Page last updated: 2024-12-11

ixabepilone

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Cross-References

ID SourceID
PubMed CID6445540
CHEMBL ID1201752
CHEBI ID63605
CHEBI ID95095
SCHEMBL ID1890345
SCHEMBL ID8386
MeSH IDM0473543

Synonyms (78)

Synonym
HY-10222
AB01273979-01
bms 247550
azaepothilone b
17-oxa-4-azabicyclo(14.1.0)heptadecane-5,9-dione, 7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-((1e)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl)-, (1s,3s,7s,10r,11s,12s,16r)-
ixabepilone [inn]
bms 247550-1
1s,3s,7s,10r,11s,12s,16r)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-((1e)-1-methyl-2-(2-methylthiazol-4-yl)ethenyl)-17-oxa-4-azabicyclo(14.1.0)heptadecane-5,9-dione
ixabepilone (jan/usan/inn)
D04645
219989-84-1
ixempra (tn)
bms-247550
nsc-710428
ixabepilone ,
bms 247550-01
16-aza-epothilone b
ixempra
aza-epothilone b
DB04845
chebi:63605 ,
CHEMBL1201752
bms-247550-01
ixempra (tm)
nsc-747973
nsc747973
7-oxa-4-azabicyclo[14.1.0]heptadecane -5, 7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(1e)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-, (1s,3s,7s,10r,11s,12s,16r)-
SCHEMBL1890345
hsdb 7738
ixabepilone [usan:inn:jan]
k27005np0a ,
unii-k27005np0a
ixempra kit
nsc 747973
ixabepilone [orange book]
ixabepilone [usp monograph]
ixabepilone [who-dd]
ixabepilone [usp-rs]
ixabepilone [vandf]
(1r,5s,6s,7r,10s,14s,16s)-6,10-dihydroxy-1,5,7,9,9-pentamethyl-14-((e)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl)-17-oxa-13-azabicyclo(14.1.0)heptadecane-8,12-dione
ixabepilone [jan]
ixabepilone [mi]
ixabepilone [hsdb]
ixabepilone [usan]
ixabepilone [mart.]
CS-0551
S7930
gtpl6824
(1r,5s,6s,7r,10s,14s,16s)-6,10-dihydroxy-1,5,7,9,9-pentamethyl-14-[(e)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-13-azabicyclo[14.1.0]heptadecane-8,12-dione
SCHEMBL8386
AC-22618
AKOS025401600
EX-A1245
SR-01000941577-1
sr-01000941577
(1s,3s,7s,10r,11s,12s,16r)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(1e)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione
CHEBI:95095
(1r,5s,6s,7r,10s,14s,16s)-6,10-dihydroxy-1,5,7,9,9-pentamethyl-14-[[e]-1-(2-methyl-1,3-thiazol-4-yl]prop-1-en-2-yl)-17-oxa-13-azabicyclo(14,1,0)heptadecane-8,12-dione
J-014409
mfcd04307791
DTXSID70870252 ,
ixabepilone (bms-247550)
Q11711607
(1s,3s,7s,10r,11s,12s,16r)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-((e)-1-(2-methylthiazol-4-yl)prop-1-en-2-yl)-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione
CCG-269752
NCGC00378665-02
GZX ,
(1~{s},3~{s},7~{s},10~{r},11~{s},12~{s},16~{r})-8,8,10,12,16-pentamethyl-3-[(~{e})-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-7,11-bis(oxidanyl)-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione
bdbm50564768
nsc710428
dtxcid90820734
l01dc04
ixabepilone (usp monograph)
epothilone-b bms 247550
ixabepilone (mart.)
ixabepilona
ixabepilonum
ixabepilone (usp-rs)

Research Excerpts

Overview

Ixabepilone is a microtubule stabilizer with activity in taxane-refractory metastatic breast cancer. It is a semi-synthetic analog of epothilone B that binds to the same site on beta tubulin as paclitaxel.

