JP7358484B2 - 併用療法 - Google Patents
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- JP7358484B2 JP7358484B2 JP2021540926A JP2021540926A JP7358484B2 JP 7358484 B2 JP7358484 B2 JP 7358484B2 JP 2021540926 A JP2021540926 A JP 2021540926A JP 2021540926 A JP2021540926 A JP 2021540926A JP 7358484 B2 JP7358484 B2 JP 7358484B2
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- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
- A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
Description
M-C-S-P(式中:
Mは、放射性核種であり;
Cは、前記放射性核種をキレート化することができるキレート剤であり;
Sは、CとPの間に共有結合した任意選択によるスペーサーであり;
Pは、Cに直接的に又はSを介して間接的に共有結合したソマトスタチン受容体結合ペプチドである)
の化合物である。
説明及び特許請求の範囲の両方における「ある(a)」、「ある(an)」、及び「その(the)」という冠詞の使用は、本明細書で特に示さない限り、又は明らかに文脈と矛盾しない限り、単数形と複数形の両方を網羅すると解釈されるものとする。「含む(comprising)」、「有する(having)」、「~の(beingof)」(例えば、「放射性核種及びキレート剤に連結された細胞受容体結合有機部分の」錯体におけるような)、「含む(including)」、及び「含有する(containing)」という用語は、特に断りのない限り、非制限用語として解釈されるものとする(すなわち、「~を含むが、これらに限定されない」を意味する)。加えて、「含む(comprising)」又は別の非制限用語がある実施形態で使用されるときは必ず、同じ実施形態が、中間用語「から本質的になる」又は制限用語「からなる」を使用してより狭義に言明されることがあることが理解されるものとする。
本明細書で使用する場合、「放射性標識」という用語は、典型的には金属性の放射性核種元素で標識された化合物を指す。したがって、放射性標識ソマトスタチン受容体結合化合物は、放射性核種を含み、且つソマトスタチン受容体に対して特異的な結合親和性を有する化合物である。本開示の幾つかの実施形態では、前記放射性標識ソマトスタチン受容体結合化合物は、少なくともSSTR2受容体に対して特異的な結合親和性を有する。
M-C-S-P(式中:
・ Mは、放射性核種であり;
・ Cは、前記放射性核種をキレート化することができるキレート剤であり;
・ Sは、CとPの間に共有結合した任意選択によるスペーサーであり;
・ Pは、例えばそのN末端を介して、直接的に又はSを介して間接的にCに共有結合したソマトスタチン受容体結合ペプチドである)
の化合物である。
DOTA-OC:[DOTA0,D-Phe1]オクトレオチド、
DOTA-TOC:[DOTA0,D-Phe1,Tyr3]オクトレオチド、エドトレオチド(INN)、
これは、次式によって表される:
DOTA-TATE:[DOTA0,D-Phe1,Tyr3]オクトレオテート、DOTA-Tyr3-オクトレオテート、DOTA-d-Phe-Cys-Tyr-d-Trp-Lys-Thr-Cys-Thr(シクロ2,7)、オキソドトレオチド(INN)、これは、次式によって表される:
DOTA-VAP:[DOTA0,D-Phe1,Tyr3]バプレオチド。
