CALICHEAMICIN DERIVATIVE-CARRIER CONJUGATES

• Main Authors: MERCHANT NISHITH, RUBINO JOSEPH THOMAS, SIMPSON JOHN MCLEAN, KUNTZ ARTHUR, POPPLEWELL ANDREW GEORGE, JAIN NEERA, ROBBINS PAUL DAVID, MORAN JUSTIN KEITH, VIDUNAS EUGENE JOSEPH, RUPPEN MARK EDWARD, DAMLE NITIN KRISHNAJI, DIJOSEPH JOHN FRANCIS
• Format: Patent
• Language: English; Japanese
• Published: 02.04.2015
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug load significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF).SOLUTION: Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also disclosed. Monomeric calicheamicin derivative/anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also disclosed. 【課題】以前に報告された手法よりも有意に高い薬物負荷で、凝集およびコンジュゲーションの低い画分（ＬＣＦ）を減らした単量体細胞傷害性ドラッグ−キャリアコンジュゲートの調製法を開示した。【解決手段】細胞傷害性ドラッグ誘導体−抗体コンジュゲート、そのコンジュゲートからなる組成物およびそのコンジュゲートの使用もまた開示した。単量体カリチェアミシン誘導体−抗ＣＤ２２抗体コンジュゲート、そのコンジュゲートからなる組成物およびそのコンジュゲートの使用もまた開示した。【選択図】なし