ExcerptReferenceRelevance
"Ixabepilone is a microtubule stabilizer with activity in taxane-refractory metastatic breast cancer and low susceptibility to taxane-resistance mechanisms including multidrug-resistant phenotypes and high β-III tubulin expression. "( TITAN: phase III study of doxorubicin/cyclophosphamide followed by ixabepilone or paclitaxel in early-stage triple-negative breast cancer.
Arrowsmith, ER; Bosserman, LD; Brufsky, A; Bubis, JA; Burris, HA; Bury, M; Daniel, BR; Drosick, DR; Eakle, J; Goble, SA; Gravenor, DS; Hainsworth, JD; Harwin, WN; Inhorn, RC; Keaton, MR; Kudrik, F; Manalo, Y; Pendergrass, K; Priego, VM; Rodriguez, GI; Silver, C; Yardley, DA; Young, RR, 2017
)
2.13
"Ixabepilone is a novel drug for treatment of advanced breast cancer. "( Severe cardiotoxicity associated with ixabepilone use in metastatic breast cancer.
Butler, KH; Hayes, BD; Santiago, MJ, 2013
)
2.1
"Ixabepilone is a tubulin-inhibiting agent with low susceptibility to multiple resistance mechanisms including β3T isoform expression in several tumor models."( Randomized phase II study of ixabepilone or paclitaxel plus carboplatin in patients with non-small-cell lung cancer prospectively stratified by beta-3 tubulin status.
Edelman, MJ; Kaleta, R; Kim, HT; Luft, AV; Mukhopadhyay, P; Quoix, E; Reck, M; Schneider, CP; Trifan, OC; Tsai, CM; Whitaker, L, 2013
)
1.4
"Ixabepilone is an effective chemotherapy in metastatic breast cancer that has been pretreated with anthracyclines and is resistant or refractory to taxanes. "( Dose-dense FEC followed by dose-dense ixabepilone as neoadjuvant treatment for breast cancer patients: a feasibility study.
Barni, S; Bordonaro, R; Bruzzi, P; Carrozza, F; Clavarezza, M; Coati, F; Cognetti, F; Daniele, B; De Matteis, A; De Placido, S; Del Mastro, L; Ferrandina, G; Olmeo, NA; Turazza, M, 2013
)
2.1
"Ixabepilone is a semi-synthetic analog of epothilone B that binds to the same site on beta tubulin as paclitaxel and may be a more potent polymerizer of tubulin."( A Phase II evaluation of ixabepilone (IND #59699, NSC #710428) in the treatment of recurrent or persistent leiomyosarcoma of the uterus: an NRG Oncology/Gynecologic Oncology Group Study.
Blessing, JA; Dizon, DS; Duska, LR; Hanjani, P; Mannel, RS; Rose, PG; Rotmensch, J, 2014
)
1.43
"Ixabepilone is a member of the epothilone class of antineoplastic agents with activity against taxane-resistant tumors, and low susceptibility to common mechanisms of tumor resistance. "( Neoadjuvant Ixabepilone/Carboplatin/Trastuzumab in HER2-Positive Operable Breast Cancer: A Phase II Trial of the Sarah Cannon Research Institute.
Bechhold, RG; Daniel, B; Daniel, D; Eakle, JF; Finney, L; Hainsworth, JD; Yardley, DA; Zubkus, JD, 2015
)
2.24
"Ixabepilone is a microtubule-stabilizing agent approved for metastatic breast cancer. "( Phase II Clinical Trial of Ixabepilone in Metastatic Cervical Carcinoma.
Balasubramaniam, S; Bates, S; Burotto, M; Edgerly, M; Fojo, T; Kotz, H; Poruchynsky, M; Velarde, M; Wilkerson, J, 2015
)
2.16
"Ixabepilone is a well-tolerated and effective drug in MBC at the approved dose. "( Evaluation of the pharmacokinetics of ixabepilone for the treatment of breast cancer.
Chicchinelli, N; D'Alessio, A; De Luca, A; Gallo, M; Maiello, MR; Normanno, N; Pergameno, M; Piccirilli, MS, 2015
)
2.13
"Ixabepilone is a new generation microtubule-stabilizing agent, which has been expected to be more efficacious than conventional taxanes."( Antitumor activity of Cetuximab in combination with Ixabepilone on triple negative breast cancer stem cells.
Chang, JC; Choi, DS; Dobrolecki, L; Ghosh, M; Landis, MD; Liang, DH; Rodriguez, AA; Tanei, T, 2016
)
1.41
"Ixabepilone is an analog of epothilone, a microtubule stabilizer causing mitotic arrest of the cell cycle approved for the treatment of metastatic and locally advanced treatment-resistant breast cancer."( Chemotherapy reaction induced by ixabepilone, a microtubule stabilizing agent, mimicking extramammary Paget's disease in a patient with breast carcinoma.
Fung, MA; Kiuru, M; Millsop, JW; Petukhova, T; Sharon, VR, 2016
)
1.44
"Ixabepilone (Ixempra) is an epothilone B that has demonstrated preclinical activity against a variety of tumor types and has recently been US FDA approved (application for registration ongoing in Europe) as a single agent for the treatment of taxane-refractory metastatic breast cancer, or in combination with capecitabine for patients with advanced breast cancer refractory to anthracyclines and taxanes."( Ixabepilone for the treatment of taxane-refractory breast cancer.
Moulder, SL, 2008
)
2.51
"Ixabepilone is a semisynthetic analogue of epothilone B, a novel microtubule-stabilizing agent. "( The efficacy and safety of ixabepilone monotherapy in the treatment of breast and gynecologic malignancies.
Gupta, D; Mani, S, 2009
)
2.09
"Ixabepilone (BMS247550) is a semisynthetic derivative of the natural product that optimizes the properties observed with epothilone B. "( Ixabepilone: a new active chemotherapy in the treatment of breast cancer.
Bazan, F; Chaigneau, L; Demarchi, M; Pivot, X; Villanueva, C; Vuillemin, AT, 2009
)
3.24
"Ixabepilone is a novel microtubule-stabilizing agent with clinical efficacy in advanced breast cancer, including patients whose disease has progressed on prior anthracyclines and taxanes. "( Proactive management of adverse events maintains the clinical benefit of ixabepilone.
Yardley, DA, 2009
)
2.03
"Ixabepilone is an antineoplastic agent from the epothilone class that was FDA-approved in October 2007 for the treatment of metastatic or locally advanced breast cancer."( Budget impact analysis of ixabepilone used according to FDA approved labeling in treatment-resistant metastatic breast cancer.
Corey-Lisle, P; Ho, J; Todorova, L; Whillans, F; Yuan, Y; Zhang, L,
)
1.15
"Ixabepilone is a novel microtubule-stabilising agent used as monotherapy or in combination with capecitabine to treat taxane- and anthracycline-refractory breast cancer. "( Sensory-motor axonal peripheral neuropathy in an advanced breast cancer patient treated with ixabepilone.
Bosch-Barrera, J; Espinós, J; Gállego Pérez-Larraya, J; Gómez-Ibáñez, A; Iriarte, J, 2009
)
2.02
"Ixabepilone is a member of a novel class of antineoplastic agents, the epothilones, that has demonstrated activity in a number of human solid tumor types and is the first agent in this class to be approved by the Food and Drug Administration (FDA) for the treatment of metastatic or locally advanced breast cancer, that is resistant/refractory to anthracyclines, taxanes, and/or capecitabine."( Identifying subsets of metastatic breast cancer patients likely to benefit from treatment with the epothilone B analog ixabepilone.
Harichand-Herdt, S; O'regan, RM, 2010
)
1.29
"Ixabepilone is a microtubule-stabilizing agent with activity in adult solid tumors and in pediatric tumor xenograft models that are resistant to paclitaxel. "( Phase II trial of ixabepilone administered daily for five days in children and young adults with refractory solid tumors: a report from the children's oncology group.
Adamson, PC; Balis, FM; Blaney, SM; Fox, E; Goodspeed, W; Goodwin, A; Hartley, G; Jacobs, S; Krailo, M; Navid, F; Wexler, L; Widemann, BC, 2010
)
2.14
"Ixabepilone is a semisynthetic epothilone B analogue that is active in taxane-resistant cell lines and has shown activity in patients with refractory breast and ovarian cancer. "( Phase I trial of ixabepilone plus pegylated liposomal doxorubicin in patients with adenocarcinoma of breast or ovary.
Caputo, T; Christos, P; Chuang, E; Cobham, M; Donovan, D; Doyle, A; Goldberg, GL; Kessler, R; Sparano, JA; Vahdat, L; Wiener, N, 2010
)
2.14
"Ixabepilone is an epothilone, a novel class of non-taxane microtubule stabilizing agents. "( A phase I/II trial and pharmacokinetic study of ixabepilone in adult patients with recurrent high-grade gliomas.
Batchelor, T; Carson, KA; Desideri, S; Fisher, J; Grossman, SA; He, X; Lesser, G; Mikkelsen, T; Mikkelson, T; Peereboom, DM; Phuphanich, S; Supko, JG, 2010
)
2.06
"Ixabepilone is a semisynthetic analogue of epothilone B with low susceptibility to multiple mechanisms of tumor-cell resistance."( Ixabepilone plus capecitabine for breast cancer patients with an early metastatic relapse after adjuvant chemotherapy: two clinical trials.
Fornier, M, 2010
)
2.52
"Ixabepilone is an epothilone B analogue with activity in a variety of solid malignancies, including prostate cancer. "( Phase II trial of weekly ixabepilone in men with metastatic castrate-resistant prostate cancer (E3803): a trial of the Eastern Cooperative Oncology Group.
Carducci, M; Chen, YH; Dipaola, R; Liu, G; Wilding, G, 2012
)
2.13
"Ixabepilone is a synthetic analogue of epothilone B approved for the treatment of patients with metastatic or locally advanced breast cancer in combination with capecitabine for cancer resistant to an anthracycline and a taxane, and as monotherapy for cancer resistant or refractory to anthracyclines, taxanes, and capecitabine. "( Managing ixabepilone adverse events with dose reduction.
Valero, V, 2013
)
2.25
"Ixabepilone (BMS-247550) is an epothilone B analog that stabilizes microtubules and has antitumor activity in taxane-refractory patients in phase I studies. "( Phase II clinical trial of ixabepilone (BMS-247550), an epothilone B analog, in metastatic and locally advanced breast cancer.
Berman, AW; Brufsky, A; Fojo, T; Lee, JJ; Low, JA; Mannan, N; Poruchynsky, MS; Steinberg, SM; Swain, SM; Wedam, SB; Yang, SX, 2005
)
2.07
"Ixabepilone, which is an epothilone-B analog, has activity against taxane-resistant cell lines and as first-line therapy for men with hormone-refractory prostate carcinoma (HRPC)."( A retrospective evaluation of second-line chemotherapy response in hormone-refractory prostate carcinoma: second line taxane-based therapy after first-line epothilone-B analog ixabepilone (BMS-247550) therapy.
Galsky, MD; Kelly, WK; Oh, WK; Rohs, NC; Rosenberg, JE; Small, EJ; Weinberg, VK, 2006
)
1.25
"Ixabepilone (BMS-247550) is a semisynthetic analog of epothilone B that has shown antitumor activity both in vitro and in vivo, including taxane-resistant human tumor xenograft models."( Development of novel chemotherapeutic agents to evade the mechanisms of multidrug resistance (MDR).
Lee, JJ; Swain, SM, 2005
)
1.05
"Ixabepilone is a new class of non-taxane microtubule-stabilizing agents. "( Dermatological toxicity of ixabepilone.
Conlin, AK; Vahdat, L,
)
1.87
"Ixabepilone (BMS-247550) is a semi-synthetic, microtubule stabilizing epothilone B analogue which is more potent than taxanes and has displayed activity in taxane-resistant patients. "( Human mass balance study of the novel anticancer agent ixabepilone using accelerator mass spectrometry.
Beijnen, JH; Beumer, JH; Cohen, MB; Duncan, GF; Galbraith, S; Garner, RC; Griffin, T; Schellens, JH, 2007
)
2.03
"Ixabepilone (BMS-247550) is a semi-synthetic analog of epothilone B that has been characterized as a microtubule stabilizing agent with a mechanism of action distinct from taxanes. "( A phase II study of ixabepilone (BMS-247550) in metastatic renal-cell carcinoma.
Colevas, AD; Karrison, T; Manchen, E; Posadas, EM; Stadler, WM; Undevia, S; Vokes, EE; Wade, JL, 2007
)
2.11
"Ixabepilone is an epothilone B analog that binds to microtubules and results in microtubule stabilization and mitotic arrest. "( Phase II trial of ixabepilone, an epothilone B analog, in patients with metastatic breast cancer previously untreated with taxanes.
Berman, AW; Chow, CK; Denduluri, N; Lee, JJ; Low, JA; Steinberg, SM; Swain, SM; Vatas, U; Walshe, JM; Yang, SX, 2007
)
2.12
"Ixabepilone (BMS-247550) is an epothilone analog that optimizes the properties of naturally occurring epothilone B. "( Phase II clinical trial of ixabepilone (BMS-247550), an epothilone B analog, in patients with taxane-resistant metastatic breast cancer.
Baselga, J; Bunnell, CA; Burris, HA; Conté, P; Fornier, M; Fumoleau, P; Guarneri, V; Klimovsky, J; Lebwohl, D; Lluch, A; Martin, M; Poulart, V; Rivera, E; Tabernero, J; Thomas, E; Vahdat, LT; Viens, P, 2007
)
2.08
"Ixabepilone is a rationally designed, semisynthetic analogue of natural epothilone B, which displays reduced susceptibility to a range of common tumor resistance mechanisms."( Ixabepilone, first in a new class of antineoplastic agents: the natural epothilones and their analogues.
Fornier, MN, 2007
)
2.5
"Ixabepilone is a tubulin-polymerizing agent with potential activity in squamous cell carcinoma of the head and neck (SCCHN). "( A randomized phase II study of ixabepilone (BMS-247550) given daily x 5 days every 3 weeks or weekly in patients with metastatic or recurrent squamous cell cancer of the head and neck: an Eastern Cooperative Oncology Group study.
Argiris, A; Axelrod, R; Burtness, BA; Forastiere, AA; Manola, J, 2008
)
2.07
"Ixabepilone is an analogue of natural epothilone B with activity against a wide range of tumor types, including drug-resistant tumors."( Ixabepilone: a novel antineoplastic agent with low susceptibility to multiple tumor resistance mechanisms.
Vahdat, L, 2008
)
2.51
"Ixabepilone is a good CYP3A4 substrate in vitro; however, in humans, it is likely to be cleared by multiple mechanisms. "( The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of ixabepilone: a first in class epothilone B analogue in late-phase clinical development.
André, F; Cohen, M; Cömezoglu, SN; Comprelli, A; Goel, S; Goldberg, G; Horwitz, SB; Humphreys, WG; Iacono, L; Jayabalan, D; Ly, VT; Mani, S; McDaid, H; Perrin, L; Xu, C; Zhang, D, 2008
)
2.02

