Page last updated: 2024-11-12

umirolimus

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Description

umirolimus: sirolimus derivative from a biodegradable polylactic acid polymer; possesses enhanced anti-inflammatory and antiproliferative activity with an improved pharmacokinetic profile; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23230457
CHEBI ID177399
MeSH IDM0507755

Synonyms (4)

Synonym
(1r,9s,12s,15r,16e,18r,19r,21r,23s,24e,26e,28e,30s,32s,35r)-12-[(2r)-1-[(1s,3r,4r)-4-(2-ethoxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26
CHEBI:177399
851536-75-9
umirolimus

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The goals of this study were to identify the highest safe intravenous dose of BA9, to evaluate the dose-dependent pharmacokinetics of BA9 after intravenous administration in humans, and to characterize early clinical symptoms of BA9 toxicity in healthy subjects."( Randomized, double-blind, placebo-controlled, single intravenous dose-escalation study to evaluate the safety, tolerability, and pharmacokinetics of the novel coronary smooth muscle cell proliferation inhibitor Biolimus A9 in healthy individuals.
Bendrick-Peart, J; Betts, R; Christians, U; Clavijo, C; Dingmann, C; Shulze, J; Steudel, W; Zhang, YL, 2011
)
0.37
"To evaluate the incidence of major adverse cardiac events (cardiac death, or acute myocardial infarct, or target vessel revascularization) at one year in "real world" patients."( Safety and efficacy of biolimus-eluting stent with biodegradable polymer: insights from EINSTEIN (Evaluation of Next-generation drug-eluting STEnt IN patients with coronary artery disease) Registry.
Abizaid, AA; Almeida, AG; Almeida, BO; Caixeta, A; de Brito Júnior, FS; El Mouallem, AM; Nascimento, TC; Perin, MA; Souza, CF,
)
0.13
" At one-year, major adverse cardiac events occurred in 11."( Safety and efficacy of biolimus-eluting stent with biodegradable polymer: insights from EINSTEIN (Evaluation of Next-generation drug-eluting STEnt IN patients with coronary artery disease) Registry.
Abizaid, AA; Almeida, AG; Almeida, BO; Caixeta, A; de Brito Júnior, FS; El Mouallem, AM; Nascimento, TC; Perin, MA; Souza, CF,
)
0.13
"The present Registry suggests that new generation biolimus A9 drug-eluting stents are safe and effective in a "real world", all-comers patients, showing low rates of major cardiac adverse events on long-term follow-up."( Safety and efficacy of biolimus-eluting stent with biodegradable polymer: insights from EINSTEIN (Evaluation of Next-generation drug-eluting STEnt IN patients with coronary artery disease) Registry.
Abizaid, AA; Almeida, AG; Almeida, BO; Caixeta, A; de Brito Júnior, FS; El Mouallem, AM; Nascimento, TC; Perin, MA; Souza, CF,
)
0.13
"Biodegradable-polymer drug-eluting stents (BP-DES) were developed to be as effective as second-generation durable-polymer drug-eluting stents (DP-DES) and as safe >1 year as bare-metal stents (BMS)."( Long-term efficacy and safety of biodegradable-polymer biolimus-eluting stents: main results of the Basel Stent Kosten-Effektivitäts Trial-PROspective Validation Examination II (BASKET-PROVE II), a randomized, controlled noninferiority 2-year outcome tria
Alber, H; Buser, P; Conen, D; Eberli, F; Galatius, S; Gilgen, N; Hoffmann, A; Jeger, R; Kaiser, C; Kurz, DJ; Moccetti, T; Müller, C; Naber, C; Pedrazzini, G; Pfisterer, M; Rickenbacher, P; Rickli, H; Skov Jensen, J; Steiner, M; Vogt, DR; Von Felten, S; Vuillomenet, A; Wadt Hansen, K; Wanitschek, M; Weilenmann, D, 2015
)
0.42
" Safety parameters included the frequency of peri-procedural complications, and major adverse cardiac events (MACE), a composite of cardiac death, myocardial infarction (MI) and any clinically-indicated revascularization at 2 years."( Long-term safety and feasibility of three-vessel multimodality intravascular imaging in patients with ST-elevation myocardial infarction: the IBIS-4 (integrated biomarker and imaging study) substudy.
Dijkstra, J; Garcia-Garcia, HM; Heg, D; Holmvang, L; Kelbæk, H; Landmesser, U; Lüscher, TF; Meier, B; Moschovitis, A; Noble, S; Pedrazzini, G; Räber, L; Radu, MD; Roffi, M; Saunamäki, K; Stefanini, GG; Taniwaki, M; Wenaweser, P; Windecker, S, 2015
)
0.42
"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
" We assessed major adverse cardiac events (MACE) defined as the composite of cardiac death, non-fatal myocardial infarction (MI), and clinical-driven target vessel revascularization at 12 months."( Effectiveness and Safety of Biolimus A9™-Eluting stEnt in Patients with AcUTe Coronary sYndrome; A Multicenter, Observational Study (BEAUTY Study).
Ahn, Y; Bae, JH; Bae, JW; Cha, KS; Chae, JK; Cho, JH; Hong, YJ; Hur, SH; Hwang, JY; Hwang, SH; Jeong, MH; Kim, DI; Kim, HK; Kim, SW; Kim, W; Koh, YY; Lee, JH; Lee, SW; Lee, SY; Lim, SY; Oh, SK; Park, HS; Park, JS; Park, KH; Rha, SW; Rhew, JY, 2018
)
0.48
" After propensity score with matching, the primary endpoint was major adverse cardiac events (MACE; a composite of all-cause death, myocardial infarction, target lesion revascularization [TLR], and stent thrombosis [ST]), while its components along with target vessel revascularization (TVR) secondary endpoints."( Safety and efficacy of polymer-free biolimus-eluting stents versus ultrathin stents in unprotected left main or coronary bifurcation: A propensity score analysis from the RAIN and CHANCE registries.
Bernardi, A; Capodanno, D; Chieffo, A; Cortese, B; D'Ascenzo, F; D'Urbano, M; De Ferrari, GM; De Luca, L; Di Biasi, M; di Mario, C; Escaned, J; Franzé, A; Gaido, L; Gangor, A; Giammaria, M; Helft, G; Huczek, Z; Ielasi, A; Infantino, V; Latini, RA; Mitomo, S; Piazza, F; Poli, A; Rognoni, A; Romeo, F; Saglietto, A; Sheiban, I; Smolka, G; Trabattoni, D; Ugo, F; Varbella, F, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" BA9 had a terminal half-life of 90."( Randomized, double-blind, placebo-controlled, single intravenous dose-escalation study to evaluate the safety, tolerability, and pharmacokinetics of the novel coronary smooth muscle cell proliferation inhibitor Biolimus A9 in healthy individuals.
Bendrick-Peart, J; Betts, R; Christians, U; Clavijo, C; Dingmann, C; Shulze, J; Steudel, W; Zhang, YL, 2011
)
0.37
"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
)
0.37
" 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
" A significant association between loaded biolimus A9 dose adjusted by patient weight and pharmacokinetic parameters was observed."( Favorable pharmacokinetics of biolimus A9 after deployment of Nobori stent for coronary artery disease: insights from Nobori PK study in Japanese subjects.
Mitsudo, K; Nakamura, M; Otsuka, Y; Ueda, Y, 2012
)
0.38
[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]

