Identification
- Summary
Copper oxodotreotide Cu-64 is a Cu labeled somatostatin analog used in positron emission tomography to detect certain types of neuroendocrine tumors.
- Generic Name
- Copper oxodotreotide Cu-64
- DrugBank Accession Number
- DB15873
- Background
Copper Cu 64 dotatate is a newly approved Cu labeled somatostatin analog and has several advantages over 68Ga-labeled somatostatin analogs for positron emission tomography (PET).1 Copper Cu 64 dotatate has a longer half-life and can be produced once a day as opposed to several times a day, and lower positron energy lending to improved spatial resolution.1 Further studies should be performed to compare the two tracers.
Further, PET using Copper Cu 64 dotatate has been found to perform better than the current gold standard of single-photon emission computed tomography (SPECT) using 111In-DTPA-octreotide.1 In a head-to-head trial, the former tracer detected twice as many lesions as the latter.1
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Copper oxodotreotide Cu-64 (DB15873)
- Weight
- Average: 1497.55
Monoisotopic: 1496.508926883 - Chemical Formula
- C65H88CuN14O19S2
- Synonyms
- 64Cu-dotatate
- Copper 64-DOTA-tate
- Copper Cu-64 dotatate
- Copper dotatate Cu-64
- Copper oxodotreotide Cu-64
Pharmacology
- Indication
Copper Cu 64 Dotatate is a radiopharmaceutical used with positron emission tomography(PET) to locate somatostatin receptor-positive neuroendocrine tumors.2
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic process Somatostatin receptor positive neuroendocrine tumours •••••••••••• ••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Not Available
- Mechanism of action
The main target of the positron-emitting Copper Cu 64 dotatate is somatostatin receptor type 2 (SSTR2).2 SSTR2 is frequently overexpressed in malignant neuroendocrine cells; therefore, accumulation of the radionuclide at the site permits PET imaging to occur.2
Target Actions Organism ASomatostatin receptor type 2 binderHumans - Absorption
Radioactivity can be identified in the kidney, liver, adrenal glands, spleen, and pituitary glands 1-3 hours after copper Cu 64 dotatate is administered.2
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
16% - 40% of the original radioactivity was detected in urine 6 hours after the intravenous administration of a single dose.2
- Half-life
The half-life of Copper Cu 64 is 12.7 hours.2
- Clearance
Not Available
- Adverse Effects
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If radiation overdose occurs, patients should be advised to drink plenty of water and to void frequently to increase the rate of elimination of the radionuclide.2 In certain cases, it may be appropriate to administer a diuretic.2
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareLanreotide The therapeutic efficacy of Lanreotide can be decreased when used in combination with Copper oxodotreotide Cu-64. Octreotide The therapeutic efficacy of Octreotide can be decreased when used in combination with Copper oxodotreotide Cu-64. Pasireotide The therapeutic efficacy of Pasireotide can be decreased when used in combination with Copper oxodotreotide Cu-64. Somatostatin The therapeutic efficacy of Somatostatin can be decreased when used in combination with Copper oxodotreotide Cu-64. - Food Interactions
- Take with fluids. Patients should remain well hydrated before and after imaging with copper Cu 64 dotatate to limit radiation exposure.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Detectnet Injection, solution 1.0 mCi/1mL Intravenous Curium US LLC 2020-09-14 Not applicable US 
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- N3858377KC
- CAS number
- 1426155-87-4
- InChI Key
- IJRLLVFQGCCPPI-NVGRTJHCSA-L
- InChI
- InChI=1S/C65H90N14O19S2.Cu/c1-38(80)56-64(96)73-51(63(95)75-57(39(2)81)65(97)98)37-100-99-36-50(72-59(91)47(28-40-10-4-3-5-11-40)68-52(83)32-76-20-22-77(33-53(84)85)24-26-79(35-55(88)89)27-25-78(23-21-76)34-54(86)87)62(94)70-48(29-41-15-17-43(82)18-16-41)60(92)71-49(30-42-31-67-45-13-7-6-12-44(42)45)61(93)69-46(58(90)74-56)14-8-9-19-66;/h3-7,10-13,15-18,31,38-39,46-51,56-57,67,80-82H,8-9,14,19-30,32-37,66H2,1-2H3,(H,68,83)(H,69,93)(H,70,94)(H,71,92)(H,72,91)(H,73,96)(H,74,90)(H,75,95)(H,84,85)(H,86,87)(H,88,89)(H,97,98);/q;+2/p-2/t38-,39-,46+,47-,48+,49-,50+,51+,56+,57+;/m1./s1/i;1+0
- IUPAC Name
- (64Cu)copper(2+) 2-[7-({[(1R)-1-{[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-{[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl}-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-[(1H-indol-3-yl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-19-yl]carbamoyl}-2-phenylethyl]carbamoyl}methyl)-4-(carboxylatomethyl)-10-(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetate
- SMILES
- [64Cu++].C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)CN2CCN(CC(O)=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC2)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@H](CC2=CNC3=C2C=CC=C3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(O)=O
References
- General References
- Pfeifer A, Knigge U, Binderup T, Mortensen J, Oturai P, Loft A, Berthelsen AK, Langer SW, Rasmussen P, Elema D, von Benzon E, Hojgaard L, Kjaer A: 64Cu-DOTATATE PET for Neuroendocrine Tumors: A Prospective Head-to-Head Comparison with 111In-DTPA-Octreotide in 112 Patients. J Nucl Med. 2015 Jun;56(6):847-54. doi: 10.2967/jnumed.115.156539. Epub 2015 May 7. [Article]
- FDA Approved Drug Products: Detectnet (copper Cu 64 dotatate injection) for intravenous use [Link]
- RadiologyInfo.org: Positron Emission Tomography - Computed Tomography (PET/CT) [Link]
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Diagnostic Neuroendocrine Tumors 1 2 Enrolling by Invitation Diagnostic Gastroenteropancreatic Neuroendocrine Tumors / Metastatic Neuroendocrine Carcinoma / Neuroendocrine Carcinomas (NEC) / Neuroendocrine Tumors 1 1 Not Yet Recruiting Treatment Neuroendocrine Tumors / Somatostatin Receptor-positive Neuroendocrine Tumor 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 1.0 mCi/1mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10159759 No 2018-12-25 2032-08-23 US US10383961 No 2019-08-20 2032-08-23 US US11160888 No 2021-11-02 2032-08-23 US
Properties
- State
- Not Available
- Experimental Properties
Property Value Source Radioactivity (mCi/mL) 1 https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213227s000lbl.pdf - Predicted Properties
Property Value Source Water Solubility 0.103 mg/mL ALOGPS logP -1.3 ALOGPS logP -8.4 Chemaxon logS -4.2 ALOGPS pKa (Strongest Acidic) 0.47 Chemaxon pKa (Strongest Basic) 10.28 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 24 Chemaxon Hydrogen Donor Count 15 Chemaxon Polar Surface Area 503.12 Å2 Chemaxon Rotatable Bond Count 26 Chemaxon Refractivity 386.51 m3·mol-1 Chemaxon Polarizability 143.59 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and ...
- Gene Name
- SSTR2
- Uniprot ID
- P30874
- Uniprot Name
- Somatostatin receptor type 2
- Molecular Weight
- 41332.37 Da
References
- FDA Approved Drug Products: Detectnet (copper Cu 64 dotatate injection) for intravenous use [Link]
Drug created at September 22, 2020 14:40 / Updated at March 04, 2021 09:26