JP2017510607A5 - - Google Patents

Info

Publication number

JP2017510607A5

JP2017510607A5 JP2016561731A JP2016561731A JP2017510607A5 JP 2017510607 A5 JP2017510607 A5 JP 2017510607A5 JP 2016561731 A JP2016561731 A JP 2016561731A JP 2016561731 A JP2016561731 A JP 2016561731A JP 2017510607 A5 JP2017510607 A5 JP 2017510607A5

Authority

JP

Japan

Prior art keywords

day

siponimod

dosage form

treatment

medicament

Prior art date

2015-04-08

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 claims description 134
• 229950005693 siponimod Drugs 0.000 claims description 134
• 239000002552 dosage form Substances 0.000 claims description 56
• 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 40
• 239000003814 drug Substances 0.000 claims description 32
• 201000008628 secondary progressive multiple sclerosis Diseases 0.000 claims description 31
• 208000007118 chronic progressive multiple sclerosis Diseases 0.000 claims description 30
• 238000012423 maintenance Methods 0.000 claims description 23
• 230000001363 autoimmune Effects 0.000 claims description 11
• 208000023275 Autoimmune disease Diseases 0.000 claims description 10
• 238000001727 in vivo Methods 0.000 claims description 10
• 230000002057 chronotropic effect Effects 0.000 claims description 9
• 230000000694 effects Effects 0.000 claims description 9
• 208000016285 Movement disease Diseases 0.000 claims description 8
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
• 208000035475 disorder Diseases 0.000 claims description 7
• 230000003902 lesion Effects 0.000 claims description 6
• 239000008363 phosphate buffer Substances 0.000 claims description 6
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 6
• 229920000053 polysorbate 80 Polymers 0.000 claims description 6
• VKZRWSNIWNFCIQ-WDSKDSINSA-N (2s)-2-[2-[[(1s)-1,2-dicarboxyethyl]amino]ethylamino]butanedioic acid Chemical compound OC(=O)C[C@@H](C(O)=O)NCCN[C@H](C(O)=O)CC(O)=O VKZRWSNIWNFCIQ-WDSKDSINSA-N 0.000 claims description 4
• 238000000338 in vitro Methods 0.000 claims description 4
• 239000003223 protective agent Substances 0.000 claims description 3
• OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims description 2
• 208000034189 Sclerosis Diseases 0.000 claims description 2
• 239000004067 bulking agent Substances 0.000 claims description 2
• 239000004359 castor oil Substances 0.000 claims description 2
• 235000019438 castor oil Nutrition 0.000 claims description 2
• 239000007884 disintegrant Substances 0.000 claims description 2
• 230000005713 exacerbation Effects 0.000 claims description 2
• 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 claims description 2
• 229940049654 glyceryl behenate Drugs 0.000 claims description 2
• FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims description 2
• 229940046813 glyceryl palmitostearate Drugs 0.000 claims description 2
• 239000008172 hydrogenated vegetable oil Substances 0.000 claims description 2
• 238000004519 manufacturing process Methods 0.000 claims description 2
• 201000006417 multiple sclerosis Diseases 0.000 claims description 2
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
• 230000000750 progressive effect Effects 0.000 claims description 2
• 229940114926 stearate Drugs 0.000 claims description 2
• 229940079593 drug Drugs 0.000 claims 6
• 239000011814 protection agent Substances 0.000 claims 1
• 238000000034 method Methods 0.000 description 5
• 230000000747 cardiac effect Effects 0.000 description 1
• 238000012544 monitoring process Methods 0.000 description 1