General Information of This Target
Target ID
PATR0EGDKN
Target Name
DNA topoisomerase 1 (TOP1)
Gene Name
TOP1
Gene ID
7150
Synonym
DNA topoisomerase I
Sequence
MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKK
HKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEP
EDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKD
KDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKF
YYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC
DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGL
FRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENI
QGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALY
FIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNK
VPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ
QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLAD
ARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSK
LNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF

    Click to Show/Hide
Family
the type IB topoisomerase family
Function
Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a single-strand break via transesterification at a target site in duplex DNA. The scissile phosphodiester is attacked by the catalytic tyrosine of the enzyme, resulting in the formation of a DNA-(3'-phosphotyrosyl)- enzyme intermediate and the expulsion of a 5'-OH DNA strand. The free DNA strand then rotates around the intact phosphodiester bond on the opposing strand, thus removing DNA supercoils. Finally, in the religation step, the DNA 5'-OH attacks the covalent intermediate to expel the active-site tyrosine and restore the DNA phosphodiester backbone. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. Involved in the circadian transcription of the core circadian clock component BMAL1 by altering the chromatin structure around the ROR response elements (ROREs) on the BMAL1 promoter.

    Click to Show/Hide
Uniprot Entry
TOP1_HUMAN
HGNC ID
HGNC:11986
KEGG ID
hsa:7150
Full List of The ADC Related to This Target
Approved
Click To Hide/Show 2 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
Trastuzumab deruxtecan
Trastuzumab
ERBB2
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[1]
Sacituzumab govitecan
Sacituzumab
TACSTD2
Active metabolite of irinotecan SN38
CL2A
[2]
Phase 3
Click To Hide/Show 4 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
Datopotamab deruxtecan
Datopotamab
TACSTD2
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[3]
Patritumab deruxtecan
Patritumab
ERBB3
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[4]
SHR-A1811
Trastuzumab
ERBB2
SHR9265
Mc-Gly-Gly-Phe-Gly
[5]
SKB-264
Sacituzumab
TACSTD2
KL610023
Pyrimidine-CL2A-carbonate
