EA016487B1 - Лечение резистентных к лекарственным препаратам опухолей - Google Patents
Лечение резистентных к лекарственным препаратам опухолей Download PDFInfo
- Publication number
- EA016487B1 EA016487B1 EA200870073A EA200870073A EA016487B1 EA 016487 B1 EA016487 B1 EA 016487B1 EA 200870073 A EA200870073 A EA 200870073A EA 200870073 A EA200870073 A EA 200870073A EA 016487 B1 EA016487 B1 EA 016487B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- tumor
- drug
- leukemia
- topoisomerase
- resistant
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims abstract description 33
- 239000003814 drug Substances 0.000 title claims abstract description 26
- 229940079593 drug Drugs 0.000 title claims abstract description 18
- 108090000323 DNA Topoisomerases Proteins 0.000 claims abstract description 25
- 102000003915 DNA Topoisomerases Human genes 0.000 claims abstract description 25
- 108090000623 proteins and genes Proteins 0.000 claims abstract description 8
- 102000054765 polymorphisms of proteins Human genes 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 5
- 208000032839 leukemia Diseases 0.000 claims description 5
- 208000025113 myeloid leukemia Diseases 0.000 claims description 5
- 201000001514 prostate carcinoma Diseases 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims description 2
- 206010007275 Carcinoid tumour Diseases 0.000 claims description 2
- 206010052399 Neuroendocrine tumour Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 210000000988 bone and bone Anatomy 0.000 claims description 2
- 208000002458 carcinoid tumor Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 208000016065 neuroendocrine neoplasm Diseases 0.000 claims description 2
- 201000011519 neuroendocrine tumor Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010024305 Leukaemia monocytic Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000006894 monocytic leukemia Diseases 0.000 claims 1
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical class C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 abstract description 24
- 238000002360 preparation method Methods 0.000 abstract description 3
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 17
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 description 13
- 229940127093 camptothecin Drugs 0.000 description 13
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 description 13
- 241001465754 Metazoa Species 0.000 description 11
- 210000004027 cell Anatomy 0.000 description 11
- 239000002609 medium Substances 0.000 description 10
- 230000037396 body weight Effects 0.000 description 9
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 description 9
- 229960000303 topotecan Drugs 0.000 description 8
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 8
- 230000035772 mutation Effects 0.000 description 7
- 229920001817 Agar Polymers 0.000 description 6
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 description 6
- 239000008272 agar Substances 0.000 description 6
- 239000002246 antineoplastic agent Substances 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 229960004768 irinotecan Drugs 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 206010033128 Ovarian cancer Diseases 0.000 description 5
- UIVFUQKYVFCEKJ-OPTOVBNMSA-N gimatecan Chemical compound C1=CC=C2C(\C=N\OC(C)(C)C)=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UIVFUQKYVFCEKJ-OPTOVBNMSA-N 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 4
- 229930012538 Paclitaxel Natural products 0.000 description 4
- 101710183280 Topoisomerase Proteins 0.000 description 4
- 230000000259 anti-tumor effect Effects 0.000 description 4
- 238000010790 dilution Methods 0.000 description 4
- 239000012895 dilution Substances 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 229960001592 paclitaxel Drugs 0.000 description 4
- 239000007858 starting material Substances 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 210000004881 tumor cell Anatomy 0.000 description 4
- 210000005253 yeast cell Anatomy 0.000 description 4
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 3
- 229960004562 carboplatin Drugs 0.000 description 3
- 239000000969 carrier Substances 0.000 description 3
