Page last updated: 2024-11-12

er-086526

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Description

eribulin: a halichondrin B derivative that suppresses microtubule growth and acts as an antimitotic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

eribulin : A fully synthetic macrocyclic ketone analogue of marine sponge natural products. Inhibits growth phase of microtubules via tubulin-based antimitotic mechanism, which leads to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage [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]

Cross-References

ID SourceID
PubMed CID11354606
CHEMBL ID1683590
CHEBI ID63587
SCHEMBL ID15783821
MeSH IDM0493225

Synonyms (40)

Synonym
er-086526
nsc-707389
b 1939
eribulin [inn]
unii-lr24g6354g
lr24g6354g ,
er 086526
(1s,3s,6s,9s,12s,14r,16r,18s,20r,21r,22s,26r,29s,31r,32s,35r,36s)-20-[(2s)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-bis(methylene)-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1(3,32).1(3,33).1(6,9).1(12,16).0(18,22).0(29,36).0(31,35)]hentetra
CHEBI:63587 ,
2-(3-amino-2-hydroxypropyl)hexacosahydro-3-methoxy-26-methyl-20,27-bis(methylene)11,15-18,21-24,28-triepoxy-7,9-ethano-12,15-methano-9h,15h-furo(3,2-i)furo(2',3'-5,6)pyrano(4,3-b)(1,4)dioxacyclopentacosin-5-(4h)-one
eribulin
253128-41-5
gtpl6813
CHEMBL1683590
eribulin [who-dd]
eribulin [vandf]
eribulin [mart.]
eribulin [mi]
DB08871
HY-13442
SCHEMBL15783821
(1s,3s,6s,9s,12s,14r,16r,18s,20r,21r,22s,26r,29s,31r,32s,33r,35r,36s)-20-[(2s)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1~3,32~.1~3,33~.1~6,9~.1~12,16~.0~18,22~.0~29,36~.0~31,35~]hente
UFNVPOGXISZXJD-JBQZKEIOSA-N
(1s,3s,6s,9s,12s,14r,16r,18s,20r,21r,22s,26r,29s,31r,32s,33r,35r,36s)-20-[(2s)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-o
e7389-lf
Q408717
NCGC00510497-02
AT36513
MS-31267
DTXSID101009321 ,
(1s,3s,6s,9s,12s,14r,16r,18s,20r,21r,22s,26r,29s,31r,32s,35r,36s)-20-((2s)-3-amino-2-hydroxypropyl)-21-methoxy-14-methyl-8,15-bis(methylene)-2,19,30,34,37,39,40,41-octaoxanonacyclo(24.9.2.1(3,32).1(3,33).1(6,9).1(12,16).0(18,22).0(29,36).0(31,35))hentetra
l01xx41
eribuline
eribulin (mart.)
eribulinum
dtxcid701436148
eribulina
EX-A4873D
BP-29357
AKOS040740784