[6]
Phase 2
Click To Hide/Show 17 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
Labetuzumab govitecan
Labetuzumab
CEACAM5
Active metabolite of irinotecan SN38
CL2A
[7]
Ifinatamab deruxtecan
Ifinatamab
CD276
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[8]
BL-B01D1
SI-B001
ERBB3; EGFR
Camptothecin analogue ED04
Mc-Gly-Gly-Phe-Gly
[9]
AZD-8205
INT016
VTCN1
Topoisomerase I inhibitor
Mal-PEG8-Val-Ala
[10]
DB-1303
Undisclosed
ERBB2
P1003
Mc-Gly-Gly-Phe-Gly
[11]
DB-1305
Undisclosed
TACSTD2
P1003
Mc-Gly-Gly-Phe-Gly
[12]
IBI-354
Undisclosed
ERBB2
DX-8951 derivative (DXd)
PODS-CHX-A"-DTPA
[13]
PRO-1160
Undisclosed
CD70
Exatecan
Cys-11 ADC linker
[14]
PRO-1184
Undisclosed
FOLR1
Exatecan
Cys-11 ADC linker
[15]
SHR-A1904
Undisclosed
CLDN18.2
SHR9265
Mc-Gly-Gly-Phe-Gly
[16]
SHR-A1921
Undisclosed
TACSTD2
SHR9265
Mc-Gly-Gly-Phe-Gly
[17]
AZD-5335
Undisclosed
FOLR1
Proprietary DNA topoisomerase I inhibitor
Undisclosed
[18]
ESG-401
Sacituzumab
TACSTD2
Active metabolite of irinotecan SN38
Undisclosed
[19]
FDA-022
Undisclosed
ERBB2
Topoisomerase I inhibitor
Undisclosed
[20]
MHB088C
Undisclosed
CD276
Proprietary DNA topoisomerase I inhibitor
Undisclosed
[21]
MHB036C
Undisclosed
TACSTD2
Topoisomerase I inhibitor
Undisclosed
[22]
CBX-12
Undisclosed
Undisclosed
Exatecan
Undisclosed
[23]
Phase 1
Click To Hide/Show 5 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
DS-6000
Undisclosed
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[24]
DS-6157a
Undisclosed
GPR20
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[25]
Epratuzumab-SN38
Epratuzumab
CD22
Active metabolite of irinotecan SN38
CL2A
[26]
TQB2102
Undisclosed
HER2 ECD2; HER2 ECD4
Topoisomerase I inhibitor
Enzyme-cleavable linker
[27]
BL-M11D1
Undisclosed
CD33
Camptothecin analogue ED04
Undisclosed
[28]
IND
Click To Hide/Show 2 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
9MW-2921
Undisclosed
TACSTD2
Topoisomerase I inhibitor
Undisclosed
[29]
7MW-3711
Undisclosed
CD276
Topoisomerase I inhibitor
Undisclosed
[30]
Clinical candidate
Click To Hide/Show 18 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
IMMU-140
IMMU-114
HLA-DRA
Active metabolite of irinotecan SN38
CL2A
[31]
A7R-ADC-SN38
Anti-IL7R mAb A7R
IL7R
Active metabolite of irinotecan SN38
Mal-PEG12-carbamate-PEG27
[32]
ZW-191
Humanized Anti-FOLR1 IgG1 mAb
FOLR1
ZD06519
Mc-Gly-Gly-Phe-Gly-AM
[33]
ZW-220
Fully humanized Anti-SLC34A2 IgG1 mAb
SLC34A2
ZD06519
Mc-Gly-Gly-Phe-Gly-AM
[34]
DpADC
Undisclosed
TACSTD2
Topo1 inhibitor+immune agonist
Undisclosed
[35]
HER2 targeted DEP conjugate
Trastuzumab
ERBB2
Active metabolite of irinotecan SN38
