NO321502B1 - Progestogen-fritt kombinert preparat for behandling av benigne gynekologiske sykdommer - Google Patents
Progestogen-fritt kombinert preparat for behandling av benigne gynekologiske sykdommer Download PDFInfo
- Publication number
- NO321502B1 NO321502B1 NO19954611A NO954611A NO321502B1 NO 321502 B1 NO321502 B1 NO 321502B1 NO 19954611 A NO19954611 A NO 19954611A NO 954611 A NO954611 A NO 954611A NO 321502 B1 NO321502 B1 NO 321502B1
- Authority
- NO
- Norway
- Prior art keywords
- preparation
- hormone
- gonadotropin
- releasing hormone
- estrogen
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 125
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 22
- 201000010099 disease Diseases 0.000 title claims abstract description 18
- 238000011282 treatment Methods 0.000 title claims description 26
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 claims abstract description 82
- 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 claims abstract description 79
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 claims abstract description 77
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 claims abstract description 75
- 239000000203 mixture Substances 0.000 claims abstract description 45
- 230000001076 estrogenic effect Effects 0.000 claims abstract description 24
- 230000001548 androgenic effect Effects 0.000 claims abstract description 9
- 239000000262 estrogen Substances 0.000 claims description 55
- 229940011871 estrogen Drugs 0.000 claims description 54
- 238000009472 formulation Methods 0.000 claims description 33
- 229940088597 hormone Drugs 0.000 claims description 31
- 239000005556 hormone Substances 0.000 claims description 31
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims description 28
- 210000002966 serum Anatomy 0.000 claims description 28
- 239000000556 agonist Substances 0.000 claims description 27
- 239000003098 androgen Substances 0.000 claims description 24
- 239000003488 releasing hormone Substances 0.000 claims description 22
- 238000004519 manufacturing process Methods 0.000 claims description 17
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound 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 claims description 16
- 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 claims description 15
- 229960005309 estradiol Drugs 0.000 claims description 14
- 229930182833 estradiol Natural products 0.000 claims description 14
- 230000002611 ovarian Effects 0.000 claims description 14
- 229960003604 testosterone Drugs 0.000 claims description 14
- 102000006771 Gonadotropins Human genes 0.000 claims description 10
- 108010086677 Gonadotropins Proteins 0.000 claims description 10
- 239000002622 gonadotropin Substances 0.000 claims description 10
- 108010037003 Buserelin Proteins 0.000 claims description 9
- 241000124008 Mammalia Species 0.000 claims description 9
- 206010030247 Oestrogen deficiency Diseases 0.000 claims description 9
- 229960002719 buserelin Drugs 0.000 claims description 9
- CUWODFFVMXJOKD-UVLQAERKSA-N buserelin Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 CUWODFFVMXJOKD-UVLQAERKSA-N 0.000 claims description 9
- 208000024891 symptom Diseases 0.000 claims description 9
- 229960003387 progesterone Drugs 0.000 claims description 8
- 239000000186 progesterone Substances 0.000 claims description 8
- 238000007918 intramuscular administration Methods 0.000 claims description 7
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims description 6
- 208000032023 Signs and Symptoms Diseases 0.000 claims description 6
- 229960001348 estriol Drugs 0.000 claims description 6
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims description 6
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims description 5
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims description 5
- 229960003399 estrone Drugs 0.000 claims description 5
- VXKHXGOKWPXYNA-PGBVPBMZSA-N triptorelin Chemical group C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=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 VXKHXGOKWPXYNA-PGBVPBMZSA-N 0.000 claims description 5
- GCKMFJBGXUYNAG-UHFFFAOYSA-N 17alpha-methyltestosterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C)(O)C1(C)CC2 GCKMFJBGXUYNAG-UHFFFAOYSA-N 0.000 claims description 4
- GCKMFJBGXUYNAG-HLXURNFRSA-N Methyltestosterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@](C)(O)[C@@]1(C)CC2 GCKMFJBGXUYNAG-HLXURNFRSA-N 0.000 claims description 4
- 108010050144 Triptorelin Pamoate Proteins 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 229960001566 methyltestosterone Drugs 0.000 claims description 4
- 238000007920 subcutaneous administration Methods 0.000 claims description 4
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 3
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 claims description 3
- GJKXGJCSJWBJEZ-XRSSZCMZSA-N Deslorelin Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CNC2=CC=CC=C12 GJKXGJCSJWBJEZ-XRSSZCMZSA-N 0.000 claims description 3