Effects

Ixabepilone has been approved as monotherapy in patients with metastatic and locally advanced breast cancer refractory to taxanes, anthracyclines, and capecitabine. The drug has also been evaluated in combination with cape citabine in a randomized, phase III trial demonstrating a benefit.

ExcerptReferenceRelevance
"Ixabepilone has demonstrated activity in cancers that have become taxane-resistant as well as those that never had any demonstrable taxane susceptibility."( Profile and potential of ixabepilone in the treatment of pancreatic cancer.
Pishvaian, MJ; Smaglo, BG, 2014
)
1.43
"Ixabepilone has activity in anthracycline/taxanes-resistant breast cancer."( Phase II Randomized Study of Ixabepilone Versus Observation in Patients With Significant Residual Disease After Neoadjuvant Systemic Therapy for HER2-Negative Breast Cancer.
Alvarez, RH; Gonzalez-Angulo, AM; Green, MC; Hortobagyi, GN; Ibrahim, NK; Koenig, KB; Krishnamurthy, S; Lei, X; Litton, JK; Meric-Bernstam, F; Murray, JL; Nair, L; Valero, V, 2015
)
1.43
"Ixabepilone has demonstrated activity in patients with tumors that are estrogen receptor-, progesterone receptor-, and HER2-negative."( Clinical experience with epothilones in patients with breast cancer.
Buzdar, AU, 2008
)
1.07
"Ixabepilone has also been approved as monotherapy in patients with metastatic and locally advanced breast cancer refractory to taxanes, anthracyclines, and capecitabine."( Ixabepilone: a new antimitotic for the treatment of metastatic breast cancer.
Bhushan, S; Walko, CM, 2008
)
2.51
"Ixabepilone has also been evaluated in combination with capecitabine in a randomized, phase III trial demonstrating a benefit for the combination compared with single-agent capecitabine for patients resistant to anthracyclines and taxanes."( Application of epothilones in breast cancer therapy.
Cianfrocca, M, 2008
)
1.07
"Ixabepilone has demonstrated activity in first-, second-, and subsequent-lines of therapy and in different subtypes of patients with advanced disease."( Ixabepilone: a novel microtubule-stabilizing agent for the treatment of metastatic breast cancer.
Goodin, S, 2008
)
2.51
"Ixabepilone has been shown to have preclinical activity in chemotherapy-sensitive and chemotherapy-resistant tumor models, and synergistic antitumor activity with other chemotherapeutic and targeted agents."( Clinical development of ixabepilone and other epothilones in patients with advanced solid tumors.
Davies, A; Lee, J; Rivera, E, 2008
)
1.37
"Ixabepilone has shown antitumour activity in tumour cell lines in vitro and in several animal tumour models, including those that display key mechanisms of resistance to other anticancer agents."( Ixabepilone: in locally advanced or metastatic breast cancer.
Moen, MD, 2009
)
2.52
"Ixabepilone has no meaningful activity in either chemotherapy-naïve (previously untreated) or previously treated patients with metastatic melanoma. "( A phase II trial of the epothilone B analog ixabepilone (BMS-247550) in patients with metastatic melanoma.
Christos, PJ; Doyle, LA; Haas, N; Hamilton, A; Jones, A; Liddell, S; Millward, M; Muggia, FM; Ott, PA; Pavlick, AC; Shore, T, 2010
)
2.06
"Ixabepilone has single-agent activity in these patients and has demonstrated synergy with capecitabine in this setting."( Ixabepilone plus capecitabine for Chinese patients with metastatic breast cancer progressing after anthracycline and taxane treatment.
Fan, Y; Wang, J; Xu, B, 2010
)
2.52
"Ixabepilone has shown promising clinical data in metastatic breast cancer (MBC) and may be particularly valuable in patients showing progression after treatment with standard chemotherapy. "( Ixabepilone: clinical role in metastatic breast cancer.
Denduluri, N; Swain, S, 2011
)
3.25
"Ixabepilone has modest single-agent activity in patients with recurrent chemosensitive aggressive lymphomas."( A phase 2 study of epothilone B analog BMS-247550 (NSC 710428) in patients with relapsed aggressive non-Hodgkin lymphomas.
Churpek, JE; Conner, K; Hagemeister, F; Karrison, T; Kline, J; Pro, B; Smith, SM; van Besien, K; Wade, JL, 2013
)
1.11
"Ixabepilone has demonstrated activity in patients with chemotherapy-naive metastatic HRPC. "( Ixabepilone (epothilone B analogue BMS-247550) is active in chemotherapy-naive patients with hormone-refractory prostate cancer: a Southwest Oncology Group trial S0111.
Colevas, AD; Crawford, ED; Hussain, M; Lara, PN; Petrylak, DP; Sakr, WA; Tangen, CM; Vaishampayan, UN, 2005
)
3.21
"Ixabepilone has demonstrated consistent preclinical activity and seems active against various taxane-sensible and taxane-resistant cell lines, including those with overexpression of multidrug resistance and with mutations in the beta-tubulin gene."( Efficacy and safety of ixabepilone, a novel epothilone analogue.
Dufresne, A; Pivot, X; Villanueva, C, 2007
)
1.37
"Ixabepilone has single-agent activity in these patients and has demonstrated synergy with capecitabine in this setting."( Ixabepilone plus capecitabine for metastatic breast cancer progressing after anthracycline and taxane treatment.
Campone, M; Chan, VF; Chung, HC; de Mendoza, FH; Fein, LE; Gomez, HL; Jassem, J; Klimovsky, JV; Lerzo, GL; Li, RK; Mukhopadhyay, P; Peck, RA; Pivot, XB; Roché, HH; Thomas, ES; Vahdat, LT; Xu, B, 2007
)
2.5
"Ixabepilone has shown promising phase II clinical efficacy and acceptable tolerability in a wide range of cancers, including heavily pretreated and drug-resistant tumors."( Preclinical discovery of ixabepilone, a highly active antineoplastic agent.
Borzilleri, R; Fairchild, CR; Kamath, A; Kramer, R; Lee, FY; Smykla, R; Vite, G, 2008
)
1.37
"Ixabepilone has reduced susceptibility to resistance due to P-gp overexpression, tubulin mutations, and alterations in beta-tubulin isotype expression."( Preclinical efficacy spectrum and pharmacokinetics of ixabepilone.
Fairchild, CR; Johnston, K; Kramer, R; Lee, FY; McGlinchey, K; Menard, K; Peterson, RW; Smykla, R; Vite, G; Wiebesiek, A, 2009
)
1.32
"Ixabepilone has demonstrated efficacy as monotherapy or in combination with capecitabine in anthracycline- and taxane-pretreated/resistant metastatic breast cancer (MBC), and has recently been approved for use in resistant/refractory MBC."( Ixabepilone: a novel antineoplastic agent with low susceptibility to multiple tumor resistance mechanisms.
Vahdat, L, 2008
)
2.51

