Drug General Information
Drug ID D07HOB
Drug Name Irinotecan
Synonyms Biotecan; Camptosar; Irinotecanum; IRINOTECAN HYDROCHLORIDE Trihydrate; Irinotecan Hcl; Irinotecan hydrochloride; CP0; Biotecan (TN); Campto (TN); Camptosar (TN); Irinotecan (INN); Irinotecan [INN:BAN]; Irinotecanum [INN-Latin]; IRINOTECAN, CPT-11; Camptosar, Campto, CPT-11, Irinotecan; (+)-Irinotecan; (4S)-4,11-DIETHYL-4-HYDROXY-3,14-DIOXO-3,4,12,14-TETRAHYDRO-1H-PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLIN-9-YL 1,4'-BIPIPERIDINE-1'-CARBOXYLATE; (4S)-4,11-Diethyl-4-hydroxy-3,14-dioxo-4,12-dihydro-1H-pyrano[3,4-f]quinolino[2,3-a]indolizin-9-yl 4-piperidylpiperidinecarboxylate; Irinotecan (TOPO1 inhibitor); Onivyde
Drug Type Small molecular drug
Therapeutic Class Anticancer Agents
Company Pfizer Pharmaceuticals
Structure D07HOB
Drug Resistance Mutations
Target Name UDP-glucuronosyltransferase 1-1 (UGT1A1) Target Info
Gene Name UGT1A1
Uniprot ID UD11_HUMAN
Species Homo sapiens
Reference Sequence MAVESQGGRPLVLGLLLCVLGPVVSHAGKILLIPVDGSHWLSMLGAIQQLQQRGHEIVVL
APDASLYIRDGAFYTLKTYPVPFQREDVKESFVSLGHNVFENDSFLQRVIKTYKKIKKDS
AMLLSGCSHLLHNKELMASLAESSFDVMLTDPFLPCSPIVAQYLSLPTVFFLHALPCSLE
FEATQCPNPFSYVPRPLSSHSDHMTFLQRVKNMLIAFSQNFLCDVVYSPYATLASEFLQR
EVTVQDLLSSASVWLFRSDFVKDYPRPIMPNMVFVGGINCLHQNPLSQEFEAYINASGEH
GIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDL
LGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTS
EDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHD
LTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH [Homo
sapiens]
Targeted Disease Colorectal cancer
Drug Resistance Mutations
Mutation info Missense: P229Q [1]
Target Name Toposisomerase-1 (TOP1) Target Info
Gene Name TOP1
Uniprot ID TOP1_HUMAN
Species Homo sapiens
Reference Sequence MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKK
HKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEP
EDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKD
KDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKF
YYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC
DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGL
FRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENI
QGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALY
FIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNK
VPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ
QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLAD
ARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSK
LNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF [Homo sapiens]
Targeted Disease Colorectal cancer
Drug Resistance Mutations
Mutation info Missense: E710G [2]
Mutation info Missense: L617H [2]
Mutation info Missense: R621I [2]
References
REF 1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 2 New Topoisomerase I mutations are associated with resistance to camptothecin.Mol Cancer.2011 May 27;10:64.

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