JP7265600B2 - 癌を治療するためのkras阻害剤の投与 - Google Patents
癌を治療するためのkras阻害剤の投与 Download PDFInfo
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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Description
本出願は、2019年5月14日出願の米国仮特許出願第62/847,862号及び2019年6月27日に出願の米国仮特許出願第62/867,747号の利益を主張するものであり、前記特許はどちらも本明細書に完全に記載されているかのように全体として及びあらゆる目的のために参照により本明細書に組み込まれる。
第1実施形態では、本開示は、癌を治療する方法であって、それを必要とする対象に180mg、360mg、720mg若しくは960mgの1日量で化合物Aを投与するステップを含み、ここで化合物Aが、以下の構造:
本明細書に開示した方法の実施形態では、対象には化合物Aが本明細書に開示した用量で少なくとも1カ月間、少なくとも6週間、少なくとも2カ月間、少なくとも3カ月間、少なくとも4カ月間、少なくとも5カ月間又は少なくとも6カ月間投与される。
一部の実施形態では、本明細書に開示した方法における化合物Aによって治療される対象は、少なくとも1種以上の先行全身性癌療法を受けていた対象である(例えば、化合物Aは、第2選択又は第3選択療法である)。一部の実施形態では、本明細書に開示した方法における化合物Aによって治療される対象は、少なくとも1種の先行全身性癌の後に疾患の増悪を有する対象である(即ち、化合物Aは、第2選択療法である)。一部の実施形態では、本明細書に開示した方法における化合物Aによって治療される対象は、少なくとも2種の先行全身性癌療法の後に疾患の増悪を有する対象である(即ち、化合物Aは、第3選択療法である)。先行全身性癌療法は、規制当局(例えば、FDA又はEMA)によって所定のタイプ及び病期の癌の治療として承認された任意の療法であり得る。一部の場合に、先行全身性癌療法は、規制当局によっては未だ承認されていないが臨床試験を受けている癌療法である。対象が先行全身性癌療法を受けていた場合は、一部の場合に、対象は、化合物Aを用いる本明細書に開示した療法を開始する前に、少なくとも1カ月間、少なくとも2カ月間、少なくとも3カ月間、少なくとも4カ月間、少なくとも5カ月間又は少なくとも6カ月間に渡り何れかの全身性癌療法を受けていなかった。
血液学的毒性:発熱性好中球減少症;好中球減少性感染症;グレード4の好中球減少症;>7日間のグレード≧3の血小板減少症;≧2のグレードの出血を伴うグレード3の血小板減少症;グレード4の血小板減少症;グレード4の貧血
非血液学的毒性:グレード≧4の嘔吐若しくは下痢;グレード3の下痢若しくは最高の医療支援にもかかわらず4日間以上持続するグレード3の嘔吐;最高の医療支援にもかかわらず3日間以上に渡るグレード≧3の悪心;何れかの他のグレード≧3のAE
本開示は、他の経路若しくは同じ経路の他の成分を調節することが知られている薬剤又は更に標的酵素の重複するセットが化合物A又はその薬学的に許容される塩と組み合わせて使用される、併用療法の方法も又提供する。一態様では、そのような療法は、相乗的又は相加的な治療効果を提供するために、本明細書に開示した化合物Aと化学療法剤との併用を含むが、これには限定されない。
A.最初の結果
化合物Aの投与試験:本試験には、KRAS G12C突然変異を有する癌であると同定された患者が登録された。患者は、局所進行性若しくは転移性KRAS G12C突然変異固形腫瘍を有する成人患者であった。全患者は、以前に腫瘍のタイプ及び疾患病期に依存する先行標準療法を受けていた。進行性脳転移を示した患者はいなかった。投与試験を受ける患者は、次の診断を受けていた:14例は非小細胞肺癌(NSCLC)、10例は結腸直腸癌(CRC)及び2例は別のKRAS G12C突然変異固形腫瘍の診断を受けていた。化合物Aは、指定用量で1日1回経口投与された。患者には180mg、360mg、720mg又は960mgの用量の化合物Aが投与され、6週間毎に放射線による精査が実施された。
この試験の更新された結果は、これによりその内容が全体として本明細書に組み込まれる、スペインのバルセロナで2019年9月27日~10月1日まで開催された欧州臨床腫瘍学会議(European Society of Medical Onclology(ESMO))の会議でGovindan,R.,et.al.,“Phase 1 Study of AMG 510,a Novel KRASG12C Inhibitor,in Advanced Solid Tumors With KRAS p.G12C Mutation”によってポスターとして提示されている。本試験の詳細な結果は、それらの内容が全体として本明細書に組み込まれる、米国眼治療学会議(ASCO)の2020年5月29~31日の会議(バーチャル)でFakih,M.G.,et al.,‘‘CodeBreak 100:activity of AMG 510,a novel small molecule inhibitor of KRASG12C,in patients with advanced colorectal cancer’’及びHong,D.S.,et al.,“CodeBreak 100:Phase 1 study of AMG 510,a novel KRASG12C inhibitor,in patients with advanced solid tumors other than non-small-cell lung cancer(NSCLC)and colorectal cancer(CRC)’’によって提示されるであろう。
