Microtubule destabilizer (tubulin polymerization inhibitor) Tumor checkpoint controller Treatment of advanced glioblastoma multiforme

被引：0

作者：

Tiu, Crescens

Lopez, Juanita ^{[1
]}

机构：

[1] Royal Marsden Hosp, Drug Dev Unit, Sutton, England

来源：

DRUGS OF THE FUTURE | 2022年 / 47卷 / 09期

关键词：

Lisavanbulin; BAL-101553; Avanbulin; BAL-27862; Glioblastoma multiforme; Tubulin-binding  agent; End-binding protein; OVARIAN-CANCER CELLS; ADJUVANT TEMOZOLOMIDE; BAL101553; RADIOTHERAPY; BAL27862; CONCOMITANT; AGENT;

D O I：

10.1358/dof.2022.47.9.3417140

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Lisavanbulin (BAL-101553), a prodrug of avanbulin (BAL-27862), is a novel small molecule tubulin-binding agent, promoting tumor cell death through spindle assembly check-point activation, and is currently in phase I/IIa development in advanced glioblastoma multiforme (GBM). Daily contin-uous oral lisavanbulin is well tolerated with an established pharmacokinetic and safety profile. Expression of end-binding protein 1 (EB1), which is involved in microtubule function, has been identified as a potential response-predictive marker for lisavanbulin with profound long-lasting responses seen in EB1+ recurrent GBM. A biomarker-selected phase II study is currently ongoing in patients with recurrent GBM whose archival tumor tissue tests positive for EB1 (NCT02490800); and a combination dose-escalation study with standard of care radiation in patients with newly diagnosed GBM (NCT03250299) is recruiting.

引用

页码：651 / 659

页数：9

共 41 条

[31] A unique microtubule-targeted agent with a potential for the treatment of human brain tumors [J].

Schmitt-Hoffmann, Anne ;

Klauer, Dominique ;

Gebhardt, Klaus ;

Fullhardt, Pascal ;

Brendle, Alain ;

Hardgreaves, Patrick ;

Schlaefle, Caroline ;

Bucher, Christian ;

Spickermann, Jochen ;

Defoin, Rosalie ;

Burger, Karin ;

Van Vuong ;

Bachmann, Felix ;

Pruschy, Martin ;

Lane, Heidi .

MOLECULAR CANCER THERAPEUTICS, 2009, 8 (12)

[32] Reactions of methyl 4-aminofurazan-3-carboximidate with nitrogen-containing nucleophiles [J].

Sergievskii, AV ;

Pirogov, SV ;

Mel'nikova, SF ;

Tselinskii, IV .

RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2001, 37 (05) :717-720

[33] The novel microtubule targeting agent BAL101553 in combination with radiotherapy in treatment-refractory tumor models [J].

Sharma, Ashish ;

Broggini-Tenzer, Angela ;

Van Vuong ;

Messikommer, Alessandra ;

Nytko, Katarzyna J. ;

Guckenberger, Matthias ;

Bachmann, Felix ;

Lane, Heidi A. ;

Pruschy, Martin .

RADIOTHERAPY AND ONCOLOGY, 2017, 124 (03) :433-438

[34] Expression of end-binding protein 1 (EB1), a potential response-predictive biomarker for lisavanbulin, in glioblastoma and various other solid tumor types. [J].

Skowronska, Magdalena ;

Tiu, Crescens Diane ;

Tzankov, Alexandar ;

Konig, Fatima ;

Lewis, Joanne ;

Vivanco, Igor ;

Kleinschmidt, Malte ;

Beebe, Kirk ;

Anderson, Stephanie ;

Bachmann, Felix ;

Engelhardt, Marc ;

Lane, Heidi A. ;

Kaindl, Thomas ;

Stan, Alexandru C. ;

Plummer, Elizabeth Ruth ;

Evans, T. R. Jeffry ;

Zlobec, Inti ;

Lopez, Juanita Suzanne .

JOURNAL OF CLINICAL ONCOLOGY, 2021, 39 (15)

[35] A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines [J].

Stepanov, Andrei I. ;

Astrat'ev, Alexander A. ;

Sheremetev, Aleksei B. ;

Lagutina, Nataliya K. ;

Palysaeva, Nadezhda V. ;

Tyurin, Aleksei Yu. ;

Aleksandrova, Nataliya S. ;

Sadchikova, Nataliya P. ;

Suponitsky, Kyrill Yu. ;

Atamanenko, Olga P. ;

Konyushkin, Leonid D. ;

Semenov, Roman V. ;

Firgang, Sergei I. ;

Kiselyov, Alex S. ;

Semenova, Marina N. ;

Semenov, Victor V. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 94 :237-251

[36] Radiotherapy plus concomitant and adjuvant temozolomide for glioblastoma [J].

Stupp, R ;

Mason, WP ;

van den Bent, MJ ;

Weller, M ;

Fisher, B ;

Taphoorn, MJB ;

Belanger, K ;

Brandes, AA ;

Marosi, C ;

Bogdahn, U ;

Curschmann, J ;

Janzer, RC ;

Ludwin, SK ;

Gorlia, T ;

Allgeier, A ;

Lacombe, D ;

Cairncross, JG ;

Eisenhauer, E ;

Mirimanoff, RO ;

Van Den Weyngaert, D ;

Kaendler, S ;

Krauseneck, P ;

Vinolas, N ;

Villa, S ;

Wurm, RE ;

Maillot, MHB ;

Spagnolli, F ;

Kantor, G ;

Malhaire, JP ;

Renard, L ;

De Witte, O ;

Scandolaro, L ;

Vecht, CJ ;

Maingon, P ;

Lutterbach, J ;

Kobierska, A ;

Bolla, M ;

Souchon, R ;

Mitine, C ;

Tzuk-Shina, T ;

Kuten, A ;

Haferkamp, G ;

de Greve, J ;

Priou, F ;

Menten, J ;

Rutten, I ;

Clavere, P ;

Malmstrom, A ;

Jancar, B ;

Newlands, E .

NEW ENGLAND JOURNAL OF MEDICINE, 2005, 352 (10) :987-996

[37] Effects of radiotherapy with concomitant and adjuvant temozolomide versus radiotherapy alone on survival in glioblastoma in a randomised phase III study: 5-year analysis of the EORTC-NCIC trial [J].

Stupp, Roger ;

Hegi, Monika E. ;

Mason, Warren P. ;

van den Bent, Martin J. ;

Taphoorn, Martin J. B. ;

Janzer, Robert C. ;

Ludwin, Samuel K. ;

Allgeier, Anouk ;

Fisher, Barbara ;

Belanger, Karl ;

Hau, Peter ;

Brandes, Alba A. ;

Gijtenbeek, Johanna ;

Marosi, Christine ;

Vecht, Charles J. ;

Mokhtari, Karima ;

Wesseling, Pieter ;

Villa, Salvador ;

Eisenhauer, Elizabeth ;

Gorlia, Thierry ;

Weller, Michael ;

Lacombe, Denis ;

Cairncross, J. Gregory ;

Mirimanoff, Rene-Olivier .

LANCET ONCOLOGY, 2009, 10 (05) :459-466

[38] The potential utility of end-binding protein 1 (EB1) as response-predictive biomarker for lisavanbulin: Final results from a phase I study of lisavanbulin (BAL101553) in adult patients with recurrent glioblastoma (GBM) [J].

Tiu, C. ;

Tzankov, A. ;

Plummer, R. ;

Rulach, R. ;

Vivanco, I. ;

Mulholland, P. J. ;

Gurel, B. ;

Figueiredo, I. ;

Haris, N. Md. ;

Anderson, S. ;

Bachmann, F. ;

Engelhardt, M. ;

Kaindl, T. ;

Lane, H. ;

Litherland, K. ;

Pognan, C. ;

Berezowska, S. ;

Evans, J. ;

Kristeleit, R. ;

Lopez, J. S. .

ANNALS OF ONCOLOGY, 2020, 31 :S404-S404

[39]

Tselinskii I.V., 1999, CHEMINFORM, V30, P1

[40]

Wang Z., Patent No. [WO2016041489, 2016041489]

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