JP2018532715A5 - - Google Patents

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Publication number

JP2018532715A5

JP2018532715A5 JP2018512876A JP2018512876A JP2018532715A5 JP 2018532715 A5 JP2018532715 A5 JP 2018532715A5 JP 2018512876 A JP2018512876 A JP 2018512876A JP 2018512876 A JP2018512876 A JP 2018512876A JP 2018532715 A5 JP2018532715 A5 JP 2018532715A5

Authority

JP

Japan

Prior art keywords

amino acid

region

seq

acid sequence

sequence shown

Prior art date

2016-09-09

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

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• 125000003275 alpha amino acid group Chemical group 0.000 claims description 158
• 102100035360 Cerebellar degeneration-related antigen 1 Human genes 0.000 claims description 49
• 229940049595 antibody-drug conjugate Drugs 0.000 claims description 29
• 206010028980 Neoplasm Diseases 0.000 claims description 15
• 201000011510 cancer Diseases 0.000 claims description 15
• 239000007787 solid Substances 0.000 claims description 15
• 230000037396 body weight Effects 0.000 claims description 11
• 238000006467 substitution reaction Methods 0.000 claims description 10
• 238000009115 maintenance therapy Methods 0.000 claims description 8
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 7
• 239000008194 pharmaceutical composition Substances 0.000 claims description 7
• 239000000611 antibody drug conjugate Substances 0.000 claims description 6
• 206010060862 Prostate cancer Diseases 0.000 claims description 5
• 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 5
• 108010044540 auristatin Proteins 0.000 claims description 5
• 238000012986 modification Methods 0.000 claims description 5
• 230000004048 modification Effects 0.000 claims description 5
• IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims description 4
• 150000001413 amino acids Chemical class 0.000 claims description 4
• 238000001802 infusion Methods 0.000 claims description 4
• 108010093470 monomethyl auristatin E Proteins 0.000 claims description 4
• 230000000284 resting effect Effects 0.000 claims description 4
• 150000003839 salts Chemical class 0.000 claims description 4
• 125000003396 thiol group Chemical group [H]S* 0.000 claims description 4
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
• 239000003937 drug carrier Substances 0.000 claims description 3
• 201000005202 lung cancer Diseases 0.000 claims description 3
• 208000020816 lung neoplasm Diseases 0.000 claims description 3
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 3
• 229910052717 sulfur Inorganic materials 0.000 claims description 3
• 125000004434 sulfur atom Chemical group 0.000 claims description 3
• 210000003679 cervix uteri Anatomy 0.000 claims description 2
• 238000002648 combination therapy Methods 0.000 claims description 2
• 210000004696 endometrium Anatomy 0.000 claims description 2
• 210000003238 esophagus Anatomy 0.000 claims description 2
• 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
• 238000002347 injection Methods 0.000 claims description 2
• 239000007924 injection Substances 0.000 claims description 2
• 238000001990 intravenous administration Methods 0.000 claims description 2
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
• 210000001672 ovary Anatomy 0.000 claims description 2
• 210000002307 prostate Anatomy 0.000 claims description 2
• 238000009097 single-agent therapy Methods 0.000 claims description 2
• 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
• 210000003932 urinary bladder Anatomy 0.000 claims description 2
• 239000003814 drug Substances 0.000 claims 28
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
• 201000010536 head and neck cancer Diseases 0.000 claims 1
• 210000004072 lung Anatomy 0.000 claims 1
• 238000000034 method Methods 0.000 description 9
• 206010005003 Bladder cancer Diseases 0.000 description 1
• 206010014733 Endometrial cancer Diseases 0.000 description 1
• 206010014759 Endometrial neoplasm Diseases 0.000 description 1
• 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
• 206010033128 Ovarian cancer Diseases 0.000 description 1
• 206010061535 Ovarian neoplasm Diseases 0.000 description 1
• 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
• 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
• 201000010881 cervical cancer Diseases 0.000 description 1
• 201000004101 esophageal cancer Diseases 0.000 description 1
• 210000003128 head Anatomy 0.000 description 1
• 208000026037 malignant tumor of neck Diseases 0.000 description 1
• 210000003739 neck Anatomy 0.000 description 1
• 210000000496 pancreas Anatomy 0.000 description 1
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
• 201000005112 urinary bladder cancer Diseases 0.000 description 1