- 229930182830 galactose Natural products 0.000 description 3
- 229950009073 gimatecan Drugs 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- 230000012010 growth Effects 0.000 description 3
- XIXADJRWDQXREU-UHFFFAOYSA-M lithium acetate Chemical compound [Li+].CC([O-])=O XIXADJRWDQXREU-UHFFFAOYSA-M 0.000 description 3
- 230000007170 pathology Effects 0.000 description 3
- 238000013207 serial dilution Methods 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 229940035893 uracil Drugs 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 101000830681 Homo sapiens DNA topoisomerase 1 Proteins 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 229940123237 Taxane Drugs 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- BFNBIHQBYMNNAN-UHFFFAOYSA-N ammonium sulfate Chemical compound N.N.OS(O)(=O)=O BFNBIHQBYMNNAN-UHFFFAOYSA-N 0.000 description 2
- 229910052921 ammonium sulfate Inorganic materials 0.000 description 2
- 235000011130 ammonium sulphate Nutrition 0.000 description 2
- 230000001093 anti-cancer Effects 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 238000004113 cell culture Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000002512 chemotherapy Methods 0.000 description 2
- 229940127089 cytotoxic agent Drugs 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 239000013612 plasmid Substances 0.000 description 2
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 230000004044 response Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 231100001274 therapeutic index Toxicity 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 230000001131 transforming effect Effects 0.000 description 2
- 238000002054 transplantation Methods 0.000 description 2
- 230000004614 tumor growth Effects 0.000 description 2
- 239000013598 vector Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- FBDOJYYTMIHHDH-OZBJMMHXSA-N (19S)-19-ethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-2,4,6,8,10,14,20-heptaen-18-one Chemical compound CC[C@@]1(O)C(=O)OCC2=CN3Cc4cc5ccccc5nc4C3C=C12 FBDOJYYTMIHHDH-OZBJMMHXSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 229930024421 Adenine Natural products 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
- 101100454193 Arabidopsis thaliana AAA1 gene Proteins 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- 201000007651 Brooke-Spiegler syndrome Diseases 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 108020004705 Codon Proteins 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 1
- 206010010356 Congenital anomaly Diseases 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 206010013710 Drug interaction Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 241000402754 Erythranthe moschata Species 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- 102000048120 Galactokinases Human genes 0.000 description 1
- 108700023157 Galactokinases Proteins 0.000 description 1
- 102000003886 Glycoproteins Human genes 0.000 description 1
- 108090000288 Glycoproteins Proteins 0.000 description 1
- 208000017604 Hodgkin disease Diseases 0.000 description 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
- 229920004011 Macrolon® Polymers 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000001888 Peptone Substances 0.000 description 1
- 108010080698 Peptones Proteins 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 1
- 229920000954 Polyglycolide Polymers 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 239000007984 Tris EDTA buffer Substances 0.000 description 1
- 229960000643 adenine Drugs 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 description 1
- 229940077388 benzenesulfonate Drugs 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 101150107661 bot1 gene Proteins 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000002060 circadian Effects 0.000 description 1
- 229940001468 citrate Drugs 0.000 description 1
- 239000004927 clay Substances 0.000 description 1
- 238000010367 cloning Methods 0.000 description 1
- 239000007376 cm-medium Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 description 1