- UOACKFBJUYNSLK-XRKIENNPSA-N Estradiol Cypionate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H](C4=CC=C(O)C=C4CC3)CC[C@@]21C)C(=O)CCC1CCCC1 UOACKFBJUYNSLK-XRKIENNPSA-N 0.000 claims description 3
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims description 3
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 3
- 102400000932 Gonadoliberin-1 Human genes 0.000 claims description 3
- 108010069236 Goserelin Proteins 0.000 claims description 3
- BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 claims description 3
- 101500026183 Homo sapiens Gonadoliberin-1 Proteins 0.000 claims description 3
- 108010000817 Leuprolide Proteins 0.000 claims description 3
- 108010021717 Nafarelin Proteins 0.000 claims description 3
- 229920000081 Polyestradiol phosphate Polymers 0.000 claims description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
- 229960005408 deslorelin Drugs 0.000 claims description 3
- 108700025485 deslorelin Proteins 0.000 claims description 3
- RGLYKWWBQGJZGM-ISLYRVAYSA-N diethylstilbestrol Chemical compound C=1C=C(O)C=CC=1C(/CC)=C(\CC)C1=CC=C(O)C=C1 RGLYKWWBQGJZGM-ISLYRVAYSA-N 0.000 claims description 3
- 229960000452 diethylstilbestrol Drugs 0.000 claims description 3
- 229950002007 estradiol benzoate Drugs 0.000 claims description 3
- 229960005416 estradiol cypionate Drugs 0.000 claims description 3
- 229960004766 estradiol valerate Drugs 0.000 claims description 3
- 229950008385 estrone sulphate Drugs 0.000 claims description 3
- 229960002568 ethinylestradiol Drugs 0.000 claims description 3
- 229960001442 gonadorelin Drugs 0.000 claims description 3
- 229960002913 goserelin Drugs 0.000 claims description 3
- 108700020746 histrelin Proteins 0.000 claims description 3
- HHXHVIJIIXKSOE-QILQGKCVSA-N histrelin Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)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)CC(N=C1)=CN1CC1=CC=CC=C1 HHXHVIJIIXKSOE-QILQGKCVSA-N 0.000 claims description 3
- 229960002193 histrelin Drugs 0.000 claims description 3
- 229960004338 leuprorelin Drugs 0.000 claims description 3
- IMSSROKUHAOUJS-MJCUULBUSA-N mestranol Chemical compound C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(OC)=CC=C3[C@H]21 IMSSROKUHAOUJS-MJCUULBUSA-N 0.000 claims description 3
- 229960001390 mestranol Drugs 0.000 claims description 3
- 229960002333 nafarelin Drugs 0.000 claims description 3
- RWHUEXWOYVBUCI-ITQXDASVSA-N nafarelin Chemical compound C([C@@H](C(=O)N[C@H](CC=1C=C2C=CC=CC2=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(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=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 RWHUEXWOYVBUCI-ITQXDASVSA-N 0.000 claims description 3
- 229960001298 polyestradiol phosphate Drugs 0.000 claims description 3
- 229910052939 potassium sulfate Inorganic materials 0.000 claims description 3
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 claims description 2
- WRWBCPJQPDHXTJ-DTMQFJJTSA-N Methandriol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@](C)(O)[C@@]1(C)CC2 WRWBCPJQPDHXTJ-DTMQFJJTSA-N 0.000 claims description 2
- JKWKMORAXJQQSR-MOPIKTETSA-N Nandrolone Decanoate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCCCCC)[C@@]1(C)CC2 JKWKMORAXJQQSR-MOPIKTETSA-N 0.000 claims description 2
- QSLJIVKCVHQPLV-PEMPUTJUSA-N Oxandrin Chemical compound C([C@@H]1CC2)C(=O)OC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@](C)(O)[C@@]2(C)CC1 QSLJIVKCVHQPLV-PEMPUTJUSA-N 0.000 claims description 2
- LKAJKIOFIWVMDJ-IYRCEVNGSA-N Stanazolol Chemical compound C([C@@H]1CC[C@H]2[C@@H]3CC[C@@]([C@]3(CC[C@@H]2[C@@]1(C)C1)C)(O)C)C2=C1C=NN2 LKAJKIOFIWVMDJ-IYRCEVNGSA-N 0.000 claims description 2
- PDMMFKSKQVNJMI-BLQWBTBKSA-N Testosterone propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CC)[C@@]1(C)CC2 PDMMFKSKQVNJMI-BLQWBTBKSA-N 0.000 claims description 2
- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 claims description 2
- 229960003473 androstanolone Drugs 0.000 claims description 2
- 229960005471 androstenedione Drugs 0.000 claims description 2
- AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 claims description 2
- POZRVZJJTULAOH-LHZXLZLDSA-N danazol Chemical compound C1[C@]2(C)[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=CC2=C1C=NO2 POZRVZJJTULAOH-LHZXLZLDSA-N 0.000 claims description 2
- 229960000766 danazol Drugs 0.000 claims description 2
- NOTIQUSPUUHHEH-UXOVVSIBSA-N dromostanolone propionate Chemical compound C([C@@H]1CC2)C(=O)[C@H](C)C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](OC(=O)CC)[C@@]2(C)CC1 NOTIQUSPUUHHEH-UXOVVSIBSA-N 0.000 claims description 2
- 229950004683 drostanolone propionate Drugs 0.000 claims description 2
- AOXRBFRFYPMWLR-XGXHKTLJSA-N ethylestrenol Chemical compound C1CC2=CCCC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](CC)(O)[C@@]1(C)CC2 AOXRBFRFYPMWLR-XGXHKTLJSA-N 0.000 claims description 2
- 229960001460 ethylestrenol Drugs 0.000 claims description 2
- 229960001833 methandriol Drugs 0.000 claims description 2
- 229960001935 nandrolone decanoate Drugs 0.000 claims description 2
- UBWXUGDQUBIEIZ-QNTYDACNSA-N nandrolone phenpropionate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@H]4CCC(=O)C=C4CC3)CC[C@@]21C)C(=O)CCC1=CC=CC=C1 UBWXUGDQUBIEIZ-QNTYDACNSA-N 0.000 claims description 2
- 229960001133 nandrolone phenpropionate Drugs 0.000 claims description 2
- 229960000464 oxandrolone Drugs 0.000 claims description 2
- ICMWWNHDUZJFDW-DHODBPELSA-N oxymetholone Chemical compound C([C@@H]1CC2)C(=O)\C(=C/O)C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@](C)(O)[C@@]2(C)CC1 ICMWWNHDUZJFDW-DHODBPELSA-N 0.000 claims description 2
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims description 2
- 235000011151 potassium sulphates Nutrition 0.000 claims description 2
- 229960000912 stanozolol Drugs 0.000 claims description 2
- 229910021653 sulphate ion Inorganic materials 0.000 claims description 2
- 229960005353 testolactone Drugs 0.000 claims description 2
- BPEWUONYVDABNZ-DZBHQSCQSA-N testolactone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(OC(=O)CC4)[C@@H]4[C@@H]3CCC2=C1 BPEWUONYVDABNZ-DZBHQSCQSA-N 0.000 claims description 2
- HPFVBGJFAYZEBE-ZLQWOROUSA-N testosterone cypionate Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(CCC(=O)C=C4CC3)C)CC[C@@]21C)C(=O)CCC1CCCC1 HPFVBGJFAYZEBE-ZLQWOROUSA-N 0.000 claims description 2
- 229960000921 testosterone cypionate Drugs 0.000 claims description 2
- VOCBWIIFXDYGNZ-IXKNJLPQSA-N testosterone enanthate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCCCC)[C@@]1(C)CC2 VOCBWIIFXDYGNZ-IXKNJLPQSA-N 0.000 claims description 2
- 229960003484 testosterone enanthate Drugs 0.000 claims description 2
- 229960001712 testosterone propionate Drugs 0.000 claims description 2
- NMJREATYWWNIKX-UHFFFAOYSA-N GnRH Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CC(C)C)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 NMJREATYWWNIKX-UHFFFAOYSA-N 0.000 claims 2
- JKKFKPJIXZFSSB-CBZIJGRNSA-N estrone 3-sulfate Chemical compound OS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 JKKFKPJIXZFSSB-CBZIJGRNSA-N 0.000 claims 2
- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](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)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 claims 2
- 229960001424 quinestrol Drugs 0.000 claims 2
- PWZUUYSISTUNDW-VAFBSOEGSA-N quinestrol Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@]4(O)C#C)C)CC2=CC=3OC1CCCC1 PWZUUYSISTUNDW-VAFBSOEGSA-N 0.000 claims 2
- 239000001120 potassium sulphate Substances 0.000 claims 1
- 238000000034 method Methods 0.000 abstract description 14
- 230000002357 endometrial effect Effects 0.000 abstract description 4
- 230000000638 stimulation Effects 0.000 abstract description 4
- 230000000694 effects Effects 0.000 description 24
- 238000009164 estrogen replacement therapy Methods 0.000 description 16
- 206010006187 Breast cancer Diseases 0.000 description 15
- 208000026310 Breast neoplasm Diseases 0.000 description 15
- 239000003094 microcapsule Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 12
- 239000003814 drug Substances 0.000 description 12
- 239000004005 microsphere Substances 0.000 description 12
- 230000009467 reduction Effects 0.000 description 12
- 150000003431 steroids Chemical class 0.000 description 12
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 11
- 239000003433 contraceptive agent Substances 0.000 description 11
- 230000002254 contraceptive effect Effects 0.000 description 11
- 239000000583 progesterone congener Substances 0.000 description 11
- 230000001629 suppression Effects 0.000 description 9
- 239000011162 core material Substances 0.000 description 8
- 239000000835 fiber Substances 0.000 description 8
- 230000001965 increasing effect Effects 0.000 description 8
- 108700012941 GNRH1 Proteins 0.000 description 7
- 206010033128 Ovarian cancer Diseases 0.000 description 7
- 206010061535 Ovarian neoplasm Diseases 0.000 description 7
- 239000013543 active substance Substances 0.000 description 7
- 230000002411 adverse Effects 0.000 description 7
- 210000000988 bone and bone Anatomy 0.000 description 7
- 239000002775 capsule Substances 0.000 description 7
- 230000029849 luteinization Effects 0.000 description 7
- 239000000463 material Substances 0.000 description 7
- 229920000642 polymer Polymers 0.000 description 7
- 102000009151 Luteinizing Hormone Human genes 0.000 description 6
- 108010073521 Luteinizing Hormone Proteins 0.000 description 6
- 206010036618 Premenstrual syndrome Diseases 0.000 description 6
- 230000009286 beneficial effect Effects 0.000 description 6
- 229940040129 luteinizing hormone Drugs 0.000 description 6
- 229940095055 progestogen systemic hormonal contraceptives Drugs 0.000 description 6
- 229940030486 androgens Drugs 0.000 description 5
- 238000013270 controlled release Methods 0.000 description 5
- 238000013461 design Methods 0.000 description 5
- 239000007943 implant Substances 0.000 description 5
- 229910052500 inorganic mineral Inorganic materials 0.000 description 5
- 230000007774 longterm Effects 0.000 description 5
- 239000011707 mineral Substances 0.000 description 5
- -1 poly(hydroxybutyric acid) Polymers 0.000 description 5
- 229920000260 silastic Polymers 0.000 description 5
- 108090001030 Lipoproteins Proteins 0.000 description 4
- 102000004895 Lipoproteins Human genes 0.000 description 4
- 210000000481 breast Anatomy 0.000 description 4
- 230000007423 decrease Effects 0.000 description 4
- 208000035475 disorder Diseases 0.000 description 4
- 230000001544 dysphoric effect Effects 0.000 description 4
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 description 4
- 150000002632 lipids Chemical class 0.000 description 4
- 229960002985 medroxyprogesterone acetate Drugs 0.000 description 4
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 description 4
- 230000009245 menopause Effects 0.000 description 4
- 230000027758 ovulation cycle Effects 0.000 description 4
- 230000001072 progestational effect Effects 0.000 description 4
- 230000002035 prolonged effect Effects 0.000 description 4
- 230000028327 secretion Effects 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 239000006213 vaginal ring Substances 0.000 description 4
- 239000003981 vehicle Substances 0.000 description 4
- 229920000089 Cyclic olefin copolymer Polymers 0.000 description 3
- 241000283073 Equus caballus Species 0.000 description 3
- 206010060800 Hot flush Diseases 0.000 description 3
- 206010027304 Menopausal symptoms Diseases 0.000 description 3
- 206010046798 Uterine leiomyoma Diseases 0.000 description 3
- 206010047486 Virilism Diseases 0.000 description 3
- 229920002988 biodegradable polymer Polymers 0.000 description 3
- 239000004621 biodegradable polymer Substances 0.000 description 3
- 229920001577 copolymer Polymers 0.000 description 3
- 238000009792 diffusion process Methods 0.000 description 3
- 238000012377 drug delivery Methods 0.000 description 3
- 230000006870 function Effects 0.000 description 3
- 239000003163 gonadal steroid hormone Substances 0.000 description 3
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 description 3
- 201000010260 leiomyoma Diseases 0.000 description 3
- RGLRXNKKBLIBQS-XNHQSDQCSA-N leuprolide acetate Chemical compound CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](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)CC1=CC=C(O)C=C1 RGLRXNKKBLIBQS-XNHQSDQCSA-N 0.000 description 3
- 210000004914 menses Anatomy 0.000 description 3
- 238000009806 oophorectomy Methods 0.000 description 3
- 230000011599 ovarian follicle development Effects 0.000 description 3
- 210000001672 ovary Anatomy 0.000 description 3
- 230000016087 ovulation Effects 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- 229940044953 vaginal ring Drugs 0.000 description 3
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 description 2
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 description 2
- 206010003439 Artificial menopause Diseases 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- 102100030797 Conserved oligomeric Golgi complex subunit 2 Human genes 0.000 description 2
- 201000009273 Endometriosis Diseases 0.000 description 2
- 206010019233 Headaches Diseases 0.000 description 2
- 101000920113 Homo sapiens Conserved oligomeric Golgi complex subunit 2 Proteins 0.000 description 2
- 206010022998 Irritability Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 206010036049 Polycystic ovaries Diseases 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- HZEQBCVBILBTEP-ZFINNJDLSA-N estropipate Chemical compound C1CNCCN1.OS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 HZEQBCVBILBTEP-ZFINNJDLSA-N 0.000 description 2
- 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 description 2
- 231100000869 headache Toxicity 0.000 description 2
- 238000002657 hormone replacement therapy Methods 0.000 description 2
- 238000009802 hysterectomy Methods 0.000 description 2
- 231100000546 inhibition of ovulation Toxicity 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 230000003278 mimic effect Effects 0.000 description 2
- 229940127234 oral contraceptive Drugs 0.000 description 2
- 239000003539 oral contraceptive agent Substances 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 230000002085 persistent effect Effects 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 230000001817 pituitary effect Effects 0.000 description 2
- 229920001610 polycaprolactone Polymers 0.000 description 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 230000002441 reversible effect Effects 0.000 description 2
- 229920002379 silicone rubber Polymers 0.000 description 2
- 239000004945 silicone rubber Substances 0.000 description 2
- 238000009987 spinning Methods 0.000 description 2
- 238000004659 sterilization and disinfection Methods 0.000 description 2
