{"meta":{"totalResults":6,"from":0},"results":[{"aliases":[{"type":"Synonym","name":"irinotecan"},{"type":"CodeName","name":"CPT-11"},{"type":"ForeignBrandName","name":"Campto"},{"type":"USBrandName","name":"Camptosar"},{"type":"CodeName","name":"U-101440E"},{"type":"ForeignBrandName","name":"Irinomedac"},{"type":"ChemicalStructureName","name":"(+)-(4S)-4,11-diethyl-4-hydroxy-9-[(4-piperidino-piperidino)carbonyloxy]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinol-3,14,(4H,12H)-dione"},{"type":"ChemicalStructureName","name":"(+)-7-ethyl-10-hydroxycamptothecine 10-[1,4'-bipiperidine]-1'-carboxylate"},{"type":"ChemicalStructureName","name":"7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin"},{"type":"Synonym","name":"camptothecin-11"},{"type":"Synonym","name":"irinotecan HCl"},{"type":"ChemicalStructureName","name":"[1,4'-bipiperidine]-1'-carboxylic acid (S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester"},{"type":"INDCode","name":"42459"},{"type":"NSCNumber","name":"616348"},{"type":"CASRegistryName","name":"100286-90-6"},{"type":"CASRegistryName","name":"136572-09-3"},{"type":"Synonym","name":"irinotecan hydrochloride trihydrate"},{"type":"Synonym","name":"irinotecan monohydrochloride trihydrate"}],"definition":{"html":"The hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.","text":"The hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/irinotecanhydrochloride","text":"Irinotecan Hydrochloride"},"nciConceptId":"C1381","nciConceptName":"Irinotecan Hydrochloride","termId":41714,"name":"irinotecan hydrochloride","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-hydrochloride"},{"aliases":[{"type":"CodeName","name":"LY01616"},{"type":"CodeName","name":"LY 01616"},{"type":"CodeName","name":"LY-01616"},{"type":"Synonym","name":"liposome LY01616"},{"type":"Synonym","name":"irinotecan/floxuridine liposome LY01616"},{"type":"Synonym","name":"irinotecan HCl/floxuridine liposome LY01616"},{"type":"Synonym","name":"irinotecan and floxuridine liposome LY01616"}],"definition":{"html":"A liposomal formulation composed of a combination of two antineoplastic agents, the hydrochloride (HCl) salt form of irinotecan, a semisynthetic camptothecin analogue, and floxuridine, a fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP), with potential antineoplastic activity. Upon administration of irinotecan HCl/floxuridine liposome LY01616, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Floxuridine, as an antimetabolite, inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. Liposome encapsulation of two antineoplastic agents at an optimal ratio can promote efficient drug delivery, improve efficacy and increase the synergistic effect.\n","text":"A liposomal formulation composed of a combination of two antineoplastic agents, the hydrochloride (HCl) salt form of irinotecan, a semisynthetic camptothecin analogue, and floxuridine, a fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP), with potential antineoplastic activity. Upon administration of irinotecan HCl/floxuridine liposome LY01616, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Floxuridine, as an antimetabolite, inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. Liposome encapsulation of two antineoplastic agents at an optimal ratio can promote efficient drug delivery, improve efficacy and increase the synergistic effect.\n"},"drugInfoSummaryLink":null,"nciConceptId":"C200906","nciConceptName":"Irinotecan Hydrochloride and Floxuridine Liposome LY01616","termId":813125,"name":"irinotecan hydrochloride and floxuridine liposome LY01616","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-hydrochloride-and-floxuridine-liposome-ly01616"},{"aliases":[{"type":"Synonym","name":"liposomal irinotecan HR070803"},{"type":"CodeName","name":"HR070803"},{"type":"CodeName","name":"HR 070803"},{"type":"CodeName","name":"HR-070803"}],"definition":{"html":"A liposomal formulation of the semisynthetic camptothecin analogue irinotecan, with potential antineoplastic activity. Upon administration of irinotecan liposome HR070803, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell.","text":"A liposomal formulation of the semisynthetic camptothecin analogue irinotecan, with potential antineoplastic activity. Upon administration of irinotecan liposome HR070803, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell."},"drugInfoSummaryLink":null,"nciConceptId":"C200345","nciConceptName":"Irinotecan Liposome HR070803","termId":812954,"name":"irinotecan liposome HR070803","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-liposome-hr070803"},{"aliases":[{"type":"CodeName","name":"PEP-02"},{"type":"CodeName","name":"PEP02"},{"type":"USBrandName","name":"Onivyde"},{"type":"CASRegistryName","name":"1361317-83-0"},{"type":"Synonym","name":"irinotecan liposome"},{"type":"CodeName","name":"MM-398"},{"type":"CodeName","name":"MM398"},{"type":"CodeName","name":"MM 398"},{"type":"Synonym","name":"nal-IRI"},{"type":"Synonym","name":"nanoliposomal irinotecan"},{"type":"Synonym","name":"nanoparticle liposome formulation of irinotecan"},{"type":"Synonym","name":"irinotecan hydrochloride as sucrosulfate salt form liposomal formulation"},{"type":"Synonym","name":"nanoliposomal irinotecan as sucrosofate"},{"type":"Synonym","name":"irinotecan sucrosofate-containing pegylated liposomal formulation"},{"type":"Synonym","name":"irinotecan sucrosofate liposome"}],"definition":{"html":"A liposomal dispersion formulated with the semisynthetic camptothecin analogue irinotecan, provided as the hydrochloride trihydrate form, which is encapsulated and entrapped within liposomes in a gelated or precipitated state as the irinotecan sucrose octasulfate (sucrosulfate) salt form, with potential antineoplastic activity. Upon administration of the liposomes containing irinotecan sucrosulfate, irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. During the S-phase, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell, extends the circulation of irinotecan, and prolongs the duration of active therapy at the site of tumor to inhibit tumor growth.","text":"A liposomal dispersion formulated with the semisynthetic camptothecin analogue irinotecan, provided as the hydrochloride trihydrate form, which is encapsulated and entrapped within liposomes in a gelated or precipitated state as the irinotecan sucrose octasulfate (sucrosulfate) salt form, with potential antineoplastic activity. Upon administration of the liposomes containing irinotecan sucrosulfate, irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. During the S-phase, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell, extends the circulation of irinotecan, and prolongs the duration of active therapy at the site of tumor to inhibit tumor growth."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/irinotecan-hydrochloride-liposome","text":"Irinotecan Sucrosofate"},"nciConceptId":"C82676","nciConceptName":"Irinotecan Sucrosofate","termId":632436,"name":"irinotecan sucrosofate","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-sucrosofate"},{"aliases":[{"type":"CodeName","name":"CM-BC2"},{"type":"Synonym","name":"irinotecan hydrochloride drug-eluting beads"}],"definition":{"html":"Microporous hydrospheres of polyvinylalcohol (PVA) impregnated with irinotecan with potential antineoplastic activity. In transarterial chemoembolization (TACE), irinotecan-eluting beads are administered into blood vessels that feed the tumor, occluding tumor blood vessels and inducing ischemic tumor necrosis while simultaneously delivering high-dose chemotherapy locally. Irinotecan, a semisynthetic derivative of camptothecin, inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death.","text":"Microporous hydrospheres of polyvinylalcohol (PVA) impregnated with irinotecan with potential antineoplastic activity. In transarterial chemoembolization (TACE), irinotecan-eluting beads are administered into blood vessels that feed the tumor, occluding tumor blood vessels and inducing ischemic tumor necrosis while simultaneously delivering high-dose chemotherapy locally. Irinotecan, a semisynthetic derivative of camptothecin, inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death."},"drugInfoSummaryLink":null,"nciConceptId":"C82682","nciConceptName":"Irinotecan-Eluting Beads","termId":632992,"name":"irinotecan-eluting beads","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-eluting-beads"},{"aliases":[{"type":"ForeignBrandName","name":"Oratecan"}],"definition":{"html":"An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death.  P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors,  preventing the intracellular accumulation of various cytotoxic agents.\n","text":"An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death.  P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors,  preventing the intracellular accumulation of various cytotoxic agents.\n"},"drugInfoSummaryLink":null,"nciConceptId":"C88280","nciConceptName":"Irinotecan/P-glycoprotein Inhibitor HM30181AK Combination Tablet","termId":656527,"name":"irinotecan/P-glycoprotein inhibitor HM30181AK combination tablet","firstLetter":"i","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"irinotecan-p-glycoprotein-inhibitor-hm30181ak-combination-tablet"}],"links":null}