Page last updated: 2024-11-13

kpt-276

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

Description

KPT-276: a selective inhibitor of nuclear export; inhibits both the XPO1 gene and the CRM1 protein [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71493501
SCHEMBL ID14678596
SCHEMBL ID14676980
MeSH IDM0592178

Synonyms (14)

Synonym
kpt-276
1421919-75-6
(2e)-3-{3-[3,5-bis(trifluoromethyl)phenyl]-1h-1,2,4-triazol-1-yl}-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
SCHEMBL14678596
SCHEMBL14676980
kpt276
AS-72911
3-{3-[3,5-bis(trifluoromethyl)phenyl]-1h-1,2,4-triazol-1-yl}-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
(z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
Q27461879
jchawrdhmuslmm-owojbtedsa-n
(z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1h-1,2,4-triazol-1-yl)-1-(3,3-
A919853
(e)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" In both animal models the anti-lymphoma activity of selinexor is enhanced through combination with DEX or EVER."( Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone.
Aboukameel, A; Azmi, AS; Baloglu, E; Bhutani, D; Carlson, R; Elloul, S; Kauffman, M; Mohammad, RM; Muqbil, I; Senapedis, W; Shacham, S; Zonder, J, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" Orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein have been recently developed."( Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia.
Blum, W; Caligiuri, M; Croce, CM; Garzon, R; Kauffman, M; Klisovic, R; Marcucci, G; Na, C; Ranganathan, P; Santhanam, R; Shacham, S; Walker, A; Yu, X, 2012
)
0.38

Dosage Studied

ExcerptRelevanceReference
" Binding to XPO1 was quantitated from SINE compound treated adherent and suspension cells in vitro, dosed ex vivo human peripheral blood mononuclear cells (PBMCs), and PBMCs from mice dosed orally with drug in vivo."( A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds.
Baloglu, E; Crochiere, ML; Del Alamo, D; Donovan, S; Kauffman, M; Klebanov, B; Landesman, Y; Lee, M; Shacham, S, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's10 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.21 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (10.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]