Undisclosed
[36]
DS-3939
Gatipotuzumab
MUC1
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[37]
SMP-190
Undisclosed
Undisclosed
DX-8951 derivative (DXd)
Unique hydrophilic Linker
[38]
PRO-1102
Trastuzumab
ERBB2
Exatecan
Cleavable hydrophilic linker
[39]
STRO-003
SP11285
ROR1
Exatecan
SC3417
[40]
CUSP06
Undisclosed
CDH6
Exatecan
Protease cleavable linker
[41]
HMBD-501
Undisclosed
ERBB3
Exatecan
Undisclosed
[42]
NV104
Undisclosed
CD276
Irinotecan
Undisclosed
[43]
NV103
Undisclosed
CD99
Irinotecan
Undisclosed
[44]
DAN-311
Undisclosed
ERBB2
Camptothecin
Undisclosed
[45]
DB-1311
Undisclosed
CD276
Proprietary DNA topoisomerase I inhibitor
Undisclosed
[46]
DB-1310
Undisclosed
ERBB3
Proprietary DNA topoisomerase I inhibitor
Maleimide tetrapeptide-based cleavable linker
[47]
AMB-101
Undisclosed
Undisclosed
Topoisomerase I inhibitor
Undisclosed
[48]
Investigative
Click To Hide/Show 149 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
CAC10-CPT-LB
Brentuximab
TNFRSF8
Methylenedioxy CPT2 (CPT2)
Mc-PEG4-Val-Lys-Gly
[49]
CAC10-CPT-LC
Brentuximab
TNFRSF8
Methylenedioxy CPT2 (CPT2)
Mc-PEG8-Val-Lys-Gly
[49]
H00-CPT-LC
Anti-CD30 mAb h00
TNFRSF8
Methylenedioxy CPT2 (CPT2)
Mc-PEG8-Val-Lys-Gly
[49]
CAC10-GT
Brentuximab
TNFRSF8
Active metabolite of irinotecan SN38
CL2A
[49]
Mil40-5
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mc-Val-Ala-PABC
[50]
Mil40-6
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mal-PEG2-Val-Ala-PABC
[50]
Mil40-7
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mal-PEG4-Val-Ala-PABC
[50]
Mil40-8
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mal-PEG8-Val-Ala-PABC
[50]
40H3-CL2A-SN38
Anti-EGFR mAb 40H3
EGFR
Active metabolite of irinotecan SN38
CL2A
[51]
40H3-Deruxtecan
Anti-EGFR mAb 40H3
EGFR
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[51]
Emab-CL2E-SN38
Epratuzumab
CD22
Active metabolite of irinotecan SN38
CL2E
[52]
N501-SN38
Anti-5T4 n501 (nanobody)
TPBG
Active metabolite of irinotecan SN38
CL2A
[53]
M603-SN38 DAR6
Anti-5T4 mAb m603
TPBG
Active metabolite of irinotecan SN38
CL2A
[53]
CAC10-CPT-LA
Brentuximab
TNFRSF8
Methylenedioxy CPT1 (CPT1)
Mc-PEG4-Val-Lys-Gly
[49]
H00-CPT-LA
Anti-CD30 mAb h00
TNFRSF8
Methylenedioxy CPT1 (CPT1)
Mc-PEG4-Val-Lys-Gly
[49]
H00-CPT-LB
Anti-CD30 mAb h00
TNFRSF8
Methylenedioxy CPT2 (CPT2)
Mc-PEG4-Val-Lys-Gly
[49]
H00-GT
Anti-CD30 mAb h00
TNFRSF8
Active metabolite of irinotecan SN38
CL2A
[54]
VL-DAB31-SN38
Rabbit derived VL single-domain Anti-ody
Undisclosed
Active metabolite of irinotecan SN38
Mal-Cyc-PEG3-DAB
[55]
ROS-responsive SN38 ADC
Rabbit derived VL single-domain Anti-ody
Undisclosed
