Page last updated: 2024-11-11

zotarolimus

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

Description

zotarolimus: synthetic analog of rapamycin; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9876378
CHEMBL ID219410
CHEBI ID135897
SCHEMBL ID67389
MeSH IDM0472306

Synonyms (38)

Synonym
221877-54-9
endeavor
zotarolimus
CHEBI:135897
mdt-4107
abt-578
CHEMBL219410 ,
(1r,9s,12s,15r,16e,18r,19r,21r,23s,24e,26e,28e,30s,32s,35r)-1,18-dihydroxy-19,30-dimethoxy-12-[(2r)-1-[(1s,3r,4s)-3-methoxy-4-(1h-1,2,3,4-tetrazol-1-yl)cyclohexyl]propan-2-yl]-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0^{4,9}]hexatriac
bdbm50174276
abt 578
abt578
zotarilumus
rapamycin, 42-deoxy-42-(1h-tetrazol-1-yl)-, (42s)-
a 179578
h4gxr80ize ,
zotarolimus [usan:inn]
unii-h4gxr80ize
zotarolimus [inn]
zotarolimus [usan]
zotarolimus [mart.]
zotarolimus [who-dd]
S7091
gtpl7974
SCHEMBL67389
AC-31528
HY-12424
CS-5715
J-014574
NCGC00386351-01
DTXSID50873387
zotarolimus (abt-578)
zotarolimus; abt-578
EX-A2216
mfcd09752954
Q15410168
CCG-270596
AS-56346
AKOS037645037

Research Excerpts

Overview

Zotarolimus is a semi-synthetic derivative of rapamycin and a novel immunosuppressive agent used to prevent graft rejection. It is an anti-proliferative drug used exclusively in the design of coronary drug eluting stent.

ExcerptReferenceRelevance
"Zotarolimus is a semi-synthetic derivative of rapamycin and a novel immunosuppressive agent used to prevent graft rejection. "( The Anti-Cancer Effects of a Zotarolimus and 5-Fluorouracil Combination Treatment on A549 Cell-Derived Tumors in BALB/c Nude Mice.
Chang, GR; Chiou, RY; Hou, PH; Kuo, CY; Lin, CF; Lin, TC; Wang, CM; Wu, CF; Wu, CY; Yang, WC, 2021
)
2.36
"Zotarolimus is a semi-synthetic derivative of rapamycin and an inhibitor of mammalian target of rapamycin (mTOR) signaling. "( Anti-Cancer Effects of Zotarolimus Combined with 5-Fluorouracil Treatment in HCT-116 Colorectal Cancer-Bearing BALB/c Nude Mice.
Chang, GR; Chen, CH; Kuo, CY; Liao, HJ; Lin, TC; Lin, WL; Tsai, MY; Wang, YC, 2021
)
2.37
"Zotarolimus is an anti-proliferative drug used exclusively in the design of coronary drug eluting stent."( Zotarolimus for the treatment of coronary artery disease: pathophysiology, DES design, clinical evaluation and future perspective.
Brugaletta, S; Burzotta, F; Sabaté, M, 2009
)
3.24
"Zotarolimus is a recently developed pharmacologic agent with both antiproliferative and anti-inflammatory properties."( Overview of pharmacology and clinical trials program with the zotarolimus-eluting endeavor stent.
Kandzari, DE; Leon, MB, 2006
)
1.3

Effects

ExcerptReferenceRelevance
"The zotarolimus-eluting stent has shown larger in-stent late lumen loss compared to sirolimus-eluting stents in previous studies. "( A randomized, prospective, two-center comparison of sirolimus-eluting stent and zotarolimus-eluting stent in acute ST-elevation myocardial infarction: the SEZE trial.
Chae, IH; Cho, YS; Choi, DJ; Chung, WY; Kang, J; Kim, KI; Kim, MA; Kim, SH; Park, HJ; Seo, JB; Suh, JW; Yang, HM; Youn, TJ; Zo, JH, 2012
)
1.16

Treatment

ExcerptReferenceRelevance
"Zotarolimus-eluting stent treatment compared to sirolimus-eluting stent treatment was associated with increased rates of MACE (8·7% vs. "( Zotarolimus-eluting vs. sirolimus-eluting coronary stents in patients with and without acute coronary syndromes: a SORT OUT III substudy.
Hansen, PR; Jensen, LO; Kaltoft, A; Kelbaek, H; Lassen, JF; Madsen, M; Maeng, M; Ravkilde, J; Sørensen, HT; Thayssen, P; Thim, T; Thuesen, L; Tilsted, HH, 2012
)
3.26

Toxicity

ExcerptReferenceRelevance
" ABT-578 was shown to be safe over a wide range of systemic exposures."( A phase I multiple-dose escalation study characterizing pharmacokinetics and safety of ABT-578 in healthy subjects.
Awni, WM; Chiu, W; Edeki, T; Freeney, T; Granneman, RG; Ji, Q; Karyekar, CS; Locke, C; O'Dea, R; Pradhan, RS; Schwartz, LB, 2005
)
0.33
"Zotarolimus-eluting stents (ZESs) have been shown to be safe and effective in randomised trials."( Long-term safety and efficacy are observed after implantation of Zotarolimus-Eluting stent in real-world clinical practice.
Hong, EC; Lee, CH; Lim, IH; Lim, YT; Low, AF; Tai, BC; Tan, HC; Teo, SG, 2008
)
2.03
"In this real-world clinical experience, ZES was associated with a low incidence of adverse cardiac events at a medium follow-up of one and half years."( Long-term safety and efficacy are observed after implantation of Zotarolimus-Eluting stent in real-world clinical practice.
Hong, EC; Lee, CH; Lim, IH; Lim, YT; Low, AF; Tai, BC; Tan, HC; Teo, SG, 2008
)
0.58
" The primary end point was major adverse cardiac events (death, MI, and ischemia-driven target vessel revascularization) at 12 months."( Comparison of the efficacy and safety of zotarolimus-, sirolimus-, and paclitaxel-eluting stents in patients with ST-elevation myocardial infarction.
Cheong, SS; Cho, YH; Hong, MK; Hong, TJ; Jeong, MH; Kim, JJ; Kim, KS; Kim, YH; Lee, CW; Lee, JH; Lee, NH; Lee, SG; Lee, SH; Lim, DS; Park, DW; Park, SJ; Park, SW; Seong, IW; Seung, KB; Yang, JY; Yoon, J; Yun, SC, 2009
)
0.62
" The primary end point was the rate of major adverse cardiac events (MACE) at 12 months."( Safety and effectiveness of the Endeavor zotarolimus-eluting stent in real-world clinical practice: 12-month data from the E-Five registry.
Liu, M; Lotan, C; Mauri, L; Meredith, IT; Rothman, MT, 2009
)
0.62
" The primary endpoint was a composite of major adverse cardiac events within 9 months: cardiac death, myocardial infarction, and target vessel revascularisation."( Efficacy and safety of zotarolimus-eluting and sirolimus-eluting coronary stents in routine clinical care (SORT OUT III): a randomised controlled superiority trial.
Aarøe, J; Abildgaard, U; Abildstrøm, SZ; Bøtker, HE; Christiansen, EH; Engstrøm, T; Hansen, KN; Hansen, PR; Jensen, JS; Jensen, LO; Johnsen, SP; Kaltoft, A; Kelbaek, H; Kristensen, SD; Krusell, LR; Lassen, JF; Madsen, M; Maeng, M; Rasmussen, K; Ravkilde, J; Sørensen, HT; Thayssen, P; Thuesen, L; Tilsted, HH, 2010
)
0.67
" The endpoints were major adverse cardiac events (MACE) and stent thrombosis rates."( Eighteen-month clinical safety and efficacy outcomes of sirolimus-, paclitaxel- and zotarolimus-drug eluting stents in diabetic patients undergoing percutaneous coronary intervention for complex coronary artery stenosis.
Chong, E; Hou, XM; Liang, S; Poh, KK; Tan, HC, 2010
)
0.59
"The Endeavor ZES has been shown to be safe and efficacious for treatment of single, de novo lesions in patients with stable coronary artery disease."( Extended follow-up safety and effectiveness of the Endeavor zotarolimus-eluting stent in real-world clinical practice: two-year follow-up from the E-Five Registry.
Erglis, A; Lotan, C; Meredith, I; Parikh, K; Rothman, M, 2011
)
0.61
" The primary end point was a composite of major adverse cardiac events (MACE) (death, myocardial infarction, and ischemia-driven target vessel revascularization) at 12 months."( Comparison of zotarolimus-eluting stents with sirolimus- and paclitaxel-eluting stents for coronary revascularization: the ZEST (comparison of the efficacy and safety of zotarolimus-eluting stent with sirolimus-eluting and paclitaxel-eluting stent for cor
Chae, JK; Cheong, SS; Choi, YJ; Hong, TJ; Hur, SH; Jang, Y; Jeong, MH; Kang, SJ; Kim, HS; Kim, KS; Kim, YH; Lee, CW; Lee, JH; Lee, NH; Lee, SG; Lee, SW; Lim, DS; Park, DW; Park, HS; Park, SJ; Park, SW; Seong, IW; Seung, KB; Tahk, SJ; Yang, JY; Yoon, J; Yun, SC, 2010
)
0.72
" The primary efficacy outcomes were target lesion revascularization (TLR), target vessel revascularization (TVR), and major adverse cardiac events (MACE); safety outcomes were stent thrombosis (ST), myocardial infarction (MI), and cardiac death."( Efficacy and safety of zotarolimus-eluting stents compared with sirolimus-eluting stents in patients undergoing percutaneous coronary interventions--a meta-analysis of randomized controlled trials.
Du, H; Fan, J; Ling, Z; Wu, J; Xiao, P; Yin, Y; Zrenner, B, 2013
)
0.7
"02) and major adverse cardiac events (16."( Final 5-year outcomes from the Endeavor zotarolimus-eluting stent clinical trial program: comparison of safety and efficacy with first-generation drug-eluting and bare-metal stents.
Fajadet, J; Kandzari, DE; Leon, MB; Mauri, L; Meredith, I; Wijns, W, 2013
)
0.66
" Adverse clinical events were independently adjudicated."( Safety of second-generation drug-eluting stents three years after randomised use in the TWENTE trial.
de Man, FH; Doggen, CJ; Lam, MK; Linssen, GC; Louwerenburg, JH; Löwik, MM; Sen, H; Stoel, MG; Tandjung, K; van Houwelingen, KG; von Birgelen, C, 2015
)
0.42
"Implantation of R-ZES in real-world patients with long coronary artery lesions is safe with comparable efficacy to what is observed in the treatment of less complex lesions."( Prospective study to evaluate safety and efficacy of Zotarolimus Eluting Stent (PSEZES) in patients with long coronary artery lesions.
Babu, S; Bahuleyan, CG; Krishna Kumar, VV,
)
0.38
"gov updated to Mar 2014 with safety [major adverse cardiac events (MACE)], all-cause mortality, non-fatal myocardial infarction (MI), stent thrombosis (ST) and efficacy [target vessel revascularization (TVR), target lesion revascularization (TLR), target vessel failure (TVF), target lesion failure (TLF)] endpoints and follow-up of ≥12 months were identified."( Safety and efficacy of everolimus-eluting stent versus zotarolimus-eluting stent: A meta-analysis of randomized controlled clinical trials and observational studies.
Gu, H; Hua, K; Li, W; Wang, Y; Yang, J, 2015
)
0.66
"In percutaneous coronary intervention (PCI) patients new-generation drug-eluting stent (DES) has reduced adverse events in comparison to early-generation DES."( Three-year efficacy and safety of new- versus early-generation drug-eluting stents for unprotected left main coronary artery disease insights from the ISAR-LEFT MAIN and ISAR-LEFT MAIN 2 trials.
Byrne, RA; Cassese, S; Fusaro, M; Ibrahim, T; Kastrati, A; Kreutzer, J; Kufner, S; Laugwitz, KL; Mehilli, J; Schunkert, H; Tiroch, K; Tölg, R; Valgimigli, M; Xhepa, E, 2016
)
0.43
" The primary endpoint was the composite of death, myocardial infarction (MI), target lesion revascularization and stroke (MACCE, major adverse cardiac and cerebrovascular event)."( Three-year efficacy and safety of new- versus early-generation drug-eluting stents for unprotected left main coronary artery disease insights from the ISAR-LEFT MAIN and ISAR-LEFT MAIN 2 trials.
Byrne, RA; Cassese, S; Fusaro, M; Ibrahim, T; Kastrati, A; Kreutzer, J; Kufner, S; Laugwitz, KL; Mehilli, J; Schunkert, H; Tiroch, K; Tölg, R; Valgimigli, M; Xhepa, E, 2016
)
0.43
" The primary endpoint was major adverse cardiac events (MACE) defined by a composite of death, nonfatal myocardial infarction and stroke."( Does stent strut design impact clinical outcomes: comparative safety and efficacy of Endeavor Resolute versus Resolute Integrity zotarolimus-eluting stents.
Chong, AY; Di Santo, P; Dick, A; Froeschl, M; Harnett, DT; Hibbert, B; Labinaz, M; Le May, MR; Moreland, R; Pourdjabbar, A; Ramirez, FD; Simard, T; Singh, K; So, DY, 2015
)
0.62
"Patients with diabetes and coronary artery disease remain at high risk for adverse cardiovascular events after percutaneous coronary intervention."( Efficacy and safety of everolimus and zotarolimus-eluting stents versus first-generation drug-eluting stents in patients with diabetes: A meta-analysis of randomized trials.
Baber, U; Bavishi, C; Dangas, GD; Kini, AS; Moreno, P; Panwar, S; Pirrotta, S; Sharma, SK; Tamis-Holland, J, 2017
)
0.73
" Efficacy [target vessel revascularization (TVR) and target lesion revascularization (TLR)] and safety [major adverse cardiac events (MACE), all-cause and cardiac mortality, myocardial infarction, stent thrombosis] outcomes were evaluated."( Efficacy and safety of everolimus and zotarolimus-eluting stents versus first-generation drug-eluting stents in patients with diabetes: A meta-analysis of randomized trials.
Baber, U; Bavishi, C; Dangas, GD; Kini, AS; Moreno, P; Panwar, S; Pirrotta, S; Sharma, SK; Tamis-Holland, J, 2017
)
0.73
"In patients with diabetes and coronary artery disease undergoing stenting, EES is the most efficacious and safe DES."( Efficacy and safety of everolimus and zotarolimus-eluting stents versus first-generation drug-eluting stents in patients with diabetes: A meta-analysis of randomized trials.
Baber, U; Bavishi, C; Dangas, GD; Kini, AS; Moreno, P; Panwar, S; Pirrotta, S; Sharma, SK; Tamis-Holland, J, 2017
)
0.73
"Individual trials are often underpowered to show differences for low-frequency adverse events."( 5-Year Safety and Efficacy of Resolute Zotarolimus-Eluting Stent: The RESOLUTE Global Clinical Trial Program.
Chen, L; Chen, S; Hiremath, S; Mauri, L; Neumann, FJ; Qiao, S; Saito, S; Silber, S; Xu, B; Yang, Y; Yeh, RW, 2017
)
0.72
"Women with acute myocardial infarction (MI) undergoing mechanical reperfusion remain at increased risk of adverse cardiac events and mortality compared with their male counterparts."( Long-term Safety and Efficacy of New-Generation Drug-Eluting Stents in Women With Acute Myocardial Infarction: From the Women in Innovation and Drug-Eluting Stents (WIN-DES) Collaboration.
Baber, U; Camenzind, E; Chieffo, A; Dangas, GD; Faggioni, M; Farhan, S; Galatius, S; Giustino, G; Harari, R; Itchhaporia, D; Jeger, RV; Kandzari, D; Kastrati, A; Kim, HS; Kimura, T; Leon, MB; Mehran, R; Mehta, L; Morice, MC; Sartori, S; Serruys, PW; Sharma, M; Smits, PC; Sorrentino, S; Stefanini, GG; Steg, PG; Stone, GW; Valgimigli, M; Von Birgelen, C; Weisz, G; Wijns, W; Windecker, S, 2017
)
0.46
" The primary outcome measured was the composite of major adverse cardiac events (MACE), including cardiac death, myocardial infarction (MI), or ischaemia-driven target lesion revascularisation at the 12-month follow-up."( Safety of six-month dual antiplatelet therapy after second-generation drug-eluting stent implantation: OPTIMA-C Randomised Clinical Trial and OCT Substudy.
Cho, DK; Choi, S; Hong, BK; Hong, MK; Jang, Y; Jeon, DW; Kang, TS; Kang, WC; Kim, BK; Kim, BO; Kim, JS; Kim, S; Kim, YH; Kwon, HM; Lee, BK; Lee, OH; Min, PK; Shin, DH; Woo, SI; Yoon, YW, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"We retrospectively analyzed data from pharmacokinetic studies of patients implanted with an 18-mm DES: Cypher stent (sirolimus, n = 10), Endeavor stent (zotarolimus, n = 7), Xience V stent (everolimus, n = 6), and Nobori stent (biolimus A9, n = 10), in multicenter trials of Japan."( Comparison of pharmacokinetics of the limus-eluting stents in Japanese patients.
Mitsudo, K; Nakamura, M; Otsuka, Y; Saito, S; Shuto, H, 2011
)
0.57
" The other pharmacokinetic parameters of four DESs differed according to characteristics of the coated drug."( Comparison of pharmacokinetics of the limus-eluting stents in Japanese patients.
Mitsudo, K; Nakamura, M; Otsuka, Y; Saito, S; Shuto, H, 2011
)
0.37
"In Japanese patients, systemic exposure was low, regardless of the type of limus drug eluted from the stents; but specific pharmacokinetic activities were varied according to the drug characteristics, concentration, and DES design."( Comparison of pharmacokinetics of the limus-eluting stents in Japanese patients.
Mitsudo, K; Nakamura, M; Otsuka, Y; Saito, S; Shuto, H, 2011
)
0.37

