194
Views
63
CrossRef citations to date
0
Altmetric
Original Research

Comprehensive kinase profile of pacritinib, a nonmyelosuppressive Janus kinase 2 inhibitor

, , , , &
Pages 11-19 | Published online: 16 Aug 2016

References

  • RaneSGReddyEPJanus kinases: components of multiple signaling pathwaysOncogene200019495662567911114747
  • HarrisonCKiladjianJJAl-AliHKJAK inhibition with ruxolitinib versus best available therapy for myelofibrosisN Engl J Med2012366978779822375970
  • VerstovsekSMesaRAGotlibJA double-blind, placebo-controlled trial of ruxolitinib for myelofibrosisN Engl J Med2012366979980722375971
  • WilliamADLeeACBlanchardSDiscovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6). 1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphomaJ Med Chem201154134638465821604762
  • HartSGohKCNovotny-DiermayrVSB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignanciesLeukemia201125111751175921691275
  • HartSGohKCNovotny-DiermayrVPacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemiaBlood Cancer J2011111e4422829080
  • VerstovsekSDeegHJOdenikeOPhase 1/2 study of SB1518, a novel JAK2/FLT3 inhibitor, in the treatment of primary myelofibrosisProceedings of the 53rd Annual Meeting of the American Society of HematologyDecember 10–13, 2011Chicago, IL Abstract 3082
  • VerstovsekSOdenikeOScottBPhase 1 dose-escalation trial of SB1518, a novel JAK2/FLT3 inhibitor, in acute and chronic myeloid diseases, including primary or post-essential thrombocythemia/poly-cythemia vera myelofibrosisProceedings of the 51st Annual Meeting of the American Society of HematologyDecember 5–8, 2009New Orleans, LA Abstract 3905
  • VerstovsekSPassamontiFRambaldiAA phase 2 study of INCB018424, an oral, selective JAK1/JAK2 inhibitor, in patients with advanced polycythemia vera (PV) and essential thrombocythemia (ET) refractory to hydroxyureaProceedings of the 51st Annual Meeting of the American Society of HematologyDecember 5–8, 2009New Orleans, LA Abstract 311
  • YounesAFanaleMMclaughlinPPhase-I study of the novel oral JAK-2 inhibitor SB1518 in patients with relapsed lymphoma: evidence of clinical and biologic activityProceedings of the 51st Annual Meeting of the American Society of HematologyDecember 5–8, 2009New Orleans, LA Abstract 588
  • YounesAFanaleMMclaughlinPCopelandARZhuJDe Castro FariaSPhase 1 study of a novel oral JAK-2 inhibitor SB1518 in patients with relapsed lymphoma: evidence of clinical and biologic activity in multiple lymphoma subtypesProceedings of the 53rd Annual Meeting of the American Society of HematologyDecember 10–13, 2011Chicago, IL Abstract 2830
  • KomrokjiRSWadleighMSeymourJFResults of a phase 2 study of pacritinib (SB1518), a novel oral JAK2 inhibitor, in patients with primary, post-polycythemia vera, and post-essential thrombocythemia myelofibrosisProceedings of the 53rd Annual Meeting of the American Society of HematologyDecember 10–13, 2011Chicago, IL Abstract 282
  • VerstovsekSMesaRAGotlibJLong-term outcomes of ruxolitinib therapy in patients with myelofibrosis: 3-year update from COMFORT-IProceedings of the 55th Annual Meeting of the American Society of HematologyDecember 7–10, 2013New Orleans, LA Abstract 2830
  • MesaRAEgyedMSzokeAResults of the PERSIST-1 phase III study of pacritinib (PAC) versus best available therapy (BAT) in primary myelofibrosis (PMF), post-polycythemia vera myelofibrosis (PPV-MF), or post-essential thrombocythemia-myelofibrosis (PET-MF)Proceedings of the 2015 Annual Meeting of the American Society of Clinical OncologyMay 29–June 2, 2015Chicago, IL
  • LevineRLWadleighMCoolsJActivating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosisCancer Cell20057438739715837627
  • LuXLevineRTongWExpression of a homodimeric type 1 cytokine receptor is required for JAK2V617F-mediated transformationProc Natl Acad Sci U S A200510252189621896716365288
  • RumiEPietraDPascuttoCClinical effect of driver mutations of JAK2, CALR, or MPL in primary myelofibrosisBlood201412471062106924986690
  • ReillyJTFLT3 and its role in the pathogenesis of acute myeloid leukaemiaLeuk Lymphoma20034411712691136
  • TickenbrockLMuller-TidowCBerdelWEServeHEmerging Flt3 kinase inhibitors in the treatment of leukaemiaExpert Opin Emerg Drugs200611115316516503833
  • SteensmaDPMcClureRFKarpJEJAK2 V617F is a rare finding in de novo acute myeloid leukemia, but STAT3 activation is common and remains unexplainedLeukemia200620697197816598306
  • AnastassiadisTDeaconSWDevarajanKMaHPetersonJRComprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivityNat Biotechnol201129111039104522037377
  • YeeTWHastieTJReduced-rank vector generalized linear modelsStat Model200331541
  • van der LooMPJDistribution based outlier detection for univariate dataDiscussion paper 10003The HagueStatistics Netherland2010
  • RhyasenGWBolanosLFangJTargeting IRAK1 as a therapeutic approach for myelodysplastic syndromeCancer Cell20132419010423845443