- 230000008961 swelling Effects 0.000 description 2
- 230000037317 transdermal delivery Effects 0.000 description 2
- 230000001457 vasomotor Effects 0.000 description 2
- 230000004584 weight gain Effects 0.000 description 2
- 235000019786 weight gain Nutrition 0.000 description 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- 206010000060 Abdominal distension Diseases 0.000 description 1
- 206010054196 Affect lability Diseases 0.000 description 1
- 201000005670 Anovulation Diseases 0.000 description 1
- 206010002659 Anovulatory cycle Diseases 0.000 description 1
- 208000006820 Arthralgia Diseases 0.000 description 1
- 208000010392 Bone Fractures Diseases 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- WDPFQABQVGJEBZ-MAKOZQESSA-N Bothermon Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1.O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 WDPFQABQVGJEBZ-MAKOZQESSA-N 0.000 description 1
- 206010006312 Breast swelling Diseases 0.000 description 1
- 206010006313 Breast tenderness Diseases 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 206010011971 Decreased interest Diseases 0.000 description 1
- 208000034423 Delivery Diseases 0.000 description 1
- 206010017076 Fracture Diseases 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
- 108010023302 HDL Cholesterol Proteins 0.000 description 1
- 206010020112 Hirsutism Diseases 0.000 description 1
- 208000033830 Hot Flashes Diseases 0.000 description 1
- 108010028554 LDL Cholesterol Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010029216 Nervousness Diseases 0.000 description 1
- 206010067572 Oestrogenic effect Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 206010036018 Pollakiuria Diseases 0.000 description 1
- 229920001244 Poly(D,L-lactide) Polymers 0.000 description 1
- 229930182556 Polyacetal Natural products 0.000 description 1
- 229920000954 Polyglycolide Polymers 0.000 description 1
- 229920001710 Polyorthoester Polymers 0.000 description 1
- 239000004820 Pressure-sensitive adhesive Substances 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 208000032140 Sleepiness Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- 206010071018 Urogenital atrophy Diseases 0.000 description 1
- 206010046788 Uterine haemorrhage Diseases 0.000 description 1
- 206010046910 Vaginal haemorrhage Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 206010047791 Vulvovaginal dryness Diseases 0.000 description 1
- 208000021017 Weight Gain Diseases 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 238000011292 agonist therapy Methods 0.000 description 1
- 238000009165 androgen replacement therapy Methods 0.000 description 1
- 231100000552 anovulation Toxicity 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 208000013404 behavioral symptom Diseases 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 239000012867 bioactive agent Substances 0.000 description 1
- 238000006065 biodegradation reaction Methods 0.000 description 1
- 208000024330 bloating Diseases 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000015271 coagulation Effects 0.000 description 1
- 238000005345 coagulation Methods 0.000 description 1
- 230000002301 combined effect Effects 0.000 description 1
- 235000019788 craving Nutrition 0.000 description 1
- 239000002178 crystalline material Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 230000004821 effect on bone Effects 0.000 description 1
- 230000001278 effect on cholesterol Effects 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 239000000806 elastomer Substances 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 201000006828 endometrial hyperplasia Diseases 0.000 description 1
- 229940081345 estropipate Drugs 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000002474 gonadorelin antagonist Substances 0.000 description 1
- 229940094892 gonadotropins Drugs 0.000 description 1
- 239000008240 homogeneous mixture Substances 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 238000001794 hormone therapy Methods 0.000 description 1
- 210000003016 hypothalamus Anatomy 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 229960004400 levonorgestrel Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 238000007726 management method Methods 0.000 description 1
- 231100000794 masculinization Toxicity 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000007778 menstrual function Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000013080 microcrystalline material Substances 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 208000013465 muscle pain Diseases 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000008447 perception Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 0.000 description 1
- 239000002745 poly(ortho ester) Substances 0.000 description 1
- 239000004632 polycaprolactone Substances 0.000 description 1
- 239000004626 polylactic acid Substances 0.000 description 1
- 229920006324 polyoxymethylene Polymers 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 206010036601 premature menopause Diseases 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000001850 reproductive effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000036299 sexual function Effects 0.000 description 1
- 239000002210 silicon-based material Substances 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000022925 sleep disturbance Diseases 0.000 description 1
- 230000037321 sleepiness Effects 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 230000010009 steroidogenesis Effects 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 229920002994 synthetic fiber Polymers 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 229960004824 triptorelin Drugs 0.000 description 1
- 230000009677 vaginal delivery Effects 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 230000036642 wellbeing Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
- A61K9/0036—Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S424/00—Drug, bio-affecting and body treating compositions
- Y10S424/14—Topical contraceptives and spermacides
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Reproductive Health (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Plant Substances (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/062,883 US5340585A (en) | 1991-04-12 | 1993-05-17 | Method and formulations for use in treating benign gynecological disorders |
| PCT/US1994/005222 WO1994026207A1 (en) | 1993-05-17 | 1994-05-12 | Methods and formulations for use in treating benign gynecological disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO954611D0 NO954611D0 (no) | 1995-11-15 |
| NO954611L NO954611L (no) | 1996-01-16 |
| NO321502B1 true NO321502B1 (no) | 2006-05-15 |
Family
ID=22045464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO19954611A NO321502B1 (no) | 1993-05-17 | 1995-11-15 | Progestogen-fritt kombinert preparat for behandling av benigne gynekologiske sykdommer |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US5340585A (pt) |
| EP (1) | EP0748190B1 (pt) |
| AT (1) | ATE245992T1 (pt) |
| CA (1) | CA2162261A1 (pt) |
| DE (1) | DE69432990T2 (pt) |
| DK (1) | DK0748190T3 (pt) |
| ES (1) | ES2204917T3 (pt) |
| NO (1) | NO321502B1 (pt) |
| PT (1) | PT748190E (pt) |
| WO (1) | WO1994026207A1 (pt) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6090925A (en) | 1993-03-09 | 2000-07-18 | Epic Therapeutics, Inc. | Macromolecular microparticles and methods of production and use |
| US5981719A (en) | 1993-03-09 | 1999-11-09 | Epic Therapeutics, Inc. | Macromolecular microparticles and methods of production and use |
| US5824286A (en) * | 1994-04-26 | 1998-10-20 | The Medical College Of Hampton Roads | Mammography method |
| US5843901A (en) * | 1995-06-07 | 1998-12-01 | Advanced Research & Technology Institute | LHRH antagonist peptides |
| US5861431A (en) * | 1995-06-07 | 1999-01-19 | Iotek, Inc. | Incontinence treatment |
| DK1007080T3 (da) * | 1996-08-30 | 2007-07-30 | Peptech Ltd | Formulering til vedvarende frigivelse af peptidagonister og analoger af GnRH |
| US6416778B1 (en) | 1997-01-24 | 2002-07-09 | Femmepharma | Pharmaceutical preparations and methods for their regional administration |
| US5993856A (en) * | 1997-01-24 | 1999-11-30 | Femmepharma | Pharmaceutical preparations and methods for their administration |
| JPH10279499A (ja) * | 1997-04-04 | 1998-10-20 | Takeda Chem Ind Ltd | 子宮粘膜適用製剤 |
| PT981327E (pt) * | 1997-05-07 | 2003-02-28 | Galen Chemicals Ltd | Dispositivos intravaginais de libertacao de farmacos para a administracao de testosterona e percursores da testosterona |
| DE19815060A1 (de) * | 1998-04-03 | 1999-10-14 | Jenapharm Gmbh | Pharmazeutische Präparate zur Therapie von Nebenwirkungen während und/oder nach einer GnRHa-Therapie |
| US20040167111A1 (en) * | 1998-04-15 | 2004-08-26 | Michael Oettel | Pharmaceutical preparations for treating side effects during and/or after GnRHa therapy |
| US6217844B1 (en) | 1998-04-27 | 2001-04-17 | Praecis Pharmaceuticals, Inc. | Methods for detecting lesions in dense breast tissue using LHRH antagonists |
| US6265393B1 (en) | 1998-08-07 | 2001-07-24 | Heinrichs William Leroy | Prevention of endometriosis signs or symptons |
| US6498153B1 (en) | 1998-12-31 | 2002-12-24 | Akzo Nobel N.V. | Extended release growth promoting two component composition |
| AU5181200A (en) * | 1999-06-04 | 2000-12-28 | General Hospital Corporation, The | Pharmaceutical formulations for treating postmenopausal and perimenopausal women, and their use |
| US6503894B1 (en) | 2000-08-30 | 2003-01-07 | Unimed Pharmaceuticals, Inc. | Pharmaceutical composition and method for treating hypogonadism |
| US20040092494A9 (en) * | 2000-08-30 | 2004-05-13 | Dudley Robert E. | Method of increasing testosterone and related steroid concentrations in women |
| AU2001295359A1 (en) * | 2000-10-30 | 2002-05-15 | University Of Zurich | GnRH analogues for treatment of urinary incontinence |