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The adverse effect profile of eribulin in this trial was similar to that of taxanes; neutropenia and peripheral neuropathy were the most frequent adverse effects."( Eribulin: Heavily pretreated breast cancer: uncertain advantages, excessive adverse effects.
, 2012
)
0.38
" The most frequent adverse events observed in patients receiving eribulin were asthenia/fatigue, neutropenia, alopecia, peripheral neuropathy and nausea."( Effectiveness and safety of eribulin mesylate: a new therapeutic option in the treatment of metastatic breast cancer.
Kelly, CM; O'Sullivan Coyne, G; Walsh, J, 2012
)
0.38
" The proportion reporting at least one adverse event (any grade) with C, G, V, and E was 45%, 65%, 75%, and 63%."( A comparison of toxicity and health care resource use between eribulin, capecitabine, gemcitabine, and vinorelbine in patients with metastatic breast cancer treated in a community oncology setting.
Beegle, N; Blau, S; Cox, D; Dranitsaris, G; Faria, C; Kalberer, T, 2015
)
0.42
" In terms of adverse events(AEs), observed cases of hematotoxicity were of neutropenia(75%), leucopenia(75%), and anemia(80%)."( [Efficacy and safety of eribulin for metastatic breast cancer patients].
Egawa, C; Hamanaka, M; Hashimoto, N; Kato, T; Kawashima, H; Kusama, H; Matsushita, K; Mukai, Y; Nakahira, S; Okishiro, M; Sakisaka, H; Suzuki, R; Takatsuka, Y; Takeda, Y; Takeno, A; Tamura, S; Taniguchi, H, 2014
)
0.4
" No hypersensitivity reactions and no toxic deaths were seen."( A retrospective safety and efficacy analysis of the first patients treated with eribulin for metastatic breast cancer in Stockholm, Sweden.
Bergh, J; Falato, C; Foukakis, T; Kessler, L; Margolin, S, 2015
)
0.42
"Eribulin administered outside of a clinical trial in patients with advanced breast cancer was safe and well tolerated."( A retrospective safety and efficacy analysis of the first patients treated with eribulin for metastatic breast cancer in Stockholm, Sweden.
Bergh, J; Falato, C; Foukakis, T; Kessler, L; Margolin, S, 2015
)
0.42
" Most common grade 3-4 adverse events (AEs) were neutropenia (38%), asthenia (10%) and peripheral neuropathy (7%)."( [Efficacy, safety and cost of eribulin in patients with metastatic breast cancer].
Bazan, F; Chaigneau, L; Curtit, E; Dobi, E; Mansi, L; Meneveau, N; Montcuquet, P; Nerich, V; Paillard, MJ; Pivot, X; Thiery-Vuillemin, A; Villanueva, C, 2015
)
0.42
" Dose delays, reductions, and interruptions due to treatment-emergent adverse events occurred in 35."( Safety and tolerability of eribulin mesylate in patients with pretreated metastatic breast cancer.
Barbour, S; Berrak, E; Cox, D; Goodin, S; Song, J, 2015
)
0.42
"The most frequent grade 3 hematologic adverse events were neutropenia (56%) and anemia (20%)."( Safety of eribulin mesylate and concomitant radiotherapy for metastatic breast cancer: a single-center experience.
Agresti, B; Baldazzi, V; Bernini, M; Bianchi, S; Casella, D; De Luca Cardillo, C; Desideri, I; Detti, B; Di Cataldo, V; Fambrini, M; Francolini, G; Greto, D; Livi, L; Loi, M; Mangoni, M; Meattini, I; Nori, J; Orzalesi, L; Sanchez, LJ; Scotti, V, 2016
)
0.43
" No hypersensitivity reactions and no toxic deaths were observed."( Efficacy and safety of eribulin monotherapy in patients with heavily pretreated metastatic breast cancer.
Akin, S; Aksoy, S; Altundag, K; Ates, O; Babacan, T; Cenoli, A; Karakas, Y; Kertmen, N; Kilickap, S; Ozisik, Y; Sarici, F; Sever, AR,
)
0.13
"Eribulin monotherapy is an effective and safe regimen for MBC patients."( Efficacy and safety of eribulin monotherapy in patients with heavily pretreated metastatic breast cancer.
Akin, S; Aksoy, S; Altundag, K; Ates, O; Babacan, T; Cenoli, A; Karakas, Y; Kertmen, N; Kilickap, S; Ozisik, Y; Sarici, F; Sever, AR,
)
0.13
"6% of adverse eventsBGrade 3; however, the recovery was rapid."( [Treatment Continuation and Safety of Eribulin for the Treatment of Metastatic Breast Cancer].
Adachi, S; Asano, H; Ito, D; Iwai, M; Kamei, K; Okada, K; Usami, E; Yoshimura, T, 2016
)
0.43
" The common grade 3/4 adverse events were neutropenia (25 patients; 53."( Efficacy and safety of eribulin as first- to third-line treatment in patients with advanced or metastatic breast cancer previously treated with anthracyclines and taxanes.
Kai, Y; Kurashita, K; Maeda, S; Mashino, K; Minami, S; Mitsuyama, S; Nishimura, R; Saimura, M; Shimokawa, M; Tamura, K; Yano, H, 2017
)
0.46
" The most experienced adverse event was asthenia/fatigue (58%), followed by neutropenia (30%)."( Efficacy and safety of eribulin in taxane-refractory patients in the 'real world'.
Barni, S; Cinieri, S; Del Mastro, L; Latorre, A; Lorusso, V; Porcu, L; Puglisi, F, 2017
)
0.46
" The most common adverse event was neutropenia, which occurred in 57% of eribulin patients and 49% of TPC patients at all grades."( A randomized, open-label, multicenter, phase 3 study to compare the efficacy and safety of eribulin to treatment of physician's choice in patients with advanced non-small cell lung cancer.
Barlesi, F; Felip, E; Guo, M; Iannotti, N; Katakami, N; Kim, JH; Nokihara, H; Olivo, M; Satouchi, M; Spigel, DR; Yang, JC, 2017
)
0.46
" We compared the relative dose intensity (RDI), tumor response, progression-free survival (PFS), overall survival (OS), and adverse events between the groups."( Efficacy and safety of eribulin in patients with locally advanced or metastatic breast cancer not meeting trial eligibility criteria: a retrospective study.
Bun, S; Fujiwara, Y; Iizumi, S; Kodaira, M; Noguchi, E; Shimizu, C; Shimoi, T; Shimomura, A; Tamura, K; Tsushita, N; Yonemori, K; Yunokawa, M, 2017
)
0.46
" Initial dose reduction and treatment discontinuation due to adverse events (AEs) were more common in the ineligible group (initial dose reduction: 23."( Efficacy and safety of eribulin in patients with locally advanced or metastatic breast cancer not meeting trial eligibility criteria: a retrospective study.
Bun, S; Fujiwara, Y; Iizumi, S; Kodaira, M; Noguchi, E; Shimizu, C; Shimoi, T; Shimomura, A; Tamura, K; Tsushita, N; Yonemori, K; Yunokawa, M, 2017
)
0.46
"6%) experienced an adverse event (AE) related to treatment including 129 (51."( Safety Results and Analysis of Eribulin Efficacy according to Previous Microtubules-Inhibitors Sensitivity in the French Prospective Expanded Access Program for Heavily Pre-treated Metastatic Breast Cancer.
Bertucci, F; Brain, E; Diéras, V; Extra, JM; Gonçalves, A; Monneur, A; Pivot, X; Provansal, M; Roché, H; Sabatier, R; Tarpin, C; Viens, P; Zemmour, C, 2018
)
0.48
