Page last updated: 2024-10-15

psma-617

Description

PSMA-617: inhibits prostate-specific membrane antigen; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122706786
CHEMBL ID4594280
SCHEMBL ID21316439
SCHEMBL ID21501570
SCHEMBL ID20180896
MeSH IDM000611218

Synonyms (37)

Synonym
S8670
psma617 tfa
1702967-37-0 (free base)
(((s)-1-carboxy-5-((s)-3-(naphthalen-2-yl)-2-((1r,4s)-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carboxamido)propanamido)pentyl)carbamoyl)-l-glutamic acid tetra(trifluoroacetic acid)
SCHEMBL21316439
SCHEMBL21501570
SCHEMBL20180896
vipivotide tetraxetan
HY-117410
CS-0065894
vipivotide tetraxetan [usan:inn]
unii-4ym1w0egq5
who 11010
D11697
vipivotide tetraxetan (usan/inn)
vipivotide tetraxetan [inn]
1702967-37-0
4YM1W0EGQ5 ,
-lysine, n2-((((1s)-1,3-dicarboxypropyl)amino)carbonyl)-n6-(3-(2-naphthalenyl)-n-((trans-4-(((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetyl)amino)methyl)cyclohexyl)carbonyl)--alanyl)-
n-((n6-(3-(naphthalen-2-yl)-n-(trans-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carbonyl)-l-alanyl)-llysin-n2-yl)carbonyl)-l-glutamic acid
l-lysine, n2-((((1s)-1,3-dicarboxypropyl)amino)carbonyl)-n6-(3-(2-naphthalenyl)-n-(2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetyl)-l-alanyl-trans-4-(aminomethyl)cyclohexanecarbonyl)-
dkfz-psma-617
vipivotide tetraxetan [usan]
psma617
n2-((((1s)-1,3-dicarboxypropyl)amino)carbonyl)-n6-(3-(2-naphthalenyl)-n-((trans-4-(((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetyl)amino)methyl)cyclohexyl)carbonyl)-l-alanyl)-l-lysine
psma-617
(((s)-1-carboxy-5-((s)-3-(naphthalen-2-yl)-2-((1r,4s)-4-((2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetamido)methyl)cyclohexane-1-carboxamido)propanamido)pentyl)carbamoyl)-l-glutamic acid ,
F82270
MS-31892
vipivotide tetraxetan (psma-617)
(2s)-2-[[(1s)-1-carboxy-5-[[(2s)-3-naphthalen-2-yl-2-[[4-[[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]methyl]cyclohexanecarbonyl]amino]propanoyl]amino]pentyl]carbamoylamino]pentanedioic acid
EX-A5885
CHEMBL4594280
bdbm50544833
CTC96737
gtpl11982
AKOS040735693

Toxicity

This review aims to provide practical advice and clinical considerations for working with [177Lu]Lu-PSMA-617. Nurses coordinate safe care for patients receiving this therapy.

ExcerptReference
" However, dry mouth is a common side effect that caused about a quarter of patients to stop therapy."( Activity and Adverse Events of Actinium-225-PSMA-617 in Advanced Metastatic Castration-resistant Prostate Cancer After Failure of Lutetium-177-PSMA.
Beheshti, A; Bruchertseifer, F; D'Alessandria, C; Eiber, M; Feuerecker, B; Gafita, A; Gschwend, JE; Heck, M; Knorr, K; Kratochwil, C; Morgenstern, A; Pickhard, A; Retz, M; Seidl, C; Tauber, R; Weber, WA, 2021
)
" Xerostomia and myelosuppression are common early treatment-emergent adverse events in patients receiving this therapy; however, data on long-term toxicity are relatively scarce."( Delayed Nephrotoxicity After 225Ac-PSMA-617 Radioligand Therapy.
Gill, HJS; Maheshwari, P; Satapathy, S; Sharma, A; Sood, A, 2022
)
"This review aims to provide practical advice and clinical considerations for working with [177Lu]Lu-PSMA-617; particularly, regarding the role of nurses in managing radiation safety, monitoring and reporting of adverse events, and counseling patients receiving this therapy."( Practical Guidance on [177Lu]Lu-PSMA-617 Treatment, Including Radiation Safety, Adverse Event Monitoring, and Patient Counseling.
Floyd, R; Gardner, L; Spitz, A; Sutton, J, 2023
)
"Nurses coordinate safe care for patients receiving [177Lu]Lu-PSMA-617 by facilitating communication among physicians, managing logistic concerns, monitoring for adverse events related to treatment, providing education, and counseling patients and caregivers throughout treatment."( Practical Guidance on [177Lu]Lu-PSMA-617 Treatment, Including Radiation Safety, Adverse Event Monitoring, and Patient Counseling.
Floyd, R; Gardner, L; Spitz, A; Sutton, J, 2023
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate carboxypeptidase 2Homo sapiens (human)IC50 (µMol)0.01090.00030.83169.5000AID1666719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
proteolysisGlutamate carboxypeptidase 2Homo sapiens (human)
folic acid-containing compound metabolic processGlutamate carboxypeptidase 2Homo sapiens (human)
C-terminal protein deglutamylationGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
metallocarboxypeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
peptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
dipeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
metal ion bindingGlutamate carboxypeptidase 2Homo sapiens (human)
Ac-Asp-Glu bindingGlutamate carboxypeptidase 2Homo sapiens (human)
tetrahydrofolyl-poly(glutamate) polymer bindingGlutamate carboxypeptidase 2Homo sapiens (human)
carboxypeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
cytoplasmGlutamate carboxypeptidase 2Homo sapiens (human)
plasma membraneGlutamate carboxypeptidase 2Homo sapiens (human)
cell surfaceGlutamate carboxypeptidase 2Homo sapiens (human)
membraneGlutamate carboxypeptidase 2Homo sapiens (human)
extracellular exosomeGlutamate carboxypeptidase 2Homo sapiens (human)
plasma membraneGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1666719Displacement of [125I]MIP-1095 from PSMA in human PC3-PIP cells after 1 hr by gamma counter analysis
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (117)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's35 (29.91)24.3611
2020's82 (70.09)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 (%)
Trials12 (10.08%)5.53%
Reviews6 (5.04%)6.00%
Case Studies12 (10.08%)4.05%
Observational3 (2.52%)0.25%
Other86 (72.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]