JP2022551164A - 骨髄異形成症候群及び急性骨髄性白血病を治療するための併用療法 - Google Patents
骨髄異形成症候群及び急性骨髄性白血病を治療するための併用療法 Download PDFInfo
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Abstract
Description
本出願は、2019年10月18日に出願された米国特許仮出願第62/916,949号、2019年12月6日に出願された米国特許仮出願第62/944,851号、及び2020年5月28日に出願された米国特許仮出願第63/031,438号の優先権の利益を主張するものであり、これらの各々は、すべての目的のためにその全体が参照により本明細書に組み込まれる。
本出願は、EFS-Webを介して提出された配列表を含み、その全体が参照により本明細書に組み込まれる。2020年10月9日に作成された当該ASCIIコピーは、FSI-006_P3F_SLと名付けられ、145,290バイトのサイズである。
特許請求の範囲及び本明細書で使用される用語は、特に明記しない限り、以下に特定されるように定義される。
抗体:
抗CD47剤
CD47抗体
抗SIRPα剤
SIRPα抗体
併用療法のための追加の薬剤
キナーゼ挿入ドメイン受容体(KDR)、キネシン様タンパク質KIF11、カーステンマウス肉腫ウイルスがん遺伝子ホモログ(KRAS)遺伝子、キスぺプチン(KiSS-1)受容体、KIT遺伝子、v-kit Hardy-Zuckerman4ネコ肉腫ウイルスがん遺伝子ホモログ(KIT)チロシンキナーゼ、ラクトフェリン、ラノステロール-14デメチラーゼ、LDL受容体関連タンパク質1、白血球免疫グロブリン様受容体サブファミリーBメンバー1(ILT 2)、白血球免疫グロブリン様受容体サブファミリーBメンバー2(ILT 4)、ロイコトリエンA4ヒドロラーゼ、リステリオリジン、L-セレクチン、黄体ホルモン受容体、リアーゼ、リンパ球活性化遺伝子3タンパク質(LAG-3)、リンパ球抗原75、リンパ球機能抗原3受容体、リンパ球特異的プロテインキナーゼ(LCK)、リンホタクチン、Lyn(Lck/Yes novel)チロシンキナーゼ、リジンデメチラーゼ(KDM1、KDM2、KDM4、KDM5、KDM6、A/B/C/Dなど)、リゾホスファチジン酸-1受容体、リソソーム関連膜タンパク質ファミリー(LAMP)遺伝子、リジルオキシダーゼホモログ2、リジルオキシダーゼタンパク質(LOX)、5-リポキシゲナーゼ(5-LOX)、造血前駆細胞キナーゼ1(HPK1)、肝細胞成長因子受容体(MET)遺伝子、マクロファージコロニー刺激因子(MCSF)リガンド、マクロファージ遊走阻害因子、MAGEC1遺伝子、MAGEC2遺伝子、主要ヴォールトタンパク質、MAPK活性化プロテインキナーゼ(MK2)、Mas関連Gタンパク質結合受容体、マトリックスメタロプロテアーゼ(MMP2、MMP9などのMMP)、Mcl-1分化タンパク質、Mdm2 p53結合タンパク質、Mdm4タンパク質、メランA(MART-1)、黒色腫抗原、メラニン細胞タンパク質Pmel 17、メラニン細胞刺激ホルモンリガンド、黒色腫抗原ファミリーA3(MAGEA3)遺伝子、黒色腫関連抗原(例えば、1、2、3、6など)、膜銅アミンオキシダーゼ、メソテリン、METチロシンキナーゼ、代謝型グルタミン酸受容体1、メタロレダクターゼSTEAP1(前立腺1の6回膜貫通上皮抗原)、メタスチン、メチオニンアミノペプチダーゼ-2、メチルトランスフェラーゼ、ミトコンドリア3ケトアシルCoAチオラーゼ、マイトジェン活性化プロテインキナーゼ(MAPK)、マイトジェン活性化プロテインキナーゼ(MEK1、MEK2などのMEK)、mTOR(ラパマイシン標的タンパク質(セリン/スレオニンキナーゼ))、mTOR複合体(1、2など)、ムチン(1、5A、16など)、mut Tホモログ(MTH1などのMTH)、Mycがん原遺伝子タンパク質、骨髄系細胞白血病1(MCL1)遺伝子、ミリストイル化アラニン富化プロテインキナーゼC基質(MARCKS)タンパク質、NAD ADPリボシルトランスフェラーゼ、ナトリウム利尿ペプチド受容体C、神経細胞接着分子1、ニューロキニン1(NK1)受容体、ニューロキニン受容体、ニューロピリン2、NFカッパB活性化タンパク質、NIMA関連キナーゼ9(NEK 9)、一酸化窒素シンターゼ、NK細胞受容体、NK3受容体、NKG2 A B活性化NK受容体、NLRP3(NACHT LRR PYDドメインタンパク質3)修飾因子、ノルアドレナリン輸送体、ノッチ(ノッチ-2受容体、ノッチ-3受容体、ノッチ-4受容体など)、核赤血球2関連因子2、核因子(NF)カッパB、ヌクレオリン、ヌクレオホスミン、ヌクレオホスミン-未分化リンパ腫キナーゼ(NPM-ALK)、2オキソグルタル酸デヒドロゲナーゼ、2,5-オリゴアデニル酸シンターゼ、O-メチルグルタミンDNAメチルトランスフェラーゼ、オピオイド受容体(デルタなど)、オルニチンデカルボキシラーゼ、オロチン酸ホスホリボシルトランスフェラーゼ、オーファン核ホルモン受容体NR4A1、オステオカルシン、破骨細胞分化因子、オステオポンチン、OX-40(腫瘍壊死因子受容体スーパーファミリーメンバー4 TNFRSF4又はCD134)受容体、P3タンパク質、p38キナーゼ、p38 MAPキナーゼ、p53腫瘍抑制タンパク質、副甲状腺ホルモンリガンド、ペルオキシソーム増殖因子活性化受容体(アルファ、デルタ、ガンマなどのPPAR)、P-糖タンパク質(1など)、ホスファターゼ・テンシンホモログ(PTEN)、ホスファチジルイノシトール3キナーゼ(PI3K)、ホスホイノシチド-3キナーゼ(アルファ、デルタガンマなどのPI3K)、ホスホリラーゼキナーゼ(PK)、PKN3遺伝子、胎盤成長因子、血小板由来成長因子(アルファ、ベータなどのPDGF)、血小板由来成長因子(アルファ、ベータなどのPDGF)、多剤耐性輸送体、プレキシンB1、PLK1遺伝子、ポロ様キナーゼ(PLK)、ポロ様キナーゼ1、ポリ(ADP-リボーズ)ポリメラーゼ(PARP1、PARP2、及びPARP3、PARP7、並びにモノ-PARPなどのPARP)、好ましくは黒色腫で発現される抗原(PRAME)遺伝子、プレニル結合タンパク質(PrPB)、高可能性転写因子(Probable transcription factor)PML、プロゲステロン受容体、プログラム細胞死1(PD-1)、プログラム細胞死リガンド1阻害剤(PD-L1)、プロサポシン(PSAP)遺伝子、プロスタノイド受容体(EP4)、プロスタグランジンE2シンターゼ、前立腺特異的抗原、前立腺酸性ホスファターゼ、プロテアソーム、タンパク質E7、タンパク質ファルネシルトランスフェラーゼ、プロテインキナーゼ(A、B、CなどのPK)、タンパク質チロシンキナーゼ、タンパク質チロシンホスファターゼベータ、がん原遺伝子セリン/スレオニンプロテインキナーゼ(PIM-1、PIM-2、PIM-3などのPIM)、P-セレクチン、プリンヌクレオシドホスホリラーゼ、プリン作動性受容体P2Xリガンド開口型イオンチャネル7(P2X7)、ピルビン酸デヒドロゲナーゼ(PDH)、ピルビン酸デヒドロゲナーゼキナーゼ、ピルビン酸キナーゼ(PYK)、5-アルファレダクターゼ、Rafプロテインキナーゼ(1、Bなど)、RAF1遺伝子、Ras遺伝子、Ras GTPase、RET遺伝子、Retチロシンキナーゼ受容体、網膜芽細胞関連タンパク質、レチノイン酸受容体(ガンマなど)、レチノイドX受容体、Rheb(脳で富化されるRasホモログ)GTPase、Rho(Rasホモログ)関連プロテインキナーゼ2、リボヌクレアーゼ、リボヌクレオチドレダクターゼ(M2サブユニットなど)、リボソームタンパク質S6キナーゼ、RNAポリメラーゼ(I、IIなど)、Ron(Recepteur d’Origine Nantais)チロシンキナーゼ、ROS1(ROSがん原遺伝子1、受容体チロシンキナーゼ)遺伝子、Ros1チロシンキナーゼ、Runt関連転写因子3、ガンマセクレターゼ、S100カルシウム結合タンパク質A9、Sarco内質カルシウムATPase、カスパーゼの第2のミトコンドリア由来活性化因子(SMAC)タンパク質、分泌frizzled関連タンパク質-2、分泌ホスホリパーゼA2、セマフォリン-4D、セリンプロテアーゼ、セリン/スレオニンキナーゼ(STK)、セリン/スレオニンプロテインキナーゼ(TBK1などのTBK)、シグナル伝達兼転写(STAT-1、STAT-3、STAT-5などのSTAT)、シグナル伝達リンパ球性活性化分子(SLAM)ファミリーメンバー7、前立腺の6回膜貫通上皮抗原(STEAP)遺伝子、SLサイトカインリガンド、スムーズンド(SMO)受容体、ナトリウムヨウ化物共輸送体、ナトリウムリン酸共輸送体2B、ソマトスタチン受容体(1、2、3、4、5など)、ソニックヘッジホッグタンパク質、セブンレスの息子(SOS)、特異的タンパク質(Sp1)転写因子、スフィンゴミエリンシンターゼ、スフィンゴシンキナーゼ(1、2など)、スフィンゴシン-1-リン酸受容体1、脾臓チロシンキナーゼ(SYK)、SRC遺伝子、Src-チロシンキナーゼ、スタビリン-1(STAB1)、STAT3遺伝子、ステロイドスルファターゼ、インターフェロン遺伝子の刺激因子(STING)受容体、インターフェロン遺伝子の刺激因子タンパク質、間質細胞由来因子1リガンド、SUMO(小さいユビキチン様修飾因子)、スーパーオキシドディスムターゼ、チロシンシグナル伝達修飾因子の抑制因子(SOCS)、サバイビンタンパク質、シナプシン3、シンデカン1、シヌクレインアルファ、T細胞表面糖タンパク質CD28、tank結合キナーゼ(TBK)、TATAボックス結合タンパク質関連因子RNAポリメラーゼIサブユニットB(TAF1B)遺伝子、T細胞CD3糖タンパク質ゼータ鎖、T細胞分化抗原CD6、T細胞免疫グロブリン及びムチンドメイン含有-3(TIM-3)、T細胞糖タンパク質CD8、Tecタンパク質チロシンキナーゼ、Tekチロシンキナーゼ受容体、テロメラーゼ、テロメラーゼ逆転写酵(TERT)遺伝子、テネイシン、スリープライム修復エクソヌクレアーゼ1(TREX1)、スリープライム修復エクソヌクレアーゼ2(TREX2)、トロンボポエチン受容体、チミジンキナーゼ、チミジンホスホリラーゼ、チミジル酸シンターゼ、チモシン(アルファ1など)、甲状腺ホルモン受容体、甲状腺刺激ホルモン受容体、組織因子、TNF関連アポトーシス誘導リガンド、TNFR1関連デスドメインタンパク質、TNF関連アポトーシス誘導リガンド(TRAIL)受容体、TNFSF11遺伝子、TNFSF9遺伝子、Toll様受容体(1~13などのTLR)、トポイソメラーゼ(I、II、IIIなど)、転写因子、トランスフェラーゼ、トランスフェリン(TF)、トランスフォーミング成長因子アルファ(TGFα)、トランスフォーミング成長因子ベータ(TGFB)及びそのアイソフォーム、TGFベータ2リガンド、トランスフォーミング