Actions

Ixabepilone may enhance the antitumor effects of antiangiogenic therapy by direct cytotoxicity and also indirectly via the killing of tumor-associated endothelial cells.

ExcerptReferenceRelevance
"Ixabepilone may enhance the antitumor effects of antiangiogenic therapy by direct cytotoxicity and also indirectly via the killing of tumor-associated endothelial cells. "( Synergistic antitumor activity of ixabepilone (BMS-247550) plus bevacizumab in multiple in vivo tumor models.
Castaneda, S; Covello, KL; Fairchild, CR; Fargnoli, J; Hawken, DR; Kan, D; Kramer, R; Lee, FY; Lewin, A; Ryseck, RP; Wen, ML, 2008
)
2.07
"Ixabepilone can cause tumor regression in some patients with metastatic renal cell carcinoma and could be considered in combination regimens with other therapies."( A phase II clinical trial of ixabepilone (Ixempra; BMS-247550; NSC 710428), an epothilone B analog, in patients with metastatic renal cell carcinoma.
Bates, S; Edgerly, M; Fojo, T; Huang, H; Huff, LM; Kotz, H; Menefee, M; Poruchynsky, M; Zhuang, S, 2010
)
2.09

Treatment

ExcerptReferenceRelevance
"ixabepilone treatment also induced a 2-fold to 25-fold increase in detyrosinated alpha-tubulin levels in 11 of 13 serial biopsies and a 2-fold to 100-fold increase in acetylated alpha-tubulin in 11 of 12 serial biopsies obtained from patients receiving ixabepilone."( Evidence for microtubule target engagement in tumors of patients receiving ixabepilone.
Bates, SE; Fojo, T; Hung, L; Hung, YE; Linehan, WM; Poruchynsky, MS; Robey, RW; Sackett, DL; Zhuang, SH, 2007
)
1.29

Toxicity

The principal dose-limiting adverse events of ixabepilone's standard dose (40 mg/m(2) administered by 3-hour infusion once every 3 weeks) are peripheral neuropathy, neutropenia, and fatigue.

ExcerptReferenceRelevance
" The safety profile of single-agent ixabepilone and combination ixabepilone plus capecitabine therapy is reviewed, outlining the steps to effectively manage and prevent common adverse events."( Proactive management of adverse events maintains the clinical benefit of ixabepilone.
Yardley, DA, 2009
)
0.86
" Adverse events consistent with known toxicities of each agent were observed in the selected trials and related to dose and administration schedule."( Visceral disease in patients with metastatic breast cancer: efficacy and safety of treatment with ixabepilone and other chemotherapeutic agents.
Yardley, DA, 2010
)
0.58
" The principal dose-limiting adverse events (AEs) of ixabepilone's standard dose (40 mg/m(2) administered by 3-hour infusion once every 3 weeks) are peripheral neuropathy, neutropenia, and fatigue."( Managing ixabepilone adverse events with dose reduction.
Valero, V, 2013
)
1.06
" The most commonly reported adverse effects are peripheral neuropathies and hematologic issues such as neutropenia."( Severe cardiotoxicity associated with ixabepilone use in metastatic breast cancer.
Butler, KH; Hayes, BD; Santiago, MJ, 2013
)
0.66
"Clinicians should maintain broad differential diagnoses that include adverse reactions to drugs relatively new to the market."( Severe cardiotoxicity associated with ixabepilone use in metastatic breast cancer.
Butler, KH; Hayes, BD; Santiago, MJ, 2013
)
0.66
" In the ixabepilone plus capecitabine arm, grade 3/4 hematologic adverse events (AEs) were similar in both subgroups except leukopenia and febrile neutropenia, which had a higher incidence in patients aged ≥ 65 years."( Efficacy and safety of ixabepilone plus capecitabine in elderly patients with anthracycline- and taxane-pretreated metastatic breast cancer.
Baselga, J; Bosserman, L; Gómez, H; Li, RK; Mukhopadhyay, P; Sparano, JA; Vahdat, LT; Valero, V; Vrdoljak, E, 2013
)
1.13

Pharmacokinetics

The pharmacokinetic profile of ixabepilone was established in mice and humans. Coadministration of sunitinib with ixapilone on a weekly (but not every 3 week) schedule was associated with a significant increase in the half-life.