- 229960003668 docetaxel Drugs 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 238000010410 dusting Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 229940050410 gluconate Drugs 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 230000003862 health status Effects 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 102000056859 human TOP1 Human genes 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 1
- 125000001841 imino group Chemical group [H]N=* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 238000001361 intraarterial administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000007914 intraventricular administration Methods 0.000 description 1
- 229940001447 lactate Drugs 0.000 description 1
- 150000002596 lactones Chemical class 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 208000003747 lymphoid leukemia Diseases 0.000 description 1
- 229920002521 macromolecule Polymers 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000036457 multidrug resistance Effects 0.000 description 1
- 210000005170 neoplastic cell Anatomy 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 239000006179 pH buffering agent Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 235000019319 peptone Nutrition 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000013600 plasmid vector Substances 0.000 description 1
- 150000003057 platinum Chemical class 0.000 description 1
- 229910052697 platinum Inorganic materials 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- VHXNKPBCCMUMSW-FQEVSTJZSA-N rubitecan Chemical compound C1=CC([N+]([O-])=O)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VHXNKPBCCMUMSW-FQEVSTJZSA-N 0.000 description 1
- 229950009213 rubitecan Drugs 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 238000002741 site-directed mutagenesis Methods 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05027997 | 2005-12-21 | ||
| PCT/EP2006/069666 WO2007071603A1 (en) | 2005-12-21 | 2006-12-13 | Treatment of drug-resistant tumors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200870073A1 EA200870073A1 (ru) | 2009-12-30 |
| EA016487B1 true EA016487B1 (ru) | 2012-05-30 |
Family
ID=35911064
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200870073A EA016487B1 (ru) | 2005-12-21 | 2006-12-13 | Лечение резистентных к лекарственным препаратам опухолей |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7888368B2 (enExample) |
| EP (1) | EP1962850B1 (enExample) |
| JP (1) | JP5657205B2 (enExample) |
| KR (1) | KR101366868B1 (enExample) |
| CN (1) | CN101340910B (enExample) |
| AT (1) | ATE548038T1 (enExample) |
| AU (1) | AU2006328607B2 (enExample) |
| BR (1) | BRPI0620209A2 (enExample) |
| CA (1) | CA2631868C (enExample) |
| CY (1) | CY1112814T1 (enExample) |
| DK (1) | DK1962850T3 (enExample) |
| EA (1) | EA016487B1 (enExample) |
| ES (1) | ES2382819T3 (enExample) |
| HR (1) | HRP20120359T1 (enExample) |
| PL (1) | PL1962850T3 (enExample) |
| PT (1) | PT1962850E (enExample) |
| RS (1) | RS52272B (enExample) |
| SI (1) | SI1962850T1 (enExample) |
| WO (1) | WO2007071603A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008098701A1 (en) * | 2007-02-13 | 2008-08-21 | Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. | Broad-spectrum anti-cancer treatment based on iminocamptothecin derivatives |
| JP5765937B2 (ja) * | 2007-08-01 | 2015-08-19 | シグマ−タウ・インドゥストリエ・ファルマチェウチケ・リウニテ・ソシエタ・ペル・アチオニＳｉｇｍａ−Ｔａｕ Ｉｎｄｕｓｔｒｉｅ Ｆａｒｍａｃｅｕｔｉｃｈｅ Ｒｉｕｎｉｔｅ Ｓｏｃｉｅｔａ Ｐｅｒ Ａｚｉｏｎｉ | 小児腫瘍の治療 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997031003A1 (en) * | 1996-02-23 | 1997-08-28 | Istituto Nazionale Per Lo Studio E La Cura Dei Tumori | Camptothecin derivatives and the use thereof as antitumor agents |
| EP1044977A1 (en) * | 1999-03-09 | 2000-10-18 | Sigma-Tau Industrie Farmaceutiche Riunite S.p.A. | Camptothecin derivatives having antitumor activity |
-
2006
- 2006-12-13 BR BRPI0620209-8A patent/BRPI0620209A2/pt not_active IP Right Cessation
- 2006-12-13 SI SI200631316T patent/SI1962850T1/sl unknown
- 2006-12-13 PT PT06830600T patent/PT1962850E/pt unknown
- 2006-12-13 EP EP06830600A patent/EP1962850B1/en active Active
- 2006-12-13 WO PCT/EP2006/069666 patent/WO2007071603A1/en not_active Ceased
- 2006-12-13 CN CN2006800482417A patent/CN101340910B/zh not_active Expired - Fee Related
