The targeted delivery of potent cytotoxic molecules into cancer cells is considered a promising anticancer strategy. The design of clinically effective antibody-drug conjugates (ADCs), in which biologically active drugs are coupled through chemical linkers to monoclonal antibodies, has presented challenges for pharmaceutical researchers. After 30 years of intensive research and development activities, only seven ADCs have been approved for clinical use; two have received fast-track designation and two breakthrough therapy designation from the Food and Drug Administration. There is continued interest in the field, as documented by the growing number of candidates in clinical development. This review aims to summarize the most recent innovations that have been applied to the design of ADCs undergoing early- and late-stage clinical trials. Discovery and rational optimization of new payloads, chemical linkers, and antibody formats have improved the therapeutic index of next-generation ADCs, ultimately resulting in improved clinical benefit for the patients.
机构:
Fred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USAFred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USA
Appelbaum, Frederick R.
;
Bernstein, Irwin D.
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机构:
Fred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USAFred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USA
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Axup, Jun Y.
;
Bajjuri, Krishna M.
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h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Bajjuri, Krishna M.
;
Ritland, Melissa
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h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Ritland, Melissa
;
Hutchins, Benjamin M.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Hutchins, Benjamin M.
;
Kim, Chan Hyuk
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Kim, Chan Hyuk
;
Kazane, Stephanie A.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Kazane, Stephanie A.
;
Halder, Rajkumar
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Halder, Rajkumar
;
Forsyth, Jane S.
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h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Forsyth, Jane S.
;
Santidrian, Antonio F.
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h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Santidrian, Antonio F.
;
Stafin, Karin
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h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Stafin, Karin
;
Lu, Yingchun
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Lu, Yingchun
;
Hon Tran
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Hon Tran
;
Seller, Aaron J.
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h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Seller, Aaron J.
;
Biroce, Sandra L.
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h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Biroce, Sandra L.
;
Szydlik, Aga
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机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Szydlik, Aga
;
Pinkstaff, Jason K.
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h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Pinkstaff, Jason K.
;
Tian, Feng
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Tian, Feng
;
Sinha, Subhash C.
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h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Sinha, Subhash C.
;
Felding-Habermann, Brunhilde
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h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Felding-Habermann, Brunhilde
;
Smider, Vaughn V.
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h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Smider, Vaughn V.
;
Schultz, Peter G.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
机构:
Fred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USAFred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USA
Appelbaum, Frederick R.
;
Bernstein, Irwin D.
论文数: 0引用数: 0
h-index: 0
机构:
Fred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USAFred Hutchinson Canc Res Ctr, 1100 Fairview Ave North,D5-310,POB 19024, Seattle, WA 98109 USA
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Axup, Jun Y.
;
Bajjuri, Krishna M.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Bajjuri, Krishna M.
;
Ritland, Melissa
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Ritland, Melissa
;
Hutchins, Benjamin M.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Hutchins, Benjamin M.
;
Kim, Chan Hyuk
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Kim, Chan Hyuk
;
Kazane, Stephanie A.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Kazane, Stephanie A.
;
Halder, Rajkumar
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Halder, Rajkumar
;
Forsyth, Jane S.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Forsyth, Jane S.
;
Santidrian, Antonio F.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Santidrian, Antonio F.
;
Stafin, Karin
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Stafin, Karin
;
Lu, Yingchun
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Lu, Yingchun
;
Hon Tran
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Hon Tran
;
Seller, Aaron J.
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Seller, Aaron J.
;
Biroce, Sandra L.
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Biroce, Sandra L.
;
Szydlik, Aga
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Szydlik, Aga
;
Pinkstaff, Jason K.
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Pinkstaff, Jason K.
;
Tian, Feng
论文数: 0引用数: 0
h-index: 0
机构:
Ambrx Inc, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Tian, Feng
;
Sinha, Subhash C.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Sinha, Subhash C.
;
Felding-Habermann, Brunhilde
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol & Expt Med, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Felding-Habermann, Brunhilde
;
Smider, Vaughn V.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
Smider, Vaughn V.
;
Schultz, Peter G.
论文数: 0引用数: 0
h-index: 0
机构:
Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USAScripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA