DE60113975T2 - Verwendung von fulvestrant in der behandlung von resistentem brustkrebs - Google Patents
Verwendung von fulvestrant in der behandlung von resistentem brustkrebs Download PDFInfo
- Publication number
- DE60113975T2 DE60113975T2 DE60113975T DE60113975T DE60113975T2 DE 60113975 T2 DE60113975 T2 DE 60113975T2 DE 60113975 T DE60113975 T DE 60113975T DE 60113975 T DE60113975 T DE 60113975T DE 60113975 T2 DE60113975 T2 DE 60113975T2
- Authority
- DE
- Germany
- Prior art keywords
- treatment
- lesions
- study
- fulvestrant
- breast cancer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 95
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 title claims abstract description 56
- 229960002258 fulvestrant Drugs 0.000 title claims abstract description 51
- 206010006187 Breast cancer Diseases 0.000 title claims abstract description 41
- 208000026310 Breast neoplasm Diseases 0.000 title claims abstract description 32
- 239000003886 aromatase inhibitor Substances 0.000 claims abstract description 17
- 229940122815 Aromatase inhibitor Drugs 0.000 claims abstract description 11
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 37
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 31
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 29
- 229960002932 anastrozole Drugs 0.000 claims description 20
- 229960003437 aminoglutethimide Drugs 0.000 claims description 18
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 claims description 18
- 229960003881 letrozole Drugs 0.000 claims description 18
- 229960001603 tamoxifen Drugs 0.000 claims description 18
- 239000003814 drug Substances 0.000 claims description 14
- 229940079593 drug Drugs 0.000 claims description 12
- 229940088597 hormone Drugs 0.000 claims description 11
- 239000005556 hormone Substances 0.000 claims description 11
- 238000010255 intramuscular injection Methods 0.000 claims description 3
- 239000007927 intramuscular injection Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000000333 selective estrogen receptor modulator Substances 0.000 abstract description 5
- 229940095743 selective estrogen receptor modulator Drugs 0.000 abstract description 5
- 230000003902 lesion Effects 0.000 description 57
- 230000004044 response Effects 0.000 description 44
- 206010028980 Neoplasm Diseases 0.000 description 30
- 201000010099 disease Diseases 0.000 description 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 27
- 206010061728 Bone lesion Diseases 0.000 description 22
- 239000000203 mixture Substances 0.000 description 17
- 206010061818 Disease progression Diseases 0.000 description 16
- 230000005750 disease progression Effects 0.000 description 16
- 239000008194 pharmaceutical composition Substances 0.000 description 15
- 238000009472 formulation Methods 0.000 description 14
- 238000002347 injection Methods 0.000 description 13
- 239000007924 injection Substances 0.000 description 13
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 12
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 12
- 229940011871 estrogen Drugs 0.000 description 12
- 239000000262 estrogen Substances 0.000 description 12
- 230000036961 partial effect Effects 0.000 description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 11
- 238000007469 bone scintigraphy Methods 0.000 description 11
- 238000002595 magnetic resonance imaging Methods 0.000 description 10
- 238000000034 method Methods 0.000 description 9
- 229940046836 anti-estrogen Drugs 0.000 description 8
- 230000001833 anti-estrogenic effect Effects 0.000 description 8
- 230000008901 benefit Effects 0.000 description 8
- 239000000328 estrogen antagonist Substances 0.000 description 8
- 102000015694 estrogen receptors Human genes 0.000 description 8
- 108010038795 estrogen receptors Proteins 0.000 description 8
- 238000012216 screening Methods 0.000 description 8
- 230000002018 overexpression Effects 0.000 description 7
- 230000009885 systemic effect Effects 0.000 description 7
- 206010027476 Metastases Diseases 0.000 description 6
- 229940046844 aromatase inhibitors Drugs 0.000 description 6
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 6
- 201000011510 cancer Diseases 0.000 description 6
- 238000001514 detection method Methods 0.000 description 6
