Drug General Information
Drug ID D0AZ3C
Drug Name Imatinib
Synonyms Cgp 57148; Glamox; Glamox (TN); Gleevec (TN); Glivec (TN); Imatinib (INN); Imatinib (STI571); Imatinib Methansulfonate; Imatinib [INN:BAN]; 112GI019; 152459-95-5; BKJ8M8G5HI; CCRIS 9076; CGP-57148; CHEMBL941; Imatinib free base; STI; UNII-BKJ8M8G5HI
Drug Type Small molecular drug
Therapeutic Class Anticancer Agents
Company Novartis AG
Structure D0AZ3C
Drug Resistance Mutations
Target Name Tyrosine-protein kinase ABL1(ABL1) Target Info
Gene Name ABL1
Uniprot ID ABL1_HUMAN
Species Homo sapiens
Reference Sequence MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSE
NDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVN
SLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTAS
DGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERT
DITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQ
LLGVCTREPPFYIITEFMTYGNLLDYLRECNRQEVNAVVLLYMATQISSAMEYLEKKNFI
HRDLAARNCLVGENHLVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKS
DVWAFGVLLWEIATYGMSPYPGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNP
SDRPSFAEIHQAFETMFQESSISDEVEKELGKQGVRGAVSTLLQAPELPTKTRTSRRAAE
HRDTTDVPEMPHSKGQGESDPLDHEPAVSPLLPRKERGPPEGGLNEDERLLPKDKKTNLF
SALIKKKKKTAPTPPKRSSSFREMDGQPERRGAGEEEGRDISNGALAFTPLDTADPAKSP
KPSNGAGVPNGALRESGGSGFRSPHLWKKSSTLTSSRLATGEEEGGGSSSKRFLRSCSAS
CVPHGAKDTEWRSVTLPRDLQSTGRQFDSSTFGGHKSEKPALPRKRAGENRSDQVTRGTV
TPPPRLVKKNEEAADEVFKDIMESSPGSSPPNLTPKPLRRQVTVAPASGLPHKEEAGKGS
ALGTPAAAEPVTPTSKAGSGAPGGTSKGPAEESRVRRHKHSSESPGRDKGKLSRLKPAPP
PPPAASAGKAGGKPSQSPSQEAAGEAVLGAKTKATSLVDAVNSDAAKPSQPGEGLKKPVL
PATPKPQSAKPSGTPISPAPVPSTLPSASSALAGDQPSSTAFIPLISTRVSLRKTRQPPE
RIASGAITKGVVLDSTEALCLAISRNSEQMASHSAVLEAGKNLYTFCVSYVDSIQQMRNK
FAFREAINKLENNLRELQICPATAGSGPAATQDFSKLLSSVKEISDIVQR [Homo sap
iens]
Targeted Disease Gastrointestinal stromal tumor; Leukemia
Drug Resistance Mutations
Mutation info Missense: T315I [1]
Mutation Frequency 9 out of 94 patients
Mutation info Missense: F317L [1]
Mutation Frequency 9 out of 94 patients
Mutation info Missense: M244V [2]
Mutation Frequency 8 out of 53 patients
Mutation info Missense: M351T [3]
Mutation Frequency 7 out of 77 patients
Mutation info Missense: E355G [4]
Mutation Frequency 7 out of 17 patients
Mutation info Missense: Y253H [5]
Mutation Frequency 6 out of 60 patients
Mutation info Missense: G250E [6]
Mutation Frequency 6 out of 36 patients
Mutation info Missense: E255K [1]
Mutation Frequency 4 out of 94 patients
Mutation info Missense: F359V [2]
Mutation Frequency 4 out of 53 patients
Mutation info Missense: V379I [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: S417Y [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: F311L [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: H396R [1]
Mutation Frequency 3 out of 94 patients
Mutation info Missense: E255V [1]
Mutation Frequency 3 out of 94 patients
Mutation info Missense: Y253F [2]
Mutation Frequency 3 out of 53 patients
Mutation info Missense: F486S [2]
Mutation Frequency 3 out of 53 patients
Mutation info Missense: L387M [8]
Mutation Frequency 3 out of 40 patients
Mutation info Missense: L248V [9]
Mutation Frequency 27 out of 144 patients
Mutation info Missense: Q252H [10]
Mutation Frequency 23 out of 66 patients in all ABL mutations
Mutation info Missense: E459K [1]
Mutation Frequency 2 out of 94 patients
Mutation info Missense: F359C [1]
Mutation Frequency 2 out of 94 patients
Mutation info Missense: F311I [1]
Mutation Frequency 2 out of 94 patients
Mutation info Missense: E459G [1]
Mutation Frequency 2 out of 94 patients
Mutation info Missense: F359I [2]
Mutation Frequency 2 out of 53 patients
Mutation info Missense: L298V [6]
Mutation Frequency 2 out of 36 patients
Mutation info Missense: D276G [11]
Mutation Frequency 16 out of 49 patients in all ABL mutations
Mutation info Missense: L364I [1]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: A397P [3]
Mutation Frequency 1 out of 77 patients
Mutation info Missense: E450G [12]
Mutation Frequency 1 out of 62 patients
Mutation info Missense: H396P [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: L384M [13]
Mutation Frequency 1 out of 4 patients
Mutation info Missense: V299L [14], [15], [16], [17]
Mutation info Missense: M388L [1], [2], [14]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: F382L [18], [2], [14]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: E450A [12], [19], [14]
Mutation Frequency 1 out of 62 patients
Mutation info Missense: I418V [2], [19], [14]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: A433T [1], [20], [14]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: E292V [1], [2], [14]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: E355A [1], [14], [21]
