408:. However, unlike paclitaxel, it does not induce these pro-tumor effects in Type I cells." The detrimental effects attributed to paclitaxel were alleged to be "...due to paclitaxel-induced enhancement of NF-κB and ERK activities, and cytokine production (e.g. IL-6), which promote chemoresistance and tumor progression." The latter study also reported promising results, concluding that filanesib "...potently induces cell cycle block and subsequent death in leukemic cells via the mitochondrial pathway and has the potential to eradicate AML progenitor cells." However, a clinical trial published in 2012 on patients with advanced myeloid leukemias found that the drug exhibited a "relative lack of clinical activity"; the trial was therefore halted before it was scheduled to end.
231:
24:
723:
Ocio, E. M.; Richardson, P. G.; Rajkumar, S. V.; Palumbo, A.; Mateos, M. V.; Orlowski, R.; Kumar, S.; Usmani, S.; Roodman, D.; Niesvizky, R.; Einsele, H.; Anderson, K. C.; Dimopoulos, M. A.; Avet-Loiseau, H.; Mellqvist, U. H.; Turesson, I.; Merlini, G.; Schots, R.; McCarthy, P.; Bergsagel, L.; Chim,
462:; the results concluded that 16 percent of patients who had received a median of six prior therapies responded to single-agent filanesib. In the week after this presentation, Array BioPharma's stock fell by 16%. In February 2014, a review was published by researchers from the
601:
Khoury, H. J.; Garcia-Manero, G.; Borthakur, G.; Kadia, T.; Foudray, M. C.; Arellano, M.; Langston, A.; Bethelmie-Bryan, B.; Rush, S.; Litwiler, K.; Karan, S.; Simmons, H.; Marcus, A. I.; Ptaszynski, M.; Kantarjian, H. (2012).
454:, though it is possible that it may cause low blood cell counts as well. Shah et al. have conducted a phase II study of filanesib both by itself, and in combination with dexamethasone, presented at the annual meeting of the
112:
446:
concluded that filanesib was "effective in monotherapy as well as in combination with dexamethasone in heavily pretreated patients." According to Jatin Shah, an assistant professor at
940:
Chari, A; Htut, M; Zonder, JA; Fay, JW; Jakubowiak, AJ; Levy, JB; Lau, K; Burt, SM; Tunquist, BJ; Hilder, BW; Rush, SA; Walker, DH; Ptaszynski, M; Kaufman, JL (15 November 2016).
485:
had a favorable safety profile. The same study reported that this combination of drugs "appears to have durable activity in patients with recurrent/refractory multiple myeloma."
773:
438:(i.e. the time until the cancer recurs). A previous trial had reported that 37% of patients receiving filanesib in conjunction with carfilzomib showed lower levels of
447:
270:
774:"Array BioPharma Announces Positive Interim Results From Combination Trial Of ARRY-520 With Kyprolis At The 2013 European Hematology Association Congress"
254:
InChI=1S/C20H22F2N4O2S/c1-25(28-2)19(27)26-20(11-6-12-23,14-7-4-3-5-8-14)29-18(24-26)16-13-15(21)9-10-17(16)22/h3-5,7-10,13H,6,11-12,23H2,1-2H3/t20-/m0/s1
442:, also known as "M protein", whereas only 16% of controls (i.e. those receiving only carfilzomib) showed such a reduction. In addition, a report by the
655:
849:
443:
942:"A phase 1 dose-escalation study of filanesib plus bortezomib and dexamethasone in patients with recurrent/refractory multiple myeloma"
994:
726:"New drugs and novel mechanisms of action in multiple myeloma in 2013: A report from the international myeloma working group (imwG)"
245:
862:
724:
J.; Lahuerta, J. J.; Shah, J.; Reiman, A.; Mikhael, J.; Zweegman, S.; Lonial, S.; Comenzo, R.; Chng, W. J.; Moreau, P. (2013).