- 238000011156 evaluation Methods 0.000 description 6
- 210000004185 liver Anatomy 0.000 description 6
- 238000002560 therapeutic procedure Methods 0.000 description 6
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 description 5
- 108010082126 Alanine transaminase Proteins 0.000 description 5
- 101100314454 Caenorhabditis elegans tra-1 gene Proteins 0.000 description 5
- 206010066901 Treatment failure Diseases 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 229940087861 faslodex Drugs 0.000 description 5
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 description 5
- 230000007170 pathology Effects 0.000 description 5
- 230000000750 progressive effect Effects 0.000 description 5
- 238000001959 radiotherapy Methods 0.000 description 5
- 229940066675 ricinoleate Drugs 0.000 description 5
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 206010006002 Bone pain Diseases 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 4
- 230000000259 anti-tumor effect Effects 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 4
- 238000007918 intramuscular administration Methods 0.000 description 4
- 210000004072 lung Anatomy 0.000 description 4
- 230000000010 osteolytic effect Effects 0.000 description 4
- 208000037821 progressive disease Diseases 0.000 description 4
- 238000002604 ultrasonography Methods 0.000 description 4
- 239000003981 vehicle Substances 0.000 description 4
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 3
- 208000030507 AIDS Diseases 0.000 description 3
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 3
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 3
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
- 241000725303 Human immunodeficiency virus Species 0.000 description 3
- 206010061217 Infestation Diseases 0.000 description 3
- 238000011360 adjunctive therapy Methods 0.000 description 3
- 230000002411 adverse Effects 0.000 description 3
- 230000001270 agonistic effect Effects 0.000 description 3
- 239000003146 anticoagulant agent Substances 0.000 description 3
- 229940127219 anticoagulant drug Drugs 0.000 description 3
- 229960002903 benzyl benzoate Drugs 0.000 description 3
- 230000036772 blood pressure Effects 0.000 description 3
- 210000000988 bone and bone Anatomy 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 238000002591 computed tomography Methods 0.000 description 3
- 238000013461 design Methods 0.000 description 3
- 230000012010 growth Effects 0.000 description 3
- 230000002489 hematologic effect Effects 0.000 description 3
- 238000009806 oophorectomy Methods 0.000 description 3
- 230000002611 ovarian Effects 0.000 description 3
- 239000000583 progesterone congener Substances 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 230000003637 steroidlike Effects 0.000 description 3
- 229940122361 Bisphosphonate Drugs 0.000 description 2
- 206010055113 Breast cancer metastatic Diseases 0.000 description 2
- 208000020446 Cardiac disease Diseases 0.000 description 2
- 206010053567 Coagulopathies Diseases 0.000 description 2
- 208000032843 Hemorrhage Diseases 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 208000005250 Spontaneous Fractures Diseases 0.000 description 2
- 230000003042 antagnostic effect Effects 0.000 description 2
- 238000013176 antiplatelet therapy Methods 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 230000002146 bilateral effect Effects 0.000 description 2
- 150000004663 bisphosphonates Chemical class 0.000 description 2
- 208000034158 bleeding Diseases 0.000 description 2
- 230000000740 bleeding effect Effects 0.000 description 2
- 238000011976 chest X-ray Methods 0.000 description 2
- 230000035602 clotting Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000000875 corresponding effect Effects 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
- 210000000172 cytosol Anatomy 0.000 description 2
- 230000034994 death Effects 0.000 description 2
- 231100000517 death Toxicity 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000006866 deterioration Effects 0.000 description 2
- 230000002124 endocrine Effects 0.000 description 2
- JBTWLSYIZRCDFO-UHFFFAOYSA-N ethyl methyl carbonate Chemical compound CCOC(=O)OC JBTWLSYIZRCDFO-UHFFFAOYSA-N 0.000 description 2
- 230000007717 exclusion Effects 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 208000002672 hepatitis B Diseases 0.000 description 2
- 229940125697 hormonal agent Drugs 0.000 description 2
- 238000003384 imaging method Methods 0.000 description 2
- 238000002991 immunohistochemical analysis Methods 0.000 description 2
- 230000002055 immunohistochemical effect Effects 0.000 description 2
- 238000007901 in situ hybridization Methods 0.000 description 2
- 230000008595 infiltration Effects 0.000 description 2
- 238000001764 infiltration Methods 0.000 description 2
- 230000000977 initiatory effect Effects 0.000 description 2
- 239000003041 laboratory chemical Substances 0.000 description 2
- 238000011866 long-term treatment Methods 0.000 description 2
- 230000004199 lung function Effects 0.000 description 2
- 210000001165 lymph node Anatomy 0.000 description 2
- 230000007434 lytic lesion Effects 0.000 description 2
- 206010025482 malaise Diseases 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 230000005906 menstruation Effects 0.000 description 2
- 230000009401 metastasis Effects 0.000 description 2
- 230000001394 metastastic effect Effects 0.000 description 2
- 206010061289 metastatic neoplasm Diseases 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 238000011275 oncology therapy Methods 0.000 description 2
- 230000001582 osteoblastic effect Effects 0.000 description 2
- 108090000468 progesterone receptors Proteins 0.000 description 2
- 235000018102 proteins Nutrition 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 210000004872 soft tissue Anatomy 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- 238000010186 staining Methods 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 238000013185 thoracic computed tomography Methods 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- 210000004291 uterus Anatomy 0.000 description 2
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 1
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 1
- -1 4,4,5,5,5-pentafluoropentylsulfinyl Chemical group 0.000 description 1
- DODQJNMQWMSYGS-QPLCGJKRSA-N 4-[(z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-phenylbut-1-en-2-yl]phenol Chemical compound C=1C=C(O)C=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 DODQJNMQWMSYGS-QPLCGJKRSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 102000009027 Albumins Human genes 0.000 description 1
- 108010088751 Albumins Proteins 0.000 description 1
- 241001136792 Alle Species 0.000 description 1
- 201000000736 Amenorrhea Diseases 0.000 description 1
- 206010001928 Amenorrhoea Diseases 0.000 description 1
- 206010003445 Ascites Diseases 0.000 description 1
- 108010003415 Aspartate Aminotransferases Proteins 0.000 description 1
- 102000004625 Aspartate Aminotransferases Human genes 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 206010008479 Chest Pain Diseases 0.000 description 1
- 101000904177 Clupea pallasii Gonadoliberin-1 Proteins 0.000 description 1
- 206010010305 Confusional state Diseases 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 230000004544 DNA amplification Effects 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 206010017076 Fracture Diseases 0.000 description 1
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 description 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 208000005176 Hepatitis C Diseases 0.000 description 1
- 206010019842 Hepatomegaly Diseases 0.000 description 1
- 101000889443 Homo sapiens Trefoil factor 1 Proteins 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 206010060800 Hot flush Diseases 0.000 description 1
- 206010025102 Lung infiltration Diseases 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
- 108010073521 Luteinizing Hormone Proteins 0.000 description 1
- 206010025282 Lymphoedema Diseases 0.000 description 1
- 241000489861 Maximus Species 0.000 description 1
- 206010027452 Metastases to bone Diseases 0.000 description 1
- 206010027458 Metastases to lung Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010034156 Pathological fracture Diseases 0.000 description 1
- 208000002151 Pleural effusion Diseases 0.000 description 1
- 102100025803 Progesterone receptor Human genes 0.000 description 1
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 1
- 208000001871 Tachycardia Diseases 0.000 description 1
- 238000008050 Total Bilirubin Reagent Methods 0.000 description 1
- 102100039175 Trefoil factor 1 Human genes 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000008484 agonism Effects 0.000 description 1
- 231100000540 amenorrhea Toxicity 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 229940030486 androgens Drugs 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 229940078010 arimidex Drugs 0.000 description 1
- 235000019445 benzyl alcohol Nutrition 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000004820 blood count Methods 0.000 description 1
- 238000009534 blood test Methods 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000001217 buttock Anatomy 0.000 description 1
- 230000002308 calcification Effects 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 231100000504 carcinogenesis Toxicity 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 208000019065 cervical carcinoma Diseases 0.000 description 1
- 238000001311 chemical methods and process Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 210000000038 chest Anatomy 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 238000011970 concomitant therapy Methods 0.000 description 1
- 229940124301 concurrent medication Drugs 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 230000002380 cytological effect Effects 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 238000009164 estrogen replacement therapy Methods 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 229940087476 femara Drugs 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 238000005534 hematocrit Methods 0.000 description 1
- 208000031169 hemorrhagic disease Diseases 0.000 description 1
- 208000010710 hepatitis C virus infection Diseases 0.000 description 1
- 244000144980 herd Species 0.000 description 1
- 238000011532 immunohistochemical staining Methods 0.000 description 1
- 238000003364 immunohistochemistry Methods 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 1
- 229940075495 isopropyl palmitate Drugs 0.000 description 1
- 229960004125 ketoconazole Drugs 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940040129 luteinizing hormone Drugs 0.000 description 1
- 208000002502 lymphedema Diseases 0.000 description 1
- 230000002101 lytic effect Effects 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 210000005015 mediastinal lymph node Anatomy 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 208000037819 metastatic cancer Diseases 0.000 description 1
- 208000011575 metastatic malignant neoplasm Diseases 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 210000000440 neutrophil Anatomy 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000010606 normalization Methods 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 238000003752 polymerase chain reaction Methods 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 102000003998 progesterone receptors Human genes 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 230000018883 protein targeting Effects 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000003439 radiotherapeutic effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000003488 releasing hormone Substances 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- WBHHMMIMDMUBKC-XLNAKTSKSA-N ricinelaidic acid Chemical compound CCCCCC[C@@H](O)C\C=C\CCCCCCCC(O)=O WBHHMMIMDMUBKC-XLNAKTSKSA-N 0.000 description 1
- 229960003656 ricinoleic acid Drugs 0.000 description 1
- FEUQNCSVHBHROZ-UHFFFAOYSA-N ricinoleic acid Natural products CCCCCCC(O[Si](C)(C)C)CC=CCCCCCCCC(=O)OC FEUQNCSVHBHROZ-UHFFFAOYSA-N 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000000405 serological effect Effects 0.000 description 1
- 208000020352 skin basal cell carcinoma Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000013517 stratification Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 230000009469 supplementation Effects 0.000 description 1
- 230000006794 tachycardia Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 210000000115 thoracic cavity Anatomy 0.000 description 1
- WZDGZWOAQTVYBX-XOINTXKNSA-N tibolone Chemical compound C([C@@H]12)C[C@]3(C)[C@@](C#C)(O)CC[C@H]3[C@@H]1[C@H](C)CC1=C2CCC(=O)C1 WZDGZWOAQTVYBX-XOINTXKNSA-N 0.000 description 1