ExcerptReferenceRelevance
" These findings validate in vitro pharmacodynamic observations."( Validation of the pharmacodynamics of BMS-247550, an analogue of epothilone B, during a phase I clinical study.
Horwitz, SB; Mani, S; McDaid, HM; Muggia, F; Shen, HJ; Sonnichsen, D, 2002
)
0.31
" The mean terminal half-life of BMS-247550 was 16."( Phase I trial and pharmacokinetic study of BMS-247550, an epothilone B analog, administered intravenously on a daily schedule for five days.
Abraham, J; Agrawal, M; Bakke, S; Balis, FM; Bates, S; Damle, B; Davis, L; Edgerly, M; Fojo, T; Kotz, H; Lebwohl, D; Rutt, A; Sonnichsen, D; Widemann, B, 2003
)
0.32
" The mean pharmacokinetic parameter values during course 1 for clearance, volume of distribution, and apparent terminal elimination half-life at the 40 mg/m(2) (recommended Phase II dose) dose level were 21 liters/h/m(2), 826 liters/m(2), and 35 h (excluding one outlier of 516 h), respectively."( Phase I clinical and pharmacokinetic study of BMS-247550, a novel derivative of epothilone B, in solid tumors.
Cohen, MB; Griffin, T; Hamilton, A; Hochster, H; Horwitz, SB; Khabelle, D; Lebwohl, DE; Liebes, L; Mani, S; McDaid, H; Muggia, F, 2004
)
0.32
" The pharmacokinetic profile of ixabepilone was established in mice and humans."( Preclinical efficacy spectrum and pharmacokinetics of ixabepilone.
Fairchild, CR; Johnston, K; Kramer, R; Lee, FY; McGlinchey, K; Menard, K; Peterson, RW; Smykla, R; Vite, G; Wiebesiek, A, 2009
)
0.88
" 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
" Eligibility criteria, dose levels, definitions of DLT and MTD, and pharmacokinetic sampling times were designed to be as similar as possible to the adult phase I trial of ixabepilone on the same schedule."( Phase I trial and pharmacokinetic study of ixabepilone administered daily for 5 days in children and adolescents with refractory solid tumors.
Balis, FM; Fojo, T; Fox, E; Goodspeed, W; Goodwin, A; Widemann, BC, 2009
)
0.81
"4 L/kg, and half-life was 14 hours."( Phase I trial and pharmacokinetic study of ixabepilone administered daily for 5 days in children and adolescents with refractory solid tumors.
Balis, FM; Fojo, T; Fox, E; Goodspeed, W; Goodwin, A; Widemann, BC, 2009
)
0.62
" Pharmacokinetic parameters in children and adolescents were highly variable but similar to adults."( Phase I trial and pharmacokinetic study of ixabepilone administered daily for 5 days in children and adolescents with refractory solid tumors.
Balis, FM; Fojo, T; Fox, E; Goodspeed, W; Goodwin, A; Widemann, BC, 2009
)
0.62
" Blood was sampled during cycle 1 for pharmacokinetic analysis of ixabepilone (both schedules) and carboplatin (schedule B)."( A phase I and pharmacokinetic study of ixabepilone in combination with Carboplatin in patients with advanced solid malignancies.
Boddy, AV; Carmichael, J; Cohen, M; Fyfe, D; Griffin, M; Hewitt, P; Namouni, F; Plummer, R; Verrill, M; Woll, P, 2008
)
0.85
" Ixabepilone and carboplatin pharmacokinetics were similar to those using either drug as monotherapy, indicating an absence of pharmacokinetic drug interactions."( A phase I and pharmacokinetic study of ixabepilone in combination with Carboplatin in patients with advanced solid malignancies.
Boddy, AV; Carmichael, J; Cohen, M; Fyfe, D; Griffin, M; Hewitt, P; Namouni, F; Plummer, R; Verrill, M; Woll, P, 2008
)
1.53
" A phase I/II and pharmacokinetic trial of ixabepilone was conducted in patients with recurrent high-grade gliomas."( A phase I/II trial and pharmacokinetic study of ixabepilone in adult patients with recurrent high-grade gliomas.
Batchelor, T; Carson, KA; Desideri, S; Fisher, J; Grossman, SA; He, X; Lesser, G; Mikkelsen, T; Mikkelson, T; Peereboom, DM; Phuphanich, S; Supko, JG, 2010
)
0.88
" Coadministration of sunitinib with ixabepilone on a weekly (but not every 3 week) schedule was associated with a significant increase in the half-life and a significant decrease in the clearance of ixabepilone."( A Phase I Clinical, Pharmacokinetic, and Pharmacodynamic Study of Weekly or Every Three Week Ixabepilone and Daily Sunitinib in Patients with Advanced Solid Tumors.
Benedetto, P; Flores, A; Kovacs, K; Kwon, D; Merchan, JR; Montero, AJ; Rocha-Lima, C; Trent, JC, 2016
)
0.93

Compound-Compound Interactions

The maximum-tolerated dose of ixabepilone in combination with epirubicin was 30 mg/m2 (the recommended dose for phase II evaluation) The dose-limiting toxicity dose was 35 mg/ m2 with grade 4 neutropenia.

ExcerptReferenceRelevance
" Pharmacokinetic data suggested no drug-drug interaction."( Safety of repeated administrations of ixabepilone given as a 3-hour infusion every other week in combination with irinotecan in patients with advanced malignancies.
Boige, V; Cohen, M; Delbaldo, C; Faivre, S; Namouni, F; Pautier, P; Peck, R; Raymond, E; Soria, JC, 2008
)
0.62
"To describe the considerations leading to marketing approval of ixabepilone in combination with capecitabine and as monotherapy for the treatment of advanced breast cancer that is refractory to other chemotherapies."( Ixabepilone in combination with capecitabine and as monotherapy for treatment of advanced breast cancer refractory to previous chemotherapies.
Aziz, R; Booth, B; Bullock, J; Dagher, R; Harapanhalli, R; Jiang, X; Justice, R; Kaminskas, E; Kasliwal, R; Lechleider, RJ; Leighton, J; Pazdur, R; Pope, S; Sridhara, R, 2008
)
2.03
"On October 16, 2007, the Food and Drug Administration approved ixabepilone for injection in combination with capecitabine or as monotherapy for the treatment of patients with advanced breast cancer who have experienced disease progression on previous chemotherapies."( Ixabepilone in combination with capecitabine and as monotherapy for treatment of advanced breast cancer refractory to previous chemotherapies.
Aziz, R; Booth, B; Bullock, J; Dagher, R; Harapanhalli, R; Jiang, X; Justice, R; Kaminskas, E; Kasliwal, R; Lechleider, RJ; Leighton, J; Pazdur, R; Pope, S; Sridhara, R, 2008
)
2.03
" The maximum-tolerated dose of ixabepilone in combination with epirubicin was 30 mg/m2 (the recommended dose for phase II evaluation), and the dose-limiting toxicity dose was 35 mg/m2 with grade 4 neutropenia."( A phase I study of ixabepilone in combination with epirubicin in patients with metastatic breast cancer.
Cottura, E; Dalenc, F; De Benedictis, E; Deslandres, M; Gianni, L; Gladieff, L; Govi, S; Locatelli, A; Messina, M; Roché, H; Zambetti, M, 2012
)
0.99
"The objectives of this phase I trial were to determine the maximum-tolerated dose (MTD), toxicity profile, dose-limiting toxicities (DLT), pharmacokinetics, and the recommended phase II dose for ixabepilone in combination with epirubicin in women with metastatic breast cancer."( A phase I study of ixabepilone in combination with epirubicin in patients with metastatic breast cancer.
Cottura, E; Dalenc, F; De Benedictis, E; Deslandres, M; Gianni, L; Gladieff, L; Govi, S; Locatelli, A; Messina, M; Roché, H; Zambetti, M, 2012
)
0.9
"Forty-two women were treated at 3 different dose levels of ixabepilone: 25 (n = 6), 30 (n = 30), and 35 mg/m(2) (n = 6) in combination with 75 mg/m(2) epirubicin."( A phase I study of ixabepilone in combination with epirubicin in patients with metastatic breast cancer.
Cottura, E; Dalenc, F; De Benedictis, E; Deslandres, M; Gianni, L; Gladieff, L; Govi, S; Locatelli, A; Messina, M; Roché, H; Zambetti, M, 2012
)
0.95
" Here we aim to investigate whether the EGFR monoclonal antibody Cetuximab, in combination with Ixabepilone, is more effective in eliminating CSC populations compared to chemotherapy alone in TNBC."( Antitumor activity of Cetuximab in combination with Ixabepilone on triple negative breast cancer stem cells.
Chang, JC; Choi, DS; Dobrolecki, L; Ghosh, M; Landis, MD; Liang, DH; Rodriguez, AA; Tanei, T, 2016
)
0.9

Dosage Studied

These results suggest that the combination of ixabepilone and mitoxantrone is both feasible and active in castration-resistant prostate cancer. In previous work, a dose-neuropathy model was developed using dosing and patient-reported outcome data from Cancer and Leukemia Group B 40502.

ExcerptRelevanceReference
" Dosing schedules of 40 mg/m2 and 50 mg/m2 over 3 hours were also evaluated."( Phase I study of the novel epothilone analog ixabepilone (BMS-247550) in patients with advanced solid tumors and lymphomas.
Aghajanian, C; Burris, HA; Cohen, MB; Dupont, J; Greco, FA; Hensley, ML; Jones, S; O'Connor, OA; Peck, R; Sabbatini, P; Spriggs, DR, 2007
)
0.6
" Given previous results, however, other dosing schedules may be worthy of further investigation."( A phase II study of ixabepilone (BMS-247550) in metastatic renal-cell carcinoma.
Colevas, AD; Karrison, T; Manchen, E; Posadas, EM; Stadler, WM; Undevia, S; Vokes, EE; Wade, JL, 2007
)
0.66
" Finally, the dosing and administration of ixabepilone and pharmacoeconomic considerations are discussed."( Ixabepilone: a novel microtubule inhibitor for the treatment of locally advanced or metastatic breast cancer.
Steinberg, M, 2008
)
2.05
" The most clinically relevant adverse events associated with its use have been myelosuppression and peripheral neuropathy, which is primarily sensory and cumulative but reversible within six weeks of a dosage reduction or the discontinuation of therapy."( Ixabepilone: a novel microtubule-stabilizing agent for the treatment of metastatic breast cancer.
Goodin, S, 2008
)
1.79
" This dose is 33% higher than the MTD in adults receiving the same dosing schedule."( Phase I trial and pharmacokinetic study of ixabepilone administered daily for 5 days in children and adolescents with refractory solid tumors.
Balis, FM; Fojo, T; Fox, E; Goodspeed, W; Goodwin, A; Widemann, BC, 2009
)
0.62
"These results suggest that the combination of ixabepilone and mitoxantrone is feasible and active in CRPC and requires dosing with pegfilgrastim."( Phase I study of ixabepilone, mitoxantrone, and prednisone in patients with metastatic castration-resistant prostate cancer previously treated with docetaxel-based therapy: a study of the department of defense prostate cancer clinical trials consortium.
Beer, TM; Harzstark, AL; Hussain, M; Mathew, P; Pagliaro, LC; Rosenberg, JE; Ryan, CJ; Ryan, CW; Sharib, J; Small, EJ; Smith, DC; Weinberg, VK, 2009
)
0.95
" Dose modification including dose reduction and dosing schedule modification may be utilized to manage toxicities, but this must be based on careful hematologic, neurologic, and liver function monitoring."( Optimizing ixabepilone treatment schedules in patients with advanced or metastatic breast cancer.
Egerton, N, 2010
)
0.75
" Peripheral neuropathy with ixabepilone was generally reversible and was effectively managed by dosage reduction in most patients."( Ixabepilone plus capecitabine for breast cancer patients with an early metastatic relapse after adjuvant chemotherapy: two clinical trials.
Fornier, M, 2010
)
2.1
" We report a case of RRD induced by ixabepilone, an epothilone antineoplastic agent, with successful rechallenge utilizing an alternative dosing regimen."( Successful rechallenge after ixabepilone-induced radiation recall dermatitis using an alternative dosing strategy.
Abraham, J; Ford, JN; Jordan, C; Newton, M, 2013
)
0.96
" More information is required on dosage and scheduling of ixabepilone in combination with other agents, including novel targeted therapies."( Managing ixabepilone adverse events with dose reduction.
Valero, V, 2013
)
1.05
" In addition, these data suggest that weekly dosing of ixabepilone may be less active than Q3W dosing, but with less neutropenia."( A randomized, phase II, three-arm study of two schedules of ixabepilone or paclitaxel plus bevacizumab as first-line therapy for metastatic breast cancer.
Aldrighetti, D; Amadori, D; Campone, M; Conte, P; Lee, F; Liu, D; McHenry, MB; Melisko, M; Pivot, X; Rugo, HS; Villanueva, C; Wardley, A, 2013
)
0.88
"These results suggest that the combination of ixabepilone and mitoxantrone is both feasible and active in castration-resistant prostate cancer and requires dosing with pegfilgrastim."( Ixabepilone, mitoxantrone, and prednisone for metastatic castration-resistant prostate cancer after docetaxel-based therapy: a phase 2 study of the Department Of Defense Prostate Cancer Clinical Trials Consortium.
Beer, TM; Harzstark, AL; Liu, G; Pagliaro, LC; Rosenberg, JE; Ryan, CJ; Sharib, J; Small, EJ; Smith, DC; Weinberg, VK, 2011
)
2.07
"This multicenter, open-label, randomized phase II trial compared the efficacy and tolerability of weekly ixabepilone versus the standard 3 weekly dosing regimen."( Phase II randomized trial of weekly and every-3-week ixabepilone in metastatic breast cancer patients.
Asmar, L; Koutrelakos, N; McDowell, DO; Mukhopadhyay, P; O'Shaughnessy, J; Rabe, A; Shao, SH; Smith, JW; Vukelja, S; Wang, Y; Wentworth-Hartung, N; Whittaker, T, 2013
)
0.85
" The most important challenges that ongoing clinical trials are still addressing are: the optimal dosing schedule that might improve the risk/benefit ratio, the clinical efficacy of ixabepilone in early breast cancer, the efficacy in triple-negative breast cancer (TNBC) patients and the identification of biomarkers predictive of response."( Evaluation of the pharmacokinetics of ixabepilone for the treatment of breast cancer.
Chicchinelli, N; D'Alessio, A; De Luca, A; Gallo, M; Maiello, MR; Normanno, N; Pergameno, M; Piccirilli, MS, 2015
)
0.88
" 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
)
1.02
" In previous work, a dose-neuropathy model was developed using dosing and patient-reported outcome data from Cancer and Leukemia Group B 40502 (Alliance), a randomized phase III trial of paclitaxel, nanoparticle albumin-bound paclitaxel or ixabepilone as first-line chemotherapy for locally recurrent or metastatic breast cancer."( Personalized Management of Chemotherapy-Induced Peripheral Neuropathy Based on a Patient Reported Outcome: CALGB 40502 (Alliance).
Barry, WT; Gobburu, JV; Gray, E; Hudis, C; Lad, TE; Lyss, AP; Mehrotra, S; Moreno-Aspitia, A; Overmoyer, B; Ratain, MJ; Rugo, HS; Sharma, MR; Toppmeyer, DL; Velasco, M; Winer, EP; Wu, K, 2020
)
0.74
[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 (5)

ClassDescription
1,3-thiazoles
beta-hydroxy ketoneA ketone containing a hydroxy group on the beta-carbon relative to the C=O group.
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.
macrocycleA cyclic compound containing nine or more atoms as part of the cyclic system.
epoxideAny cyclic ether in which the oxygen atom forms part of a 3-membered 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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency0.46610.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency0.46610.00339.158239.8107AID1347411
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apoptosis regulator Bcl-2Homo sapiens (human)Kd0.33700.00060.95874.8000AID1738988
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (155)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
protein polyubiquitinationApoptosis regulator Bcl-2Homo sapiens (human)
apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
response to cytokineApoptosis regulator Bcl-2Homo sapiens (human)
B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of calcium ion transportApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
ossificationApoptosis regulator Bcl-2Homo sapiens (human)
ovarian follicle developmentApoptosis regulator Bcl-2Homo sapiens (human)
metanephros developmentApoptosis regulator Bcl-2Homo sapiens (human)
branching involved in ureteric bud morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
behavioral fear responseApoptosis regulator Bcl-2Homo sapiens (human)
B cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
release of cytochrome c from mitochondriaApoptosis regulator Bcl-2Homo sapiens (human)
regulation of cell-matrix adhesionApoptosis regulator Bcl-2Homo sapiens (human)
lymphoid progenitor cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
B cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
response to ischemiaApoptosis regulator Bcl-2Homo sapiens (human)
renal system processApoptosis regulator Bcl-2Homo sapiens (human)
melanin metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of nitrogen utilizationApoptosis regulator Bcl-2Homo sapiens (human)
autophagyApoptosis regulator Bcl-2Homo sapiens (human)
humoral immune responseApoptosis regulator Bcl-2Homo sapiens (human)
DNA damage responseApoptosis regulator Bcl-2Homo sapiens (human)
actin filament organizationApoptosis regulator Bcl-2Homo sapiens (human)
axonogenesisApoptosis regulator Bcl-2Homo sapiens (human)
female pregnancyApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell population proliferationApoptosis regulator Bcl-2Homo sapiens (human)
male gonad developmentApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressApoptosis regulator Bcl-2Homo sapiens (human)
response to radiationApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
post-embryonic developmentApoptosis regulator Bcl-2Homo sapiens (human)
response to iron ionApoptosis regulator Bcl-2Homo sapiens (human)
response to UV-BApoptosis regulator Bcl-2Homo sapiens (human)
response to gamma radiationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of gene expressionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of autophagyApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
regulation of glycoprotein biosynthetic processApoptosis regulator Bcl-2Homo sapiens (human)
mesenchymal cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
cochlear nucleus developmentApoptosis regulator Bcl-2Homo sapiens (human)
gland morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
regulation of transmembrane transporter activityApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of ossificationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
hair follicle morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
axon regenerationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein stabilityApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
glomerulus developmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cellular pH reductionApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein localizationApoptosis regulator Bcl-2Homo sapiens (human)
myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
T cell differentiation in thymusApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationApoptosis regulator Bcl-2Homo sapiens (human)
osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
response to nicotineApoptosis regulator Bcl-2Homo sapiens (human)
organ growthApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of multicellular organism growthApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to glucose starvationApoptosis regulator Bcl-2Homo sapiens (human)
response to hydrogen peroxideApoptosis regulator Bcl-2Homo sapiens (human)
neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
T cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
CD8-positive, alpha-beta T cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
ear developmentApoptosis regulator Bcl-2Homo sapiens (human)
regulation of viral genome replicationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane permeabilityApoptosis regulator Bcl-2Homo sapiens (human)
focal adhesion assemblyApoptosis regulator Bcl-2Homo sapiens (human)
spleen developmentApoptosis regulator Bcl-2Homo sapiens (human)
thymus developmentApoptosis regulator Bcl-2Homo sapiens (human)
digestive tract morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
oocyte developmentApoptosis regulator Bcl-2Homo sapiens (human)
skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
pigment granule organizationApoptosis regulator Bcl-2Homo sapiens (human)
stem cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
homeostasis of number of cells within a tissueApoptosis regulator Bcl-2Homo sapiens (human)
B cell receptor signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
response to glucocorticoidApoptosis regulator Bcl-2Homo sapiens (human)
neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
defense response to virusApoptosis regulator Bcl-2Homo sapiens (human)
establishment of localization in cellApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane potentialApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of mitochondrial depolarizationApoptosis regulator Bcl-2Homo sapiens (human)
hematopoietic stem cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to organic substanceApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to hypoxiaApoptosis regulator Bcl-2Homo sapiens (human)
reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cell-cell adhesionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorApoptosis regulator Bcl-2Homo sapiens (human)
epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of anoikisApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protease bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
channel activityApoptosis regulator Bcl-2Homo sapiens (human)
channel inhibitor activityApoptosis regulator Bcl-2Homo sapiens (human)
ubiquitin protein ligase bindingApoptosis regulator Bcl-2Homo sapiens (human)
identical protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
sequence-specific DNA bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein heterodimerization activityApoptosis regulator Bcl-2Homo sapiens (human)
BH3 domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein phosphatase 2A bindingApoptosis regulator Bcl-2Homo sapiens (human)
molecular adaptor activityApoptosis regulator Bcl-2Homo sapiens (human)
DNA-binding transcription factor bindingApoptosis regulator Bcl-2Homo sapiens (human)
BH domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum membraneApoptosis regulator Bcl-2Homo sapiens (human)
nucleusApoptosis regulator Bcl-2Homo sapiens (human)
cytoplasmApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrionApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulumApoptosis regulator Bcl-2Homo sapiens (human)
cytosolApoptosis regulator Bcl-2Homo sapiens (human)
membraneApoptosis regulator Bcl-2Homo sapiens (human)
nuclear membraneApoptosis regulator Bcl-2Homo sapiens (human)
myelin sheathApoptosis regulator Bcl-2Homo sapiens (human)
BAD-BCL-2 complexApoptosis regulator Bcl-2Homo sapiens (human)
protein-containing complexApoptosis regulator Bcl-2Homo sapiens (human)
pore complexApoptosis regulator Bcl-2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (87)

