JPWO2020236562A5 - - Google Patents
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- Publication number
- JPWO2020236562A5 JPWO2020236562A5 JP2021568514A JP2021568514A JPWO2020236562A5 JP WO2020236562 A5 JPWO2020236562 A5 JP WO2020236562A5 JP 2021568514 A JP2021568514 A JP 2021568514A JP 2021568514 A JP2021568514 A JP 2021568514A JP WO2020236562 A5 JPWO2020236562 A5 JP WO2020236562A5
- Authority
- JP
- Japan
- Prior art keywords
- eflornithine
- sulindac
- patient
- medicament
- agent
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 claims description 88
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims description 39
- 229960000894 sulindac Drugs 0.000 claims description 37
- 229960002759 eflornithine Drugs 0.000 claims description 35
- VLCYCQAOQCDTCN-UHFFFAOYSA-N eflornithine Chemical compound NCCCC(N)(C(F)F)C(O)=O VLCYCQAOQCDTCN-UHFFFAOYSA-N 0.000 claims description 35
- 239000000203 mixture Substances 0.000 claims description 22
- 201000006107 Familial adenomatous polyposis Diseases 0.000 claims description 21
- 208000029664 classic familial adenomatous polyposis Diseases 0.000 claims description 21
- 108700028369 Alleles Proteins 0.000 claims description 16
- 101150010646 ODC1 gene Proteins 0.000 claims description 16
- 238000009472 formulation Methods 0.000 claims description 16
- 210000003750 lower gastrointestinal tract Anatomy 0.000 claims description 15
- 230000001934 delay Effects 0.000 claims description 9
- FJPAMFNRCFEGSD-UHFFFAOYSA-N eflornithine hydrochloride monohydrate Chemical group O.Cl.NCCCC(N)(C(F)F)C(O)=O FJPAMFNRCFEGSD-UHFFFAOYSA-N 0.000 claims description 8
- 208000003200 Adenoma Diseases 0.000 claims description 7
- 206010001233 Adenoma benign Diseases 0.000 claims description 7
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 210000001072 colon Anatomy 0.000 claims description 5
- VKDGNNYJFSHYKD-UHFFFAOYSA-N 2,5-diamino-2-(difluoromethyl)pentanoic acid;hydron;chloride Chemical group Cl.NCCCC(N)(C(F)F)C(O)=O VKDGNNYJFSHYKD-UHFFFAOYSA-N 0.000 claims description 4
- 229960002046 eflornithine hydrochloride Drugs 0.000 claims description 4
- 239000007902 hard capsule Substances 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- 239000007901 soft capsule Substances 0.000 claims description 4
- 239000003826 tablet Substances 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 230000015572 biosynthetic process Effects 0.000 claims description 3
- 238000012143 endoscopic resection Methods 0.000 claims description 3
- 208000015768 polyposis Diseases 0.000 claims description 3
- 238000002271 resection Methods 0.000 claims description 3
- 238000001356 surgical procedure Methods 0.000 claims description 3
- 239000002552 dosage form Substances 0.000 claims description 2
- -1 eflornithine HCl monohydrate Chemical class 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- 210000000664 rectum Anatomy 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 19
- 239000003795 chemical substances by application Substances 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 2
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 206010033109 Ototoxicity Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
- 229940063655 aluminum stearate Drugs 0.000 description 1
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 1
- 239000004327 boric acid Substances 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 229940078456 calcium stearate Drugs 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 229940057948 magnesium stearate Drugs 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- 231100000262 ototoxicity Toxicity 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 1
- 229940080350 sodium stearate Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962849590P | 2019-05-17 | 2019-05-17 | |
| US62/849,590 | 2019-05-17 | ||
| PCT/US2020/033080 WO2020236562A1 (en) | 2019-05-17 | 2020-05-15 | Methods for treating familial adenomatous polyposis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022532766A JP2022532766A (ja) | 2022-07-19 |
| JPWO2020236562A5 true JPWO2020236562A5 (https=) | 2023-05-16 |
| JP2022532766A5 JP2022532766A5 (https=) | 2023-05-16 |
Family
ID=70978606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021568514A Pending JP2022532766A (ja) | 2019-05-17 | 2020-05-15 | 家族性腺腫性ポリポーシスを処置するための方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (3) | US10945981B2 (https=) |
| EP (1) | EP3968971A1 (https=) |
| JP (1) | JP2022532766A (https=) |
| CN (1) | CN114096240A (https=) |
| WO (1) | WO2020236562A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7262118B2 (ja) * | 2016-10-06 | 2023-04-21 | オーバス セラピューティクス インコーポレイテッド | 医薬組成物およびその使用 |
| JP2022532766A (ja) * | 2019-05-17 | 2022-07-19 | キャンサー プリベンション ファーマシューティカルズ，インコーポレイテッド | 家族性腺腫性ポリポーシスを処置するための方法 |
| WO2023283427A2 (en) * | 2021-07-09 | 2023-01-12 | Verdure Biotech, Inc. | Enteric and delayed release formulations of locally bioavailable drugs (lbd) targeting the colon |
| WO2026013052A1 (en) * | 2024-07-09 | 2026-01-15 | Institut National de la Santé et de la Recherche Médicale | Methods of treating familial adenomatous polyposis |
| US12605349B2 (en) | 2024-09-05 | 2026-04-21 | Orbus Therapeutics, Inc. | Methods of treating grade 3 astrocytoma |
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| JP2022532766A (ja) * | 2019-05-17 | 2022-07-19 | キャンサー プリベンション ファーマシューティカルズ，インコーポレイテッド | 家族性腺腫性ポリポーシスを処置するための方法 |
-
2020
- 2020-05-15 JP JP2021568514A patent/JP2022532766A/ja active Pending
- 2020-05-15 WO PCT/US2020/033080 patent/WO2020236562A1/en not_active Ceased
- 2020-05-15 US US16/875,156 patent/US10945981B2/en active Active
- 2020-05-15 CN CN202080050079.2A patent/CN114096240A/zh active Pending
- 2020-05-15 EP EP20730839.6A patent/EP3968971A1/en active Pending
-
2021
- 2021-03-15 US US17/201,877 patent/US20220040130A1/en not_active Abandoned
-
2024
- 2024-11-22 US US18/956,720 patent/US20250186380A1/en active Pending
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