Drug Information
General Information of This Drug
| Drug ID | DRG00052 | |||||
|---|---|---|---|---|---|---|
| Drug Name | Copper-64 | |||||
| Synonyms |
Copper-64; Copper, isotope of mass 64; Copper Cu-64; 13981-25-4; 2MK2L64N0S; UNII-2MK2L64N0S; 64Cu radioisotope; Copper, Cu-64; (~64~Cu)Copper; DTXSID10930607; Q27254977
Click to Show/Hide
|
|||||
| Target(s) | Human Deoxyribonucleic acid (hDNA) | Target Info | ||||
| Structure |
|
|||||
| Formula |
Cu
|
|||||
| #Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 63.929 | ||||
| Lipid-water partition coefficient (xlogp) | Not Available | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 0 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 0 | |||||
| Rotatable Bond Count (rotbonds) | 0 | |||||
| PubChem CID | ||||||
| Canonical smiles |
[Cu]
|
|||||
| InChI |
InChI=1S/Cu/i1+0
|
|||||
| InChIKey |
RYGMFSIKBFXOCR-IGMARMGPSA-N
|
|||||
| IUPAC Name |
copper-64
|
|||||
Each Peptide-drug Conjugate Related to This Drug
Full Information of The Activity Data of The PDC(s) Related to This Drug
Copper dotatate Cu-64 [Approved]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroendocrine neoplasms | ||||
| Efficacy Data | PET75% overall specificities | 92% | |||
| Evaluation Method | PET/CT | ||||
| Patients Enrolled |
38 patients with NEN.
|
||||
| Administration Dosage | 142 MBq | ||||
| MOA of PDC |
Somatostatin analogues radiolabeled with the radioisotope 68Ga, e.g. [68Ga]Ga-DOTATATE and [68Ga]Ga-DOTATOC, are currently the predominately used tracers for PET imaging of patients with NEN. However, the 64Cu-labeled SSR targeting somatostatin analogue [64Cu]Cu-DOTATATE is emerging as an alternative to 68Ga-labeled radiotracers. Although 64Cu has a lower branching ratio for + decay than 68Ga (18% vs 89%), 64Cu has the advantage of a longer half-life (12.7 h vs 68 min) and shorter positron range (0.7 mm vs 3.5 mm) where the latter at least in theory should lead to better spatial resolution. The effective whole-body dose is 6.3 mSv for a 200 MBq injection of [64Cu]Cu-DOTATATE or 4.7 mSv for the United States Food and Drug Administration (FDA) recommended dose of 148 MBq.
Click to Show/Hide
|
||||
| Description |
The median [64Cu]Cu-DOTATATE activity dose could be reduced from 191 to 142 MBq without decline in diagnostic image quality (P = 0.62), diagnostic lesion confidence (P = 1.0), or number of lesions detected in major organs or regions (P = 0.19-0.71). Sensitivity and specificity for detection of liver disease were 100% (26/26 patients) and 100% (12/12), respectively, for both PET75% and PET50%. Overall sensitivity for detection of NEN was 100% (26/26) for both PET75% and PET50%, and overall specificities were 92% (11/12) and 100% (12/12) for PET75 and PET50, respectively. Following dose-blinded post hoc review, the PET75% specificity was adjusted to 100% (12/12).
Click to Show/Hide
|
||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroendocrine neoplasms | ||||
| Efficacy Data | PET75% overall sensitivity | 100% | |||
| Evaluation Method | PET/CT | ||||
| Patients Enrolled |
38 patients with NEN.
|
||||
| Administration Dosage | 142 MBq | ||||
| MOA of PDC |
Somatostatin analogues radiolabeled with the radioisotope 68Ga, e.g. [68Ga]Ga-DOTATATE and [68Ga]Ga-DOTATOC, are currently the predominately used tracers for PET imaging of patients with NEN. However, the 64Cu-labeled SSR targeting somatostatin analogue [64Cu]Cu-DOTATATE is emerging as an alternative to 68Ga-labeled radiotracers. Although 64Cu has a lower branching ratio for + decay than 68Ga (18% vs 89%), 64Cu has the advantage of a longer half-life (12.7 h vs 68 min) and shorter positron range (0.7 mm vs 3.5 mm) where the latter at least in theory should lead to better spatial resolution. The effective whole-body dose is 6.3 mSv for a 200 MBq injection of [64Cu]Cu-DOTATATE or 4.7 mSv for the United States Food and Drug Administration (FDA) recommended dose of 148 MBq.