成長因子TGF-B受容体キナーゼ、トランスグルタミナーゼ、転位関連タンパク質、膜貫通糖タンパク質NMB、Trop-2カルシウムシグナルトランスデューサー、栄養膜糖タンパク質(TPBG)遺伝子、栄養膜糖タンパク質、トロポミオシン受容体キナーゼ(Trk)受容体(TrkA、TrkB、TrkCなど)、トリプトファン2,3-ジオキシゲナーゼ(TDO)、トリプトファン5-ヒドロキシラーゼ、チューブリン、腫瘍壊死因子(アルファ、ベータなどのTNF)、腫瘍壊死因子13C受容体、腫瘍進行遺伝子座2(TPL2)、腫瘍タンパク質53(TP53)遺伝子、腫瘍抑制候補2(TUSC2)遺伝子、腫瘍特異的ネオ抗原、チロシナーゼ、チロシンヒドロキシラーゼ、チロシンキナーゼ(TK)、チロシンキナーゼ受容体、チロシンキナーゼ受容体、チロシンキナーゼ受容体、免疫グロブリン様及びEGF様ドメインを伴うチロシンキナーゼ(TIE)受容体、チロシンプロテインキナーゼABL1阻害剤、ユビキチン、ユビキチンカルボキシルヒドロラーゼアイソザイムL5、ユビキチンチオエステラーゼ14、ユビキチンコンジュゲート酵E2I(UBE2I、UBC9)、ユビキチン特異的プロセシングプロテアーゼ7(USP7)、ウレアーゼ、ウロキナーゼプラスミノーゲン活性化因子、ウテログロビン、バニロイドVR1、血管細胞接着タンパク質1、血管内皮成長因子受容体(VEGFR)、T細胞活性化のVドメインIg抑制因子(VISTA)、VEGF-1受容体、VEGF-2受容体、VEGF-3受容体、VEGF-A、VEGF-B、ビメンチン、ビタミンD3受容体、がん原遺伝子チロシン-プロテインキナーゼ、Mer(Merチロシンキナーゼ受容体修飾因子)、YAP(Yes関連タンパク質修飾因子)es、Wee-1プロテインキナーゼ、ウェルナー症候群RecQ1様ヘリカーゼ(WRN)、ウイルムス腫瘍抗原1、ウイルムス腫瘍タンパク質、WWドメイン含有転写調節因子タンパク質1(TAZ)、X連鎖アポトーシス抑制タンパク質、ジンクフィンガータンパク質転写因子、又はそれらの組み合わせを含むが、これらに
限定されない標的(例えば、ポリペプチド又はポリヌクレオチド)の阻害剤、アゴニスト、アンタゴニスト、リガンド、調節剤、刺激因子、遮断薬、活性化因子、又は抑制因子を含むが、これらに限定されない1つ以上の追加の治療薬と組み合わされる。
CC-90011などのリジン特異的ヒストンデメチラーゼ1阻害剤;MEDI 1191などのIL-12 Mrna;RGT-100などのRIG-I調節剤;SB-9200及びIR-103などのNOD2調節剤;レボノルゲストレルなどのプロゲステロン受容体アゴニスト;CC-92480、CC-90009などのタンパク質セレブロン調節剤;イベルドミドなどのタンパク質セレブロン調節剤/DNA結合タンパク質Ikaros阻害剤/ジンクフィンガー結合タンパク質Aiolos阻害剤;アリトレチノイン、ベキサロテン(経口製剤)などのレチノイドX受容体調節剤;GSK-3145095などのRIP-1キナーゼ阻害剤;AZD9833などの選択的エストロゲン受容体分解剤;TAK-981などのSUMO阻害剤;エルトロンボパグなどのトロンボポエチン受容体アゴニスト;レボチロキシンナトリウムなどの甲状腺ホルモン受容体アゴニスト;タソネルミンなどのTNFアゴニスト;CC-95251などのチロシンホスファターゼ基質1阻害剤;ネラチニブ、ツカチニブ(ONT-380)などのHER2阻害剤;テセバチニブなどのEGFR/ErbB2/Ephb4阻害剤;TAK-788などのEGFR/HER2阻害剤;DZD-9008などのEGFRファミリーチロシンキナーゼ受容体阻害剤;バリチニブなどのEGFR/ErbB-2阻害剤;PF-06747775、EGF816(ナザルチニブ)、ASP8273、ACEA-0010、BI-1482694などの変異選択的EGFR阻害剤;MM-310などのepha2阻害剤;MAK683などのポリコームタンパク質(EED)阻害剤;プララトレキサートなどのDHFR阻害剤/葉酸輸送体1調節剤/葉酸受容体アンタゴニスト;ペメトレキセドニナトリウムなどのDHFR/GARトランスホルミラーゼ/チミミジル酸シンターゼ/トランスフェラーゼ阻害剤;ラリメチニブなどのp38 MAPキナーゼ阻害剤;MS203、PF-06939999、GSK3368715、GSK3326595などのPRMT阻害剤;オパガニブなどのスフィンゴシンキナーゼ2(SK2)阻害剤;オマベロキソロン(RTA-408)などの核赤血球2関連因子2刺激因子;LOXO-195、ONO-7579などのトロポミオシン受容体キナーゼ(TRK)阻害剤;GO-203-2Cなどのムチン1阻害剤;BIO-11006などのMARCKSタンパク質阻害剤;アルフォリチキソリンなどの葉酸アンタゴニスト;GR-MD-02などのガレクチン-3阻害剤;RX-5902などのリン酸化P68阻害剤;ofranergene obadenovecなどのCD95/TNF調節剤;INCB-053914などのpan-PIMキナーゼ阻害剤;EGEN-001、タボキノゲンテルセプラスミドなどのIL-12遺伝子刺激因子;TAS-116、PEN-866などの熱ショックタンパク質HSP90阻害剤;MP-0250などのVEGF/HGFアンタゴニスト;ベバシズマブバイオシミラーなどのVEGFリガンド阻害剤;ラムシルマブなどのVEGF受容体アンタゴニスト/VEGFリガンド阻害剤;VEGF-1/VEGF-2/VEGF-3受容体アンタゴニスト;フルキンチニブなど;HLA-A2402/HLA-A0201制限エピトープペプチドワクチンなどのVEGF-1/VEGF-2受容体調節剤;アフリベルセプトなどの胎盤成長因子リガンド阻害剤/VEGF-Aリガンド阻害剤;ASN-002などのSYKチロシンキナーゼ/JAKチロシンキナーゼ阻害剤;ラロトレクチニブ硫酸塩などのTrkチロシンキナーゼ受容体阻害剤;CS-12912などのJAK3/JAK1/TBK1キナーゼ阻害剤;AD-IL24などのIL-24アンタゴニスト;BMS-986299などのNLRP3(NACHT LRR PYDドメインタンパク質3)調節剤;RGT-100などのRIG-Iアゴニスト;トプサリシンなどのエロリジン刺激因子;HM-30181AなどのP糖タンパク質1阻害剤;ARRY-382、BLZ-945などのCSF-1アンタゴニスト;JTX-1811、I-309、SB-649701、HG-1013、RAP-310などのCCR8阻害剤;SEL-403などの抗メソセリン抗体;アグラチマゲンベサデノベクなどのチミジンキナーゼ刺激因子;PCM-075、オンバンセルチブなどのPolo様キナーゼ1阻害剤;ペボネジスタット(MLN-4924)、TAS-4464などのNAE阻害剤;アバドミド(CC-122)などの多経路調節剤;ペボネジスタットなどのアミロイドタンパク質結合タンパク質-1阻害剤/ユビキチンリガーゼ調節剤;チオストレプトプトンなどのFoxM1阻害剤;TAK-243などのUBA1阻害剤;VAL-201などのSrcチロシンキナーゼ阻害剤;VDA-1102などのVDAC/HK阻害剤;ロヒニチブ、eFT226などのElf4a阻害剤;ad-p53などのTP53遺伝子刺激因子;トレチノインなどのレチノイン酸受容体アゴニスト;SY-1425などのレチノイン酸受容体アルファ(RARα)阻害剤;YC8-02などのSIRT3阻害剤;オラプテストペゴル(NOX-A12)などの間質細胞由来因子1リガンド阻害剤;MDNA-55などのIL-4受容体調節剤;ペグジラリギナーゼなどのアルギナーゼI刺激因子;イリノテカン塩酸塩、オニバイドなどのトポイソメラーゼI阻害剤;PEG-SN38(フィルテカンペゴル)などのトポイソメラーゼI阻害剤/低酸素誘導因子-1アルファ阻害剤;PT-2977、PT-2385などの低酸素誘導性因子-1アルファ阻害剤;プロロイキン(アルデスロイキン、IL-2)などのCD122(IL-2受容体)アゴニスト;ペグ化IL-2(例えば、NKTR-214);IL-2の修飾バリアント(例えば、THOR-707);NKTR-262などのTLR7/TLR8アゴニスト;DS-0509、GS-9620、LHC-165、TMX-101(イミキモド)などのTLR7アゴニスト;ケベトリンなどのp53腫瘍抑制タンパク質刺激因子;ALRN-6924などのMdm4/Mdm2 p53結合タンパク質阻害剤;フィラネシブ(ARRY-520)などのキネシンスピンドルタンパク質(KSP)阻害剤;FPT-155などのCD80-fc融合タンパク質阻害剤;KO-539などのメニン及び混合形質型白血病(MLL)阻害剤;RGX-104などの肝臓x受容体アゴニスト;ペグイロデカキン(AM-0010)などのIL-10アゴニスト;ボロラニブなどのVEGFR/PDGFR阻害剤;CA-4948などのIRAK4阻害剤;OPN-305などの抗TLR-2抗体;CBP-501などのカルモジュリン調節剤。
S11-001)などの細菌性ベクターワクチン;nadofaragene firadenovecなどのアデノウイルスベクターワクチン;自己Gp96ワクチン;
CVactm、tapuldencel-T、eltrapuldencel-T、SL-701、BSK01TM、rocapuldencel-T(AGS-003)、DCVAC、CVactm、stapuldencel-T、eltrapuldencel-T、SL-701、BSK01TM、ADXS31-142、自家樹状細胞ワクチン(転移性悪性黒色腫、皮内/静脈内、Universitatsklinikum Erlangen)などの樹状細胞ワクチン;タリモジンラヘルパレプベク、pexastimogene devacirepvec、GL-ONC1、MG1-MA3、パルボウイルスH-1、ProstAtak、エナデノチュシレブ、MG1MA3、ASN-002(TG-1042)などの腫瘍溶解性ワクチン;CVAC-301、CMP-001、CreaVax-BC、PF-06753512、VBI-1901、TG-4010、ProscaVax(商標)などの治療ワクチン;Vigil(登録商標)(IND-14205)、Oncoquest-Lワクチンなどの腫瘍細胞ワクチン;PVS-RIPOなどの弱毒性組換え血清型1ポリオウイルスワクチン;Adagloxad simolenin;MEDI-0457;DPV-001腫瘍由来オートファゴソームリッチがんワクチン;CV-9209、LV-305などのRNAワクチン;MEDI-0457、MVI-816、INO-5401などのDNAワクチン;MVA-p53などのp53を発現する修飾されたワクシニアウイルスAnkaraワクチン;DPX-Survivac;BriaVax(商標);GI-6301;GI-6207;GI-4000;IO-103;AGEN-2017、GEN-010、NeoVax、RG-6180、GEN-009、PGV-001(TLR-3アゴニスト)、GRANITE-001、NEO-PV-01などのネオ抗原ペプチドワクチン;PhosphoSynVax(商標)などの熱ショックタンパク質を標的とするペプチドワクチン;Vitespen(HSPPC-96-C)、アルドキソルビシンを含有するNANT結腸直腸がんワクチン、自家腫瘍細胞ワクチン+全身性CpG-B+IFN-アルファ(がん)、IO-120+IO-103(PD-L 