次式によって表される:
(aii)キレート剤に連結された細胞受容体結合有機部分
によって形成される錯体と;
(b)放射線分解に対する少なくとも1つの安定剤と
を含み、
前記放射性核種が、少なくとも100MBq/mL、好ましくは少なくとも250MBq/mLの体積放射能をもたらす濃度で存在する、医薬水溶液。
(aii)キレート剤が連結したソマトスタチン受容体結合有機部分である、DOTA-TATE(オキソドトレオチド)又はDOTA-TOC(エドトレオチド)
によって形成される錯体と;
(bi)0.5~1mg/mLの濃度で存在する、放射線分解に対する第1の安定剤としてのゲンチシン酸又はその塩と;
(bii)2.0~5.0mg/mLの濃度で存在する、放射線分解に対する第2の安定剤としてのアスコルビン酸又はその塩と
を含む、医薬水溶液。
を更に含む、実施形態23による医薬水溶液。
を更に含む、実施形態23又は24による医薬水溶液。
(1)以下によって、放射性核種と、キレート剤が連結した細胞受容体結合有機部分との錯体を形成する工程
(1.1)放射性核種を含む水溶液を調製する工程;
(1.2)キレート剤が連結した細胞受容体結合有機部分、第1の安定剤、任意選択により第2の安定剤を含む水溶液を調製する工程;並びに
(1.3)工程(1.1)及び(1.2)で得られた溶液を混合し、得られた混合物を加熱する工程;
(2)以下によって、工程(1)によって得られた錯体溶液を希釈する工程
(2.1)任意選択により第2の安定剤を含む水性希釈溶液を調製する工程;並びに
(2.2.)工程(1)によって得られた錯体溶液を、工程(2.1)で得られた希釈溶液と混合する工程
を含み得る。
本明細書で使用する場合、PARP阻害剤とは、酵素ポリADPリボースポリメラーゼの薬理学的阻害剤を指す。
本開示は、癌を有する対象を治療する方法であって、前記対象にペプチド受容体放射性核種療法(PRRT)とPARP阻害剤療法との組み合わせを投与する工程を含む方法を対象とする。
本発明は、本明細書で定義する通りの放射性核種177Lu(ルテチウム-177)及びキレート剤に連結されたソマトスタチン受容体結合ペプチドによって形成された錯体、又は本明細書で定義する通りの医薬水溶液を、以下に概説する1種又は複数の治療剤と合わせた組み合わせ又は併用療法を更に提供する。
177LuCl3は、商業的供給元、例えば、I.D.B.HollandBV社から得ることができる。DOTA0-Tyr3-オクトレオテートは、商業的供給元、例えば、piCHEMForschungs-undEntwicklungsGmbH(オーストリア)から得ることができる。製剤の他のすべての成分は、様々な供給元から市販されている。
製剤の組成
製剤(177Lu-DOTA0-Tyr3-オクトレオテートの370MBq/mLの輸液)は、基準日時(較正時間(tc))で370MBq/mLの体積放射能を有する177Lu-DOTA0-Tyr3-オクトレオテートを原薬として含有する、滅菌した即時使用可能な輸液として設計される。較正時間(tc)は、製造終了に相当し(EOP=t0)、最初のQCバイアルの放射能を測定する時間である。製剤の貯蔵寿命は、較正時間後72時間に設定する。製剤は、注射時間に7.4GBqの放射能の送達を可能にするのに適した量の溶液を含有する単回用量バイアルである。
製剤の製造
74GBqのバッチサイズ(2Ciのバッチサイズ)の場合、HCl中約74GBqである177LuCl3溶液を、DOTA-Tyr3-オクトレオテート(約2mg)溶液、及び酸化防止剤(及び放射線分解に対する安定剤)(すなわち、ゲンチシン酸、約157mg)と緩衝系(すなわち、酢酸緩衝液系)とを含有する反応緩衝液溶液と一緒に混合して合計約5.5mLの溶液とし、それを約90~約98℃の温度で15分以内に行う放射性標識に使用する。
CA20948腫瘍モデルを使用する併用療法
BALB-c免疫不全マウスに神経内分泌腫瘍細胞を異種移植した。治療機会を延ばすために、PARP阻害剤の投与をPRRT注射の2日前から開始し、合計14日間行った。
PRRTの群とPRRT+オラパリブの群からの動物は両方とも、注射後3日で始まる腫瘍の縮小を示した。PRRT+オラパリブの群からの平均腫瘍サイズの方が速く減少し、小さいサイズになった。PRRT+オラパリブでの腫瘍再増殖までの時間は、PRRTと比較して有意に増加する。腫瘍再増殖の速度は、両方の群で同じである。PRRT+オラパリブの生存中央値は、PRRTと比較して有意に増加し、PRRT+オラパリブの群における1匹の動物(10%)は、臨床での完全奏功を示した。オラパリブによる腫瘍増殖及び生存への効果は、ビヒクルと比較して何も観察されなかった(図1を参照されたい)。
このinvivo実験は活性を示すことから、オラパリブのこのレジメンがGEP-NETにおけるPRRTの放射線増感剤として使用できることが示される。
Claims (13)
- 癌の治療を必要とする対象における癌の治療における使用のための、放射性標識ソマトスタチン受容体結合化合物を含む医薬組成物であって、放射性標識ソマトスタチン受容体結合化合物が、 177 Lu-DOTA-TATE( 177 Lu-オキソドトレオチド)であり、前記医薬組成物は、オラパリブ、ニラパリブ、及びルカパリブから選択されるPARP阻害剤と組み合わせて投与され、PARP阻害剤が、前記医薬組成物の1回目の投与の7~2日前に最初に投与される、医薬組成物。
- 前記癌が、消化管及び膵臓の神経内分泌腫瘍である、膵消化管神経内分泌腫瘍(GEP-NET)である、請求項1に記載の医薬組成物。
- 2~4用量の7.4GBqの177Lu-DOTA-TATEが対象に投与される、請求項1又は2に記載の医薬組成物。
- 177Lu-DOTA-TATEの投与が、6~10週毎に行われる、請求項3に記載の医薬組成物。
- ソマトスタチン受容体結合化合物療法とPARP阻害剤療法との併用効果によって、全体的な奏効率が、単一のPPRTと比較して、少なくとも10%、20%、30%、40%、又は少なくとも50%まで増加する、請求項1~4のいずれか一項に記載の医薬組成物。
- 前記癌が神経内分泌腫瘍である、請求項1~5のいずれか一項に記載の医薬組成物。
- 前記神経内分泌腫瘍が、膵消化管神経内分泌腫瘍(GEP-NET)、カルチノイド腫瘍、膵神経内分泌腫瘍、下垂体腺腫、副腎腫瘍、メルケル細胞癌、乳癌、非ホジキンリンパ腫、ホジキンリンパ腫、頭頸部腫瘍、尿路上皮癌(膀胱)、腎細胞癌、肝細胞癌、GIST、神経芽細胞腫、胆管腫瘍、子宮頸部腫瘍、ユーイング肉腫、骨肉腫、小細胞肺癌、前立腺癌、メラノーマ、髄膜腫、神経膠腫、髄芽腫、血管芽腫、テント上原始神経外胚葉性腫瘍、及び感覚神経芽細胞腫からなる群から選択される、請求項6に記載の医薬組成物。
- 前記神経内分泌腫瘍が、機能性カルチノイド腫瘍、インスリノーマ、ガストリノーマ、血管作動性腸ペプチド(VIP)オーマ、グルカゴノーマ、セロトニノーマ、ヒスタミノーマ、ACTHオーマ、褐色細胞腫、及びソマトスタチノーマからなる群から選択される、請求項6に記載の医薬組成物。
- 前記神経内分泌腫瘍が、低グレード、中グレード、又は高グレードの神経内分泌腫瘍である、請求項6に記載の医薬組成物。
- 前記神経内分泌腫瘍が手術不能なGEP-NETである、請求項6に記載の医薬組成物。
- 前記神経内分泌腫瘍が、68Ga-DOTA-TATE PETスキャンによって示されるSSTR陽性疾患である、請求項6に記載の医薬組成物。
- PARP阻害剤が、オラパリブである、請求項1に記載の医薬組成物。
- オラパリブが、300mg、400mg、若しくは800mgの投薬量で1日1回、又は50mg~400mgの投薬量で1日2回、必要とする対象に投与される、請求項12に記載の医薬組成物。
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