| US20020107230A1 (en) * | 2000-12-22 | 2002-08-08 | Waldon R. Forrest | Methods and formulations for the treatment of female sexual dysfunction |
| EP1260225A1 (en) * | 2001-05-18 | 2002-11-27 | Pantarhei Bioscience B.V. | A pharmaceutical composition for use in hormone replacement therapy |
| PT1390040E (pt) * | 2001-05-18 | 2007-04-30 | Pantarhei Bioscience Bv | Composição farmacêutica para ser utilizado na terapia hormonal de substituição. |
| US7732430B2 (en) * | 2001-05-23 | 2010-06-08 | Pantarhei Bioscience B.V. | Drug delivery system comprising a tetrahydroxilated estrogen for use in hormonal contraception |
| ATE449606T1 (de) * | 2001-05-23 | 2009-12-15 | Pantarhei Bioscience Bv | Tetrahydroxylierte estrogen enthaltendes arzneistoffverabreichungssystem zur verwendung in hormonalen kontrazeption |
| WO2003018026A1 (en) * | 2001-08-31 | 2003-03-06 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| WO2003041718A1 (en) * | 2001-11-15 | 2003-05-22 | Pantarhei Bioscience B.V. | Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy |
| JP2005513080A (ja) * | 2001-12-20 | 2005-05-12 | フェムファーマ， インコーポレイテッド | 薬物の膣送達 |
| US20030191096A1 (en) * | 2002-04-03 | 2003-10-09 | Leonard Thomas W. | Method of hormonal therapy |
| EP1511498B1 (en) * | 2002-06-11 | 2012-11-21 | Pantarhei Bioscience B.V. | A method of treating human skin and a skin care composition for use in such a method |
| WO2003103684A1 (en) * | 2002-06-11 | 2003-12-18 | Pantarhei Bioscience B.V. | Method of treating or preventing immune mediated disorders and pharmaceutical formulation for use therein |
| EP1526856B1 (en) * | 2002-07-12 | 2008-01-02 | Pantarhei Bioscience B.V. | Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy |
| US6960337B2 (en) * | 2002-08-02 | 2005-11-01 | Balance Pharmaceuticals, Inc. | Methods and compositions for treating benign gynecological disorders |
| US7029657B2 (en) * | 2002-08-02 | 2006-04-18 | Balance Pharmaceuticals, Inc. | Nasal spray steroid formulation and method |
| US6958142B2 (en) * | 2002-08-02 | 2005-10-25 | Balance Pharmaceuticals, Inc. | Nasal spray formulation and method |
| CA2503549C (en) | 2002-10-23 | 2012-07-10 | Pantarhei Bioscience B.V. | Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy |
| US9173836B2 (en) | 2003-01-02 | 2015-11-03 | FemmeParma Holding Company, Inc. | Pharmaceutical preparations for treatments of diseases and disorders of the breast |
| MXPA05007266A (es) * | 2003-01-02 | 2006-01-17 | Femmepharma Holding Co Inc | Preparaciones farmaceuticas para tratamientos de enfermedades y trastornos del seno. |
| US7833545B2 (en) * | 2003-04-29 | 2010-11-16 | The General Hospital Corporation | Methods and devices for the sustained release of multiple drugs |
| EP1617859A1 (en) * | 2003-04-30 | 2006-01-25 | Debiopharm S.A. | Methods and compositions using gonadotropin hormone releasing hormone |
| DK1624878T3 (da) * | 2003-05-22 | 2007-01-08 | Pantarhei Bioscience Bv | Anvendelse af præparater som omfatter en östrogen komponent til behandling og forebyggelse af muskel-skelet-smerte |
| WO2005063276A1 (en) * | 2003-12-23 | 2005-07-14 | Debiopharm S.A. | Methods and compositions using gonadotropin hormone releasing hormone |
| TR201815853T4 (tr) | 2005-10-12 | 2018-11-21 | Besins Healthcare Sarl | Hipogonadizmin tedavisinde kullanıma yönelik geliştirilmiş testosteron jeli. |
| WO2008083158A2 (en) * | 2006-12-26 | 2008-07-10 | Femmepharma Holding Company, Inc. | Topical administration of danazol |
| EP2114412B1 (en) * | 2007-01-08 | 2010-07-14 | Pantarhei Bioscience B.V. | Method of treating or preventing infertility in a female mammal and pharmaceutical kit for use in such method |
| SI2249757T1 (sl) * | 2008-02-04 | 2017-10-30 | Ferring B.V. | Monolitni intravaginalni obroč, ki vsebuje progesteron ter postopki za njegovo izdelavo in uporabo |
| CN102215901B (zh) * | 2008-11-07 | 2014-12-03 | 联合生物医学系统有限公司 | 用于治疗和/或预防疾病的装置和方法 |
| US20110003000A1 (en) * | 2009-07-06 | 2011-01-06 | Femmepharma Holding Company, Inc. | Transvaginal Delivery of Drugs |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| ES2885523T3 (es) | 2011-11-23 | 2021-12-14 | Therapeuticsmd Inc | Formulaciones y terapias de reposición hormonal de combinación naturales |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| RU2016143081A (ru) | 2014-05-22 | 2018-06-26 | Терапьютиксмд, Инк. | Натуральные комбинированные гормонозаместительные составы и терапии |
| MY195019A (en) | 2015-06-18 | 2023-01-03 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| ME03728B (me) | 2015-06-18 | 2021-01-20 | Estetra Sprl | Orodisperzibilna dozna jedinica koja sadrži komponentu estetrola |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| US10286077B2 (en) | 2016-04-01 | 2019-05-14 | Therapeuticsmd, Inc. | Steroid hormone compositions in medium chain oils |
| US9931349B2 (en) | 2016-04-01 | 2018-04-03 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