- 2006-12-13 RS RS20120175A patent/RS52272B/sr unknown
- 2006-12-13 DK DK06830600.0T patent/DK1962850T3/da active
- 2006-12-13 CA CA2631868A patent/CA2631868C/en not_active Expired - Fee Related
- 2006-12-13 JP JP2008546388A patent/JP5657205B2/ja not_active Expired - Fee Related
- 2006-12-13 US US12/096,884 patent/US7888368B2/en not_active Expired - Fee Related
- 2006-12-13 ES ES06830600T patent/ES2382819T3/es active Active
- 2006-12-13 AU AU2006328607A patent/AU2006328607B2/en not_active Ceased
- 2006-12-13 EA EA200870073A patent/EA016487B1/ru not_active IP Right Cessation
- 2006-12-13 KR KR1020087016809A patent/KR101366868B1/ko not_active Expired - Fee Related
- 2006-12-13 HR HRP20120359TT patent/HRP20120359T1/hr unknown
- 2006-12-13 AT AT06830600T patent/ATE548038T1/de active
- 2006-12-13 PL PL06830600T patent/PL1962850T3/pl unknown
-
2012
- 2012-06-01 CY CY20121100497T patent/CY1112814T1/el unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997031003A1 (en) * | 1996-02-23 | 1997-08-28 | Istituto Nazionale Per Lo Studio E La Cura Dei Tumori | Camptothecin derivatives and the use thereof as antitumor agents |
| EP1044977A1 (en) * | 1999-03-09 | 2000-10-18 | Sigma-Tau Industrie Farmaceutiche Riunite S.p.A. | Camptothecin derivatives having antitumor activity |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101340910A (zh) | 2009-01-07 |
| EP1962850A1 (en) | 2008-09-03 |
| HRP20120359T1 (hr) | 2012-06-30 |
| JP2009520754A (ja) | 2009-05-28 |
| CN101340910B (zh) | 2012-12-12 |
| WO2007071603A1 (en) | 2007-06-28 |
| DK1962850T3 (da) | 2012-06-18 |
| ES2382819T3 (es) | 2012-06-13 |
| US7888368B2 (en) | 2011-02-15 |
| PL1962850T3 (pl) | 2012-07-31 |
| AU2006328607A1 (en) | 2007-06-28 |
| CA2631868C (en) | 2014-02-11 |
| HK1124776A1 (zh) | 2009-07-24 |
| CA2631868A1 (en) | 2007-06-28 |
| BRPI0620209A2 (pt) | 2011-11-01 |
| PT1962850E (pt) | 2012-05-21 |
| ATE548038T1 (de) | 2012-03-15 |
| AU2006328607B2 (en) | 2012-04-19 |
| JP5657205B2 (ja) | 2015-01-21 |
| EP1962850B1 (en) | 2012-03-07 |
| CY1112814T1 (el) | 2016-02-10 |
| EA200870073A1 (ru) | 2009-12-30 |
| RS52272B (sr) | 2012-10-31 |
| KR101366868B1 (ko) | 2014-02-21 |
| KR20080078055A (ko) | 2008-08-26 |
| SI1962850T1 (sl) | 2012-06-29 |
| US20080312265A1 (en) | 2008-12-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2010333082B2 (en) | 3-(indolyl)-or 3-(azaindolyl)- 4-arylmaleimide derivatives for use in the treatment of colon and gastric adenocarzinoma | |
| US20190298693A1 (en) | Yap1 inhibitors and methods | |
| TW202039439A (zh) | ４（１ｈ）－奎諾酮衍生物及其用途 | |
| Kurtzberg et al. | Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment | |
| US20210154219A1 (en) | Compounds and Methods for Treating Cancer | |
| CN106975079A (zh) | 含usp13抑制剂和parp抑制剂的药物组合物及其应用 | |
| Kurtzberg et al. | Bone marrow and tumor cell colony-forming units and human tumor xenograft efficacy of noncamptothecin and camptothecin topoisomerase I inhibitors | |
| Wang et al. | Antisense anti-MDM2 mixed-backbone oligonucleotides enhance therapeutic efficacy of topoisomerase I inhibitor irinotecan in nude mice bearing human cancer xenografts: in vivo activity and mechanisms | |
| KR20100051837A (ko) | 소아 종양의 치료 | |
| US20100239522A1 (en) | Chemotherapeutic for inducing an msh2-dependent apoptotic pathway | |
| JP6373252B2 (ja) | オーロラキナーゼ阻害薬を使用する癌の治療方法 | |
| EA016487B1 (ru) | Лечение резистентных к лекарственным препаратам опухолей | |
| De Cesare et al. | Preclinical efficacy of ST1976, a novel camptothecin analog of the 7-oxyiminomethyl series | |
| US8853233B2 (en) | Broad-spectrum anti-cancer treatment based on iminocamptothecin derivatives | |
| TWI472330B (zh) | 用於癌症治療之增敏劑、套組及用途 | |
| Samor et al. | The role of polyamine architecture on the pharmacological activity of open lactone camptothecin− polyamine conjugates | |
| US20210379047A1 (en) | Combination Therapies For Treating Cancer | |
| CN111297870B (zh) | 硝基苯甲酸类化合物在制备治疗肿瘤的药物中的应用 | |
| CN121108109A (zh) | 一种靶向alk蛋白的protac化合物及其抗肿瘤应用 | |
| SK397391A3 (sk) | 9,10-Substituované kamptotecíny, farmaceutický prípravok s ich obsahom a medziprodukt |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |