JP2005504787A5 - - Google Patents

Info

Publication number

JP2005504787A5

JP2005504787A5 JP2003526373A JP2003526373A JP2005504787A5 JP 2005504787 A5 JP2005504787 A5 JP 2005504787A5 JP 2003526373 A JP2003526373 A JP 2003526373A JP 2003526373 A JP2003526373 A JP 2003526373A JP 2005504787 A5 JP2005504787 A5 JP 2005504787A5

Authority

JP

Japan

Prior art keywords

suspension

peptide

hydrophobic peptide

aqueous suspension

gnrh

Prior art date

2002-08-27

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.)

Pending

Links

• Espacenet
• Global Dossier
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• 238000000034 method Methods 0.000 claims 29
• 108090000765 processed proteins & peptides Proteins 0.000 claims 22
• 239000000725 suspension Substances 0.000 claims 20
• 239000007900 aqueous suspension Substances 0.000 claims 15
• 230000002209 hydrophobic effect Effects 0.000 claims 15
• 239000002474 gonadorelin antagonist Substances 0.000 claims 12
• 229940121381 gonadotrophin releasing hormone (gnrh) antagonists Drugs 0.000 claims 12
• DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 7
• 239000007951 isotonicity adjuster Substances 0.000 claims 7
• NMJREATYWWNIKX-UHFFFAOYSA-N GnRH Chemical class 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 6
• QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 6
• DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 6
• 150000002500 ions Chemical class 0.000 claims 6
• 150000003839 salts Chemical class 0.000 claims 6
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 4
• 229930195725 Mannitol Natural products 0.000 claims 4
• QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 4
• 239000012736 aqueous medium Substances 0.000 claims 4
• 239000012530 fluid Substances 0.000 claims 4
• 239000012931 lyophilized formulation Substances 0.000 claims 4
• 235000010355 mannitol Nutrition 0.000 claims 4
• 239000000594 mannitol Substances 0.000 claims 4
• 239000000546 pharmaceutical excipient Substances 0.000 claims 4
• 108010023617 abarelix Proteins 0.000 claims 3
• AIWRTTMUVOZGPW-HSPKUQOVSA-N abarelix Chemical compound C([C@@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 AIWRTTMUVOZGPW-HSPKUQOVSA-N 0.000 claims 3
• 229960002184 abarelix Drugs 0.000 claims 3
• 239000002253 acid Substances 0.000 claims 3
• 229940127233 azaline B Drugs 0.000 claims 3
• 108700008462 cetrorelix Proteins 0.000 claims 3
• 229960003230 cetrorelix Drugs 0.000 claims 3
• SBNPWPIBESPSIF-MHWMIDJBSA-N cetrorelix Chemical compound C([C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 SBNPWPIBESPSIF-MHWMIDJBSA-N 0.000 claims 3
• 238000009472 formulation Methods 0.000 claims 3
• 108700032141 ganirelix Proteins 0.000 claims 3
• 229960003794 ganirelix Drugs 0.000 claims 3
• GJNXBNATEDXMAK-PFLSVRRQSA-N ganirelix Chemical compound C([C@@H](C(=O)N[C@H](CCCCN=C(NCC)NCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN=C(NCC)NCC)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 GJNXBNATEDXMAK-PFLSVRRQSA-N 0.000 claims 3
• 239000000203 mixture Substances 0.000 claims 3
• 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 3
• 238000013268 sustained release Methods 0.000 claims 3
• 239000012730 sustained-release form Substances 0.000 claims 3
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
• NOENHWMKHNSHGX-IZOOSHNJSA-N (2s)-1-[(2s)-2-[[(2s)-2-[[(2r)-2-[[(2r)-2-[[(2s)-2-[[(2r)-2-[[(2s)-2-[[(2r)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-(ca Chemical compound C([C@H](C(=O)N[C@H](CCCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 NOENHWMKHNSHGX-IZOOSHNJSA-N 0.000 claims 2
• 108010070670 antarelix Proteins 0.000 claims 2
• 230000015572 biosynthetic process Effects 0.000 claims 2
• 238000011065 in-situ storage Methods 0.000 claims 2
• 108010083551 iturelix Proteins 0.000 claims 2
• QRYFGTULTGLGHU-NBERXCRTSA-N iturelix Chemical compound C([C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CCCCNC(=O)C=1C=NC=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)CCCNC(=O)C1=CC=CN=C1 QRYFGTULTGLGHU-NBERXCRTSA-N 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 239000013081 microcrystal Substances 0.000 claims 2
• 239000002245 particle Substances 0.000 claims 2
• 238000002360 preparation method Methods 0.000 claims 2
• 229950011372 teverelix Drugs 0.000 claims 2
• -1 antid Chemical compound 0.000 claims 1
• 239000007853 buffer solution Substances 0.000 claims 1
• 238000004108 freeze drying Methods 0.000 claims 1
• 238000001727 in vivo Methods 0.000 claims 1
• 239000007788 liquid Substances 0.000 claims 1
• 238000001694 spray drying Methods 0.000 claims 1
• 239000012929 tonicity agent Substances 0.000 claims 1