" Common grade 3/4 adverse events were neutropenia (42."( A phase II, multicenter, single-arm trial of eribulin as first- or second-line chemotherapy for HER2-negative advanced or metastatic breast cancer: evaluation of efficacy, safety, and patient-reported outcomes.
Fujioka, H; Iwamoto, M; Kawaguchi, K; Kimura, K; Matsunami, N; Morimoto, T; Nitta, T; Ogura, H; Takahashi, Y; Tanaka, S; Terasawa, R; Uchiyama, K; Yamamoto, D; Yoshidome, K, 2018
)
0.48
"Chemotherapy-induced peripheral neuropathy (CIPN) is a severe and common side effect induced by a variety of anticancer drugs."( [Peripheral neuropathy as a side effect of chemotherapy and targeted therapy].
Gießen-Jung, C; von Baumgarten, L, 2018
)
0.48
"Eribulin is active and safe in heavily pre-treated metastatic breast cancer patients."( Safety of eribulin as third-line chemotherapy in HER2-negative, advanced breast cancer pre-treated with taxanes and anthracycline: OnSITE study.
Ballesteros García, A; Borrega García, P; Chacón López-Muñíz, I; Ciruelos Gil, E; Delgado Mingorance, JI; Echarri González, MJ; García-Sáenz, JA; Izarzugaza Perón, Y; López-González, A; Manso, L; Martínez-Jañez, N; Moreno Antón, F; Olier Garate, C; Paz-Ares, L, 2019
)
0.51
"Pneumothorax has been reported as a pazopanib-associated adverse event in patients with lung metastases of soft tissue sarcoma (STS)."( Pneumothorax as an Adverse Event in Patients with Lung Metastasis of Soft Tissue Sarcoma under Eribulin Treatment.
Arihara, Y; Emori, M; Hayasaka, N; Ikeda, H; Iyama, S; Kato, J; Kobune, M; Miyanishi, K; Murase, K; Nakamura, H; Nakamura, K; Sugita, S; Takada, K, 2019
)
0.51
" However, soon after their introduction into clinical practice, chemotherapy-induced peripheral neurotoxicity (CIPN) emerged as their main non-hematological and among dose-limiting adverse events."( Vinca alkaloids, thalidomide and eribulin-induced peripheral neurotoxicity: From pathogenesis to treatment.
Alberti, P; Argyriou, AA; Islam, B; Kolb, N; Lustberg, M; Staff, NP, 2019
)
0.51
" Neutropenia was the most common grade 3/4 clinical adverse event (16."( Eribulin plus trastuzumab in pretreated HER2-positive advanced breast cancer patients: safety and efficacy. An Italian experience.
Bilancia, D; Caliolo, C; Calvani, N; Cinieri, S; Dima, G; Febbraro, A; Fedele, P; Ferrara, P; Filippelli, G; Fontanella, C; Giampaglia, M; Giordano, G; Lutrino, ES; Marino, A; Orlando, L; Quaranta, AM; Rubino, D; Scavelli, C; Schiavone, P; Zamagni, C, 2020
)
0.56
" Grade ≥ 3 adverse drug reactions (ADRs) were reported in 61."( Effectiveness and safety of eribulin in Japanese patients with HER2-negative, advanced breast cancer: a 2-year post-marketing observational study in a real-world setting.
Egawa, C; Ikezawa, H; Inoue, K; Matsuoka, T; Mukai, H; Sakata, Y; Takahashi, M; Tsurutani, J; Yamanaka, T, 2020
)
0.56
"Adverse events (AE) during oncology clinical trials are typically reported using the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE), which provides information about the frequency and severity of AEs from the provider's perspective."( A dynamic portrait of adverse events for breast cancer patients: results from a phase II clinical trial of eribulin in advanced HER2-negative breast cancer.
Burstein, HJ; Come, S; Constantine, M; Faggen, M; Filho, OM; Freedman, RA; Giobbie-Hurder, A; Lin, NU; Mayer, EL; Openshaw, T; Schneider, B; Walsh, J, 2021
)
0.62
" The only grade ≥3 clinical adverse events in >5% of patients were hypertension (39%), neutropenia (26%), thrombosis (10%), and paresthesia/dysesthesia (7%)."( First-line bevacizumab and eribulin combination therapy for HER2-negative metastatic breast cancer: Efficacy and safety in the GINECO phase II ESMERALDA study.
Brocard, F; Clatot, F; Despax, R; Emile, G; Ferrero, JM; Grenier, J; Hardy-Bessard, AC; Lortholary, A; Lucas, B; Marti, A; Martin-Babau, J; Meunier, J; Moullet, I; Savoye, AM; You, B, 2020
)
0.56
" The most common adverse events were grade 1-2 anemia (n=12, 33%), neutropenia (n=12, 33%) and grade 3-4 neuropathy (n=4, 11."( Efficacy and safety evaluation of eribulin-trastuzumab combination therapy with heavily pretreated HER2-positive metastatic breast cancer.
Altundag, K; Sarici, F,
)
0.13
"Eribulin-trastuzumab combination is an effective and safe treatment option with a low toxicity profile for aggressively pre-treated patients with metastatic breast cancer."( Efficacy and safety evaluation of eribulin-trastuzumab combination therapy with heavily pretreated HER2-positive metastatic breast cancer.
Altundag, K; Sarici, F,
)
0.13
" Primary effectiveness and safety outcomes were overall survival (OS) and adverse events (AE), respectively."( Comparative effectiveness and safety of eribulin in advanced or metastatic breast cancer: a systematic review and meta-analysis.
Johnson, BS; Qian, J; Tanni, KA; Truong, CB, 2021
)
0.62
" Progression- free survival(PFS)and the efficacy of eribulin, influencing factors, and adverse reactions were analysed."( Treatment Strategy and Safety of Eribulin in Advanced Breast Cancer.
Liu, S; Wang, X; Xue, Y, 2022
)
0.72
" However, severe adverse effects (SAEs) occur in 30-40% of the patients, and significantly reduce the patients' quality of life and disturb the recommended treatment schedules."( Risk Factor Analysis for the Occurrence of Severe Adverse Effects in Eribulin Treatment.
Dosaka-Akita, H; Kinoshita, I; Noguchi, T; Saito, Y; Shimizu, Y; Sugawara, M; Takekuma, Y; Takeshita, T; Takeuchi, S, 2022
)
0.72
" Progression-free survival (PFS), overall survival (OS), objective response rate (ORR), disease control rate (DCR), adverse effects (AEs) and health-related quality of life (HRQoL) were assessed."( Effectiveness, safety, and impact on quality of life of eribulin-based therapy in heavily pretreated patients with metastatic breast cancer: A real-world analysis.
Gui, X; Li, H; Liang, X, 2023
)
0.91
" The most common grade 3-4 adverse events were neutropenia (22."( Effectiveness, safety, and impact on quality of life of eribulin-based therapy in heavily pretreated patients with metastatic breast cancer: A real-world analysis.
Gui, X; Li, H; Liang, X, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
"Eribulin (E7389), a mechanistically unique microtubule inhibitor in phase III clinical trials for cancer, exhibits superior efficacy in vivo relative to the more potent compound ER-076349, a fact not explained by different pharmacokinetic properties."( Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions.
Aalfs, KK; Kishi, Y; Lewis, BM; Littlefield, BA; Salvato, KA; Seletsky, BM; Towle, MJ; Wels, BF; Yu, MJ; Zheng, W; Zhu, X, 2011
)
0.37
