Synthesis and characterisation of DOTA-kisspeptin-10 as a potential gallium-68/lutetium-177 pan-tumour radiopharmaceutical.

Kleynhans J, Reeve R, Driver CHS, Marjanovic-Painter B, Sathekge M, Zeevaart JR, Ebenhan T, Millar RP

Journal of neuroendocrinology7 Jan 2025Cited by 3 (Europe PMC)

PMID39775975PMCIDPMC11919473DOI10.1111/jne.13487PepBankPUB-39775975

Summary

Kisspeptin (KISS1) and its cognate receptor (KISS1R) are implicated in the progression of various cancers. A gallium-68 labelled kisspeptin-10 (KP10), the minimal biologically active structure, has potential as a pan-tumour radiopharmaceutical for the detection of cancers. Furthermore, a lutetium-177 labelled KP10 could find therapeutic application in treating oncological diseases. DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) was attached to the NH2-terminus of KP10 as we posited from our previous publications that this modification would not impair biological activity. Here, we showed that the biological activity, as monitored by stimulation of inositol phosphate accumulation in HEK293 transfected with the KISS1R gene, was indeed similar for KP10 and DOTA-KP10. The optimisation of radiolabelling with gallium-68 and lutetium-177 is described. Stability in serum, plasma and whole blood was also investigated. Pharmacokinetics and biodistribution were established with micro-PET/CT (positron emission tomography/computerised tomography) and ex vivo measurements. Dynamic studies with micro-PET/CT demonstrated that background clearance for the radiopharmaceutical was rapid with a blood half-life of 18 ± 3 min. DOTA-KP10 demonstrated preserved functionality at KISS1R and good blood clearance. These results lay the foundation for the further development of DOTA-KP10 analogues that have high binding affinity along with proteolytic resistance.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study3

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone3

In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Kisspeptin-10.

01AnimalNot a test of Kisspeptin-10 aloneAnimal study (in vivo)Pharmacokinetics
In dynamic micro-PET/CT studies, background clearance of the DOTA-KP10 radiopharmaceutical was rapid.
In plain wordsIn imaging studies in animals, the radiolabelled kisspeptin‑10 compound cleared quickly from background tissue.
Peptide
Kisspeptin-10
Outcome
Not applicableBackground clearance of the radiopharmaceutical
Study
n: not reported in source
micro-PET/CT imaging
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Dynamic studies with micro-PET/CT demonstrated that background clearance for the radiopharmaceutical was rapid with a blood half-life of 18 ± 3 min.
In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Kisspeptin-10.
Show in the study text Report a problemFND-3977597502
02AnimalNot a test of Kisspeptin-10 aloneAnimal study (in vivo)Pharmacokinetics
In dynamic micro-PET/CT studies, the blood half-life of the DOTA-KP10 radiopharmaceutical was 18 +/- 3 min.
In plain wordsIn imaging studies in animals, the radiolabelled kisspeptin‑10 compound had a blood half-life of about 18 minutes.
Peptide
Kisspeptin-10
Outcome
Not applicableBlood half-life
Study
n: not reported in source
micro-PET/CT imaging
Outcome group
Pharmacokinetics · Pharmacology
Measurements
Blood half-life
18 min
radiopharmaceutical
Source sentences
Summary
with a blood half-life of 18 ± 3 min.
In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Kisspeptin-10.
Show in the study text Report a problemFND-3977597503
03LabNot a test of Kisspeptin-10 aloneIn vitro (cells)Activity measurement
In HEK293 cells expressing KISS1R, the biological activity of DOTA-KP10 was similar to that of KP10.
In plain wordsIn lab cells, attaching DOTA to kisspeptin‑10 did not change how well it switched on its receptor.
Peptide
Kisspeptin-10
Outcome
No significant changeInositol phosphate accumulation at KISS1R
Study
n: not reported in source
HEK293 cells transfected with the KISS1R gene
Comparator
KP10
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
the biological activity, as monitored by stimulation of inositol phosphate accumulation in HEK293 transfected with the KISS1R gene, was indeed similar for KP10 and DOTA-KP10
In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Kisspeptin-10.
Show in the study text Report a problemFND-3977597501

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
10 Oct 2026, 09:43 UTC
Study results updated
Version 1
9 Oct 2026, 03:04 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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