1/PD-L2ワクチン)、HB-201、HB-202、HB-301、TheraT(登録商標)*ベースのワクチン;ポリICLC(NSC-301463)などのTLR-3アゴニスト/インターフェロン誘導因子;ナパブバカシン(BBI-608)などのSTAT-3阻害剤;CB-5083などのATPase p97阻害剤;Odomzo(登録商標)(ソニデギブ、旧LDE-225)、LEQ506、ビスモデギブ(GDC-0449)、BMS-833923、グラスデギブ(PF-04449913)、LY2940680、及びイトラコナゾールなどのスムーズンド(SMO)受容体阻害剤;インターフェロンアルファ-2b、インターフェロンアルファ-2aバイオシミラー(Biogenomics)、ropegインターフェロンアルファ-2b(AOP-2014、P-1101、PEG IFNアルファ-2b)、マルチフェロン(アルファナチベ、Viragen)、インターフェロンアルファ1b、ロフェロン-A(カンフェロン、Ro-25-3036)、インターフェロンアルファ-2aバイオ後続品(Biosidus)(インムタグ(Inmutag)、Inter 2A)、インターフェロンアルファ-2bバイオ後続品(Biosidus-ビオフェロン、シトフェロン、ガナパー(Ganapar)、Beijing Kawin Technology-カフェロン)、アルファフェロン、PEG化インターフェロンアルファ-1b、ペグインターフェロンアルファ-2bバイオ後続品(Amega)、組換えヒトインターフェロンアルファ-1b、組換えヒトインターフェロンアルファ-2a、組換えヒトインターフェロンアルファ-2b、ベルツズマブ-IFNアルファ2b connjyuge-to、Dynavax(SD-101)、及びインターフェロンアルファ-n1(Humoferon、SM-10500、スミフェロン)などのインターフェロンアルファリガンド調節剤;インターフェロンガンマ(OH-6000、Ogamma100)などのインターフェロンガンマリガンド調節剤;テルトモチド(GV-1001、HR-2802、Riavax)及びイメテルスタット(GRN-163、JNJ-63935937)などのテロメラーゼ調節剤;テモゾロミド(CCRG-81045)、デシタビン、グアデシタビン(S-110、SGI-110)、KRX-0402、RX-3117、RRx-001、及びアザシチジン(CC-486)などのDNAメチルトランスフェラーゼ阻害剤;ピキサントロン及びソブゾキサンなどのDNAジャイレース阻害剤;アムルビシンなどのDNAジャイレース阻害剤/トポイシメラーゼII阻害剤;ABT-263、ベネトクラックス(ABT-199)、ABT-737、RG7601、及びAT-101などのBcl-2ファミリータンパク質阻害剤;ノビトクラックスなどのBcl-2/Bcl-XL阻害剤;LY3039478(クレニガアセタット)、タレクスツマブ(抗Notch2/3)、BMS-906024などのNotch阻害剤;PEGPH-20などのヒアルロニダーゼ刺激因子;Herceptin HylectaなどのErbb2チロシンキナーゼ受容体阻害剤/ヒアルロニダーゼ刺激因子;SM-04755、PRI-724、WNT-974などのWnt経路阻害剤;PF-03084014、MK-0752、RO-4929097などのガンマ-セクレターゼ阻害剤;BP1001などのGrb-2(成長因子受容体結合タンパク質-2)阻害剤;ONC201、ABBV-621などのTRAIL経路誘導化合物;SCB-313などのTRAIL調節剤;VS-4718、デファクチニブ、GSK2256098などの接着斑キナーゼ阻害剤;サリデギブ、ソノデギブ(LDE225)、グラスデギブなどのヘッジホッグ阻害剤;アリセルチブ(MLN-8237)、及びAZD-2811、AMG-900、バラセルチブ、ENMD-2076などのオーロラキナーゼ阻害剤;ブリブジン、アパトルセンなどのHSPB1調節剤(熱ショックタンパク質27、HSP27);BAY-937、AZD6738、AZD6783、VX-803、VX-970(ベルゾセルチブ)及びVX-970などのATR阻害剤;AUY922、オナレスピブ(AT13387)、SNX-2112、SNX5422などのHsp90阻害剤;DS-3032b、RG7775、AMG-232、HDM201、及びイダザヌツリン(RG7388)などのマウス二重微小染色体(mdm2)がん遺伝子阻害剤;ウレルマブ、ウトミルマブ(PF-05082566)、AGEN2373、ADG-106、BT-7480、QL1806などのCD137アゴニスト;ADU-S100(MIW-815)、SB-11285、MK-1454、SR-8291、AdVCA0848、GSK-532、SYN-STING、MSA-1、SR-8291、GSK3745417などのSTINGアゴニスト;FGF-401、INCB-054828、BAY-1163877、AZD4547、JNJ-42756493、LY2874455、Debio-1347などのFGFR阻害剤;TVB-2640などの脂肪酸シンターゼ(FASN)阻害剤;A6などのCD44結合剤;LB-100などのタンパク質ホスファテアーゼ2A(PP2A)阻害剤;セビテロンネル(VT-464)、ASN-001、ODM-204、CFG920、酢酸アビラテロンなどのCYP17阻害剤;IRX4204などのRXRアゴニスト;タラデギブ、パチデギブ、ビスモデギブなどのヘッジホッグ/スムーズンド(hh/Smo)アンタゴニスト;Imprime PGGなどの補体C3調節剤;ALT-803、NKTR-255、インターロイキン-15/Fc融合タンパク質、AM-0015、NIZ-985、及びhetIL-15などのIL-15アゴニスト;タゼメトスタット、CPI-1205、GSK-2816126、PF-06821497などのEZH2(zesteホモログ2のエンハンサー)阻害剤;pelareorep、CG-0070、MV-NIS療法、HSV-1716、DS-1647、VCN-01、ONCOS-102、TBI-1401、tasadenoturev(DNX-2401)、vocimagene amiretrorepvec、RP-1、CVA21、Celyvir、LOAd-703、OBP-301、IMLYGIC(登録商標)などの腫瘍溶解性ウイルス;ピノメトスタット(EPZ-5676)などのDOT1L(ヒストンメチルトランスフェラーゼ)阻害剤Cholera毒素、リシン、Pseudomonas外毒素、Bordetella pertussisアデニル酸シクラーゼ毒素、ジフテリア毒素、及びカスパーゼ活性化因子などの毒素;BC-819などのDNAプラスミド;ボラセルチブ(PLK1)などのPLK1、2、及び3のPLK阻害剤;AZD-1775(アダボセルチブ)などのWEE1阻害剤;AT13148、KD025などのRhoキナーゼ(ROCK)阻害剤;ASTX660、debio-1143、ビリナパント、APG-1387、LCL-161などのアポトーシス阻害タンパク質(IAP)阻害剤;ルルビネクテジン(PM-1183)、CX-5461などのRNAポリメラーゼ阻害剤;PM-184、BAL-101553(リサバンブリン)、及びOXI-4503、フルオラパシン(AC-0001)、プリナブリン、ビンフルニンなどのチューブリン阻害剤;G100、GSK1795091、及びPEPA-10などのToll様受容体4(TLR-4)アゴニスト;プリチデプシンなどの伸長因子1アルファ2阻害剤;デニロイキンジフチトクスなどの伸長因子2阻害剤/インターロイキン-2リガンド/NAD ADPリボシルトランスフェラーゼ刺激因子;APG-101、APO-010、アスネルセプトなどのCD95阻害剤;DSP-7888などのWT1阻害剤;H3B-8800などのスプライシング因子3Bサブユニット1(SF3B1)阻害剤;LYC-55716などのレチノイドZ受容体ガンマ(RORγ)アゴニスト;及びSER-401、EDP-1503、MRx-0518などの微生物叢調節剤。
TNF受容体スーパーファミリー(TNFRSF)メンバーのアゴニスト又は活性化因子
免疫チェックポイント阻害剤
Toll様受容体(TLR)アゴニスト
TCRシグナル伝達調節剤
アデノシン生成及びシグナル伝達
二重特異性T細胞誘導因子(Bi-Specific T-Cell Engager)
二重及び三重特異性ナチュラルキラー(NK)細胞誘導因子
造血前駆細胞キナーゼ1(HPK1)阻害剤
アポトーシスシグナル調節キナーゼ(ASK)阻害剤
ブルトン型チロシンキナーゼ(BTK)阻害剤
サイクリン依存性キナーゼ(CDK)阻害剤
ジスコイジンドメイン受容体(DDR)阻害剤。
ヒストンデアセチラーゼ(HDAC)阻害剤
インドレアミン-ピロール-2,3-ジオキシゲナーゼ(IDO1)阻害剤;
ヤヌスキナーゼ(JAK)阻害剤
マトリックスメタロプロテアーゼ(MMP)阻害剤
RAS及びRAS経路阻害剤
脾臓チロシンキナーゼ(SYK)阻害剤
チロシンキナーゼ阻害剤(TKI)
化学療法剤(標準治療)
抗血管新生剤
抗線維化剤
抗炎症剤
腫瘍酸素化剤
免疫療法剤
がん遺伝子療法及び細胞療法
細胞療法
腫瘍を標的とする追加の薬剤
MCL1アポトーシス調節物質、BCL2ファミリーメンバー(MCL1)阻害剤
サイトカイン誘導性SH2含有タンパク質(CISH)阻害剤
遺伝子エディタ
不特定の標的を有する他の薬物
例示的な併用療法
リンパ腫又は白血病併用療法
非ホジキンリンパ腫の併用療法
マントル細胞リンパ腫の併用療法
ワルデンシュトレーム型マクログロブリン血症の併用療法
びまん性大細胞型B細胞リンパ腫併用療法
慢性リンパ球白血病併用療法
骨髄線維症の併用療法
過剰増殖性障害併用療法
低メチル化剤
造血障害
P53変異
対象の状態及び選択
投薬
プライマー剤及び初回刺激用量
投薬サイクル
投与
臨床エンドポイント
医薬組成物
キット
実施例1:血液悪性腫瘍の患者におけるアザシチジンと組み合わせたHu5F9-G4
序論
研究設計及びスキーマ
1.R/Rコホート:Hu5F9-G4を以前に受けていない再発性及び/若しくは不応性AML又はMDS患者は、安全性導入(run-in)コホートではHu5F9-G4単剤療法、又はこの研究の拡大コホートではアザシチジンと組み合わせてHu5F9-G4を受けた(合計N=最大46人)。
2.TN/Uコホート:標準的な導入化学療法に不適格なAML患者、及び以前に未治療の、IPSS-Rによる中等度/高/非常に高リスクのMDS患者で、この研究でアザシチジンと組み合わせてHu5F9-G4を受けた患者、少なくとも91人の中等度から非常に高リスクのMDS患者が治療された(合計N=最大121人)。TN/Uは、治療未処置/不適合(標準的な導入化学療法に)を表す。
