve (AUC) and Cmax than DTX. In normal tissues, docetaxel was barely detectable in brain in 1, 2, 4 and 8 h after injection. In the liver, the docetaxel concentration of DTX group was 5 folds and 3 folds higher than that of DTX-P7 group after 1 and 2 h of injection. Similar distribution was also observed in heart and lungs.
Formula
C44H59GaN6O17
#Ro5 Violations (Lipinski): 5 Molecular Weight 1011.90898
Lipid-water partition coefficient (xlogp) -2.8304
Hydrogen Bond Donor Count (hbonddonor) 9
Hydrogen Bond Acceptor Count (hbondacc) 16
Rotatable Bond Count (rotbonds) 35
Full List of Activity Data of This Peptide-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Decrease of median PSA level
44%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
After RLT the median PSA level decreased by 44%, TTV by 45.1%, SUVmean by 25.8% and RECIST by 11.3%.
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Decrease of total tumor volumes (TTV)
45%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
After RLT the median PSA level decreased by 44%, TTV by 45.1%, SUVmean by 25.8% and RECIST by 11.3%.
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Mean standardized uptake values (SUVmean)
26%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
After RLT the median PSA level decreased by 44%, TTV by 45.1%, SUVmean by 25.8% and RECIST by 11.3%.
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Progressive Disease (PD)
21.10%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
A PSA response was seen in 18 patients (47.4%), stable disease in 12 (31.6%) and progressive disease in 8 (21.1%).
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data PSA response
47.40%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
A PSA response was seen in 18 patients (47.4%), stable disease in 12 (31.6%) and progressive disease in 8 (21.1%).
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Response Evaluation Criteria in Solid Tumours (RECIST)
11.30%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
After RLT the median PSA level decreased by 44%, TTV by 45.1%, SUVmean by 25.8% and RECIST by 11.3%.
Experiment 7 Reporting the Activity Data of This PDC [1]
Indication Metastatic castration-resistant prostate cancer
Efficacy Data Stable disease (SD)
31.60%
Patients Enrolled
Patients with metastatic castration-resistant prostate cancer.
Description
A PSA response was seen in 18 patients (47.4%), stable disease in 12 (31.6%) and progressive disease in 8 (21.1%).
References
Ref 1 Response assessment using (68)Ga-PSMA ligand PET in patients undergoing (177)Lu-PSMA radioligand therapy for metastatic castration-resistant prostate cancer. Eur J Nucl Med Mol Imaging. 2019 May;46(5):1063-1072. doi: 10.1007/s00259-018-4236-4. Epub 2018 Dec 19.