最初の患者は、2018年8月27日に登録された。2019年7月17日のカットオフ日現在までに患者76例が登録されたが、それらの内患者34例はNSCLCを有していた(SCLCの患者1例(この患者はカットオフ日現在にSCLC(「他の腫瘍タイプ」カテゴリー)であると記録されていたが、カットオフ後に治験参加機関によってNSCLCに変更された)。患者45例は用量漸増コホートに登録され(総1日量180mg(N=6)、総1日量360mg(N=13)、総1日量720mg(N=11)、総1日量960mg(N=15))、患者31例は用量拡大コホートに登録され(総1日量960mg(N=31))、初回の6週間毎の精査を受けた、又は早期進行(PD)を示した55例の患者が評価可能となった。登録患者76例中、52例は治療中のままとなったが、24例はPD(N=22)及び死亡(N=2)のために治療を中止した。ここで注目に値するのは、治療関連有害事象による治療中止が1例も誘発されなかったことである。
2020年1月8日のカットオフ日現在、CRC患者42例が登録された(総1日量180mgのコホート1:患者3例、総1日量360mgのコホート2:患者10例、総1日量720mgのコホート3:患者4例;総1日量960mgのコホート4:患者25例)。メジアンフォローアップ期間は、7.9カ月間(範囲:4.2~15.9カ月間)であった。患者8例は、治療を継続した。患者34例は、疾患の進行(32例)及び患者(2例)からの要請のために治療を中止した。全登録患者は、先行ラインの全身性抗癌療法を受けていた。患者の45%は、4ライン以上の治療を受けた。
2020年1月8日のカットオフ日までに、下記の腫瘍タイプ:膵臓癌(10例)、虫垂癌(4例)、子宮内膜癌(2例)、原発巣不明癌(2例)、胆管癌(1例)、副鼻腔癌(1例)、乳頭部癌(1例)、小腸癌(1例)、黒色腫(1例)、小細胞肺癌(1例)及び食道癌(1例)の患者25例が登録された。虫垂癌の患者2例は、化合物Aのそれぞれ360及び720mgの総1日量を摂取した。残りの患者23例は、総1日量960mgの化合物Aを摂取した。メジアンフォローアップ期間は、4.3カ月間(範囲:0.1~12.6カ月間)であった。患者22例は7週間以上のフォローアップ検査を受けており、応答について評価可能であった。カットオフ日までに、患者12例は、最も一般的な原因として進行を示し、治療を中止した。全登録患者は、先行ラインの全身性抗癌療法を受けており、登録患者の84%は、2つ以上の先行ラインを受けていた。
Claims (10)
- 前記患者が、前記化合物を最初に投与する前に、少なくとも1種の全身性がん療法を受けている、請求項1に記載の医薬組成物。
- 前記患者が、前記化合物を最初に投与する前に、少なくとも2種の全身性がん療法を受けている、請求項1に記載の医薬組成物。
- 前記化合物が経口投与される、請求項1~3の何れか一項に記載の医薬組成物。
- 前記化合物が錠剤として投与される、請求項4に記載の医薬組成物。
- 前記患者が、前記化合物を最初に投与する前に、少なくとも1種の全身性がん療法を受けている、請求項6に記載の使用。
- 前記患者が、前記化合物を最初に投与する前に、少なくとも2種の全身性がん療法を受けている、請求項6に記載の使用。
- 前記化合物が経口投与される、請求項6~8の何れか一項に記載の使用。
- 前記化合物が錠剤として投与される、請求項9に記載の使用。
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Application Number | Priority Date | Filing Date | Title |
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JP2023065418A JP7300076B1 (ja) | 2019-05-14 | 2023-04-13 | 癌を治療するためのkras阻害剤の投与 |
JP2023098289A JP2023116708A (ja) | 2019-05-14 | 2023-06-15 | 癌を治療するためのkras阻害剤の投与 |
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Application Number | Priority Date | Filing Date | Title |
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US201962847862P | 2019-05-14 | 2019-05-14 | |
US62/847,862 | 2019-05-14 | ||
US201962867747P | 2019-06-27 | 2019-06-27 | |
US62/867,747 | 2019-06-27 | ||
JP2021500906A JP6963146B1 (ja) | 2019-05-14 | 2020-05-13 | 癌を治療するためのkras阻害剤の投与 |
PCT/US2020/032686 WO2020232130A1 (en) | 2019-05-14 | 2020-05-13 | Dosing of kras inhibitor for treatment of cancers |
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JP2021500906A Division JP6963146B1 (ja) | 2019-05-14 | 2020-05-13 | 癌を治療するためのkras阻害剤の投与 |
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JP2023065418A Division JP7300076B1 (ja) | 2019-05-14 | 2023-04-13 | 癌を治療するためのkras阻害剤の投与 |
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JP2022009090A JP2022009090A (ja) | 2022-01-14 |