Active metabolite of irinotecan SN38
Mal-Cyc-PEG3-DAB
[55]
HLL1-CL2A-SN38
Milatuzumab
CD74
Active metabolite of irinotecan SN38
CL2A
[56]
Mil40-11 (DAR=7.1)
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mc-PEG8-Val-Ala-PABC
[50]
Mil40-11 (DAR=3.8)
Mil40
ERBB2
Active metabolite of irinotecan SN38
Mc-PEG8-Val-Ala-PABC
[50]
M603-SN38 DAR8
Anti-5T4 mAb m603
TPBG
Active metabolite of irinotecan SN38
CL2A
[53]
M603-SN38 DAR4
Anti-5T4 mAb m603
TPBG
Active metabolite of irinotecan SN38
CL2A
[53]
HPAM4-CL2A-SN38
Anti-MUC1 mAb hPAM4
MUC1
Active metabolite of irinotecan SN38
CL2A
[57]
HA19-SN38 antibody-drug conjugate
Anti-CD19 mAb hA19
CD19
Active metabolite of irinotecan SN38
CL2A
[58]
Raludotatug deruxtecan
Raludotatug
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[59]
Tra-Exa-PSAR10
Trastuzumab
ERBB2
Exatecan
Mal-Exa-PSAR10
[60]
Tra-Exa-PSAR0
Trastuzumab
ERBB2
Exatecan
Mal-Exa-PSAR0
[60]
ZW-251
Humanized Anti-GPC3 IgG1 mAb
GPC3
ZD06519
Mc-Gly-Gly-Phe-Gly-AM
[61]
ADC1-2
Cofetuzumab
PTK7
ADC 1-2 payload
ADC 1-2 linker
[62]
ADC1-4
Cofetuzumab
PTK7
ADC 1-4 payload
ADC 1-4 linker
[62]
ADC1-11
Cofetuzumab
PTK7
ADC 1-11 payload
ADC 1-11 linker
[62]
ADC2-2
Trastuzumab
ERBB2
ADC 2-2 payload
ADC 2-2 linker
[62]
ADC2-4
Trastuzumab
ERBB2
ADC 2-4 payload
ADC 2-4 linker
[62]
ADC2-6-2
Trastuzumab
ERBB2
ADC 2-6-2 payload
ADC 2-6-2 linker
[62]
ADC2-7-2
Trastuzumab
ERBB2
ADC 2-7-2 payload
ADC 2-7-2 linker
[62]
ADC2-9-1
Trastuzumab
ERBB2
ADC 2-9-1 payload
ADC 2-9-1 linker
[62]
ADC2-9-2
Trastuzumab
ERBB2
ADC 2-9-2 payload
ADC 2-9-2 linker
[62]
ADC2-10
Trastuzumab
ERBB2
ADC 2-10 payload
ADC 2-10 linker
[62]
ADC2-11
Trastuzumab
ERBB2
ADC 2-11 payload
ADC 2-11 linker
[62]
ADC2-22
Trastuzumab
ERBB2
ADC 2-22 payload
ADC 2-22 linker
[62]
ADC2-23
Trastuzumab
ERBB2
ADC 2-23 payload
ADC 2-23 linker
[62]
ADC2-24
Trastuzumab
ERBB2
ADC 2-24 payload
ADC 2-24 linker
[62]
ADC2-25
Trastuzumab
ERBB2
ADC 2-25 payload
ADC 2-25 linker
[62]
ADC2-26
Trastuzumab
ERBB2
ADC 2-26 payload
ADC 2-26 linker
[62]
ADC2-27
Trastuzumab
ERBB2
ADC 2-27 payload
ADC 2-27 linker
[62]
ADC2-29
Trastuzumab
ERBB2
ADC 2-29 payload
ADC 2-29 linker
[62]
ADC2-30
Trastuzumab
ERBB2
ADC 2-30 payload
ADC 2-30 linker
[62]
ADC2-31
Trastuzumab
ERBB2
ADC 2-31 payload
ADC 2-31 linker
[62]
ADC2-32
Trastuzumab
ERBB2
ADC 2-32 payload
ADC 2-32 linker
[62]
ADC2-33
Trastuzumab
ERBB2
ADC 2-33 payload
ADC 2-33 linker
[62]
ADC2-34
Trastuzumab
ERBB2
ADC 2-34 payload
ADC 2-34 linker
[62]
ADC2-35
Trastuzumab
ERBB2
ADC 2-35 payload
ADC 2-35 linker
[62]
ADC2-36-1
Trastuzumab
ERBB2
ADC 2-36-1 payload
ADC 2-36-1 linker
[62]
ADC2-36-2
Trastuzumab
ERBB2
ADC 2-36-2 payload