Click to Show/Hide
|
||||
| Description |
The median [64Cu]Cu-DOTATATE activity dose could be reduced from 191 to 142 MBq without decline in diagnostic image quality (P = 0.62), diagnostic lesion confidence (P = 1.0), or number of lesions detected in major organs or regions (P = 0.19-0.71). Sensitivity and specificity for detection of liver disease were 100% (26/26 patients) and 100% (12/12), respectively, for both PET75% and PET50%. Overall sensitivity for detection of NEN was 100% (26/26) for both PET75% and PET50%, and overall specificities were 92% (11/12) and 100% (12/12) for PET75 and PET50, respectively. Following dose-blinded post hoc review, the PET75% specificity was adjusted to 100% (12/12).
Click to Show/Hide
|
||||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroendocrine neoplasms | ||||
| Efficacy Data | PET50% overall specificities | 100% | |||
| Evaluation Method | PET/CT | ||||
| Patients Enrolled |
38 patients with NEN.
|
||||
| Administration Dosage | 142 MBq | ||||
| MOA of PDC |
Somatostatin analogues radiolabeled with the radioisotope 68Ga, e.g. [68Ga]Ga-DOTATATE and [68Ga]Ga-DOTATOC, are currently the predominately used tracers for PET imaging of patients with NEN. However, the 64Cu-labeled SSR targeting somatostatin analogue [64Cu]Cu-DOTATATE is emerging as an alternative to 68Ga-labeled radiotracers. Although 64Cu has a lower branching ratio for + decay than 68Ga (18% vs 89%), 64Cu has the advantage of a longer half-life (12.7 h vs 68 min) and shorter positron range (0.7 mm vs 3.5 mm) where the latter at least in theory should lead to better spatial resolution. The effective whole-body dose is 6.3 mSv for a 200 MBq injection of [64Cu]Cu-DOTATATE or 4.7 mSv for the United States Food and Drug Administration (FDA) recommended dose of 148 MBq.
Click to Show/Hide
|
||||
| Description |
The median [64Cu]Cu-DOTATATE activity dose could be reduced from 191 to 142 MBq without decline in diagnostic image quality (P = 0.62), diagnostic lesion confidence (P = 1.0), or number of lesions detected in major organs or regions (P = 0.19-0.71). Sensitivity and specificity for detection of liver disease were 100% (26/26 patients) and 100% (12/12), respectively, for both PET75% and PET50%. Overall sensitivity for detection of NEN was 100% (26/26) for both PET75% and PET50%, and overall specificities were 92% (11/12) and 100% (12/12) for PET75 and PET50, respectively. Following dose-blinded post hoc review, the PET75% specificity was adjusted to 100% (12/12).
Click to Show/Hide
|
||||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroendocrine neoplasms | ||||
| Efficacy Data | PET50% overall sensitivity | 100% | |||
| Evaluation Method | PET/CT | ||||
| Patients Enrolled |
38 patients with NEN.
|
||||
| Administration Dosage | 142 MBq | ||||
| MOA of PDC |
Somatostatin analogues radiolabeled with the radioisotope 68Ga, e.g. [68Ga]Ga-DOTATATE and [68Ga]Ga-DOTATOC, are currently the predominately used tracers for PET imaging of patients with NEN. However, the 64Cu-labeled SSR targeting somatostatin analogue [64Cu]Cu-DOTATATE is emerging as an alternative to 68Ga-labeled radiotracers. Although 64Cu has a lower branching ratio for + decay than 68Ga (18% vs 89%), 64Cu has the advantage of a longer half-life (12.7 h vs 68 min) and shorter positron range (0.7 mm vs 3.5 mm) where the latter at least in theory should lead to better spatial resolution. The effective whole-body dose is 6.3 mSv for a 200 MBq injection of [64Cu]Cu-DOTATATE or 4.7 mSv for the United States Food and Drug Administration (FDA) recommended dose of 148 MBq.
Click to Show/Hide
|
||||
| Description |
The median [64Cu]Cu-DOTATATE activity dose could be reduced from 191 to 142 MBq without decline in diagnostic image quality (P = 0.62), diagnostic lesion confidence (P = 1.0), or number of lesions detected in major organs or regions (P = 0.19-0.71). Sensitivity and specificity for detection of liver disease were 100% (26/26 patients) and 100% (12/12), respectively, for both PET75% and PET50%. Overall sensitivity for detection of NEN was 100% (26/26) for both PET75% and PET50%, and overall specificities were 92% (11/12) and 100% (12/12) for PET75 and PET50, respectively. Following dose-blinded post hoc review, the PET75% specificity was adjusted to 100% (12/12).
Click to Show/Hide
|
||||
64Cu-NODAGA-E[c(RGDyK)]2 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Glioblastoma | ||||
| Efficacy Data | Radiochemical purity | 92%-99% | |||
| In Vivo Model | Nude mice bearing either human glioblastoma (U87MG)/human neuroendocrine (H727) xenograft tumors. | ||||
References