Mutation Frequency 2 out of 94 patients
Mutation info Missense: E453K [1], [2], [14]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: F317V [8], [14], [17]
Mutation Frequency 1 out of 40 patients
Mutation info Missense: L273M [2], [22], [14]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: T277A [14], [15], [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: V289F [6], [23], [21]
Mutation Frequency 1 out of 40 patients
Mutation info Missense: S438C [14], [15], [24]
Mutation info Missense: M343T [18], [14]
Mutation info Missense: Q252R [18], [14]
Mutation info Missense: E450K [25], [14]
Mutation Frequency 1 out of 55 patients
Mutation info Missense: F317C [14], [17]
Mutation info Missense: F317I [14], [17]
Mutation info Missense: L324Q [14], [26]
Mutation info Missense: P480L [25], [14]
Mutation Frequency 1 out of 55 patients
Mutation info Missense: E279K [14], [27]
Mutation info Missense: Y320C [14], [15]
Mutation info Missense: E453A [14], [24]
Mutation info Missense: L387F [14], [24]
Mutation info Missense: E275K [14], [28]
Mutation info Missense: E453G [14], [28]
Mutation info Missense: V289A [14]
Mutation info Missense: A399T [15]
Mutation info Missense: F359A [11]
Mutation Frequency 16 out of 49 patients in all ABL mutations
Mutation info Missense: T315N [11]
Mutation Frequency 16 out of 49 patients in all ABL mutations
Mutation info Missense: Q252E [29]
Mutation Frequency 30% of the patients
Mutation info Missense: E459Q [1]
Mutation Frequency 1 out of 94 patients
Mutation info Missense: D482V [2]
Mutation Frequency 4 out of 53 patients
Mutation info Missense: E279Z [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: E282G [2]
Mutation Frequency 2 out of 53 patients
Mutation info Missense: E352D [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: E352G [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: E453D [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: G251D [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: R328M [2]
Mutation Frequency 1 out of 53 patients
Mutation info Missense: N374Y [30]
Mutation info Missense: E279Y [19]
Mutation info Missense: E355? [19]
Mutation info Missense: E450? [19]
Mutation info Missense: E453L [19]
Mutation info Missense: F359* [19]
Mutation info Missense: F359? [19]
Mutation info Missense: Q252K [20]
Mutation Frequency 1 out of 21 patients
Mutation info Missense: K294 > RGG [31]
Mutation info Missense: A344V [14]
Mutation info Missense: A350V [14]
Mutation info Missense: A365V [14]
Mutation info Missense: A366G [14]
Mutation info Missense: A380T [14]
Mutation info Missense: D363Y [14]
Mutation info Missense: E258D [14]
Mutation info Missense: E275Q [14]
Mutation info Missense: E292Q [14]
Mutation info Missense: E355D [14]
Mutation info Missense: E373K [14]
Mutation info Missense: E450V [14]
Mutation info Missense: E453V [14]
Mutation info Missense: E459A [14]
Mutation info Missense: E459V [14]
Mutation info Missense: E507G [14]
Mutation info Missense: F359L [14]
Mutation info Missense: G250R [14]
Mutation info Missense: H396A [14]
Mutation info Missense: I242T [14]
Mutation info Missense: I293V [14]
Mutation info Missense: I418S [14]
Mutation info Missense: K247R [14]
Mutation info Missense: L370P [14]
Mutation info Missense: L387V [14]
Mutation info Missense: M237V [14]
Mutation info Missense: M472I [14]
Mutation info Missense: S417F [14]
Mutation info Missense: V280A [14]
Mutation info Missense: V289I [14]
Mutation info Missense: V371A [14]
Mutation info Missense: W261L [14]
Mutation info Missense: Y342H [14]
Mutation info Missense: Y393C [14]
Mutation info Missense: Y353H [6]
Mutation Frequency 4 out of 36 patients
Mutation info Missense: K419E [27]
Mutation info Missense: E494G [15]
Mutation info Missense: K378R [15]
Mutation info Missense: M351K [15]
Mutation info Missense: V256L [15]
Mutation info Missense: T315A [17]
Mutation info Missense: D276A [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: L340L [7]
Mutation Frequency 38 out of 45 patients
Mutation info Missense: D276N [24]
Mutation info Missense: E279A [24]
Mutation info Missense: G251E [21]
Mutation Frequency 1 out of 125 patients
Mutation info Missense: N368S [21]
Mutation Frequency 1 out of 125 patients
Mutation info Missense: G398R [32]
Mutation Frequency 33% of the patients
Target Name Mast/stem cell growth factor receptor Kit (KIT) Target Info
Gene Name KIT
Uniprot ID KIT_HUMAN
Species Homo sapiens
Reference Sequence MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV [Homo sapiens]
Targeted Disease Gastrointestinal stromal tumor; Leukemia
Drug Resistance Mutations