ADC 2-36-2 linker
[62]
ADC2-37
Trastuzumab
ERBB2
ADC 2-37 payload
ADC 2-37 linker
[62]
ADC2-38
Trastuzumab
ERBB2
ADC 2-38 payload
ADC 2-38 linker
[62]
ADC2-39
Trastuzumab
ERBB2
ADC 2-39 payload
ADC 2-39 linker
[62]
ADC2-40
Trastuzumab
ERBB2
ADC 2-40 payload
ADC 2-40 linker
[62]
ADC2-41
Trastuzumab
ERBB2
ADC 2-41 payload
ADC 2-41 linker
[62]
ADC2-42
Trastuzumab
ERBB2
ADC 2-42 payload
ADC 2-42 linker
[62]
ADC2-42-RO
Trastuzumab
ERBB2
ADC 2-42-RO payload
ADC 2-42-RO linker
[62]
ADC2-43
Trastuzumab
ERBB2
ADC 2-43 payload
ADC 2-43 linker
[62]
ADC2-44
Trastuzumab
ERBB2
ADC 2-44 payload
ADC 2-44 linker
[62]
ADC2-45
Trastuzumab
ERBB2
ADC 2-45 payload
ADC 2-45 linker
[62]
ADC2-46
Trastuzumab
ERBB2
ADC 2-46 payload
ADC 2-46 linker
[62]
ADC2-47
Trastuzumab
ERBB2
ADC 2-47 payload
ADC 2-47 linker
[62]
ADC2-48
Trastuzumab
ERBB2
ADC 2-48 payload
ADC 2-48 linker
[62]
ADC2-49
Trastuzumab
ERBB2
ADC 2-49 payload
ADC 2-49 linker
[62]
ADC2-50
Trastuzumab
ERBB2
ADC 2-50 payload
ADC 2-50 linker
[62]
ADC2-51
Trastuzumab
ERBB2
ADC 2-51 payload
ADC 2-51 linker
[62]
ADC2-53
Trastuzumab
ERBB2
ADC 2-53 payload
ADC 2-53 linker
[62]
ADC2-54
Trastuzumab
ERBB2
ADC 2-54 payload
ADC 2-54 linker
[62]
ADC2-55
Trastuzumab
ERBB2
ADC 2-55 payload
ADC 2-55 linker
[62]
ADC2-56
Trastuzumab
ERBB2
ADC 2-56 payload
ADC 2-56 linker
[62]
ADC2-57
Trastuzumab
ERBB2
ADC 2-57 payload
ADC 2-57 linker
[62]
ADC2-58
Trastuzumab
ERBB2
ADC 2-58 payload
ADC 2-58 linker
[62]
ADC2-59
Trastuzumab
ERBB2
ADC 2-59 payload
ADC 2-59 linker
[62]
ADC2-60
Trastuzumab
ERBB2
ADC 2-60 payload
ADC 2-60 linker
[62]
ADC2-61
Trastuzumab
ERBB2
ADC 2-61 payload
ADC 2-61 linker
[62]
ADC-2-62-1
Trastuzumab
ERBB2
ADC 2-62-1 payload
ADC 2-62-1 linker
[62]
ADC-2-62-2
Trastuzumab
ERBB2
ADC 2-62-2 payload
ADC 2-62-2 linker
[62]
ADC-2-63-1
Trastuzumab
ERBB2
ADC 2-63-1 payload
ADC 2-63-1 linker
[62]
ADC-2-63-2
Trastuzumab
ERBB2
ADC 2-63-2 payload
ADC 2-63-2 linker
[62]
ADC-2-64-1
Trastuzumab
ERBB2
ADC 2-64-1 payload
ADC 2-64-1 linker
[62]
ADC-2-64-2
Trastuzumab
ERBB2
ADC 2-64-2 payload
ADC 2-64-2 linker
[62]
ADC-2-65-1
Trastuzumab
ERBB2
ADC 2-65-1 payload
ADC 2-65-1 linker
[62]
ADC-2-65-2
Trastuzumab
ERBB2
ADC 2-65-2 payload
ADC 2-65-2 linker
[62]
ADC3-1
Trastuzumab
ERBB2
ADC 3-1 payload
ADC 3-1 linker
[62]
ADC3-2
Trastuzumab
ERBB2
ADC 3-2 payload
ADC 3-2 linker
[62]
ADC3-3
Trastuzumab
ERBB2
ADC 3-3 payload
ADC 3-3 linker
[62]
ADC3-4
Trastuzumab
ERBB2
ADC 3-4 payload
ADC 3-4 linker
[62]
ADC3-5
Trastuzumab
ERBB2
ADC 3-5 payload
ADC 3-5 linker
[62]
ADC3-6
Patritumab
ERBB3
ADC 3-6 payload
ADC 3-6 linker
[62]
ADC3-7
Patritumab
ERBB3
ADC 3-7 payload
ADC 3-7 linker
[62]
ADC3-8