JP2022009090A5 JP2022009090A5 (ja) | 2023-04-03 |
JP7265600B2 true JP7265600B2 (ja) | 2023-04-26 |
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JP2021500906A Active JP6963146B1 (ja) | 2019-05-14 | 2020-05-13 | 癌を治療するためのkras阻害剤の投与 |
JP2021168089A Active JP7265600B2 (ja) | 2019-05-14 | 2021-10-13 | 癌を治療するためのkras阻害剤の投与 |
JP2023065418A Active JP7300076B1 (ja) | 2019-05-14 | 2023-04-13 | 癌を治療するためのkras阻害剤の投与 |
JP2023098289A Pending JP2023116708A (ja) | 2019-05-14 | 2023-06-15 | 癌を治療するためのkras阻害剤の投与 |
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JP2023098289A Pending JP2023116708A (ja) | 2019-05-14 | 2023-06-15 | 癌を治療するためのkras阻害剤の投与 |
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US (2) | US11426404B2 (ja) |
EP (2) | EP3738593A1 (ja) |
JP (4) | JP6963146B1 (ja) |
CN (1) | CN113840606A (ja) |
AU (1) | AU2020275845A1 (ja) |
BR (1) | BR112021022812A2 (ja) |
CA (1) | CA3139519A1 (ja) |
IL (1) | IL287838A (ja) |
MA (1) | MA55959A (ja) |
MX (1) | MX2021013788A (ja) |
SG (1) | SG11202112432PA (ja) |
TW (2) | TWI826344B (ja) |
WO (1) | WO2020232130A1 (ja) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
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HUE056777T2 (hu) | 2016-12-22 | 2022-03-28 | Amgen Inc | Benzizotiazol-, izotiazolo[3,4-b]piridin-, kinazolin-, ftálazin-, pirido[2,3-d]piridazin- és pirido[2,3-d]pirimidin-származékok mint KRAS G12C inhibitorok tüdõ-, hasnyálmirigy- vagy vastagbélrák kezelésére |
JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
JP7150823B2 (ja) | 2017-09-08 | 2022-10-11 | アムジエン・インコーポレーテツド | KRas G12Cの阻害剤及びそれを使用する方法 |
US11090304B2 (en) | 2018-05-04 | 2021-08-17 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
JP7361722B2 (ja) | 2018-05-04 | 2023-10-16 | アムジエン・インコーポレーテツド | Kras g12c阻害剤及び同一物の使用方法 |
WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
EP3790886A1 (en) | 2018-05-10 | 2021-03-17 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
WO2019232419A1 (en) | 2018-06-01 | 2019-12-05 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
AU2019336588B2 (en) | 2018-06-12 | 2022-07-28 | Amgen Inc. | KRAS G12C inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer |
JP2020090482A (ja) | 2018-11-16 | 2020-06-11 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
CA3117222A1 (en) | 2018-11-19 | 2020-05-28 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
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WO2020232130A1 (en) | 2020-11-19 |
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US20200360374A1 (en) | 2020-11-19 |
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