" Pharmacokinetic sampling for determination of eribulin plasma concentration was performed up to 144 h following administration of eribulin mesylate."( Eribulin mesylate pharmacokinetics in patients with solid tumors receiving repeated oral ketoconazole.
Beijnen, JH; Copalu, W; Devriese, LA; Edwards, G; Jenner, A; Marchetti, S; Mergui-Roelvink, M; Peng, F; Reyderman, L; Schellens, JH; Wanders, J, 2013
)
0.39
" Pharmacokinetic sampling for determination of eribulin plasma concentrations was performed up to 144 h following administration."( Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin.
Beijnen, JH; Copalu, W; Devriese, LA; Edwards, G; Huitema, AD; Law, K; Marchetti, S; Peng, F; Reyderman, L; Schellens, JH; Voest, EE; Wanders, J; Witteveen, PE, 2013
)
0.39
"Fourteen patients were included and 11 patients were evaluable for pharmacokinetic analysis."( Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin.
Beijnen, JH; Copalu, W; Devriese, LA; Edwards, G; Huitema, AD; Law, K; Marchetti, S; Peng, F; Reyderman, L; Schellens, JH; Voest, EE; Wanders, J; Witteveen, PE, 2013
)
0.39
"A phase I, pharmacokinetic study was performed in patients with advanced solid tumors and normal hepatic function or Child-Pugh A (mild) or Child-Pugh B (moderate) hepatic impairment."( Pharmacokinetics of eribulin mesylate in patients with solid tumors and hepatic impairment.
Beijnen, JH; Devriese, LA; Edwards, G; Jenner, A; Marchetti, S; Mergui-Roelvink, M; Reyderman, L; Schellens, JH; Voest, EE; Wanders, J; Witteveen, PO, 2012
)
0.38
" The relationship between eribulin pharmacokinetic and neutropenia was described using a semi-physiological lifespan model for haematological toxicity."( Population pharmacokinetic-pharmacodynamic analysis for eribulin mesilate-associated neutropenia.
Beijnen, JH; Gupta, A; Huitema, AD; Hussein, Z; Schellens, JH; van Hasselt, JG, 2013
)
0.39
" To investigate its resistance mechanisms, we developed a fluorescent analog of eribulin with pharmacokinetic (PK) properties and cytotoxic activity across a human cell line panel that are sufficiently similar to the parent drug to study its cellular PK and tissue distribution."( Single-cell pharmacokinetic imaging reveals a therapeutic strategy to overcome drug resistance to the microtubule inhibitor eribulin.
Kim, E; Kohler, RH; Laughney, AM; Miller, MA; Mitchison, TJ; Orth, JD; Sprachman, MM; Weissleder, R; Yang, KS, 2014
)
0.4
" Changes in neutrophil counts over time were analyzed using a mechanistic pharmacodynamic model."( Pharmacodynamic analysis of eribulin safety in breast cancer patients using real-world postmarketing surveillance data.
Fermanelli, V; Ishii, M; Kasai, H; Kawamura, T; Matsuoka, T; Sakata, Y; Takahashi, T; Tanigawara, Y, 2018
)
0.48
" In conclusion, a robust method for released and total eribulin levels in dog plasma was developed and was successfully applied to a pharmacokinetic study in dogs to characterize the pharmacokinetic profiles."( A separate assay of released and liposomal encapsulated eribulin in dog plasma by liquid chromatography with tandem mass spectrometry for its application to a pharmacokinetic study.
Mano, Y, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" This phase I study aimed to determine the maximum tolerated dose (MTD), dose-limiting toxicities (DLTs), and pharmacokinetics in combination with cisplatin (CP) in patients with advanced solid tumours."( Phase I study of the halichondrin B analogue eribulin mesylate in combination with cisplatin in advanced solid tumors.
Carroll, MI; Chung, VM; Cristea, MC; Doyle, LA; El-Khoueiry, AB; Frankel, PH; Gandara, DR; Koczywas, M; Lau, DH; Lenz, HJ; Lim, D; Mortimer, JE; Newman, EM; Reckamp, KL; Ruel, C; Synold, TW, 2014
)
0.4
" Eribulin mesylate was administered on days 1, 8, and 15 in combination with CP day 1 every 28-day cycle."( Phase I study of the halichondrin B analogue eribulin mesylate in combination with cisplatin in advanced solid tumors.
Carroll, MI; Chung, VM; Cristea, MC; Doyle, LA; El-Khoueiry, AB; Frankel, PH; Gandara, DR; Koczywas, M; Lau, DH; Lenz, HJ; Lim, D; Mortimer, JE; Newman, EM; Reckamp, KL; Ruel, C; Synold, TW, 2014
)
0.4
"2 mg m(-2), administered on days 1 and 8, in combination with CP 75 mg m(-2), administered on day 1 is well tolerated and showed preliminary anticancer activity."( Phase I study of the halichondrin B analogue eribulin mesylate in combination with cisplatin in advanced solid tumors.
Carroll, MI; Chung, VM; Cristea, MC; Doyle, LA; El-Khoueiry, AB; Frankel, PH; Gandara, DR; Koczywas, M; Lau, DH; Lenz, HJ; Lim, D; Mortimer, JE; Newman, EM; Reckamp, KL; Ruel, C; Synold, TW, 2014
)
0.4
" Fifteen patients were enrolled in a dose escalation of eribulin mesylate in combination with pemetrexed (E+P)."( An open-label, multicenter, randomized phase Ib/II study of eribulin mesylate administered in combination with pemetrexed versus pemetrexed alone as second-line therapy in patients with advanced nonsquamous non-small-cell lung cancer.
Bondarenko, I; Dave, H; Freeman, A; Hodge, JP; Huber, B; Lieberman, R; Shelton, MJ; Shparyk, Y; Vynnychenko, I; Waller, CF, 2015
)
0.42
"4 mg/m(2) intravenously on days 1 and 8 of each cycle) combined with capecitabine (900 mg/m(2) orally twice daily on days 1-14 of each cycle [standard schedule] or 1500 mg orally twice daily using a 7-days on/7-days off schedule [weekly schedule])."( Phase II, Multicenter, Single-Arm, Feasibility Study of Eribulin Combined With Capecitabine for Adjuvant Treatment in Estrogen Receptor-Positive, Early-Stage Breast Cancer.
Berrak, E; Hoffman, AD; Jones, VE; McIntyre, K; O'Shaughnessy, J; Smith, JW; Song, JX; Vukelja, S, 2016
)
0.43
"The VERITAS (A Phase 1B open-label study to assess the safety and tolerability of everolimus in combination with eribulin in triple-negative breast cancers) trial (EudraCT number: 2014-000135-17) is a phase Ib, open label, multicenter, dose-escalation, safety, pharmacokinetic, and pharmacodynamic study based on the combination of everolimus with eribulin in sequential cohorts of metastatic triple negative breast cancer (TNBC) patients."( A Phase Ib Open-Label Study to Assess the Safety and Tolerability of Everolimus in Combination With Eribulin in Triple-Negative Breast Cancers.
Bottini, A; Cappelletti, MR; Generali, D; Gobbi, A; Milani, M; Roviello, G; Senti, C; Sigala, S; Strina, C; Zanotti, L, 2016
)
0.43
"The primary objective of the study is to identify the recommended dose of everolimus in combination with eribulin."( A Phase Ib Open-Label Study to Assess the Safety and Tolerability of Everolimus in Combination With Eribulin in Triple-Negative Breast Cancers.
Bottini, A; Cappelletti, MR; Generali, D; Gobbi, A; Milani, M; Roviello, G; Senti, C; Sigala, S; Strina, C; Zanotti, L, 2016
