Page last updated: 2024-12-10

bombesin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID16201612
CHEMBL ID437027
MeSH IDM0002763

Synonyms (20)

Synonym
ccris 3334
alytesin, 2-l-glutamine-6-l-asparagine-
31362-50-2
bombesin acetate salt hydrate, >=97% (hplc)
CHEMBL437027
bombesin 14
px9azu7qpk ,
unii-px9azu7qpk
pglu-gln-arg-leu-gly-asn-gln-trp-ala-val-gly-his-leu-met-nh2
l-methioninamide, 5-oxo-l-prolyl-l-glutaminyl-l-arginyl-l-leucylglycyl-l-asparaginyl-l-glutaminyl-l-tryptophyl-l-alanyl-l-valylglycyl-l-histidyl-l-leucyl-
5-oxo-pro-gln-arg-leu-gly-asn-gln-trp-ala-val-gly-his-leu-met-nh2
bombesin [mi]
QXZBMSIDSOZZHK-DOPDSADYSA-N
mfcd00167514
bombesin-acetate
D81821
h- pglu-gln-arg-leu-gly-asn-gln-trp-ala-val-gly-his-leu-met-nh2
h-{pyroe}qrlgnqwavghlm-nh2
AS-56033
AKOS037645006
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuropeptide Y receptor type 1Homo sapiens (human)IC50 (µMol)0.00470.00020.70318.3700AID721179
Neuromedin-B receptorHomo sapiens (human)Ki0.00200.00020.00080.0020AID42490
Gastrin-releasing peptide receptorHomo sapiens (human)IC50 (µMol)0.00200.00200.00200.0020AID721182
Gastrin-releasing peptide receptorHomo sapiens (human)Ki0.00020.00020.00610.0170AID42630
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gastrin-releasing peptide receptorHomo sapiens (human)EC50 (µMol)0.00030.00030.00030.0003AID322034
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
outflow tract morphogenesisNeuropeptide Y receptor type 1Homo sapiens (human)
glucose metabolic processNeuropeptide Y receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerNeuropeptide Y receptor type 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
locomotory behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
feeding behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of blood pressureNeuropeptide Y receptor type 1Homo sapiens (human)
sensory perception of painNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of multicellular organism growthNeuropeptide Y receptor type 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
neuropeptide signaling pathwayNeuromedin-B receptorHomo sapiens (human)
bombesin receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
negative regulation of interleukin-6 productionNeuromedin-B receptorHomo sapiens (human)
positive regulation of interferon-alpha productionNeuromedin-B receptorHomo sapiens (human)
positive regulation of osteoclast proliferationNeuromedin-B receptorHomo sapiens (human)
antiviral innate immune responseNeuromedin-B receptorHomo sapiens (human)
sneeze reflexNeuromedin-B receptorHomo sapiens (human)
positive regulation of respiratory gaseous exchangeNeuromedin-B receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayNeuromedin-B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
neuropeptide signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
learning or memoryGastrin-releasing peptide receptorHomo sapiens (human)
social behaviorGastrin-releasing peptide receptorHomo sapiens (human)
psychomotor behaviorGastrin-releasing peptide receptorHomo sapiens (human)
regulation of cell population proliferationGastrin-releasing peptide receptorHomo sapiens (human)
response to external biotic stimulusGastrin-releasing peptide receptorHomo sapiens (human)
motor behaviorGastrin-releasing peptide receptorHomo sapiens (human)
positive regulation of respiratory gaseous exchangeGastrin-releasing peptide receptorHomo sapiens (human)
positive regulation of behavioral fear responseGastrin-releasing peptide receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayGastrin-releasing peptide receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
peptide YY receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
protein bindingNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 1Homo sapiens (human)
bombesin receptor activityNeuromedin-B receptorHomo sapiens (human)
neuropeptide receptor activityNeuromedin-B receptorHomo sapiens (human)
neuropeptide receptor activityGastrin-releasing peptide receptorHomo sapiens (human)
G protein-coupled peptide receptor activityGastrin-releasing peptide receptorHomo sapiens (human)
neuropeptide bindingGastrin-releasing peptide receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 1Homo sapiens (human)
cytosolNeuromedin-B receptorHomo sapiens (human)
plasma membraneNeuromedin-B receptorHomo sapiens (human)
plasma membraneNeuromedin-B receptorHomo sapiens (human)
plasma membraneGastrin-releasing peptide receptorHomo sapiens (human)
plasma membraneGastrin-releasing peptide receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID42630In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID346406Displacement of radiolabeled bombesin from bombesin receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID751894Binding affinity to bombesin receptor (unknown origin) by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID721179Displacement of [125I]-NPY from Y1 receptor in human MCF7 cells2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Heterobivalent dual-target probe for targeting GRP and Y1 receptors on tumor cells.
AID752255Binding affinity to bombesin receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID721182Displacement of [125I]-Tyr4-BBN from human GRPR overexpressed in human T47D cells2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Heterobivalent dual-target probe for targeting GRP and Y1 receptors on tumor cells.
AID322034Displacement of 125I[Tyr4]-bombesin from GRPR expressed in human PC3 cells2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Targeting gastrin-releasing peptide receptors of prostate cancer cells for photodynamic therapy with a phthalocyanine-bombesin conjugate.
AID1336311Displacement of [125I][Tyr4]bombesin from rat cerebral cortex BB receptor measured after 60 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID42490Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (14.29)18.2507
2000's2 (28.57)29.6817
2010's4 (57.14)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (11)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pilot Study of 68-Ga PSMA 11 PET/MRI and 68-Ga RM2 PET/MRI for Evaluation of Prostate Cancer Response to HIFU or HDR Therapy [NCT03949517]Phase 1/Phase 210 participants (Anticipated)Interventional2019-04-09Suspended(stopped due to Business decision)
Open-label, Multi Center PET/CT (Positron Emission Tomography/Computed Tomography) Study for Investigation of Safety, Tolerability, Biodistribution and Diagnostic Performance of the 68Ga Labeled PET Tracer BAY86-7548 Following a Single Intravenous Adminis [NCT01205321]Phase 119 participants (Actual)Interventional2010-11-30Completed
An Open-label, Multi Center PET/CT Study for Investigation of Safety and Diagnostic Performance of the 68Ga Labeled PET Tracer [68Ga]RM2 in Patients With Primary Prostate Cancer [NCT02483884]Phase 1/Phase 230 participants (Actual)Interventional2015-05-31Terminated(stopped due to Business decision)
Assessment of the Diagnostic Value of 64Cu-SAR-BBN PET Imaging for Men With Negative PSMA PET in Prostate Cancer [NCT05613842]Phase 230 participants (Actual)Interventional2022-08-09Completed
68Ga-RM2 PET/CT for Detection of Regional Nodal and Distant Metastases in Patients With Intermediate and High-Risk Prostate Cancer [NCT03113617]Phase 244 participants (Actual)Interventional2017-04-10Completed
Open-label, Multicenter PET/CT (Positron Emission Tomography/Computed Tomography) Study for Investigation of Safety, Tolerability, Biodistribution and Diagnostic Performance of the 18F Labeled PET Tracer BAY86-4367 Following a Single Intravenous Administr [NCT00975299]Phase 116 participants (Actual)Interventional2009-09-30Terminated
A Pilot Study of 68-Ga-RM2 PET/MRI in the Evaluation of Patients With Estrogen Receptor-Positive Breast Cancer [NCT03831711]Phase 1/Phase 25 participants (Actual)Interventional2019-03-19Completed
Evaluation of Patients With Low-Risk and Intermediate-Risk Prostate Cancer Scheduled for High-Dose Rate Brachytherapy Using 68-Ga-RM2 PET, 68Ga-PSMA-11 PET and Multi Parametric MRI [NCT04264208]Phase 23 participants (Actual)Interventional2020-02-05Completed
68Ga-DOTA-Bombesin PET/MRI in the Evaluation of Patients With Prostate Cancer: A Feasibility Study [NCT02440308]Phase 210 participants (Actual)Interventional2015-04-30Completed
68Ga-RM2 PET/MRI in the Evaluation of Patients With Biochemical Recurrence of Prostate Cancer and Non-contributory CT Scans [NCT02624518]Phase 2/Phase 3122 participants (Actual)Interventional2015-11-16Completed
A Pilot Study of 68Ga PSMA 11 PET/MRI and 68Ga RM2 PET/MRI for Biopsy Guidance in Patients With Suspected Prostate Cancer [NCT03809078]Phase 220 participants (Anticipated)Interventional2019-01-14Suspended(stopped due to Business decision - funding)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02440308 (2) [back to overview]68Ga-DOTA-Bombesin Feasibility
NCT02440308 (2) [back to overview]Normal Biodistribution of 68Ga-DOTA-Bombesin
NCT02624518 (3) [back to overview]Number of Tumor Lesions Detected by 68Ga-RM2 MRI vs 68Ga-RM2 PET/MRI
NCT02624518 (3) [back to overview]Sensitivity of MRI Alone vs PET/MRI
NCT02624518 (3) [back to overview]Specificity of MR Alone vs PET/MRI
NCT03113617 (2) [back to overview]Sensitivity, Specificity, Negative and Positive Predictive Value for Detection of Regional Nodal Metastases in Comparison to Cross Sectional Imaging Performed Contemporaneously With the 68Ga-RM2 PET
NCT03113617 (2) [back to overview]Sensitivity, Specificity, Positive, and Negative Predictive Value of 68Ga-RM2 PET for the Detection of Regional Nodal Metastases Compared to Pathology at Radical Prostatectomy
NCT03831711 (1) [back to overview]Detection of ER Positive Breast Cancer and Metastases on 68-Ga RM2 PET/MRI

68Ga-DOTA-Bombesin Feasibility

Feasibility of 68Ga-DOTA-Bombesin as a radiopharmaceutical for PET/MRI was assessed as the percentage of enrolled subjects who complete the examination, and for which the PET/MRI data were evaluable. (NCT02440308)
Timeframe: Up to 1 week

Interventionpercentage of participants (Number)
68Ga-DOTA-Bombesin PET/MRI100

[back to top]

Normal Biodistribution of 68Ga-DOTA-Bombesin

Radiopharmaceutical uptake in normal organs will be evaluated visually and measured semi-quantitatively using standardized uptake values (SUV) derived from the PET/CT scan software in patients with prostate cancer. Uptake values in different tissues will be measured as SUVmean (mean value for SUV). SUVmean values reflect relative uptake of the radiolabel into the tissue. (NCT02440308)
Timeframe: 1 hour

InterventionSUV-mean (Mean)
Ascending aorta (blood pool)BladderBrain cortex (frontal lobe)CerebellumCervical vertebraeChoroid plexusColonEsophagusExtra focal uptakesFemurLiverLungGluteal fatGluteal muscleHumerusKidneyLumbar vertebraePancreasParotid glandSacrumSpleenSmall bowelStomachSubmandibular glandThoracic vertebraeThyroid
68Ga-DOTA-Bombesin PET/MRI2.28121.550.080.100.700.252.014.0812.720.341.940.480.600.790.539.510.7552.020.990.691.622.402.481.180.911.31

[back to top]

Number of Tumor Lesions Detected by 68Ga-RM2 MRI vs 68Ga-RM2 PET/MRI

Diagnostic performance of 68Ga-RM2 as a contrast imaging label will be assessed by magnetic resonance imaging (MRI) alone, or as a combined scan with positron emission tomography (PET, collectively PET/MRI). The outcome is reported as the number of tumor lesions detected with MRI alone, or with the combination PET/MRI scan, a number without dispersion. (NCT02624518)
Timeframe: 1 day

Interventionnumber of tumor lesions (Number)
MRI scanPET/MRI scan
Diagnostic (68Ga-RM2 PET/MRI)92127

[back to top]

Sensitivity of MRI Alone vs PET/MRI

Sensitivity is the ability of a test to correctly identify patients who have the prostate cancer, ie, how well 68Ga-RM2 MRI vs 68Ga-RM2 PET/MRI correctly detects patients who truly have prostate cancer. Sensitivity is defined as [TP/(TP+FN)], where TP=true-positive, and FN=false-negative. The outcome is a percentage number with 95% confidence interval (95% CI). A higher % value means a greater probability that an imaging target identified as cancerous is confirmed by histology to be cancerous, and a lower % means reduced confidence in that result. (NCT02624518)
Timeframe: 1 day

Interventionpercentage (Number)
MRI scanPET/MRI scan
Diagnostic (68Ga-RM2 PET/MRI)48.291.8

[back to top]

Specificity of MR Alone vs PET/MRI

Specificity is the ability of a test to correctly identify patients who do not have the prostate cancer, ie, how well 68Ga-RM2 MRI vs 68Ga-RM2 PET/MRI correctly detects patients who do not have prostate cancer (does not falsely return a positive result). Specificity is defined as [TN/(TN+FP)], where TN=true-negative, and FP=false-positive. The outcome is a percentage number with 95% confidence interval (95% CI). A higher % value means a greater probability that an imaging target identified as non-cancerous is confirmed by histology to be non-cancerous, and a lower % means reduced confidence in that result. (NCT02624518)
Timeframe: 1 day

Interventionpercentage of participants (Number)
MRI alonePET/MRI scan
Diagnostic (68Ga-RM2 PET/MRI)97.288.9

[back to top]

Sensitivity, Specificity, Negative and Positive Predictive Value for Detection of Regional Nodal Metastases in Comparison to Cross Sectional Imaging Performed Contemporaneously With the 68Ga-RM2 PET

True positive patient is defined as PET positive for regional nodes, pathology at prostatectomy positive for regional nodes or PET positive for regional nodes, pathology negative for regional nodes, imaging after prostatectomy demonstrates node was not removed at surgery, and follow-up biopsy or imaging demonstrates presence of nodal disease. True negative patient is defined as PET negative for regional nodes, pathology at prostatectomy negative for regional nodes. False positive patient is defined as PET positive for regional nodes, pathology at prostatectomy is negative, and imaging after prostatectomy (NCT03113617)
Timeframe: week 1 study visit following radiopharmaceutical administration, up to 2 hours to assess

Interventionpercentage of cases (Number)
SensitivitySpecificityPositive predictive valueNegative predictive value
Diagnostic (68Ga-RM2 PET/CT)22.296.266.778.1

[back to top]

Sensitivity, Specificity, Positive, and Negative Predictive Value of 68Ga-RM2 PET for the Detection of Regional Nodal Metastases Compared to Pathology at Radical Prostatectomy

True positive patient is defined as PET positive for regional nodes, pathology at prostatectomy positive for regional nodes or PET positive for regional nodes, pathology negative for regional nodes, imaging after prostatectomy demonstrates node was not removed at surgery, and follow-up biopsy or imaging demonstrates presence of nodal disease. True negative patient is defined as PET negative for regional nodes, pathology at prostatectomy negative for regional nodes. False positive patient is defined as PET positive for regional nodes, pathology at prostatectomy is negative, and imaging after prostatectomy (NCT03113617)
Timeframe: week 1 study visit following radiopharmaceutical administration, up to 2 hours to assess

Interventionpercentage of cases (Number)
SpecificitySensitivityPositive predictive valueNegative predictive value
Diagnostic (68Ga-RM2 PET/CT)55.692.371.485.7

[back to top]

Detection of ER Positive Breast Cancer and Metastases on 68-Ga RM2 PET/MRI

Number of lesions identified on 68-Ga RM2 positron emission tomography/magnetic resonance imaging (PET/MRI). The outcome will be reported as the number of participants with successful PET based detection of estrogen receptor (ER) positive breast cancer and metastases. (NCT03831711)
Timeframe: up to 2 hours

InterventionParticipants (Count of Participants)
Breast LesionsLymph Node Lesions
Diagnostic (68-Ga RM2, PET/MRI)41

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