604:"A phase 1 dose-escalation study of ARRY-520, a kinesin spindle protein inhibitor, in patients with advanced myeloid leukemias"
412:
459:
455:
466:
in Spain, which concluded that "...some of these novel agents seem promising, such as monoclonal antibodies (anti-CD38 —
357:
188:
895:
404:
cells were published. The former reported that filanesib "...has similar anti-tumor activity in EOC cells as that of
209:
554:"Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells"
552:
Carter, B Z; Mak, D H; Woessner, R; Gross, S; Schober, W D; Estrov, Z; Kantarjian, H; Andreeff, M (21 May 2009).
435:
377:
450:, the primary adverse effect of treatment with filanesib observed in trials conducted thus far is reversible
463:
419:. On October 31, 2013, it was reported that the company which developed the drug, Array BioPharma (based in
401:
850:
Filanesib (ARRY-520) Continues To Show
Promise In Heavily Pretreated Multiple Myeloma Patients (ASH 2013)
1004:
999:
477:
A 2016 phase 1 dose-escalation study found that the studied dosing regimen of filanesib combined with
458:. In December 2013, further clinical trial results were presented, also at the annual meeting of the
428:
36:
889:
Ocio, Enrique M; Mitsiades, Constantine S; Orlowski, Robert Z; Anderson, Kenneth C (February 2014).
501:
Kim, Ki Hyung; Xie, Yanhua; Tytler, Ewan M.; Woessner, Richard; Mor, Gil; Alvero, Ayesha B. (2009).
226:
78:
411:
In June 2013, preliminary results from a trial of the drug were presented at a conference of the
971:
922:
832:
755:
705:
633:
583:
534:
420:
132:
961:
953:
912:
904:
822:
814:
745:
737:
695:
623:
615:
573:
565:
524:
514:
424:
381:
293:
88:
380:(KIF11) inhibitor which has recently been proposed as a cancer treatment, specifically for
197:
778:
230:
1009:
966:
941:
917:
890:
827:
802:
750:
725:
628:
603:
578:
553:
529:
502:
397:
351:
503:"KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells"
988:
482:
177:
818:
908:
467:
451:
439:
431:
478:
471:
405:
336:
123:
423:), was planning on launching a phase III clinical trial of the drug to treat
416:
975:
926:
836:
759:
709:
637:
587:
538:
519:
867:
741:
700:
683:
569:
393:
957:
619:
164:
23:
803:"Novel Approaches to Treatment of Double-Refractory Multiple Myeloma"
660:
350:
Except where otherwise noted, data are given for materials in their
152:
111:
101:
143:
684:"Kinesin inhibitor marches toward first-in-class pivotal trial"
656:"Array Biopharma Outlines Path To Market For New Myeloma Drug"
434:
in several hundred patients. The study's primary endpoint was
427:. The study began in mid-2014, and paired filanesib with the
891:"Future agents and treatment directions in multiple myeloma"
214:
278:
CN(C(=O)N1(SC(=N1)C2=C(C=CC(=C2)F)F)(CCCN)C3=CC=CC=C3)OC
807:
American
Society of Clinical Oncology Educational Book
801:Lee, H. C.; Shah, J. J.; Orlowski, R. Z. (2013).
176:
87:
474:) or the kinesin protein inhibitor Arry-520."
396:studies on the effects of filanesib on either
448:University of Texas MD Anderson Cancer Center
8:
863:"3 Horrendous Health-Care Stocks This Week"
45:)-2-(3-Aminopropyl)-5-(2,5-difluorophenyl)-
229:
131:
15:
965:
916:
826:
749:
699:
627:
577:
528:
518:
196:
649:
647:
493:
275:
250:
225:
53:-methyl-2-phenyl-1,3,4-thiadiazole-3(2
257:Key: LLXISKGBWFTGEI-FQEVSTJZSA-N
7:
861:Speights, Keith (14 December 2013).
654:Herper, Matthew (31 October 2013).
444:International Myeloma Working Group
167:
151:
14:
507:Journal of Translational Medicine
317:
311:
305:
22:
413:European Hematology Association
354:(at 25 °C , 100 kPa).
819:10.1200/EdBook_AM.2013.33.e302
460:American Society of Hematology
456:American Society of Hematology
329:
323:
299:
1:
909:10.1586/17474086.2014.858595
896:Expert Review of Hematology
1026:
995:Experimental cancer drugs
436:progression-free survival
348:
286:
266:
241:
71:
63:
35:
30:
21:
464:University of Salamanca
378:kinesin spindle protein
520:10.1186/1479-5876-7-63
402:acute myeloid leukemia
742:10.1038/leu.2013.350
701:10.1038/nm1213-1550a
570:10.1038/leu.2009.101
429:proteasome inhibitor
37:Preferred IUPAC name
388:History of research
344: g·mol
18:
958:10.1002/cncr.30174
682:Owens, B. (2013).
620:10.1002/cncr.26664
358:Infobox references
16:
952:(21): 3327–3335.
614:(14): 3556–3564.
564:(10): 1755–1762.
421:Boulder, Colorado
366:Chemical compound
364:
363:
210:CompTox Dashboard
113:Interactive image
1017:
980:
979:
969:
937:
931:
930:
920:
886:
880:
879:
877:
875:
858:
852:
847:
841:
840:
830:
798:
792:
791:
789:
787:
770:
764:
763:
753:
720:
714:
713:
703:
679:
673:
672:
670:
668:
651:
642:
641:
631:
598:
592:
591:
581:
549:
543:
542:
532:
522:
498:
425:multiple myeloma
382:multiple myeloma
343:
331:
325:
319:
313:
307:
301:
294:Chemical formula
234:
233:
218:
216:
200:
180:
169:
155:
135:
115:
91:
26:
19:
1025:
1024:
1020:
1019:
1018:
1016:
1015:
1014:
985:
984:
983:
939:
938:
934:
888:
887:
883:
873:
871:
860:
859:
855:
848:
844:
800:
799:
795:
785:
783:
779:The Denver Post
772:
771:
767:
722:
721:
717:
688:Nature Medicine
681:
680:
676:
666:
664:
653:
652:
645:
600:
599:
595:
551:
550:
546:
500:
499:
495:
491:
390:
367:
360:
355:
341:
328:
322:
316:
310:
304:
296:
282:
279:
274:
273:
262:
259:
258:
255:
249:
248:
237:
219:
212:
203:
183:
170:
158:
138:
118:
105:
94:
81:
67:
59:
58:
12:
11:
5:
1023:
1021:
1013:
1012:
1007:
1002:
997:
987:
986:
982:
981:
932:
903:(1): 127–141.
881:
853:
842:
793:
782:. 17 June 2013
765:
736:(3): 525–542.
715:
674:
643:
593:
544:
492:
490:
487:
470:or anti-CS1 —
398:ovarian cancer
389:
386:
365:
362:
361:
356:
352:standard state
349:
346:
345:
339:
333:
332:
326:
320:
314:
308:
302:
297:
292:
289:
288:
284:
283:
281:
280:
277:
269:
268:
267:
264:
263:
261:
260:
256:
253:
252:
244:
243:
242:
239:
238:
236:
235:
227:DTXSID50237086
222:
220:
208:
205:
204:
202:
201:
193:
191:
185:
184:
182:
181:
173:
171:
163:
160:
159:
157:
156:
148:
146:
140:
139:
137:
136:
128:
126:
120:
119:
117:
116:
108:
106:
99:
96:
95:
93:
92:
84:
82:
77:
74:
73:
69:
68:
65:
61:
60:
40:
39:
33:
32:
28:
27:
13:
10:
9:
6:
4:
3:
2:
1022:
1011:
1008:
1006:
1003:
1001:
998:
996:
993:
992:
990:
977:
973:
968:
963:
959:
955:
951:
947:
943:
936:
933:
928:
924:
919:
914:
910:
906:
902:
898:
897:
892:
885:
882:
870:
869:
864:
857:
854:
851:
846:
843:
838:
834:
829:
824:
820:
816:
812:
808:
804:
797:
794:
781:
780:
775:
769:
766:
761:
757:
752:
747:
743:
739:
735:
731:
727:
719:
716:
711:
707:
702:
697:
693:
689:
685:
678:
675:
663:
662:
657:
650:
648:
644:
639:
635:
630:
625:
621:
617:
613:
609:
605:
597:
594:
589:
585:
580:
575:
571:
567:
563:
559:
555:
548:
545:
540:
536:
531:
526:
521:
516:
512:
508:
504:
497:
494:
488:
486:
484:
483:dexamethasone
480:
475:
473:
469:
465:
461:
457:
453:
449:
445:
441:
437:
433:
430:
426:
422:
418:
414:
409:
407:
403:
399:
395:
392:In 2009, two
387:
385:
383:
379:
375:
371:
359:
353:
347:
340:
338:
335:
334:
298:
295:
291:
290:
285:
276:
272:
265:
251:
247:
240:
232:
228:
224:
223:
221:
211:
207:
206:
199:
195:
194:
192:
190:
187:
186:
179:
175:
174:
172:
166:
162:
161:
154:
150:
149:
147:
145:
142:
141:
134:
130:
129:
127:
125:
122:
121:
114:
110:
109:
107:
103:
98:
97:
90:
86:
85:
83:
80:
76:
75:
70:
62:
57:)-carboxamide
56:
52:
48:
44:
38:
34:
29:
25:
20:
1005:Thiadiazoles
1000:Fluoroarenes
949:
945:
935:
900:
894:
884:
872:. Retrieved
866:
856:
845:
810:
806:
796:
784:. Retrieved
777:
768:
733:
729:
718:
694:(12): 1550.
691:
687:
677:
665:. Retrieved
659:
611:
607:
596:
561:
557:
547:
510:
506:
496:
476:
410:
391:
373:
369:
368:
72:Identifiers
64:Other names
54:
50:
46:
42:
813:: 302–306.
786:16 December
468:daratumumab
452:neutropenia
440:paraprotein
432:carfilzomib
372:(code name
287:Properties
89:885060-09-3
989:Categories
667:5 February
489:References
479:bortezomib
472:elotuzumab
406:paclitaxel
337:Molar mass
198:8A49OSO368
124:ChemSpider
100:3D model (
79:CAS Number
17:Filanesib
513:(1): 63.
417:Stockholm
400:cells or
370:Filanesib
49:-methoxy-
976:27433944
927:24350987
868:Fool.com
837:23714530
760:24253022
730:Leukemia
710:24309639
638:22139909
588:19458629
558:Leukemia
539:19619321
394:in vitro
374:ARRY-520
178:44224257
133:25069697
66:ARRY-520
967:6857452
918:4157182
874:7 April
828:3762449
751:4143389
629:4984525
579:3593228
530:2719595
376:) is a
165:PubChem
974:
964:
946:Cancer
925:
915:
835:
825:
758:
748:
708:
661:Forbes
636:
626:
608:Cancer
586:
576:
537:
527:
342:420.48
271:SMILES
153:D11754
31:Names
1010:Ureas
246:InChI
102:JSmol
972:PMID
923:PMID
876:2014
833:PMID
788:2013
756:PMID
706:PMID
669:2014
634:PMID
584:PMID
535:PMID
481:and
189:UNII
144:KEGG
962:PMC
954:doi
950:122
913:PMC
905:doi
823:PMC
815:doi
746:PMC
738:doi
696:doi
624:PMC
616:doi
612:118
574:PMC
566:doi
525:PMC
515:doi
415:in
215:EPA
168:CID
991::
970:.
960:.
948:.
944:.
921:.
911:.
899:.
893:.
865:.
831:.
821:.
811:33
809:.
805:.
776:.
754:.
744:.
734:28
732:.
728:.
704:.
692:19
690:.
686:.
658:.
646:^
632:.
622:.
610:.
606:.
582:.
572:.
562:23
560:.
556:.
533:.
523:.
509:.
505:.
384:.
309:22
303:20
41:(2
978:.
956::
929:.
907::
901:7
878:.
839:.
817::
790:.
762:.
740::
712:.
698::
671:.
640:.
618::
590:.
568::
541:.
517::
511:7
330:S
327:2
324:O
321:4
318:N
315:2
312:F
306:H
300:C
217:)
213:(
104:)
55:H
51:N
47:N
43:S
Text is available under the Creative Commons Attribution-ShareAlike License. Additional terms may apply.