Research

Studies (228)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's26 (11.40)29.6817
2010's184 (80.70)24.3611
2020's18 (7.89)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 (%)
Trials97 (41.28%)5.53%
Reviews14 (5.96%)6.00%
Case Studies19 (8.09%)4.05%
Observational20 (8.51%)0.25%
Other85 (36.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (12)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Comparison of the Everolimus Eluting (XIENCE-V®, XIENCE-Prime® or PROMUS® Stent) With the Biolimus A9 Eluting NOBORI® Stent in All-comers: a Randomized Open Label Study [NCT01233453]Phase 42,700 participants (Anticipated)Interventional2009-01-31Active, not recruiting
Randomized Study to Assess the Effect of ThRombus Aspiration on Flow Area in STEMI Patients: an Optical Frequency Domain Imaging (OFDI) Study [NCT01271361]Phase 1/Phase 2140 participants (Actual)Interventional2010-11-30Completed
Assessment of Vessel Healing After DES Implantation With STEMI, NSTEMI and Stable/Unstable Angina Patients: a Randomized Study Between Everolimus and Biolimus A9-eluting Stents: an Optical Coherence Tomography (OCT) and Intravascular Ultrasound Tissue Cha [NCT01065519]64 participants (Actual)Interventional2009-06-30Completed
Percutaneous Treatment of LONG Native Coronary Lesions With Drug-Eluting Stent-V:Everolimus-eluting(PROMUS-ELEMENT) vs. Biolimus A9-Eluting(NOBORI) Stents [NCT01186120]Phase 4500 participants (Actual)Interventional2010-08-31Completed
Clinical Trial of Nobori Versus Uncoated Stents In Acute Myocardial Infarction [NCT01401036]1,537 participants (Actual)Interventional2011-07-31Terminated(stopped due to Insufficient data collection)
Randomized Comparison of Biolimus-Eluting and Everolimus-Eluting Stents With Optical Coherence Tomography Guided Stent Implantation in ST Elevation Myocardial Infarction.A 9-Month Angiographic and Optical Coherence Tomography Follow-up. [NCT00888758]Phase 4400 participants (Anticipated)Interventional2009-05-31Not yet recruiting
Impact of IVUS-guided Chronic Total Occlusion InterVention With DrUg-eluting Stents on Mid-term Angiographic and Clinical Outcomes (CTO-IVUS Study) [NCT01563952]Phase 4400 participants (Anticipated)Interventional2010-10-31Recruiting
OPtical Frequency Domain Imaging vs. INtravascular Ultrasound in Percutaneous Coronary InterventiON (OPINION) [NCT01873027]Phase 3829 participants (Actual)Interventional2013-06-30Completed
OPtical Frequency Domain Imaging vs. INtravascular Ultrasound in Percutaneous Coronary InterventiON - OPINION Imaging [NCT01873222]Phase 3106 participants (Actual)Interventional2013-06-30Completed
A Prospective, Randomized, Non-Inferiority Trial to Determine the Safety and Efficacy of the BA9TM Drug Coated Balloon for the Treatment of In-Stent Restenosis: First-in-Man Trial (REFORM) [NCT04079192]201 participants (Actual)Interventional2020-08-07Active, not recruiting
Comparison of Healing Responses After Treatment of Complex Bifurcation Lesions With the AXXESS Biolimus A9 Eluting Stent Versus Culotte Technique Using Everolimus-eluting Stents: an Optical Coherence Tomography Analysis. [NCT00895791]0 participants (Actual)Interventional2009-06-30Withdrawn(stopped due to major protocol changes: new study submitted)
Evaluation of the Efficacy (QCA) and Safety of the BioFreedom™ Biolimus A9™ CoCr Stent in a Randomised Trial in Patients With CAD [NCT03307213]200 participants (Actual)Interventional2018-06-19Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]