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here, we examine the anti-tumor effect of zotarolimus, alone and in combination with 5-fluorouracil, on HCT-116 colorectal adenocarcinoma cells implanted in BALB/c nude mice."( Anti-Cancer Effects of Zotarolimus Combined with 5-Fluorouracil Treatment in HCT-116 Colorectal Cancer-Bearing BALB/c Nude Mice.
Chang, GR; Chen, CH; Kuo, CY; Liao, HJ; Lin, TC; Lin, WL; Tsai, MY; Wang, YC, 2021
)
1.19

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Further study is necessary to determine the dose-response and long-term effects ABT-578-eluting stents in the porcine coronary model."( Stent-based delivery of ABT-578 via a phosphorylcholine surface coating reduces neointimal formation in the porcine coronary model.
Carter, AJ; Collingwood, R; Gibson, L; Sedlik, S; Virmani, R, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
macrolideA macrocyclic lactone with a ring of twelve or more members derived from a polyketide.
lactamCyclic amides of amino carboxylic acids, having a 1-azacycloalkan-2-one structure, or analogues having unsaturation or heteroatoms replacing one or more carbon atoms of the ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase mTORHomo sapiens (human)IC50 (µMol)0.00330.00000.857510.0000AID257581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (88)

Processvia Protein(s)Taxonomy
protein destabilizationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
T-helper 1 cell lineage commitmentSerine/threonine-protein kinase mTORHomo sapiens (human)
heart morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
heart valve morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
energy reserve metabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
'de novo' pyrimidine nucleobase biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
inflammatory responseSerine/threonine-protein kinase mTORHomo sapiens (human)
DNA damage responseSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
germ cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
post-embryonic developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of autophagySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lamellipodium assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of myotube differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
neuronal action potentialSerine/threonine-protein kinase mTORHomo sapiens (human)
protein catabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of actin filament polymerizationSerine/threonine-protein kinase mTORHomo sapiens (human)
T cell costimulationSerine/threonine-protein kinase mTORHomo sapiens (human)
ruffle organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of myelinationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
TOR signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to insulin stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of actin cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
multicellular organism growthSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of circadian rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of apoptotic processSerine/threonine-protein kinase mTORHomo sapiens (human)
response to amino acidSerine/threonine-protein kinase mTORHomo sapiens (human)
anoikisSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of osteoclast differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of glycolytic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lipid biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
behavioral response to painSerine/threonine-protein kinase mTORHomo sapiens (human)
rhythmic processSerine/threonine-protein kinase mTORHomo sapiens (human)
oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
voluntary musculoskeletal movementSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of stress fiber assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of keratinocyte migrationSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleus localizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle contractionSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to methionineSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to L-leucineSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to hypoxiaSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to osmotic stressSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of membrane permeabilitySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cellular response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of protein localization to nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription of nucleolar large rRNA by RNA polymerase ISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of wound healing, spreading of epidermal cellsSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of locomotor rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cytoplasmic translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of pentose-phosphate shuntSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to leucine starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
RNA polymerase III type 1 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 2 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 3 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
TFIIIC-class transcription factor complex bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ATP bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
identical protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ribosome bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
phosphoprotein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
PML bodySerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
Golgi membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
mitochondrial outer membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomeSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
endoplasmic reticulum membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
endomembrane systemSerine/threonine-protein kinase mTORHomo sapiens (human)
membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
dendriteSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC2 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
phagocytic vesicleSerine/threonine-protein kinase mTORHomo sapiens (human)
nuclear envelopeSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID257586Efficacy in T-cell mediated adjuvant arthritis model in Lewis rat2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257585Efficacy in CD4+ T-cell mediated experimental autoimmune encephalomyelitis model in Lewis rat2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257588Cmax in male Sprague-Dawley rat administered with 2.5 mg/kg, po2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257581Inhibitory activity against FKBP122005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257584Efficacy in T-cell mediated inflammatory response by delayed type hypersensitivity model in Sprague-Dawley rat2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257592Half life in human in a multiple dose escalation study2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID257583Antiproliferative activity in Lewis rat lymph node cells in rat mixed lymphocyte reaction2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID257591Oral bioavailability in male Sprague-Dawley rat administered with 2.5 mg/kg, po2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID257590AUC in male Sprague-Dawley rat administered with 2.5 mg/kg, po2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID257589Tmax in male Sprague-Dawley rat administered with 2.5 mg/kg, po2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID1412038Apparent terminal half life in Sprague-Dawley rat at 2.5 mg/kg, iv administered as bolus dose by mass spectrometric analysis2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and biological evaluation of rapamycin-derived, next generation small molecules.
AID257587Half life in male Sprague-Dawley rat administered with 2.5 mg/kg, po2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID1412039Apparent terminal half life in Sprague-Dawley rat at 2.5 mg/kg, po administered via gavage by mass spectrometric analysis2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and biological evaluation of rapamycin-derived, next generation small molecules.
AID257582T-cell antiproliferative activity in human mixed lymphocyte reaction2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Rapamycin analogs with reduced systemic exposure.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346129Human FK506 binding protein 1A (5.2.-.- Cis-trans-isomerases)2006European heart journal, Apr, Volume: 27, Issue:8
Zotarolimus-eluting stents reduce experimental coronary artery neointimal hyperplasia after 4 weeks.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (562)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's85 (15.12)29.6817
2010's425 (75.62)24.3611
2020's52 (9.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.19

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index41.19 (24.57)
Research Supply Index6.68 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index63.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (41.19)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials217 (37.29%)5.53%
Reviews53 (9.11%)6.00%
Case Studies27 (4.64%)4.05%
Observational26 (4.47%)0.25%
Other259 (44.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]