3.継続コホート:第1相R/R AML研究でHu5F9-G4を受け、この研究でHu5F9-G4単剤療法を継続する患者(合計N=最大8人)。
R/Rコホートを2段階で評価した。10人の患者(R/R安全性コホート)を安全性導入で治療して、このR/R集団におけるHu5F9-G4単剤療法の安全性プロファイルを評価した。R/R安全性コホートにおける総合臨床、安全性、PK、及び薬力学的データに基づいて、臨床試験運営委員会(Clinical Trial Steering Committee)(CTSC)は、登録が初期のR/Rコホートの拡大段階で開始することができるかどうかを決定し、R/R拡大コホートの合計最大36人の追加の患者を治療して、アザシチジンと組み合わせてHu5F9-G4の臨床活性を評価した。R/R拡大コホートでは、Hu5F9-G4は、表2に示されるように、週に2回(1日目及び4日目)、1週目に1mg/kg;8日目に15mg/kg;11日目及び15日目に30mg/kg、並びに22日目からサイクル2の終了まで毎週30mg/kg、その後、サイクル3からそれ以降、Q2週30mg/kgを、臨床、PK、及び薬力学的データに基づいて、及びより便利な投薬レジメンの評価のために投与した。患者がサイクルにわたって1日目の治療のみを受けた場合、患者は、このサイクル以降のバランスのために、そのサイクルで新しい投薬レジメンに移行し得る。
研究設計-TN/Uコホート用量レベル
研究設計-継続コホート
1.適切なコホートは以下の基準を満たす:
a.すべてのR/Rコホート(i又はiiを満たす):
i.病理学的に確認されたAML(2017 ELN分類によって定義される;Dohner 2017)、低メチル化剤(アザシチジン又はデシタビンなど)、非集中化学療法(低用量シタラビンアラビノシドなど)、及び/又はベネトクラクスのいずれかで、以前の治療に対して再発性又は不応性である。治療は、療法の1つの以前の選択に限定される。寛解期の患者の造血幹細胞移植は、AMLの選択療法として数えられない、若しくは
ii.低メチル化剤に対して不応性(低メチル化剤の開始後のどの時点でもIWG2006基準[Cheson 2006]により疾患進行として定義されるか、又は4サイクル後にIWG2006基準による客観的奏効を達成することができない)であるか、又は低メチル化剤、非集中化学療法、若しくは標的療法のいずれかの以前の治療に対して再発性若しくは不耐性であるかのいずれかである、世界保健機関(WHO)分類に従って定義される確認されたMDS。治療は、全R/R MDS患者について、低メチル化剤療法(治験用低メチル化剤を含む)の1回の以前の選択に限定される。
b.すべてのTN/Uコホート(i又はiiを満たす):
i.WHO分類に従って定義されたMDSを有する以前に未治療の患者、IPSS-R(Greenberg 2012)リスク分類の中等度、高、又は非常に高リスク。ヒドロキシウレア、経口エトポシド、赤血球、及び/又は骨髄成長因子による以前の及び同時療法は許容される。
ii.併存症、年齢、又は他の要因による標準的なシタラビン及びアントラサイクリン導入レジメンによる治療に不適格であるか、又はそのような療法を拒否する、WHO基準によってAMLの組織学的確認を伴う以前に未治療の患者。
c.継続コホート:治験責任医師の評価によって臨床的利益を得ている、第1相AML(SCI-CD47-002)試験の能動的なHu5F9-G4療法を受けている患者。
2.研究治療の初回用量前、及びサイクル1の各Hu5F9-G4用量前のWBC数≦20×103/mcL。WBC>20×103/mcLの患者は、WBCを≦20×103/mcLに低減するために、試験全体を通してヒドロキシウレア(最大4g/日)で治療され得る。経口エトポシド(最大200mg経口[PO]/日)は、ヒドロキシウレアに不耐性であるか、又はヒドロキシウレアで十分なWBC低下を達成することができない患者に対してヒドロキシウレアの代替として与えられ得る。
3.患者がインフォームドコンセントを提供している。
4.研究プロトコルに概説されているクリニック訪問及び手順に従う意思があり、また従うことができなければならない。
R/R及びTN/Uコホートのみ(基準5~9のDO NOTは継続コホートには適用されない):
5.男性又は女性、≧18歳。
6.Eastern Cooperative Oncology Group(ECOG)パフォーマンススコアが0~2。
7.臨床的に必要とみなされる、血液輸血を受ける意思がある。
8.治療前の血液交差適合が完了している(セクション7.3.4に詳述される)。
9.以下に示す範囲内の血液学的及び生化学的指標:
a.アスパラギン酸アミノトランスフェラーゼ(AST)/血清グルタミン酸オキサロ酢酸トランスアミナーゼ(SGOT)及びアラニンアミノトランスフェラーゼ(ALT)/血清グルタミン酸ピルビン酸トランスアミナーゼ(SGPT)≦5×正常の上限(ULN)
b.患者がジルベール症候群又は遺伝的等価物の文書病歴を有する場合、ビリルビン≦1.5×ULN、又は3.0×ULN、及び主に非抱合型
c.血清クレアチニン≦1.5×ULN又は計算された糸球体濾過率(GFR)≧40mL/分/1.73m2
10.妊娠可能な女性患者は、授乳中又は妊娠予定であってはならず、登録前30日以内及び治験薬の最初の投与前72時間以内に陰性尿又は血清妊娠検査を有しなければならない。
11.妊娠可能な女性患者は、研究中1つの非常に効果的な避妊方法を使用する意思があり、Hu5F9-G4又はアザシチジンの最後の投薬のうちのいずれか遅く終わった方の後4ヶ月間継続しなければならない(セクション4.5.1)。
12.WOCBPと性的に活発であり、精管切除していない男性患者は、研究中、及びHu5F9-G4又はアザシチジンの最後の投薬のうちのいずれか遅く終わった後4ヶ月間、バリア避妊法を使用する意思がなければならない(セクション4.5.2)。
13.治験責任医師によって実現可能ではないと決定されない限り、強制治療前及び治療中の骨髄生検(トレフィン)に同意する意思がある。
除外基準
1.CD47又はSIRPα標的化剤による以前の治療(継続コホートの患者におけるHu5F9-G4を除く)。
2.1日目のHu5F9-G4投薬前の4週間以内の化学療法(ヒドロキシウレア若しくは経口エトポシドを除く)、標的化療法、免疫療法、又は放射線療法を含むがこれらに限定されない、以前の抗白血病療法。注記:局在非中枢神経系(非CNS)放射線療法、前立腺がんの黄体形成ホルモン放出ホルモン(LHRH)アゴニストによる以前のホルモン療法、並びにビスホスホネート及び核因子カッパBリガンドの受容体活性化因子(RANKL)阻害剤による治療は、排除の基準ではない。
3.TN/Uコホートのみ:任意の以前の抗白血病療法(ヒドロキシウレア又は経口エトポシドを除く)、低メチル化剤による以前の治療、及び/又は低用量シタラビン。
4.R/R拡大コホート及びTN/Uコホートのみ:進行性悪性肝腫瘍又はアザシチジン若しくはマンニトールに対する既知の過敏症を含む、アザシチジンに対する禁忌。
5.急性前骨髄球性白血病。
6.既知の遺伝性又は獲得出血障害。
7.登録前の6ヶ月以内の以前の同種異系造血幹細胞移植、活動性移植片対宿主病(GVHD)、又は移植関連免疫抑制を必要とする。
8.白血病による活動性CNS関与の臨床上の疑い。
9.研究における参加のリスク効果比を実質的に増加させるであろう、治験責任医師及び治験依頼者によって評価される顕著な医学的疾患又は状態。これには、過去6ヶ月以内の急性心筋梗塞、不安定な狭心症、制御不良の真性糖尿病、顕著な活動性感染症、及びうっ血性心不全ニューヨーク心臓協会(New York Heart Association)(NYHA)クラスIII~IVが含まれるが、これらに限定されない。
10.患者が除外基準2で定義される能動的抗がん療法中ではない、治療された基底細胞若しくは局所扁平上皮がん、局所前立腺がん、又は他の悪性腫瘍を除く、二次性悪性腫瘍。
11.精神疾患又は物質乱用の病歴は、プロトコル要件に従うか、又はインフォームドコンセントを得る能力を妨げる可能性が高い。
12.妊娠又は活発な授乳。
13.既知の活動性又は慢性B若しくはC型肝炎感染又はヒト免疫不全ウイルス(HIV)。
研究目的
エンドポイント
治験薬情報
Hu5F9-G4
アザシチジン
介入期間及び評価
患者の数
統計的方法
症例数の計算
実施例2:ヒト結果
Hu5F9-G4+アザシチジンの安全性
Hu5F9-G4+アザシチジンの有効性
TP53変異体患者応答
結論
実施例3:Hu5F9-G4及びアザシチジンは、TP53変異を有するAML患者の疾患を低減する
実施例5:Hu5F9-G4及びアザシチジンは、骨髄におけるT細胞浸潤を変化させる
実施例6:Q1W対Q2W投薬レジメンにおける抗体受容体占有率
特定の実施形態では、例えば以下の項目が提供される。
(項目1)
対象における造血障害を治療する方法であって、前記対象が、少なくとも1つのp53変異を有し、(a)CD47とSIRPα;との間の結合を阻害する単離された抗体を投与することと、(b)低メチル化剤を前記対象に投与することと、を含む、方法。
(項目2)
対象における造血障害を治療する方法であって、(a)CD47とSIRPαとの間の結合を阻害する単離された抗体を投与することと、(b)前記対象に低メチル化剤を投与することであって、前記対象が、少なくとも1つのp53変異を有すると決定されるか、又は決定されている、投与することと、を含む、方法。
(項目3)
対象における造血障害を治療する方法であって、
a.前記対象における少なくとも1つのp53変異の存在を決定する、又は決定していることと、
b.(i)CD47とSIRPαとの間の結合を阻害する単離された抗体、及び(ii)低メチル化剤を前記対象に投与する、又は投与していることと、を含む、方法。
(項目4)
前記少なくとも1つのp53変異の存在を決定することが、DNAアッセイ、RNAアッセイ、又はタンパク質アッセイを含む、項目3に記載の方法。
(項目5)
前記少なくとも1つのp53変異が存在する場合、前記抗体及び低メチル化剤が、前記対象に投与される、項目1~4のいずれか一項に記載の方法。
(項目6)
前記抗体が、抗CD47抗体又は抗SIRPα抗体である、項目1~5のいずれか一項に記載の方法。
(項目7)
前記抗CD47抗体が、体重1kg当たり10mg以上の抗体の用量で前記対象に投与される、項目1~6のいずれか一項に記載の方法。
(項目8)
前記低メチル化剤が、アザシチジン又はデシタビンである、項目1~7のいずれか一項に記載の方法。
(項目9)
前記低メチル化剤が、アザシチジンである、項目1~8のいずれか一項に記載の方法。
(項目10)
前記造血障害が、血液前がんである、項目1~9のいずれか一項に記載の方法。
(項目11)
前記造血障害が、血液がんである、項目1~9のいずれか一項に記載の方法。
(項目12)
前記造血障害が、骨髄異形成症候群(MDS)である、項目1~9のいずれか一項に記載の方法。
(項目13)
