Peptide-drug Conjugate Information

General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00039
PDC Name
68Ga-DOTATATE
Synonyms
Gatate; Dotatate gallium Ga-68; Gallium 68 dotatate; 68Ga-DOTATATE; Gallium Ga 68 dotatate; Gallium dotatate, Ga-68; Gallium (68Ga) DOTA-tate; DOTA-octreotate gallium Ga-68; Gallium-DOTA-octreotate Ga-68; (68Ga)Gallium dotatate; UNII-9L17Y0H71P; Gallium-DOTA-octreotate, Ga-68; 9L17Y0H71P; [68GA]GALLIUM DOTATATE; 1027785-90-5; Galiomedix; Gallium dotatate ga-68; GALLIUM (Ga68) DOTATATE; GALLIUM (68GA) DOTATATE [WHO-DD]; GALLIUM DOTATATE GA-68 [ORANGE BOOK]
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PDC Status
Approved
Indication
In total 1 Indication(s)
Neuroendocrine tumour
Structure
Peptide Name
3-Tyr-Octreotate
  Peptide Info 
Receptor Name
Somatostatin receptor type 1 (SSTR1)
  Receptor Info 
Drug Name
Gallium-68
  Drug Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Amide bond
  Linker Info 
Peptide Modified Type
Amino acid modifications; Cyclization modification
Modified Segment
D-amino acids
Ternimal Modification
N-terminal modification
Absorption
Dotatate gallium 68 presents a higher affinity for the somatostatin receptor subtype 2 when compared with the other gallium 68 analogues. Intravenous administration of dotatate gallium 68 is absorbed and distributed to all the somatostatin subtype 2 receptor-containing organs like pituitary, thyroid, spleen, adrenals, kidney, pancreas, prostate, liver and salivary glands. There is no uptake in cerebral cortex or in the heart and the uptake presented in thymus and lung are very low.
Distribution
The volume of distribution is registered in a range from 0.25-0.65 ml/cm3.
Excretion
In the first four hours after the intravenous administration of dotatate gallium 68 there is an elimination of about 12% of the injected dose by the urine.
Drugbank ID
DB13925
ChEBI ID
CHEMBL4297340
Formula
C65H87GaN14O19S2
#Ro5 Violations (Lipinski): 4 Molecular Weight (mw) 1500.5
Lipid-water partition coefficient (xlogp) Not Available
Hydrogen Bond Donor Count (hbonddonor) 14
Hydrogen Bond Acceptor Count (hbondacc) 26
Rotatable Bond Count (rotbonds) 23
Full List of Activity Data of This Peptide-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Neuroendocrine tumour
Efficacy Data Difference in detection ratio
11.80%
Patients Enrolled
75 patients with histologically confirmed neuroendocrine tumours and routine clinical.
MOA of PDC
18F-AlF-OC is noninferior and even superior to 68Ga-DOTATATE/NOC PET in NET patients. This validates 18F-AlF-OC as an option for clinical practice somatostatin receptor PET.
Description
The resulting mean DDR was 15.8%, with a lower margin of the 95% CI (95% CI, 9.6%-22.0%) higher than -15%, which is the prespecified boundary for noninferiority. The mean DDRs for the 68Ga-DOTATATE and 68Ga-DOTANOC subgroups were 11.8% (95% CI, 4.3-19.3) and 27.5% (95% CI, 17.8-37.1), respectively.
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Neuroendocrine tumour
Efficacy Data Median detection ratio
75.30%
Patients Enrolled
75 patients with histologically confirmed neuroendocrine tumours and routine clinical.
MOA of PDC
18F-AlF-OC is noninferior and even superior to 68Ga-DOTATATE/NOC PET in NET patients. This validates 18F-AlF-OC as an option for clinical practice somatostatin receptor PET.
Description
In total, 4,709 different tumor lesions were detected: 3,454 with 68Ga-DOTATATE/NOC and 4,278 with 18F-AlF-OC. The mean DR with 18F-AlF-OC was significantly higher than with 68Ga-DOTATATE/NOC (91.1% vs. 75.3%; P < 10-5).
References
Ref 1 (18)F-AlF-NOTA-Octreotide Outperforms (68)Ga-DOTATATE/NOC PET in Neuroendocrine Tumor Patients: Results from a Prospective, Multicenter Study. J Nucl Med. 2023 Apr;64(4):632-638. doi: 10.2967/jnumed.122.264563. Epub 2022 Oct 20.