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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1739016Induction of apoptosis in human BT-549 cells transfected with Beclin1 siRNA assessed as increase in cleaved caspase-3 level measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739050Induction of autophagy in human U251 cells assessed as increase in LC3-II expression at 0.4 uM measured after 12 to 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739015Induction of apoptosis in human BT-549 cells assessed as increase in cleaved caspase 3 level pretreated with 20 uM autophagy inhibitor, CQ for 1 hr followed by incubation with drug for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739030Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 3 mg/kg, ip administered every other day measured every 3 days by vernier caliper analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739046Downregulation of Ki67 expression in tumor tissue of BALB/c mouse xenografted with human MDA-MB-231 cells at 3 mg/kg, ip administered with compound every other day and with 10 mg/kg, ip CQ every day by immunohistochemical staining2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
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.
AID1739029Cytotoxicity against human U251 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 20 uM autophagy inhibitor, chloroquine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739004Induction of autophagy in human BT-549 cells assessed increase in LC3-II level at 0.1 to 0.2 uM preincubated with 20 uM autophagosome-lysosome fusion inhibitor, chloroquine for 1 hr followed by incubation with compound for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739049Induction of autophagy in human U251 cells assessed as increase in LC3-II expression at 0.4 to 6.4 uM measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564922Antiproliferative activity against human KB/VCR cells assessed as reduction in cell viability after 72 hrs by MTS assay2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1739048Induction of autophagy in human HepG2 cells assessed as increase in LC3-II expression at 0.4 uM measured after 12 to 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564921Selectivity index, ratio of IC50 for human KBtax cells to IC50 for human KB cells2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1739034Upregulation of Bcl-2 phosphorylation at Ser70 residue in human MDA-MB-231 cells at 0.05 to 0.4 microM incubated for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739003Induction of autophagy in human MDA-MB-231 cells assessed increase in LC3-II level at 0.1 to 0.2 uM preincubated with 20 uM autophagosome-lysosome fusion inhibitor, chloroquine for 1 hr followed by incubation with compound for 48 hrs by western blot analy2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739047Induction of autophagy in human HepG2 cells assessed as increase in LC3-II expression at 0.4 to 6.4 uM measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738992Induction of Bcl-2 phosphorylation-mediated protein degradation in human MDA-MB-231 cells assessed as decrease in Bcl-2 expression at 0.1 uM by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739007Cytotoxicity against human BT-549 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 20 uM autophagy inhibitor, chloroquine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739014Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase 3 level pretreated with 20 uM autophagy inhibitor, CQ for 1 hr followed by incubation with drug for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738989Induction of Bcl-2 phosphorylation-mediated protein degradation in human MDA-MB-231 cells assessed as decrease in Bcl-2 expression measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739006Cytotoxicity against human MDA-MB-231 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 20 uM autophagy inhibitor, chloroquine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739017Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP level pretreated with 20 uM autophagy inhibitor, CQ for 1 hr followed by incubation with drug for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
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.
AID1388652Cytotoxicity against human HCT116 cells2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment.
AID1739011Induction of autophagy in human MDA-MB-231 cells transfected with Beclin1 siRNA assessed as LC3-II level at 0.1 uM by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1204868Toxicity in metastatic breast cancer patient assessed as neuropathy rate2015European journal of medicinal chemistry, Apr-13, Volume: 94Selected hybrid natural products as tubulin modulators.
AID1739000Induction of autophagy in human BT-549 cells assessed as increase in LC3-II level at 0.1 uM by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1454745Cytotoxicity against human 1A9 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
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.
AID1738991Induction of Bcl-2 phosphorylation-mediated protein degradation in human MCF7 cells assessed as decrease in Bcl-2 expression measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739020Induction of apoptosis in human BT-549 cells assessed as viable cells incubated for 48 hrs by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 98.6%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739038Upregulation of Bcl-2 phosphorylation at Ser70 residue in human BT549 cells at 0.1 microM incubated for 12 to 36 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739025Induction of Bcl-2 phosphorylation-mediated protein degradation in human U251 cells assessed as decrease in Bcl-2 expression at 0.4 to 6.4 uM measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564847Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by MTS assay2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1739023Induction of apoptosis in human BT-549 cells assessed as necrotic cells incubated for 48 hrs by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 0.145%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564920Antiproliferative activity against human KBtax cells assessed as reduction in cell viability after 72 hrs by MTS assay2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1739026Induction of Bcl-2 phosphorylation-mediated protein degradation in human HepG2 cells assessed as decrease in Bcl-2 expression at 0.4 uM measured after 12 to 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564923Selectivity index, ratio of IC50 for human KB/VCR cells to IC50 for human KB cells2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1738994Induction of Bcl-2 phosphorylation-mediated protein degradation in human MCF7 cells assessed as decrease in Bcl-2 expression at 0.1 uM by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564925Selectivity index, ratio of IC50 for human CCRF-CEM/VBL cells to IC50 for human CCRF-CEM cells2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1738995Induction of Bcl-2 phosphorylation-mediated protein degradation in human MDA-MB-231 cells assessed as disruption of Bcl2/Beclin1 interaction at 0.2 uM measured after 48 hrs by co-immunoprecipitation analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739013Cytotoxicity against human MDA-MB-231 cells transfected with non-targeting siRNA at 0.1 to 1.6 uM measured after 48 hrs by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739001Induction of autophagy in human MCF7 cells assessed as increase in LC3-II level at 0.1 uM by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739037Upregulation of Bcl-2 phosphorylation at Ser70 residue in human MDA-MB-231 cells at 0.1 microM incubated for 12 to 36 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739044Induction of apoptosis in human BT-549 cells assessed as necrotic cells incubated for 48 hrs in presence of 20 uM autophagy inhibitor, CQ by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 0.86%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739024Induction of Bcl-2 phosphorylation-mediated protein degradation in human HepG2 cells assessed as decrease in Bcl-2 expression at 0.4 to 6.4 uM measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739035Upregulation of Bcl-2 phosphorylation at Ser70 residue in human BT549 cells at 0.05 to 0.4 microM incubated for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1739008Cytotoxicity against human MCF-7 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 20 uM autophagy inhibitor, chloroquine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
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.
AID1739021Induction of apoptosis in human BT-549 cells assessed as early apoptotic cells incubated for 48 hrs by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 0.609%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739010Cytotoxicity against human BT-549 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 2 mM autophagy inhibitor, 3-methyladenine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1739002Induction of autophagy in human BT-549 cells transfected with GFP-LC3 assessed as increase in GFP-LC3 puncta formation after 12 hrs by fluorescence microscopic analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739043Induction of apoptosis in human BT-549 cells assessed as late apoptotic cells incubated for 48 hrs in presence of 20 uM autophagy inhibitor, CQ by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 2.64%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739027Induction of Bcl-2 phosphorylation-mediated protein degradation in human U251 cells assessed as decrease in Bcl-2 expression at 0.4 uM measured after 12 to 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739040Effect on Beclin1 expression in human MDA-MB-231 cells at 0.2 uM measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739039Upregulation of Bcl-2 phosphorylation at Ser70 residue in human MCF7 cells at 0.1 microM incubated for 12 to 36 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739045Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 3 mg/kg, ip administered with compound every other day and with 10 mg/kg, ip CQ every day and measured every 3 days by vernier caliper ana2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
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.
AID1738996Induction of autophagy in human MDA-MB-231 cells assessed as increase in LC3-II level measured after 48 hrs by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564924Antiproliferative activity against human CCRF-CEM/VBL cells assessed as reduction in cell viability after 72 hrs by MTS assay2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1739033Induction of Bcl-2 phosphorylation-mediated protein degradation in human MCF7 cells assessed as decrease in Bcl-2 expression at 0.1 to 0.2 uM pretreated with proteasome inhibitor, MG132 for 2 hrs followed by incubation with compound for 48 hrs by western 2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1739042Induction of apoptosis in human BT-549 cells assessed as early apoptotic cells incubated for 48 hrs in presence of 20 uM autophagy inhibitor, CQ by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 1.94%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738999Induction of autophagy in human MDA-MB-231 cells assessed as increase in LC3-II level at 0.1 uM by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738998Induction of autophagy in human MCF-7 cells assessed as increase in LC3-II level measured after 48 hrs by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739031Induction of Bcl-2 phosphorylation-mediated protein degradation in human MDA-MB-231 cells assessed as decrease in Bcl-2 expression at 0.1 to 0.2 uM pretreated with proteasome inhibitor, MG132 for 2 hrs followed by incubation with compound for 48 hrs by we2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739005Induction of autophagy in human BT-549 cells expressing mRFP-EGFP-LC3B assessed as accumulation of yellow fluorescence signals measured after 12 hrs by fluorescence microscopic analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739028Cytotoxicity against human HepG2 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 20 uM autophagy inhibitor, chloroquine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739009Cytotoxicity against human MDA-MB-231 cells at 0.1 to 1.6 uM measured after 48 hrs in presence of 2 mM autophagy inhibitor, 3-methyladenine by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
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.
AID1738990Induction of Bcl-2 phosphorylation-mediated protein degradation in human BT549 cells assessed as decrease in Bcl-2 expression measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1564839Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTS assay2019European journal of medicinal chemistry, Nov-01, Volume: 1814(1H)-quinolone derivatives overcome acquired resistance to anti-microtubule agents by targeting the colchicine site of β-tubulin.
AID1738993Induction of Bcl-2 phosphorylation-mediated protein degradation in human BT549 cells assessed as decrease in Bcl-2 expression at 0.1 uM by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739019Induction of apoptosis in human BT-549 cells transfected with Beclin1 siRNA assessed as increase in cleaved PARP level measured after 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738988Binding affinity to human recombinant Bcl-2 expressed in Escherichia coli by Surface plasmon resonance assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739036Upregulation of Bcl-2 phosphorylation at Ser70 residue in human MCF7 cells at 0.05 to 0.4 microM incubated for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739012Cytotoxicity against human MDA-MB-231 cells transfected with Beclin1 siRNA at 0.1 to 1.6 uM measured after 48 hrs by CCK8 assay2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739041Induction of apoptosis in human BT-549 cells assessed as viable cells incubated for 48 hrs in presence of 20 uM autophagy inhibitor, CQ by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 94.6%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1739018Induction of apoptosis in human BT-549 cells assessed as increase in cleaved PARP level pretreated with 20 uM autophagy inhibitor, CQ for 1 hr followed by incubation with drug for 48 hrs by western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1738997Induction of autophagy in human BT-549 cells assessed as increase in LC3-II level measured after 48 hrs by Western blot analysis2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739022Induction of apoptosis in human BT-549 cells assessed as late apoptotic cells incubated for 48 hrs by AnnexinV-FITC and propidium iodide staining based flow cytometry analysis(Rvb = 0.599%)2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
AID1739032Induction of Bcl-2 phosphorylation-mediated protein degradation in human BT549 cells assessed as decrease in Bcl-2 expression at 0.1 to 0.2 uM pretreated with proteasome inhibitor, MG132 for 2 hrs followed by incubation with compound for 48 hrs by western2020European journal of medicinal chemistry, Aug-01, Volume: 199A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (275)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's130 (47.27)29.6817
2010's133 (48.36)24.3611
2020's12 (4.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.92

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 Index42.92 (24.57)
Research Supply Index5.95 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index66.73 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials101 (35.69%)5.53%
Reviews93 (32.86%)6.00%
Case Studies9 (3.18%)4.05%
Observational1 (0.35%)0.25%
Other79 (27.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]