)
0.43
"The VERITAS trial is expected to determine the recommended dose of everolimus in combination with eribulin in TBNC."( A Phase Ib Open-Label Study to Assess the Safety and Tolerability of Everolimus in Combination With Eribulin in Triple-Negative Breast Cancers.
Bottini, A; Cappelletti, MR; Generali, D; Gobbi, A; Milani, M; Roviello, G; Senti, C; Sigala, S; Strina, C; Zanotti, L, 2016
)
0.43
" This study investigated eribulin in combination with pertuzumab and trastuzumab for both taxane- and trastuzumab-pretreated HER2-positive ABC patients."( First report of eribulin in combination with pertuzumab and trastuzumab for advanced HER2-positive breast cancer.
Akiyama, F; Araki, K; Fukada, I; Horii, R; Ito, Y; Kobayashi, K; Ohno, S; Shibayama, T; Takahashi, S; Yanagi, H, 2017
)
0.46
"In a single-institute, single-arm, open-label, phase II trial, HER2-positive ABC patients who had previously received taxanes and trastuzumab were treated with eribulin in combination with pertuzumab and trastuzumab."( First report of eribulin in combination with pertuzumab and trastuzumab for advanced HER2-positive breast cancer.
Akiyama, F; Araki, K; Fukada, I; Horii, R; Ito, Y; Kobayashi, K; Ohno, S; Shibayama, T; Takahashi, S; Yanagi, H, 2017
)
0.46
"Eribulin in combination with pertuzumab and trastuzumab was well tolerated in heavily pretreated patients."( First report of eribulin in combination with pertuzumab and trastuzumab for advanced HER2-positive breast cancer.
Akiyama, F; Araki, K; Fukada, I; Horii, R; Ito, Y; Kobayashi, K; Ohno, S; Shibayama, T; Takahashi, S; Yanagi, H, 2017
)
0.46
" No significant increase in mean QTcF duration was observed with eribulin plus sorafenib versus eribulin alone; there were no drug-drug interactions."( Phase 1, open-label, dose-escalation study of sorafenib in combination with eribulin in patients with advanced, metastatic, or refractory solid tumors.
Eucker, J; Gomez-Roca, C; Graudenz, K; Huang, F; Lettieri, J; Marmé, F; Peña, C; Trnkova, ZJ, 2018
)
0.48
" Here, eribulin in combination with mechanistically different anticancer agents was evaluated."( Broad-spectrum Preclinical Antitumor Activity of Eribulin (Halaven®): Combination with Anticancer Agents of Differing Mechanisms.
Asano, M; DE Boisferon, MH; Littlefield, BA; Matsui, J; McGonigle, S; Nomoto, K; Towle, MJ; Uenaka, T; Wu, J, 2018
)
0.48
"Eribulin was combined with cytotoxic agents (capecitabine, carboplatin, cisplatin, doxorubicin, gemcitabine) or targeted agents (bevacizumab, BKM-120, E7449, erlotinib, everolimus, lenvatinib, palbociclib) in tumor xenograft models of breast cancer, melanoma, non-small cell lung cancer (NSCLC), and ovarian cancer."( Broad-spectrum Preclinical Antitumor Activity of Eribulin (Halaven®): Combination with Anticancer Agents of Differing Mechanisms.
Asano, M; DE Boisferon, MH; Littlefield, BA; Matsui, J; McGonigle, S; Nomoto, K; Towle, MJ; Uenaka, T; Wu, J, 2018
)
0.48
" Therefore, this study attempted to demonstrate the in vitro anti-cancer activity of high-dose vitamin C in combination with conventional treatment in breast cancer."( Effect of High-dose Vitamin C Combined With Anti-cancer Treatment on Breast Cancer Cells.
Chae, YS; Jeong, JH; Jung, JH; Lee, DH; Lee, IH; Lee, J; Lee, SJ; Park, HY, 2019
)
0.51
"This phase 1b study investigated the maximum tolerated dose (MTD; primary objective), safety, pharmacokinetics, and antitumor activity (secondary objectives) of eribulin combined with carboplatin in patients with solid tumors and, in particular, non-small cell lung cancer (NSCLC)."( A phase 1b, multicenter, open-label, dose-finding study of eribulin in combination with carboplatin in advanced solid tumors and non-small cell lung cancer.
Aisner, J; Dittrich, C; Goel, S; Jain, M; Kumar, K; Petrylak, DP; Reyderman, L; Song, J; Swami, U, 2019
)
0.51
"Vincristine combined with camptothecin derivatives showed synergy in preclinical pediatric cancer models, and the combinations are effective in treatment of childhood solid tumors."( Evaluation of Eribulin Combined with Irinotecan for Treatment of Pediatric Cancer Xenografts.
Bandyopadhyay, A; Chen, Y; Erickson, SW; Houghton, PJ; Kurmashev, D; Kurmasheva, RT; Lai, Z; Phelps, DA; Robles, AJ; Smith, MA, 2020
)
0.56
"Vincristine or eribulin, alone or combined with irinotecan, was studied in 12 xenograft models."( Evaluation of Eribulin Combined with Irinotecan for Treatment of Pediatric Cancer Xenografts.
Bandyopadhyay, A; Chen, Y; Erickson, SW; Houghton, PJ; Kurmashev, D; Kurmasheva, RT; Lai, Z; Phelps, DA; Robles, AJ; Smith, MA, 2020
)
0.56
"Eribulin combined with irinotecan was more effective than vincristine-irinotecan in 6 of 12 models."( Evaluation of Eribulin Combined with Irinotecan for Treatment of Pediatric Cancer Xenografts.
Bandyopadhyay, A; Chen, Y; Erickson, SW; Houghton, PJ; Kurmashev, D; Kurmasheva, RT; Lai, Z; Phelps, DA; Robles, AJ; Smith, MA, 2020
)
0.56
"The results of this study suggest that second-line therapy with bevacizumab in combination with eribulin has a meaningful clinical activity and may represent a potential therapeutic option for patients with HER2-negative MBC."( Eribulin in combination with bevacizumab as second-line treatment for HER2-negative metastatic breast cancer progressing after first-line therapy with paclitaxel and bevacizumab: a multicenter, phase II, single arm trial (GIM11-BERGI).
Arpino, G; Baldini, E; Bernardo, A; Bruzzese, D; De Angelis, C; De Laurentiis, M; De Placido, P; De Placido, S; De Santo, I; Del Mastro, L; Fabi, A; Forestieri, V; Gamucci, T; Giuliano, M; Lauria, R; Leo, L; Michelotti, A; Poggio, F; Russo, S, 2021
)
0.62
" This is the first published case of repeat locoregional radiation therapy in combination with eribulin."( Eribulin combined with radiation therapy in a young patient re-irradiated for a new lesion of breast cancer.
Dieng, O; Kirova, YM; Laurence, V; Logerot, C, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
" The oral bioavailability of eribulin was 62."( Interactions between the chemotherapeutic agent eribulin mesylate (E7389) and P-glycoprotein in CF-1 abcb1a-deficient mice and Caco-2 cells.
DesJardins, CS; Schuck, EL; Taur, JS; Wong, YN, 2011
)
0.37
" We targeted oral bioavailability and efficacy against multidrug resistant (MDR) tumors for further work."( Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
Carlson, EM; Cheng, H; Condon, K; Du, H; Eckley, S; Hu, Y; Jiang, Y; Kumar, V; Lewis, BM; Littlefield, BA; Narayan, S; Saxton, P; Schuck, E; Seletsky, BM; Tendyke, K; Towle, MJ; Yu, MJ; Zhang, H; Zheng, W, 2011
)
0.37