- 229960001023 tibolone Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 208000037911 visceral disease Diseases 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0008172 | 2000-04-05 | ||
| GBGB0008172.9A GB0008172D0 (en) | 2000-04-05 | 2000-04-05 | Therapy |
| PCT/GB2001/001500 WO2001074366A1 (en) | 2000-04-05 | 2001-04-02 | Use of fulvestrant in the treatment of resistant breast cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60113975D1 DE60113975D1 (de) | 2006-02-23 |
| DE60113975T2 true DE60113975T2 (de) | 2006-06-22 |
Family
ID=9889101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60113975T Expired - Lifetime DE60113975T2 (de) | 2000-04-05 | 2001-04-02 | Verwendung von fulvestrant in der behandlung von resistentem brustkrebs |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US20030158166A1 (https=) |
| EP (2) | EP1272195B1 (https=) |
| JP (1) | JP2003528919A (https=) |
| KR (1) | KR100757764B1 (https=) |
| CN (1) | CN1431905A (https=) |
| AT (1) | ATE306270T1 (https=) |
| AU (2) | AU4437201A (https=) |
| BR (1) | BR0109789A (https=) |
| CA (1) | CA2403608A1 (https=) |
| CH (1) | CH1272195H1 (https=) |
| CZ (1) | CZ303096B6 (https=) |
| DE (1) | DE60113975T2 (https=) |
| DK (1) | DK1272195T3 (https=) |
| EE (1) | EE05026B1 (https=) |
| ES (1) | ES2248300T3 (https=) |
| GB (1) | GB0008172D0 (https=) |
| HU (1) | HU230064B1 (https=) |
| IL (2) | IL151932A0 (https=) |
| IS (1) | IS2869B (https=) |
| MX (1) | MXPA02009744A (https=) |
| NO (1) | NO329949B1 (https=) |
| NZ (1) | NZ539603A (https=) |
| PL (1) | PL201175B1 (https=) |
| RU (1) | RU2265438C2 (https=) |
| SK (1) | SK287779B6 (https=) |
| UA (1) | UA80388C2 (https=) |
| WO (1) | WO2001074366A1 (https=) |
| ZA (1) | ZA200207538B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0116620D0 (en) * | 2001-07-07 | 2001-08-29 | Astrazeneca Ab | Formulation |
| HUP0400115A3 (en) * | 2001-07-07 | 2005-11-28 | Astrazeneca Ab | Pharmaceutical composition for the intramuscular administration of fulvestrant |
| EP1623713A1 (en) * | 2004-07-09 | 2006-02-08 | Proskelia SAS | Cominations of pure anti-estrogen with aromatase inhibitors |
| US8557863B2 (en) * | 2005-09-27 | 2013-10-15 | Robert Benson Aylor | Suppression and prevention of tumors |
| JP5256042B2 (ja) * | 2005-11-22 | 2013-08-07 | インサイト・コーポレイション | 癌の処置のための併用療法 |
| US7910108B2 (en) * | 2006-06-05 | 2011-03-22 | Incyte Corporation | Sheddase inhibitors combined with CD30-binding immunotherapeutics for the treatment of CD30 positive diseases |
| SG194735A1 (en) * | 2011-05-09 | 2013-12-30 | Univ Virginia Patent Found | Compositions and methods for treating cancer |
| ES2708302T3 (es) | 2011-05-20 | 2019-04-09 | Capital Business Y Gestion De Finanzas S L | Composición farmacéutica |
| WO2015106094A1 (en) * | 2014-01-10 | 2015-07-16 | Atossa Genetics Inc. | Transpapillary methods and compositions for diagnosing and treating breast conditions |
| US9421264B2 (en) * | 2014-03-28 | 2016-08-23 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| IL304863B2 (en) | 2017-09-11 | 2025-08-01 | Atossa Therapeutics Inc | Methods for making and using endoxifen |
| JP7384903B2 (ja) * | 2018-05-24 | 2023-11-21 | ケーアイ ファーマシューティカルズ，リミテッド・ライアビリティ・カンパニー | フルベストラントのプロドラッグ |
| JP7662204B2 (ja) | 2019-07-03 | 2025-04-15 | アトッサ・セラピューティクス・インコーポレイテッド | エンドキシフェンの徐放性組成物 |
| WO2021174195A2 (en) * | 2020-02-29 | 2021-09-02 | The University Of Vermon | Use of thyromimetics for the treatment of cancer |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6541669B1 (en) * | 1998-06-08 | 2003-04-01 | Theravance, Inc. | β2-adrenergic receptor agonists |
| US6465445B1 (en) * | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
-
2000
- 2000-04-05 GB GBGB0008172.9A patent/GB0008172D0/en not_active Ceased
-
2001
- 2001-02-04 UA UA2002118734A patent/UA80388C2/uk unknown
- 2001-04-02 CZ CZ20023309A patent/CZ303096B6/cs not_active IP Right Cessation
- 2001-04-02 IL IL15193201A patent/IL151932A0/xx active IP Right Grant
- 2001-04-02 AT AT01917289T patent/ATE306270T1/de active
- 2001-04-02 AU AU4437201A patent/AU4437201A/xx active Pending
- 2001-04-02 WO PCT/GB2001/001500 patent/WO2001074366A1/en not_active Ceased
- 2001-04-02 DE DE60113975T patent/DE60113975T2/de not_active Expired - Lifetime