| KR20220144885A (ko) | 2016-08-05 | 2022-10-27 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
| PT3518933T (pt) | 2016-09-30 | 2022-05-10 | Takeda Pharmaceuticals Co | Métodos de tratamento de fibroides uterinos e endometriose |
| CA3071660A1 (en) * | 2017-08-01 | 2019-02-07 | Fund Sa | Adjuvant therapy for use in prostate cancer treatment |
| JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| US11633405B2 (en) | 2020-02-07 | 2023-04-25 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical formulations |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3797494A (en) * | 1969-04-01 | 1974-03-19 | Alza Corp | Bandage for the administration of drug by controlled metering through microporous materials |
| US3731683A (en) * | 1971-06-04 | 1973-05-08 | Alza Corp | Bandage for the controlled metering of topical drugs to the skin |
| US4264575A (en) * | 1979-07-16 | 1981-04-28 | Eli Lilly And Company | Contraceptive methods and compositions |
| US4336243A (en) * | 1980-08-11 | 1982-06-22 | G. D. Searle & Co. | Transdermal nitroglycerin pad |
| US4762717A (en) * | 1986-03-21 | 1988-08-09 | The General Hospital Corporation | Continuous delivery of luteinizing hormone releasing hormone compositions in combination with sex steroid delivery for use as a contraceptive |
| US5130137A (en) * | 1989-08-09 | 1992-07-14 | The General Hospital Corporation | Continuous delivery of luteinizing hormone releasing hormone compositions in combination with sex steroid delivery for use in treating benign ovarian secretory disorders |
| US5211952A (en) * | 1991-04-12 | 1993-05-18 | University Of Southern California | Contraceptive methods and formulations for use therein |
-
1993
- 1993-05-17 US US08/062,883 patent/US5340585A/en not_active Expired - Fee Related
-
1994
- 1994-05-12 DK DK94917349T patent/DK0748190T3/da active
- 1994-05-12 AT AT94917349T patent/ATE245992T1/de not_active IP Right Cessation
- 1994-05-12 ES ES94917349T patent/ES2204917T3/es not_active Expired - Lifetime
- 1994-05-12 DE DE69432990T patent/DE69432990T2/de not_active Expired - Fee Related
- 1994-05-12 WO PCT/US1994/005222 patent/WO1994026207A1/en active IP Right Grant
- 1994-05-12 PT PT94917349T patent/PT748190E/pt unknown
- 1994-05-12 EP EP94917349A patent/EP0748190B1/en not_active Expired - Lifetime
- 1994-05-12 CA CA002162261A patent/CA2162261A1/en not_active Abandoned
-
1995
- 1995-11-15 NO NO19954611A patent/NO321502B1/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE69432990T2 (de) | 2004-04-22 |
| WO1994026207A1 (en) | 1994-11-24 |
| NO954611D0 (no) | 1995-11-15 |
| DK0748190T3 (da) | 2003-10-27 |
| ES2204917T3 (es) | 2004-05-01 |
| ATE245992T1 (de) | 2003-08-15 |
| EP0748190B1 (en) | 2003-07-30 |
| PT748190E (pt) | 2003-12-31 |
| EP0748190A1 (en) | 1996-12-18 |
| CA2162261A1 (en) | 1994-11-24 |
| EP0748190A4 (en) | 1998-06-10 |
| DE69432990D1 (de) | 2003-09-04 |
| US5340585A (en) | 1994-08-23 |
| NO954611L (no) | 1996-01-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP0748190B1 (en) | PROGESTOGEN-FREE FORMULATIONS OF GnRH AND ESTROGEN FOR TREATING BENIGN GYNECOLOGICAL DISORDERS | |
| CA2084891C (en) | Methods and formulations for use in inhibiting conception and in treating benign gynecological disorders | |
| CA2162260C (en) | Methods and formulations for use in treating oophorectomized women | |
| JP2703243B2 (ja) | 避妊薬用としての性ステロイド放出と組合わされた黄体形成ホルモン放出ホルモン組成物の連続放出 | |
| Magon | Gonadotropin releasing hormone agonists: Expanding vistas | |
| US6653286B1 (en) | Gonadotropin releasing hormone antagonist | |
| US7309691B2 (en) | Combined pharmaceutical preparation containing LHRH-analogous substances and anti estrogens for treating gynaecological disorders | |
| Reichel et al. | Goserelin (Zoladex) depot in the treatment of endometriosis | |
| GADSBY et al. | Control of corpus luteum function in the pregnant rabbit: role of estrogen and lack of a direct luteotropic role of the placenta | |
| US5116818A (en) | Method and kit for contraception with GnRH-antagonist | |
| BG63363B1 (bg) | Използване на антагонист на gnrh за получаване нафармацевтичен състав за лечение на гонадостероидно зависими заболявания | |
| Yeshaya et al. | Prolonged vaginal bleeding during central precocious puberty therapy with a long-acting gonadotropin-releasing hormone agonist | |
| Fraser | A review of the role of progestogens in hormonal replacement therapy: influence on bleeding patterns | |
| Segal | Contraceptives for the Twenty-First Century | |
| EP0378533A1 (en) | METHOD AND KIT FOR CONTRACEPTION WITH GnRH-ANTAGONIST AND PROGESTIN | |
| EP1092438B1 (en) | Pharmaceutical compositions containing growth-hormone inhibitors or their biologically active fragments for the treatment of uterine myomas | |
| Segal | Contraceptive innovations: needs and opportunities | |
| Bell et al. | Chemical control of fertility | |
| CA2244675A1 (en) | Pharmaceutical combined preparation and its use in the treatment of gynaecological disorders | |
| WOMEN | MJK HARPER |