Dosage Studied

ExcerptRelevanceReference
"Eribulin demonstrated activity with manageable tolerability (including infrequent grade 3 and no grade 4 neuropathy) in heavily pretreated patients with MBC when dosed as a short IV infusion on days 1 and 8 of a 21-day cycle."( Phase II study of eribulin mesylate, a halichondrin B analog, in patients with metastatic breast cancer previously treated with an anthracycline and a taxane.
Ashworth, S; Blum, JL; Chandrawansa, K; Chuang, E; Cole, PE; Dacosta, NA; Fabian, CJ; Fang, F; Meneses, NL; O'Shaughnessy, J; Pruitt, B; Rivera, RR; Shuster, DE; Smith, DA; Smith, J; Tan, AR; Tan-Chiu, E; Vahdat, LT; Wright, J, 2009
)
0.35
" More broadly, our results suggest that compound-specific reversibility characteristics of antimitotic agents contribute to interactions between cell-based pharmacodynamics and in vivo pharmacokinetics that define antitumor efficacy under intermittent dosing conditions."( Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions.
Aalfs, KK; Kishi, Y; Lewis, BM; Littlefield, BA; Salvato, KA; Seletsky, BM; Towle, MJ; Wels, BF; Yu, MJ; Zheng, W; Zhu, X, 2011
)
0.37
" To assess tolerability of a second dosing schedule, a cohort of taxane-pre-treated patients received eribulin on days 1 and 8 of a 21-day cycle."( A phase II study of eribulin mesylate (E7389) in patients with advanced, previously treated non-small-cell lung cancer.
Cole, PE; Das, A; Gabrail, NY; Iannotti, NO; Neubauer, M; Savin, MA; Shuster, D; Spira, AI; Yanagihara, RH; Zang, EA, 2012
)
0.38
" Here we extend those early studies by examining the effects of eribulin against a wider spectrum of human tumor xenografts in vivo, and by directly comparing the in vivo effectiveness of different dosing administration schedules."( Broad spectrum preclinical antitumor activity of eribulin (Halaven(R)): optimal effectiveness under intermittent dosing conditions.
Asano, M; Kishi, Y; Littlefield, BA; Nomoto, K; Towle, MJ; Yu, MJ, 2012
)
0.38
" Administration schedule dependence was evaluated by directly comparing q1d×5, q2d×3(×3), q4d×3, and q7d×3 schedules in the MDA-MB-435 breast cancer xenograft model, using conditions of equivalent total dosing over the course of the experiment."( Broad spectrum preclinical antitumor activity of eribulin (Halaven(R)): optimal effectiveness under intermittent dosing conditions.
Asano, M; Kishi, Y; Littlefield, BA; Nomoto, K; Towle, MJ; Yu, MJ, 2012
)
0.38
" In vivo antitumor responses at these dosing levels included tumor growth inhibition, stasis, and regression; several studies showing regression also yielded long-term tumor-free survivors."( Broad spectrum preclinical antitumor activity of eribulin (Halaven(R)): optimal effectiveness under intermittent dosing conditions.
Asano, M; Kishi, Y; Littlefield, BA; Nomoto, K; Towle, MJ; Yu, MJ, 2012
)
0.38
"The current results show that eribulin has broad spectrum preclinical antitumor activity against a wide variety of human cancer types, and indicate that maximum effectiveness and optimal tolerability are obtained using moderately intermittent dosing schedules."( Broad spectrum preclinical antitumor activity of eribulin (Halaven(R)): optimal effectiveness under intermittent dosing conditions.
Asano, M; Kishi, Y; Littlefield, BA; Nomoto, K; Towle, MJ; Yu, MJ, 2012
)
0.38
" The pharmacokinetics of the free E7389 after dosing either E7389 or E7389-LF was characterized."( Characterization of the pharmacokinetics of a liposomal formulation of eribulin mesylate (E7389) in mice.
Desjardins, C; Lai, G; Saxton, P; Schuck, E; Wong, YN; Yu, Y, 2013
)
0.39
"001) versus vehicle when measured 24 h or 2 weeks after dosing cessation, respectively."( Neuropathy-inducing effects of eribulin mesylate versus paclitaxel in mice with preexisting neuropathy.
Farah, MH; Littlefield, BA; Nomoto, K; Slusher, BS; Wozniak, KM; Wu, Y, 2013
)
0.39
"During phase Ib, E+P was tolerated only at a markedly lower dosing intensity relative to the eribulin monotherapy regimen approved for breast cancer and used in phase II studies of NSCLC."( An open-label, multicenter, randomized phase Ib/II study of eribulin mesylate administered in combination with pemetrexed versus pemetrexed alone as second-line therapy in patients with advanced nonsquamous non-small-cell lung cancer.
Bondarenko, I; Dave, H; Freeman, A; Hodge, JP; Huber, B; Lieberman, R; Shelton, MJ; Shparyk, Y; Vynnychenko, I; Waller, CF, 2015
)
0.42
" Hypothesizing that POL5551 may mobilize tumor cells from their microenvironment and sensitize them to chemotherapy, we used a "chemotherapy framing" dosing strategy."( CXCR4 Protein Epitope Mimetic Antagonist POL5551 Disrupts Metastasis and Enhances Chemotherapy Effect in Triple-Negative Breast Cancer.
Ademuyiwa, FO; Aft, RL; Amend, SR; Bauer, M; Chevalier, E; Dembowsky, K; Douglas, GJ; Esser, AK; Fontana, F; Hurchla, MA; Luker, GD; Luker, KE; Mudalagiriyappa, C; Pluard, T; Romagnoli, B; Su, X; Tuffin, G; Weilbaecher, KN; Xiang, J; Zimmermann, J, 2015
)
0.42
"9%) for eribulin than for capecitabine using the standard dosing schedule."( Phase II, Multicenter, Single-Arm, Feasibility Study of Eribulin Combined With Capecitabine for Adjuvant Treatment in Estrogen Receptor-Positive, Early-Stage Breast Cancer.
Berrak, E; Hoffman, AD; Jones, VE; McIntyre, K; O'Shaughnessy, J; Smith, JW; Song, JX; Vukelja, S, 2016
)
0.43
"Eribulin plus capecitabine with standard or weekly dosing schedules is feasible in patients with early-stage, HER2-negative, ER-positive breast cancer."( Phase II, Multicenter, Single-Arm, Feasibility Study of Eribulin Combined With Capecitabine for Adjuvant Treatment in Estrogen Receptor-Positive, Early-Stage Breast Cancer.
Berrak, E; Hoffman, AD; Jones, VE; McIntyre, K; O'Shaughnessy, J; Smith, JW; Song, JX; Vukelja, S, 2016
)
0.43
" Therefore, we retrospectively investigated the optimal approach for Eri dose adjustment and/or dosage interval adjustment."( Dose Reduction versus Dose-interval Prolongation in Eribulin Mesilate Monotherapy in Patients with Metastatic Breast Cancer: A Retrospective Comparative Study.
Ban, A; Hisada, T; Itakura, Y; Katsuragawa, K; Mishima, E; Mizutani, M; Nagamatsu, H; Oshima, Y; Sasaki, T; Tsukiyama, I; Yoshioka, Y, 2016
)
0.43
" Consistent with the acute dosing study, both drugs persisted in peripheral nervous tissues for weeks, in contrast to their rapid clearance from plasma."( Sustained Accumulation of Microtubule-Binding Chemotherapy Drugs in the Peripheral Nervous System: Correlations with Time Course and Neurotoxic Severity.
DesJardins, C; Lai, G; Littlefield, BA; Nomoto, K; Reyderman, L; Slusher, BS; Vornov, JJ; Wong, N; Wozniak, KM; Wu, Y; Yu, Y, 2016
)
0.43
"Current evidence suggests that a triweekly schedule of ixabepilone is more effective than weekly dosing in improving ORR."( Systematic review of ixabepilone for treating metastatic breast cancer.
Li, J; Ren, J; Sun, W, 2017
)
0.46
" A modified biweekly dosing schedule of eribulin was assessed for efficacy as well as improvements in hematologic toxicity."( Phase II Study of Eribulin Mesylate Administered Biweekly in Patients With Human Epidermal Growth Factor Receptor-2-negative Metastatic Breast Cancer.
Almonte, A; He, Y; Irwin, A; Jensen, L; Misir, S; O'Shaughnessy, J; Olivo, M; Smith, J; Tedesco, K; Xie, R; Zhu, W, 2020
)
0.56
" The drug effect score (DES) was calculated from the dose-response of each drug for comparison among drugs or samples."( Aurora B kinase as a therapeutic target in acute lymphoblastic leukemia.
Goto, H; Goto, S; Hamanoue, S; Inukai, T; Ito, M; Iwasaki, F; Keino, D; Kumamoto, T; Miyagawa, N; Nagai, J; Sakurai, Y; Shiomi, M; Yokosuka, T; Yoshino, Y, 2020
)
0.56
" We demonstrate steep dose-response for eribulin in osteosarcoma PDX models, implying that any deviation from achievement of effective concentrations may have a significant impact on activity."( Dose-response effect of eribulin in preclinical models of osteosarcoma by the pediatric preclinical testing consortium.
Erickson, S; Gatto, G; Gill, J; Gorlick, R; Harrison, DJ; Houghton, P; Kolb, EA; Kurmasheva, R; Roth, M; Rowshan, S; Smith, MA; Teicher, B; Zhang, W; Zhang, Z, 2020
)
0.56
" In populations such as patients with metastatic breast cancer, in which metastatic infiltration is the predominant cause of hepatic impairment, using Child-Pugh score may be problematic; in clinical practice, it has been more common for oncologists to make dosing decisions based on LFTs."( Eribulin, Child-Pugh score, and liver-function tests: lessons from pivotal breast cancer studies 301 and 305.
He, Y; Macpherson, IR; Palmieri, C, 2021
)
0.62
" Further investigations are required to establish appropriate dosage and clinical utility of MORAb-202."( First-in-Human Phase 1 Study of MORAb-202, an Antibody-Drug Conjugate Comprising Farletuzumab Linked to Eribulin Mesylate, in Patients with Folate Receptor-α-Positive Advanced Solid Tumors.
Fujiwara, Y; Furuuchi, K; Ikezawa, H; Koyama, T; Miura, T; Nakajima, R; Nomoto, M; Sato, J; Shimizu, T; Shimomura, A; Tamura, K; Yamamoto, N; Yonemori, K, 2021
)
0.62
"This pharmacokinetic/pharmacodynamic (PK/PD) study was conducted to establish the effect of different G-CSF regimens on neutropenia's incidence for patients treated by eribulin, to propose an optimal G-CSF dosing schedule."( Optimization of G-CSF dosing schedule in patients treated with eribulin: a modeling approach.
Bellio, H; Bonnin, N; Desmoulins, I; Freyer, G; Fumoleau, P; Hennequin, A; Ilie, S; Isambert, N; Ladoire, S; Lorgis, V; Macaire, P; Reda, M; Rederstorff, E; Schmitt, A; Uwer, L; You, B, 2022
)
0.72
" Final model estimates were used to calculate neutropenia's incidence following different G-CSF dosing schedules for 1000 virtual subjects."( Optimization of G-CSF dosing schedule in patients treated with eribulin: a modeling approach.
Bellio, H; Bonnin, N; Desmoulins, I; Freyer, G; Fumoleau, P; Hennequin, A; Ilie, S; Isambert, N; Ladoire, S; Lorgis, V; Macaire, P; Reda, M; Rederstorff, E; Schmitt, A; Uwer, L; You, B, 2022
)
0.72
" Schedule and dosage modifications were common, but toxicity rarely led to treatment discontinuation."( Tolerability of Eribulin and correlation between polymorphisms and neuropathy in an unselected population of female patients with metastatic breast cancer: results of the multicenter, single arm, phase IV PAINTER study.
Bertolini, AS; Bramati, A; Cassano, A; Cavanna, L; Ciccarese, M; Collovà, E; Cretella, E; Damia, G; Fabi, A; Farina, G; Ferraris, E; Garrone, O; Generali, DG; Guffanti, F; La Verde, N; Legramandi, L; Meattini, I; Moretti, A; Nunzi, M; Poletto, E; Romagnoli, E; Rulli, E; Santini, D; Scandurra, G; Torri, V; Vici, P, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
microtubule-destabilising agentAny substance that interacts with tubulin to inhibit polymerisation of microtubules.
[role 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]

Drug Classes (6)

ClassDescription
macrocycleA cyclic compound containing nine or more atoms as part of the cyclic system.
polyetherAny ether that contains more than one ether linkage.
polycyclic ether
cyclic ketone
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
cyclic ketalA ketal in the molecule of which the ketal carbon and one or both oxygen atoms thereon are members of a 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]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID579983Cytotoxicity against human DLD1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579984Cytotoxicity against human HCT15 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579808Cytotoxicity against human IMR90 cells up to 1 uM2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579809Antitumor activity against human LOX cells xenografted in athymic mouse assessed as inhibition of tumor growth at 0.1 mg/kg, iv qd administered 5 days a week for 2 weeks measured up to 2 weeks2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID1204868Toxicity in metastatic breast cancer patient assessed as neuropathy rate2015European journal of medicinal chemistry, Apr-13, Volume: 94Selected hybrid natural products as tubulin modulators.
AID1204870Toxicity in metastatic breast cancer patient assessed as incidence of peripheral neuropathy2015European journal of medicinal chemistry, Apr-13, Volume: 94Selected hybrid natural products as tubulin modulators.
AID579988Clearance in BALB/c mouse at 10 mg/kg, iv2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579985AUC (0 to infinity) in BALB/c mouse at 10 mg/kg2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579980Cytotoxicity against human MES-SA cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID1204869Toxicity in metastatic breast cancer patient assessed as incidence of neuropathy2015European journal of medicinal chemistry, Apr-13, Volume: 94Selected hybrid natural products as tubulin modulators.
AID579986Half life in BALB/c mouse at 10 mg/kg2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579989Oral bioavailability in BALB/c mouse at 10 mg/kg2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579981Cytotoxicity against human MES-SA/Dx5-Rx1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579803Antiproliferative activity against human MES-SA cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579807Antiproliferative activity against human HCT15 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579806Antiproliferative activity against human DLD1 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579804Antiproliferative activity against P-gp overexpressing human MES-SA/Dx5-Rx1 cells assessed as growth inhibition2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579982Fold resistant ratio of IC50 for human MES-SA cells to IC50 for MES-SA/Dx5-Rx1 cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579805Fold resistance, ratio of IC50 for antiproliferative activity for human MES-SA cells to IC50 for antiproliferative activity for P-gp overexpressing human MES-SA/Dx5-Rx1cells2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
AID579995Tmax in BALB/c mouse at 10 mg/kg2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID579987Volume of distribution at steady state in BALB/c mouse at 10 mg/kg, iv2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
AID1346118Human tubulin beta class I (Tubulins)2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Novel second generation analogs of eribulin. Part III: Blood-brain barrier permeability and in vivo activity in a brain tumor model.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (545)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's20 (3.67)29.6817
2010's352 (64.59)24.3611
2020's173 (31.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.48

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

MetricThis Compound (vs All)
Research Demand Index9.48 (24.57)
Research Supply Index6.52 (2.92)
Research Growth Index6.00 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials113 (19.93%)5.53%
Reviews67 (11.82%)6.00%
Case Studies74 (13.05%)4.05%
Observational22 (3.88%)0.25%
Other291 (51.32%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]