Mutation info Missense: V654A [33]
Mutation Frequency 9 out of 33 patients
Mutation info Missense: Y823D [34]
Mutation Frequency 9 out of 32 patients
Mutation info Missense: N822K [36]
Mutation Frequency 8 out of 10 patients in all KIT mutations
Mutation info Missense: D816H [36]
Mutation Frequency 8 out of 10 patients in all KIT mutations
Mutation info Missense: C809G [36]
Mutation Frequency 8 out of 10 patients in all KIT mutations
Mutation info Missense: T670I [37]
Mutation Frequency 3 out of 78 patients
Mutation info Missense: D820Y [33]
Mutation Frequency 3 out of 33 patients
Mutation info Missense: D820E [33]
Mutation Frequency 3 out of 33 patients
Mutation info Missense: D820G [38]
Mutation Frequency 21 out of 33 patients in all KIT mutations
Mutation info Missense: A829P [37]
Mutation Frequency 2 out of 78 patients
Mutation info Missense: H697Y [39], [40], [41]
Mutation info Missense: V559I [39], [40], [41]
Mutation info Missense: N822Y [38], [42], [33]
Mutation Frequency 3 out of 33 patients
Mutation info Missense: T670E [43], [33]
Mutation Frequency 14 out of 32 patients in all KIT mutations
Mutation info Missense: D820A [38], [37]
Mutation Frequency 21 out of 33 patients in all KIT mutations
Mutation info Missense: D816E [43], [44]
Mutation Frequency 14 out of 32 patients in all KIT mutations
Mutation info Missense: K642E [34], [33]
Mutation Frequency 1 out of 33 patients
Mutation info Missense: D816G [46]
Mutation info Missense: D716N [46]
Mutation info Missense: S709F [43]
Mutation info Missense: D816A [37]
Mutation Frequency 1 out of 78 patients
Mutation info Missense: S821F [47]
Mutation Frequency 1 out of 3 patients
Mutation info Deletion: D579 [33]
Mutation Frequency 1 out of 33 patients
Mutation info Missense: N680K [33]
Mutation Frequency 1 out of 33 patients
Mutation info Missense: Y578C [33]
Mutation Frequency 2 out of 33 patients
Target Name Platelet-derived growth factor receptor alpha (PDGFRA) Target Info
Gene Name PDGFRA
Uniprot ID PGFRA_HUMAN
Species Homo sapiens
Reference Sequence MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYP
MSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIY
VPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNG
TFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNN
EVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVK
EMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENL
TEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDL
VDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRD
RSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVII
SLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLG
SGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNL
LGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSY
VILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKN
LLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLA
RDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMM
VDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKK
SYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYII
PLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDS
SDLVEDSFL [Homo sapiens]
Targeted Disease Gastrointestinal stromal tumor; Leukemia
Drug Resistance Mutations
Mutation info Missense: D842V [35]
Mutation Frequency 9 out of 18 patients
Target Name Serine/threonine-protein kinase (B-raf) Target Info
Gene Name BRAF
Uniprot ID BRAF_HUMAN
Species Homo sapiens
Reference Sequence MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEH
IEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTV
TSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDS
LKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRK
TFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPI
PQEEASLAETALTSGSSPSAPASDSIGPQILTSPSPSKSIPIPQPFRPADEDHRNQFGQR
DRSSSAPNVHINTIEPVNIDDLIRDQGFRGDGGSTTGLSATPPASLPGSLTNVKALQKSP
GPQRERKSSSSSEDRNRMKTLGRRDSSDDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDV
AVKMLNVTAPTPQQLQAFKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHH
LHIIETKFEMIKLIDIARQTAQGMDYLHAKSIIHRDLKSNNIFLHEDLTVKIGDFGLATV
KSRWSGSHQFEQLSGSILWMAPEVIRMQDKNPYSFQSDVYAFGIVLYELMTGQLPYSNIN
NRDQIIFMVGRGYLSPDLSKVRSNCPKAMKRLMAECLKKKRDERPLFPQILASIELLARS
LPKIHRSASEPSLNRAGFQTEDFSLYACASPKTPIQAGGYGAFPVH [Homo sapiens
]
Targeted Disease Gastrointestinal stromal tumor; Leukemia
Drug Resistance Mutations
Mutation info Missense: V600E [45]
References
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REF 3 BCR-ABL isoforms associated with intrinsic or acquired resistance to imatinib: more heterogeneous than just ABL kinase domain point mutations Med Oncol. 2012 Mar;29(1):219-26.
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