  • Puig de la BellacasaRKarachaliouNEstrada-TejedorRTeixidoJCostaCBorrellJIALK and ROS1 as a joint target for the treatment of lung cancer: a reviewTransl Lung Cancer Res201322728625806218
  • HendersonMCGonzalesIMAroraSHigh-throughput RNAi screening identifies a role for TNK1 in growth and survival of pancreatic cancer cellsMol Cancer Res20119672473221536687
  • PolkALuYWangTColony-stimulating Factor-1 receptor is required for nurse-like cell survival in chronic lymphocytic leukemiaClin Cancer Res Epub2016622
  • ClearyMMThompsonRMahmoodSPacritinib, a dual FLT3/JAK2 inhibitor, reduces IRAK-1 signaling in acute myeloid leukemiaProceedings of the 57th Annual Meeting of the American Society of HematologyDecember 5–8, 2015Orlando, FL Abstract 570
  • Jakafi® (ruxolitinib) tablets, for oral use [prescribing information]Wilmington, DEIncyte Corporation2011
  • GotlibJJAK inhibition in the myeloproliferative neoplasms: lessons learned from the bench and bedsideHematology Am Soc Hematol Educ Program2013201352953724319228
  • GowinKEmanuelRGeyerHMesaRAThe new landscape of therapy for myelofibrosisCurr Hematol Malig Rep20138432533224101258
  • FurqanMMukhiNLeeBLiuDDysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical applicationBiomark Res201311524252238
  • PardananiALashoTSmithGBurnsCJFantinoETefferiACYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patientsLeukemia20092381441144519295546
  • ZhouTGeorgeonSMoserRMooreDJCaflischAHantschelOSpecificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348)Leukemia201428240440723823659
  • LooyengaBDHutchingsDCherniIKingsleyCWeissGJMackeiganJPSTAT3 is activated by JAK2 independent of key oncogenic driver mutations in non-small cell lung carcinomaPLoS One201272e3082022319590
  • HeineAHeldSADaeckeSNThe JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivoBlood201312271192120223770777
  • SchonbergKRudolphJVonnahmeMJAK inhibition impairs NK cell function in myeloproliferative neoplasmsCancer Res201575112187219925832652
  • TefferiARuxolitinib targets DCs: for better or worse?Blood201312271096109723950171
  • GhoreschiKLaurenceAO’SheaJJSelectivity and therapeutic inhibition of kinases: to be or not to be?Nat Immunol200910435636019295632
  • BoldinMPTaganovKDRaoDSmiR-146a is a significant brake on autoimmunity, myeloproliferation, and cancer in miceJ Exp Med201120861189120121555486
  • ZhaoJLRaoDSBoldinMPTaganovKDO’ConnellRBaltimoreDNF-κB dysregulation in microRNA-146a-deficient mice drives the development of myeloid malignanciesProc Natl Acad Sci U S A2011108229184918921576471
  • WangJQJeelallYSFergusonLLHorikawaKToll-like receptors and cancer: MYD88 mutation and inflammationFront Immunol2014536725132836
  • AgarwalABummTGCorbinASAbsence of SKP2 expression attenuates BCR-ABL-induced myeloproliferative diseaseBlood200811251960197018559973
  • McClearyMMThompsonRMahmoodSPacritinib, a dual FLT3/JAK2 inhibitor, reduces Irak-1 signaling in acute myeloid leukemiaProceedings of the 57th Annual Meeting of the American Society of HematologyDecember 5–8, 2015Orlando, FL Abstract 570
  • MaYRixLRZhangQPacritinib (PAC) synergistically potentiates azacitidine (5AZA) cytotoxicity in chronic myelomonocytic leukemia (CMML)Proceedings of the 57th Annual Meeting of the American Society of HematologyDecember 5–8, 2015Orlando, FL Abstract 1658
  • UgelSDe SanctisFMandruzzatoSBronteVTumor-induced myeloid deviation: when myeloid-derived suppressor cells meet tumor-associated macrophagesJ Clin Invest201512593365337626325033
  • BurgerJATsukadaNBurgerMZvaiflerNJDell’AquilaMKippsTJBlood-derived nurse-like cells protect chronic lymphocytic leukemia B cells from spontaneous apoptosis through stromal cell-derived factor-1Blood20009682655266311023495
  • TapWDWainbergZAAnthonySPStructure-guided blockade of csf1r kinase in tenosynovial giant-cell tumorN Engl J Med2015373542843726222558
  • PaniaguaRTChangAMarianoMMc-Fms-mediated differentiation and priming of monocyte lineage cells play a central role in autoimmune arthritisArthritis Res Ther2010121R3220181277
  • BlonskaMAgarwalNKVegaFShaping of the tumor microenvironment: Stromal cells and vesselsSemin Cancer Biol20153431325794825
  • BorgeMNanniniPRMorandePECXCL12 is a costimulator for CD4+ T cell activation and proliferation in chronic lymphocytic leukemia patientsCancer Immunol Immunother201362111312422842611
  • BorgeMRemes LenicovFNanniniPRThe expression of sphingosine-1 phosphate receptor-1 in chronic lymphocytic leukemia cells is impaired by tumor microenvironmental signals and enhanced by piceatannol and R406J Immunol201419363165317425127862
  • BurgerJAKippsTJChemokine receptors and stromal cells in the homing and homeostasis of chronic lymphocytic leukemia B cellsLeuk Lymphoma200243346146612002747
  • KnapperSGrechACahalinPAn evaluation of the tyrosine kinase inhibitor pacritinib in patients with relapsed FLT-3 mutated acute myeloid leukaemia (the UK NCRI AML 17 study)Poster presented at: 21st Congress of the European Hematology AssociationJune 9–12, 2016Copenhagen, Denmark Abstract P184