- 2001-04-02 SK SK1429-2002A patent/SK287779B6/sk not_active IP Right Cessation
- 2001-04-02 AU AU2001244372A patent/AU2001244372B2/en not_active Expired
- 2001-04-02 CN CN01810539A patent/CN1431905A/zh active Pending
- 2001-04-02 PL PL357936A patent/PL201175B1/pl unknown
- 2001-04-02 KR KR1020027013366A patent/KR100757764B1/ko not_active Expired - Lifetime
- 2001-04-02 CA CA002403608A patent/CA2403608A1/en not_active Abandoned
- 2001-04-02 DK DK01917289T patent/DK1272195T3/da active
- 2001-04-02 JP JP2001572110A patent/JP2003528919A/ja active Pending
- 2001-04-02 EE EEP200200574A patent/EE05026B1/xx unknown
- 2001-04-02 US US10/240,656 patent/US20030158166A1/en not_active Abandoned
- 2001-04-02 NZ NZ539603A patent/NZ539603A/en not_active IP Right Cessation
- 2001-04-02 CH CH01917289T patent/CH1272195H1/de unknown
- 2001-04-02 HU HU0300339A patent/HU230064B1/hu unknown
- 2001-04-02 EP EP01917289A patent/EP1272195B1/en not_active Expired - Lifetime
- 2001-04-02 ES ES01917289T patent/ES2248300T3/es not_active Expired - Lifetime
- 2001-04-02 EP EP05007561A patent/EP1586323A1/en not_active Withdrawn
- 2001-04-02 BR BR0109789-0A patent/BR0109789A/pt not_active Application Discontinuation
- 2001-04-02 MX MXPA02009744A patent/MXPA02009744A/es active IP Right Grant
- 2001-04-02 RU RU2002129355/14A patent/RU2265438C2/ru active
-
2002
- 2002-09-19 ZA ZA200207538A patent/ZA200207538B/en unknown
- 2002-09-25 IL IL151932A patent/IL151932A/en unknown
- 2002-10-01 IS IS6576A patent/IS2869B/is unknown
- 2002-10-02 NO NO20024735A patent/NO329949B1/no not_active IP Right Cessation
-
2010
- 2010-09-30 US US12/895,369 patent/US20110183949A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE60113975T2 (de) | Verwendung von fulvestrant in der behandlung von resistentem brustkrebs | |
| DE60030889T2 (de) | Verwendung von egfr tyrosine kinase hemmern zur behandlung von brustkrebs | |
| DE60318092T2 (de) | Pharmazeutische zusammensetzung enthaltend estetrolderivate und anwendung in der krebsbehandlung | |
| DE69003015T2 (de) | Behandlung von Störungen in der Postmenopause. | |
| Parisien et al. | Histomorphometric assessment of bone mass, structure, and remodeling: a comparison between healthy black and white premenopausal women | |
| Bloom et al. | Antioestrogens in treatment of breast cancer: value of nafoxidine in 52 advanced cases | |
| Bajetta et al. | Double-blind, randomised, multicentre endocrine trial comparing two letrozole doses, in postmenopausal breast cancer patients | |
| Vermess et al. | Development and experimental evaluation of a contrast medium for computed tomographic examination of the liver and spleen | |
| JP2020522525A (ja) | 子宮筋腫を治療し、月経失血を低下させるゴナドトロピン放出ホルモンアンタゴニスト投与計画 | |
| AU2001244372A1 (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| AT510868A2 (de) | Fulvestrant in einer Dosierung von 500 mg für die Behandlung fortgeschrittenen Brustkrebses | |
| DE60024118T2 (de) | Verwendung einer parathyroidhormone zur reduktion des krebsrisikos | |
| Homesley et al. | Antiestrogenic potency of toremifene and tamoxifen in postmenopausal women | |
| DE60123138T2 (de) | Verwendung von progesteronrezeptorhemmern zur behandlung von steroid-resistentem brustkrebs | |
| DE10051609A1 (de) | Hemmung der Wachstumsfaktorabhängigkeit von Tumorzellen | |
| DE69935156T2 (de) | hCG THERAPIE ZUR BEHANDLUNG VON METASTATISCHEM BRUSTKREBS | |
| DE60121980T2 (de) | Verwendung von 11beta-(4-acetylphenyl)-17beta-hydroxy-17alpha-(1,1,2,2-pentafluoroethyl)estra-4,9-dien-3-on zur herstellung eines medikaments zur behandlung von brust-, eierstock-, endometrium-krebs, myelom und meningiom | |
| EP1091744A1 (de) | 1-octadecyl-2-methyl-sn-glycero-3-phosphocholin (et180ch3) zur behandlung von humanen mammakarzinomen | |
| DE112022001882T5 (de) | Krebstherapie unter verwendung von toll-like-rezeptor-agonisten | |
| DE69006633T2 (de) | Verwendung von Gestoden zur Herstellung von Arzneimitteln. | |
| HK1081842A (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| HK1051498B (en) | Use of fulvestrant in the treatment of resistant breast cancer | |
| Schreml | 10 Jahre Therapie des Mammakarzinoms |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8363 | Opposition against the patent |