Patritumab
ERBB3
ADC 3-8 payload
ADC 3-8 linker
[62]
ADC3-9
Patritumab
ERBB3
ADC 3-9 payload
ADC 3-9 linker
[62]
ADC3-10
Patritumab
ERBB3
ADC 3-10 payload
ADC 3-10 linker
[62]
ADC3-11
Patritumab
ERBB3
ADC 3-11 payload
ADC 3-11 linker
[62]
ADC3-12
Patritumab
ERBB3
ADC 3-12 payload
ADC 3-12 linker
[62]
ADC3-13
Patritumab
ERBB3
ADC 3-13 payload
ADC 3-13 linker
[62]
ADC3-14
Patritumab
ERBB3
ADC 3-14 payload
ADC 3-14 linker
[62]
ADC3-15
Patritumab
ERBB3
ADC 3-15 payload
ADC 3-15 linker
[62]
ADC3-16
Patritumab
ERBB3
ADC 3-16 payload
ADC 3-16 linker
[62]
ADC3-17
Patritumab
ERBB3
ADC 3-17 payload
ADC 3-17 linker
[62]
ADC3-18
Patritumab
ERBB3
ADC 3-18 payload
ADC 3-18 linker
[62]
ADC3-19
Patritumab
ERBB3
ADC 3-19 payload
ADC 3-19 linker
[62]
ADC3-20
Patritumab
ERBB3
ADC 3-20 payload
ADC 3-20 linker
[62]
ADC-C2
Patritumab
ERBB3
ADC-C2 payload
ADC-C2 linker
[62]
ADC-C3
Patritumab
ERBB3
ADC-C3 payload
ADC-C3 linker
[62]
ADC-C4
Patritumab
ERBB3
ADC-C4 payload
ADC-C4 linker
[62]
ADC-C5
Patritumab
ERBB3
ADC-C5 payload
ADC-C5 linker
[62]
ADC1-1
Cofetuzumab
PTK7
ADC 1-1 payload
ADC 1-1 linker
[62]
ADC1-12
Cofetuzumab
PTK7
ADC 1-12 payload
ADC 1-12 linker
[62]
ADC2-A
Trastuzumab
ERBB2
ADC 2-A payload
ADC 2-A linker
[62]
ADC2-B
Trastuzumab
ERBB2
ADC 2-B payload
ADC 2-B linker
[62]
ADC2-12
Trastuzumab
ERBB2
ADC 2-12 payload
ADC 2-12 linker
[62]
ADC-C1
Patritumab
ERBB3
ADC-C1 payload
ADC-C1 linker
[62]
Sacituzumab-Deruxtecan
Sacituzumab
TACSTD2
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[63]
CAC10-DT
Brentuximab
TNFRSF8
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[49]
Lmab-CL2A-SN38
Labetuzumab
CEACAM5
Active metabolite of irinotecan SN38
CL2E
[52]
H00-DT
Anti-CD30 mAb h00
TNFRSF8
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[49]
Trastuzumab-L6
Trastuzumab
ERBB2
MF-6
Bridged PEG4-valine-alanine
[64]
AMT-562
Ab562
ERBB3
Exatecan
Mc-Val-Ala-PABC
[65]
Trastuzumab-T1000-exatecan
Trastuzumab
ERBB2
Exatecan
Undisclosed
[66]
cot-APTEDB-SN38
Anti-EDB Ab cot
VAMP8
Active metabolite of irinotecan SN38
Mal-PEG4-Ala
[67]
WO2022078260A1 ADC-1
Trastuzumab
ERBB2
Ln-D9
WO2022078260A1_ADC-1 linker
[68]
WO2022078260A1 ADC-2
Trastuzumab
ERBB2
Ln-D1
WO2022078260A1_ADC-2 linker
[68]
WO2022078260A1 ADC-3
Trastuzumab
ERBB2
Ln-D2
WO2022078260A1_ADC-3 linker
[68]
WO2022078260A1 ADC-4
Trastuzumab
ERBB2
Ln-D4
WO2022078260A1_ADC-4 linker
[68]
WO2022078260A1 ADC-5
Trastuzumab
ERBB2
Ln-D5
WO2022078260A1_ADC-5 linker
[68]
WO2022078260A1 ADC-6
Trastuzumab
ERBB2
Ln-D6
WO2022078260A1_ADC-6 linker
[68]
WO2022078260A1 ADC-7
Trastuzumab
ERBB2
Ln-D7
WO2022078260A1_ADC-7 linker
[68]
WO2022078260A1 ADC-8
Trastuzumab
ERBB2
Ln-D8
WO2022078260A1_ADC-8 linker
[68]
WO2022078260A1 ADC-9
Cetuximab
EGFR
Ln-D2
WO2022078260A1_ADC-9 linker
[68]
WO2022078260A1 ADC-10
Cetuximab
EGFR
Ln-D7
WO2022078260A1_ADC-10 linker
[68]
Epratuzumab-CL2E-SN-38
Epratuzumab
CD22
Active metabolite of irinotecan SN38
CL2E
[69]
Epratuzumab-SN-38
Epratuzumab
CD22
Active metabolite of irinotecan SN38
CL2A
[69]
Veltuzumab-SN-38
Veltuzumab
MS4A1
Active metabolite of irinotecan SN38
CL2A
[69]
Veltuzumab-CL2E-SN-38
Veltuzumab
MS4A1
Active metabolite of irinotecan SN38
CL2E
[69]
Labetuzumab-CL2E-SN-38
Labetuzumab
CEACAM5
Active metabolite of irinotecan SN38
CL2E
[69]
Labetuzumab-SN-38
Labetuzumab
CEACAM5
Active metabolite of irinotecan SN38
CL2A
[69]
Sacituzumab-SN-38
Sacituzumab
TACSTD2
Active metabolite of irinotecan SN38
CL2A
[69]
H01L02-DXd
Anti-CDH6 mAb H01L02
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[70]
H02L02-DXd
Anti-CDH6 mAb H02L02
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[70]
H02L03-DXd
Anti-CDH6 mAb H02L03
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[70]
H04L02-DXd
Anti-CDH6 mAb H04L02
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[70]
NOV0712-DXd
Anti-CDH6 mAb NOV0712
CDH6
DX-8951 derivative (DXd)
Mc-Gly-Gly-Phe-Gly
[70]
References
Ref 1 Trastuzumab deruxtecan versus trastuzumab emtansine in patients with HER2-positive metastatic breast cancer: updated results from DESTINY-Breast03, a randomised, open-label, phase 3 trial. Lancet. 2023 Jan 14;401(10371):105-117. doi: 10.1016/S0140-6736(22)02420-5.
Ref 2 FDA approves sacituzumab govitecan-hziy for HR-positive breast cancer; 3 Feb 2023.
Ref 3 Datopotamab Deruxtecan, a Novel TROP2-directed Antibody-drug Conjugate, Demonstrates Potent Antitumor Activity by Efficient Drug Delivery to Tumor Cells. Mol Cancer Ther. 2021 Dec;20(12):2329-2340.
Ref 4 Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, EGFR-Mutated Non-Small Cell Lung Cancer. Cancer Discov. 2022 Jan;12(1):74-89.
Ref 5 SHR-A1811, a novel anti-HER2 ADC with superior bystander effect, optimal DAR and favorable safety profiles. Cancer Res (2023) 83 (8_Supplement): LB031.
Ref 6 Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132. Front Oncol. 2022 Dec 23;12:951589.
Ref 7 Antibody conjugates of 7-ethyl-10-hydroxycamptothecin (SN-38) for targeted cancer chemotherapy. J Med Chem. 2008 Nov 13;51(21):6916-26. doi: 10.1021/jm800719t. Epub 2008 Oct 22.
Ref 8 Ifinatamab deruxtecan (I-DXd), a novel B7-H3-targeting antibody-drug conjugate, demonstrates efficient payload delivery into tumor through target-dependent internalization. Cancer Res (2023) 83 (7_Supplement): 4891.