前記造血障害が、急性骨髄性白血病(AML)である、項目1~9のいずれか一項に記載の方法。
(項目14)
前記造血障害が、クローン性造血(CH)、未確定の潜在能をもつクローン性造血(CHIP)、加齢性クローン性造血(ARCH)、意義不明の特発性血球減少症(ICUS)、又は意義不明のクローン性血球減少症(CCUS)である、項目1~9のいずれか一項に記載の方法。
(項目15)
前記p53変異が、ミスセンス変異、ナンセンス変異、フレームシフト変異、イントロン変異、切断変異、DNA結合ドメインにおける変異、又は四量体化ドメインにおける変異を含む、項目1~14のいずれか一項に記載の方法。
(項目16)
前記p53変異が、前記DNA結合ドメインにおける変異を含む、項目15に記載の方法。
(項目17)
対象が、がん療法の少なくとも1、2、3、4、5、6、7、8、9、10、又は10超の以前の選択に対して再発性又は不応性である、項目1~16のいずれか一項に記載の方法。
(項目18)
前記抗CD47抗体が、Hu5F9-G4を含む、項目1~17のいずれか一項に記載の方法。
(項目19)
前記抗CD47抗体が、Hu5F9-G4からなる、項目1~17のいずれか一項に記載の方法。
(項目20)
前記抗SIRPα抗体が、Hu1H9-G1、Hu1H9-G4、Hu3C2-G1、Hu3C2-G4、9B11-G1、9B11-G4、7E11-G1、及び7E11-G4のうちの少なくとも1つを含む、項目1~17のいずれか一項に記載の方法。
(項目21)
前記抗SIRPα抗体が、Hu1H9-G1、Hu1H9-G4、Hu3C2-G1、Hu3C2-G4、9B11-G1、9B11-G4、7E11-G1、及び7E11-G4からなる群から選択される抗体からなる、項目1~17のいずれか一項に記載の方法。
(項目22)
前記抗CD47抗体が、体重1kg当たり少なくとも10~60、20~30、30~40、40~50、50~60、10、15、20、30、40、50、又は60mgの抗体の用量で投与される、項目1~21のいずれか一項に記載の方法。
(項目23)
前記抗体が、静脈内投与される、項目1~22のいずれか一項に記載の方法。
(項目24)
前記アザシチジンが、少なくとも75mg/m 2 の用量で投与される、項目1~23のいずれか一項に記載の方法。
(項目25)
前記アザシチジンが、静脈内、皮下、又は経口投与される、項目1~24のいずれか一項に記載の方法。
(項目26)
前記抗CD47抗体が、1日目及び4日目に体重1kg当たり少なくとも1mgの抗体の初回刺激用量、続いて、8日目に体重1kg当たり少なくとも15mgの抗体の用量、続いて、15日目及び22日目に体重1kg当たり少なくとも30mgの抗体の用量を含む第1のサイクルで前記対象に投与される、項目1~25のいずれか一項に記載の方法。
(項目27)
11日目に体重1kg当たり少なくとも30mgの抗体の負荷用量を更に含む、項目26に記載の方法。
(項目28)
前記第1のサイクルが、4週間の期間である、項目26又は27に記載の方法。
(項目29)
前記アザシチジンが、前記第1のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目26又は27に記載の方法。
(項目30)
前記アザシチジンが、前記第1のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目26又は27に記載の方法。
(項目31)
前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、項目26~30のいずれか一項に記載の方法。
(項目32)
前記抗CD47抗体が、2週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、項目26~30のいずれか一項に記載の方法。
(項目33)
前記抗CD47抗体が、毎週1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、項目26~30のいずれか一項に記載の方法。
(項目34)
前記抗CD47抗体が、週に2回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、項目26~30のいずれか一項に記載の方法。
(項目35)
前記第2のサイクルが、4週間の期間である、項目33又は34に記載の方法。
(項目36)
前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、項目26~35のいずれか一項に記載の方法。
(項目37)
前記抗CD47抗体が、2週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、項目1~35のいずれか一項に記載の方法。
(項目38)
前記抗CD47抗体が、毎週1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、項目1~35のいずれか一項に記載の方法。
(項目39)
前記抗CD47抗体が、週に2回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、項目1~35のいずれか一項に記載の方法。
(項目40)
前記抗CD47抗体が、1日目に体重1kg当たり少なくとも1mgの抗体の初回刺激用量、続いて、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗体の用量を含む第1のサイクルで前記対象に投与される、項目1~25のいずれか一項に記載の方法。
(項目41)
前記抗CD47抗体が、2週間に1回、1日目及び15日目に体重1kg当たり少なくとも60mgの抗体の用量を含む第2のサイクルで前記対象に投与される、項目40に記載の方法。
(項目42)
前記第2のサイクルが、4週間の期間である、項目41に記載の方法。
(項目43)
前記アザシチジンが、前記第2のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目40~43のいずれか一項に記載の方法。
(項目44)
前記アザシチジンが、前記第2のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目40~43のいずれか一項に記載の方法。
(項目45)
前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも60mgの抗体の用量を含む第3のサイクルで前記対象に投与される、項目40~43のいずれか一項に記載の方法。
(項目46)
前記第3のサイクルが、4週間の期間である、項目40~45のいずれか一項に記載の方法。
(項目47)
前記アザシチジンが、前記第3のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目40~46のいずれか一項に記載の方法。
(項目48)
前記アザシチジンが、前記第3のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m 2 の用量で前記対象に投与される、項目40~46のいずれか一項に記載の方法。
(項目49)
前記対象が、前記抗体の投与前に、アザシチジン、デシタビン、又はシタラビンに対して不応性であると決定されるか、又は決定されており、前記方法が、アザシチジン、デシタビン、又はシタラビンに対する不応性の逆転をもたらす、項目1~48のいずれか一項に記載の方法。
(項目50)
前記抗体及び低メチル化剤の前記投与が、前記投与前に前記対象に存在するp53変異量と比較して、前記対象における前記p53変異量を低減する、項目1~49のいずれか一項に記載の方法。
(項目51)
前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象における前記p53変異量を評価することを更に含む、項目1~50のいずれか一項に記載の方法。
(項目52)
前記p53変異量が減少した場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、項目51に記載の方法。
(項目53)
前記抗体及び低メチル化剤の前記投与が、前記投与前に前記対象の骨髄中に存在する白血病幹細胞のレベルと比較して、前記対象の骨髄中に存在する白血病幹細胞のレベルを低減させる、項目1~52のいずれか一項に記載の方法。
(項目54)
前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象の骨髄中に存在する白血病幹細胞のレベルを評価することを更に含む、項目1~53のいずれか一項に記載の方法。
(項目55)
白血病幹細胞の量が減少した場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、項目54に記載の方法。
(項目56)
前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~55のいずれか一項に記載の方法。
(項目57)
前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目56に記載の方法。
(項目58)
4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目56又は57に記載の方法。
(項目59)
4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目56又は57に記載の方法。
(項目60)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、項目58又は59に記載の方法。
(項目61)
前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~55のいずれか一項に記載の方法。
(項目62)
前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目61に記載の方法。
(項目63)
4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目61又は62に記載の方法。
(項目64)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、項目63に記載の方法。
(項目65)
前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~55のいずれか一項に記載の方法。
(項目66)
前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目62に記載の方法。
(項目67)
4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目62又は66に記載の方法。
(項目68)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、抗CD47抗体が、Hu5F9-G4である、項目66又は67に記載の方法。
(項目69)
前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、前記第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~55のいずれか一項に記載の方法。
(項目70)
前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、前記第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~55のいずれか一項に記載の方法。
(項目71)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目69又は70に記載の方法。
(項目72)
4週間の第4のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目69~71のいずれか一項に記載の方法。
(項目73)
前記第4のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、項目72に記載の方法。
(項目74)
前記対象が、骨髄異形成症候群(MDS)を有するヒト対象であり、前記対象が、少なくとも1つのp53変異を有し、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~68のいずれか一項に記載の方法。
(項目75)
前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目74に記載の方法。
(項目76)
4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目74又は75に記載の方法。
(項目77)
4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目74又は75に記載の方法。
(項目78)
4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目74又は75に記載の方法。
(項目79)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、項目77又は78に記載の方法。
(項目80)
前記対象が、急性骨髄性白血病(AML)を有するヒト対象であり、前記対象が、少なくとも1つのp53変異を有し、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目1~19又は22~68のいずれか一項に記載の方法。
(項目81)
前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、項目80に記載の方法。
(項目82)
4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目80又は81に記載の方法。
(項目83)
4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目80又は81に記載の方法。
(項目84)
4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目80又は81に記載の方法。
(項目85)
前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、項目83又は84に記載の方法。
(項目86)
対象における造血障害を治療する方法であって、
a.前記対象の骨髄におけるT細胞浸潤レベルを決定する、又は決定していることと、
b.(i)CD47とSIRPαとの間の結合を阻害する単離された抗体、及び(ii)低メチル化剤を前記対象に投与する、又は投与していることと、を含む、方法。
(項目87)
前記T細胞浸潤レベルを決定することが、DNAアッセイ、RNAアッセイ、又はタンパク質アッセイを含む、項目86に記載の方法。
(項目88)
前記アッセイが、T細胞受容体配列決定、逆転写定量ポリメラーゼ連鎖反応、RNA配列決定、RNAハイブリダイゼーション、蛍光ベースのフローサイトメトリー、飛行時間型質量分析、又は免疫ブロットからなる群から選択される、項目87に記載の方法。
(項目89)
前記抗体及び低メチル化剤の前記投与が、投与前の前記骨髄におけるT細胞浸潤レベルと比較して、前記骨髄における前記T細胞浸潤レベルを変化させる、項目86~88のいずれか一項に記載の方法。
(項目90)
前記投与が、前記T細胞浸潤レベルを増加させ、前記T細胞が、CD8+CTL又はCD4+Tヘルパー(Th)細胞である、項目89に記載の方法。
(項目91)
前記投与が、前記T細胞浸潤レベルを減少させ、前記T細胞が、FOXP3 + Treg細胞である、項目86~90のいずれか一項に記載の方法。
(項目92)
前記投与が、前記骨髄における前記T細胞浸潤においてFOXP3 + Treg細胞のレベルを減少させる、項目86~90のいずれか一項に記載の方法。
(項目93)
前記投与が、前記骨髄におけるFOXP3+Treg細胞のインサイチュ発生を減少させる、項目86~90のいずれか一項に記載の方法。
(項目94)
前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象の前記骨髄における前記T細胞浸潤レベルを評価することを更に含む、項目86~93のいずれか一項に記載の方法。
(項目95)
前記骨髄における前記T細胞浸潤レベルが増加しており、前記T細胞がCD8+CTL又はCD4+Tヘルパー(Th)細胞である場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、項目94に記載の方法。
(項目96)
前記骨髄における前記T細胞浸潤レベルが減少しており、前記T細胞がFOXP3 + Treg細胞である場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、項目94に記載の方法。
(項目97)
前記抗体が、抗CD47抗体又は抗SIRPα抗体である、項目86~96のいずれか一項に記載の方法。
(項目98)
前記抗CD47抗体が、体重1kg当たり1mg以上の抗体の用量で前記対象に投与される、項目86~97のいずれか一項に記載の方法。
(項目99)
前記低メチル化剤が、アザシチジン又はデシタビンである、項目86~98のいずれか一項に記載の方法。
(項目100)
前記造血障害が、血液前がん又は血液がんである、項目86~99のいずれか一項に記載の方法。
(項目101)
前記造血障害が、急性骨髄性白血病(AML)又は骨髄異形成症候群(MDS)である、項目86~100のいずれか一項に記載の方法。
(項目102)
前記対象が、ヒト対象であり、前記対象の前記骨髄における前記T細胞浸潤レベルが、決定される対象であるか、又は決定されている対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、前記第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、前記第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、項目86~101のいずれか一項に記載の方法。
(項目103)
低リスクのMDSを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、方法。
(項目104)
低リスクのMDSを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目に80mg~800mgの範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)4週間に1回、1日目に少なくとも4800mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、方法。
(項目105)
高リスクのMDS又はAMLを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、方法。
(項目106)
高リスクのMDS又はAMLを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目及び4日目に80mg~800mgの範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に少なくとも1200mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも2400mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含み、
第3のサイクルが、(1)2週間に1回、1日目及び15日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m 2 のアザシチジンの用量を投与することと、を含む、方法。
(項目107)
アザシチジンが、静脈内投与される、項目103~106のいずれか一項に記載の方法。
Claims (107)
- 対象における造血障害を治療する方法であって、前記対象が、少なくとも1つのp53変異を有し、(a)CD47とSIRPα;との間の結合を阻害する単離された抗体を投与することと、(b)低メチル化剤を前記対象に投与することと、を含む、方法。
- 対象における造血障害を治療する方法であって、(a)CD47とSIRPαとの間の結合を阻害する単離された抗体を投与することと、(b)前記対象に低メチル化剤を投与することであって、前記対象が、少なくとも1つのp53変異を有すると決定されるか、又は決定されている、投与することと、を含む、方法。
- 対象における造血障害を治療する方法であって、
a.前記対象における少なくとも1つのp53変異の存在を決定する、又は決定していることと、
b.(i)CD47とSIRPαとの間の結合を阻害する単離された抗体、及び(ii)低メチル化剤を前記対象に投与する、又は投与していることと、を含む、方法。 - 前記少なくとも1つのp53変異の存在を決定することが、DNAアッセイ、RNAアッセイ、又はタンパク質アッセイを含む、請求項3に記載の方法。
- 前記少なくとも1つのp53変異が存在する場合、前記抗体及び低メチル化剤が、前記対象に投与される、請求項1~4のいずれか一項に記載の方法。
- 前記抗体が、抗CD47抗体又は抗SIRPα抗体である、請求項1~5のいずれか一項に記載の方法。
- 前記抗CD47抗体が、体重1kg当たり10mg以上の抗体の用量で前記対象に投与される、請求項1~6のいずれか一項に記載の方法。
- 前記低メチル化剤が、アザシチジン又はデシタビンである、請求項1~7のいずれか一項に記載の方法。
- 前記低メチル化剤が、アザシチジンである、請求項1~8のいずれか一項に記載の方法。
- 前記造血障害が、血液前がんである、請求項1~9のいずれか一項に記載の方法。
- 前記造血障害が、血液がんである、請求項1~9のいずれか一項に記載の方法。
- 前記造血障害が、骨髄異形成症候群(MDS)である、請求項1~9のいずれか一項に記載の方法。
- 前記造血障害が、急性骨髄性白血病(AML)である、請求項1~9のいずれか一項に記載の方法。
- 前記造血障害が、クローン性造血(CH)、未確定の潜在能をもつクローン性造血(CHIP)、加齢性クローン性造血(ARCH)、意義不明の特発性血球減少症(ICUS)、又は意義不明のクローン性血球減少症(CCUS)である、請求項1~9のいずれか一項に記載の方法。
- 前記p53変異が、ミスセンス変異、ナンセンス変異、フレームシフト変異、イントロン変異、切断変異、DNA結合ドメインにおける変異、又は四量体化ドメインにおける変異を含む、請求項1~14のいずれか一項に記載の方法。
- 前記p53変異が、前記DNA結合ドメインにおける変異を含む、請求項15に記載の方法。
- 対象が、がん療法の少なくとも1、2、3、4、5、6、7、8、9、10、又は10超の以前の選択に対して再発性又は不応性である、請求項1~16のいずれか一項に記載の方法。
- 前記抗CD47抗体が、Hu5F9-G4を含む、請求項1~17のいずれか一項に記載の方法。
- 前記抗CD47抗体が、Hu5F9-G4からなる、請求項1~17のいずれか一項に記載の方法。
- 前記抗SIRPα抗体が、Hu1H9-G1、Hu1H9-G4、Hu3C2-G1、Hu3C2-G4、9B11-G1、9B11-G4、7E11-G1、及び7E11-G4のうちの少なくとも1つを含む、請求項1~17のいずれか一項に記載の方法。
- 前記抗SIRPα抗体が、Hu1H9-G1、Hu1H9-G4、Hu3C2-G1、Hu3C2-G4、9B11-G1、9B11-G4、7E11-G1、及び7E11-G4からなる群から選択される抗体からなる、請求項1~17のいずれか一項に記載の方法。
- 前記抗CD47抗体が、体重1kg当たり少なくとも10~60、20~30、30~40、40~50、50~60、10、15、20、30、40、50、又は60mgの抗体の用量で投与される、請求項1~21のいずれか一項に記載の方法。
- 前記抗体が、静脈内投与される、請求項1~22のいずれか一項に記載の方法。
- 前記アザシチジンが、少なくとも75mg/m2の用量で投与される、請求項1~23のいずれか一項に記載の方法。
- 前記アザシチジンが、静脈内、皮下、又は経口投与される、請求項1~24のいずれか一項に記載の方法。
- 前記抗CD47抗体が、1日目及び4日目に体重1kg当たり少なくとも1mgの抗体の初回刺激用量、続いて、8日目に体重1kg当たり少なくとも15mgの抗体の用量、続いて、15日目及び22日目に体重1kg当たり少なくとも30mgの抗体の用量を含む第1のサイクルで前記対象に投与される、請求項1~25のいずれか一項に記載の方法。
- 11日目に体重1kg当たり少なくとも30mgの抗体の負荷用量を更に含む、請求項26に記載の方法。
- 前記第1のサイクルが、4週間の期間である、請求項26又は27に記載の方法。
- 前記アザシチジンが、前記第1のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項26又は27に記載の方法。
- 前記アザシチジンが、前記第1のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項26又は27に記載の方法。
- 前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、請求項26~30のいずれか一項に記載の方法。
- 前記抗CD47抗体が、2週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、請求項26~30のいずれか一項に記載の方法。
- 前記抗CD47抗体が、毎週1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、請求項26~30のいずれか一項に記載の方法。
- 前記抗CD47抗体が、週に2回、体重1kg当たり少なくとも30mgの抗体の用量を含む第2のサイクルで前記対象に投与される、請求項26~30のいずれか一項に記載の方法。
- 前記第2のサイクルが、4週間の期間である、請求項33又は34に記載の方法。
- 前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、請求項26~35のいずれか一項に記載の方法。
- 前記抗CD47抗体が、2週間に1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、請求項1~35のいずれか一項に記載の方法。
- 前記抗CD47抗体が、毎週1回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、請求項1~35のいずれか一項に記載の方法。
- 前記抗CD47抗体が、週に2回、体重1kg当たり少なくとも30mgの抗体の用量を含む第3のサイクルで前記対象に投与される、請求項1~35のいずれか一項に記載の方法。
- 前記抗CD47抗体が、1日目に体重1kg当たり少なくとも1mgの抗体の初回刺激用量、続いて、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗体の用量を含む第1のサイクルで前記対象に投与される、請求項1~25のいずれか一項に記載の方法。
- 前記抗CD47抗体が、2週間に1回、1日目及び15日目に体重1kg当たり少なくとも60mgの抗体の用量を含む第2のサイクルで前記対象に投与される、請求項40に記載の方法。
- 前記第2のサイクルが、4週間の期間である、請求項41に記載の方法。
- 前記アザシチジンが、前記第2のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項40~43のいずれか一項に記載の方法。
- 前記アザシチジンが、前記第2のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項40~43のいずれか一項に記載の方法。
- 前記抗CD47抗体が、4週間に1回、体重1kg当たり少なくとも60mgの抗体の用量を含む第3のサイクルで前記対象に投与される、請求項40~43のいずれか一項に記載の方法。
- 前記第3のサイクルが、4週間の期間である、請求項40~45のいずれか一項に記載の方法。
- 前記アザシチジンが、前記第3のサイクルの1~7日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項40~46のいずれか一項に記載の方法。
- 前記アザシチジンが、前記第3のサイクルの1~5日目のそれぞれの日に、少なくとも75mg/m2の用量で前記対象に投与される、請求項40~46のいずれか一項に記載の方法。
- 前記対象が、前記抗体の投与前に、アザシチジン、デシタビン、又はシタラビンに対して不応性であると決定されるか、又は決定されており、前記方法が、アザシチジン、デシタビン、又はシタラビンに対する不応性の逆転をもたらす、請求項1~48のいずれか一項に記載の方法。
- 前記抗体及び低メチル化剤の前記投与が、前記投与前に前記対象に存在するp53変異量と比較して、前記対象における前記p53変異量を低減する、請求項1~49のいずれか一項に記載の方法。
- 前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象における前記p53変異量を評価することを更に含む、請求項1~50のいずれか一項に記載の方法。
- 前記p53変異量が減少した場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、請求項51に記載の方法。
- 前記抗体及び低メチル化剤の前記投与が、前記投与前に前記対象の骨髄中に存在する白血病幹細胞のレベルと比較して、前記対象の骨髄中に存在する白血病幹細胞のレベルを低減させる、請求項1~52のいずれか一項に記載の方法。
- 前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象の骨髄中に存在する白血病幹細胞のレベルを評価することを更に含む、請求項1~53のいずれか一項に記載の方法。
- 白血病幹細胞の量が減少した場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、請求項54に記載の方法。
- 前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~55のいずれか一項に記載の方法。
- 前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項56に記載の方法。
- 4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項56又は57に記載の方法。
- 4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項56又は57に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、請求項58又は59に記載の方法。
- 前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~55のいずれか一項に記載の方法。
- 前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項61に記載の方法。
- 4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項61又は62に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、請求項63に記載の方法。
- 前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~55のいずれか一項に記載の方法。
- 前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項62に記載の方法。
- 4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項62又は66に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、抗CD47抗体が、Hu5F9-G4である、請求項66又は67に記載の方法。
- 前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、前記第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~55のいずれか一項に記載の方法。
- 前記対象が、ヒト対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、前記第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~55のいずれか一項に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項69又は70に記載の方法。
- 4週間の第4のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項69~71のいずれか一項に記載の方法。
- 前記第4のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、請求項72に記載の方法。
- 前記対象が、骨髄異形成症候群(MDS)を有するヒト対象であり、前記対象が、少なくとも1つのp53変異を有し、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~68のいずれか一項に記載の方法。
- 前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項74に記載の方法。
- 4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項74又は75に記載の方法。
- 4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項74又は75に記載の方法。
- 4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項74又は75に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、請求項77又は78に記載の方法。
- 前記対象が、急性骨髄性白血病(AML)を有するヒト対象であり、前記対象が、少なくとも1つのp53変異を有し、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項1~19又は22~68のいずれか一項に記載の方法。
- 前記第2のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返される、請求項80に記載の方法。
- 4週間の第3のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項80又は81に記載の方法。
- 4週間の第3のサイクルが、(1)2週間に1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項80又は81に記載の方法。
- 4週間の第3のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項80又は81に記載の方法。
- 前記第3のサイクルが、制限なく、又は臨床的利益が低減されるか若しくは失われるか若しくはもはや観察されなくなるまで、1回以上の追加サイクルとして繰り返され、任意選択で、前記対象が臨床的利益を失うまで、前記抗CD47抗体及びアザシチジンが前記対象に投与され、任意選択で、前記抗CD47抗体が、Hu5F9-G4である、請求項83又は84に記載の方法。
- 対象における造血障害を治療する方法であって、
a.前記対象の骨髄におけるT細胞浸潤レベルを決定する、又は決定していることと、
b.(i)CD47とSIRPαとの間の結合を阻害する単離された抗体、及び(ii)低メチル化剤を前記対象に投与する、又は投与していることと、を含む、方法。 - 前記T細胞浸潤レベルを決定することが、DNAアッセイ、RNAアッセイ、又はタンパク質アッセイを含む、請求項86に記載の方法。
- 前記アッセイが、T細胞受容体配列決定、逆転写定量ポリメラーゼ連鎖反応、RNA配列決定、RNAハイブリダイゼーション、蛍光ベースのフローサイトメトリー、飛行時間型質量分析、又は免疫ブロットからなる群から選択される、請求項87に記載の方法。
- 前記抗体及び低メチル化剤の前記投与が、投与前の前記骨髄におけるT細胞浸潤レベルと比較して、前記骨髄における前記T細胞浸潤レベルを変化させる、請求項86~88のいずれか一項に記載の方法。
- 前記投与が、前記T細胞浸潤レベルを増加させ、前記T細胞が、CD8+CTL又はCD4+Tヘルパー(Th)細胞である、請求項89に記載の方法。
- 前記投与が、前記T細胞浸潤レベルを減少させ、前記T細胞が、FOXP3+Treg細胞である、請求項86~90のいずれか一項に記載の方法。
- 前記投与が、前記骨髄における前記T細胞浸潤においてFOXP3+Treg細胞のレベルを減少させる、請求項86~90のいずれか一項に記載の方法。
- 前記投与が、前記骨髄におけるFOXP3+Treg細胞のインサイチュ発生を減少させる、請求項86~90のいずれか一項に記載の方法。
- 前記抗体及び前記低メチル化剤の少なくとも1回のサイクルの投与後に、前記対象の前記骨髄における前記T細胞浸潤レベルを評価することを更に含む、請求項86~93のいずれか一項に記載の方法。
- 前記骨髄における前記T細胞浸潤レベルが増加しており、前記T細胞がCD8+CTL又はCD4+Tヘルパー(Th)細胞である場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、請求項94に記載の方法。
- 前記骨髄における前記T細胞浸潤レベルが減少しており、前記T細胞がFOXP3+Treg細胞である場合、少なくとも追加サイクルの前記抗体及び前記低メチル化剤を投与することを更に含む、請求項94に記載の方法。
- 前記抗体が、抗CD47抗体又は抗SIRPα抗体である、請求項86~96のいずれか一項に記載の方法。
- 前記抗CD47抗体が、体重1kg当たり1mg以上の抗体の用量で前記対象に投与される、請求項86~97のいずれか一項に記載の方法。
- 前記低メチル化剤が、アザシチジン又はデシタビンである、請求項86~98のいずれか一項に記載の方法。
- 前記造血障害が、血液前がん又は血液がんである、請求項86~99のいずれか一項に記載の方法。
- 前記造血障害が、急性骨髄性白血病(AML)又は骨髄異形成症候群(MDS)である、請求項86~100のいずれか一項に記載の方法。
- 前記対象が、ヒト対象であり、前記対象の前記骨髄における前記T細胞浸潤レベルが、決定される対象であるか、又は決定されている対象であり、前記方法が、前記抗CD47抗体及び前記アザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、前記第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)11、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、前記第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、請求項86~101のいずれか一項に記載の方法。
- 低リスクのMDSを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)4週間に1回、1日目に体重1kg当たり少なくとも60mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、方法。 - 低リスクのMDSを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも2つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目に80mg~800mgの範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8、15、及び22日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(3)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)4週間に1回、1日目に少なくとも4800mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、方法。 - 高リスクのMDS又はAMLを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目及び4日目に体重1kg当たり1mg~10mgの抗体の範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に体重1kg当たり少なくとも15mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第3のサイクルが、(1)毎週1回、1日目及び15日目に体重1kg当たり少なくとも30mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、方法。 - 高リスクのMDS又はAMLを有する対象を治療する方法であって、静脈内に抗CD47抗体及びアザシチジンを、それぞれ4週間の少なくとも3つの異なるサイクルにわたって前記対象に投与することを含み、
第1のサイクルが、(1)1日目及び4日目に80mg~800mgの範囲で抗CD47抗体の初回刺激用量を投与することと、(2)8日目に少なくとも1200mgの抗CD47抗体の用量を投与することと、(3)15日目及び22日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(4)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第2のサイクルが、(1)毎週1回、1、8、15、及び22日目に体重1kg当たり少なくとも2400mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含み、
第3のサイクルが、(1)2週間に1回、1日目及び15日目に少なくとも2400mgの抗CD47抗体の用量を投与することと、(2)1~7日目のそれぞれの日に、少なくとも75mg/m2のアザシチジンの用量を投与することと、を含む、方法。 - アザシチジンが、静脈内投与される、請求項103~106のいずれか一項に記載の方法。
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WO2021076908A1 (en) | 2021-04-22 |
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