Ref 9 BL-B01D1, a novel EGFRHER3-targeting ADC, demonstrates robust anti-tumor efficacy in preclinical evaluation. Cancer Res (2023) 83 (7_Supplement): 2642.
Ref 10 Design and Preclinical Evaluation of a Novel B7-H4-Directed Antibody-Drug Conjugate, AZD8205, Alone and in Combination with the PARP1-Selective Inhibitor AZD5305. Clin Cancer Res. 2023 Mar 14;29(6):1086-1101.
Ref 11 Safety and efficacy of DB-1303 in patients with advanced/metastatic solid tumors: A multicenter, open-label, first-in-human, phase 1/2a study. Journal of Clinical Oncology 2023 41:16_suppl, 3023-3023.
Ref 12 First in human trial of DB1305 in patients with advanced malignant solid tumors. Cancer Res (2023) 83 (8_Supplement): CT248.
Ref 13 A First-in-human Study of IBI354 in Subjects With Locally Advanced Unresectable or Metastatic Solid Tumors; NCT05636215.
Ref 14 PRO1160, a novel CD70-directed antibody-drug conjugate, demonstrates robust anti-tumor activity in mouse models of renal cell carcinoma and non-Hodgkin lymphoma. Cancer Res (2022) 82 (12_Supplement): 1759.
Ref 15 PRO1184, a novel folate receptor alpha-directed antibody-drug conjugate, demonstrates robust anti-tumor activity in mouse carcinoma models. Cancer Res (2022) 82 (12_Supplement): 1085.
Ref 16 An Open-Label, Single-Arm, Multi-Center Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of SHR-A1904 in Patients With Advanced Pancreatic Cancer, NCT04928625
Ref 17 SHR-A1921, a novel TROP-2 ADC with an optimized design and well-balanced profile between efficacy and safety. Cancer Res (2023) 83 (8_Supplement): LB030.
Ref 18 First disclosure of AZD5335, a TOP1i-ADC targeting low and high FR-expressing ovarian cancer with superior preclinical activity vs FR-MTI ADC. Cancer Res (2023) 83 (8_Supplement): LB025.
Ref 19 Study of ESG401 in Adults With Solid Tumors; NCT04892342.
Ref 20 A Study of FDA022-BB05 in Subjects With Advanced Solid Malignant Tumors; NCT05564858.
Ref 21 Study of MHB088C in Participants With Advanced or Metastatic Solid Tumors; NCT05652855.
Ref 22 Study of MHB036C in Participants With Advanced or Metastatic Solid Tumors
Ref 23 TOP1-DNA Trapping by Exatecan and Combination Therapy with ATR Inhibitor. Mol Cancer Ther. 2022 Jul 5;21(7):1090-1102.
Ref 24 A Study of DS-6000a in Subjects With Advanced Renal Cell Carcinoma and Ovarian Tumors; NCT04707248.
Ref 25 A phase 1, multicenter, open-label, first-in-human study of DS-6157a in patients (pts) with advanced gastrointestinal stromal tumor (GIST). Journal of Clinical Oncology 2022 40:16_suppl, 11512-11512.
Ref 26 ADC review: basic information about Epratuzumab-SN-38.
Ref 27 Clinical trial of the TQB2102 injection in patients with advanced cancers; 2023
Ref 28 A study of BL-M11D1 in patients with relapsed/refractory acute myeloid leukemia.
Ref 29 Accelerating Development of Mabwell's ADC Plateform: Clinical Trial Application for an Innovative Drug (9MW2921) Accepted by NMPA; 5 Feb 2023.
Ref 30 Clinical Trial Application for 7MW3711 - an Innovative Drug Developed by Mabwell's ADC Platform, Accepted by NMPA.
Ref 31 IMMU-140, a Novel SN-38 Antibody-Drug Conjugate Targeting HLA-DR, Mediates Dual Cytotoxic Effects in Hematologic Cancers and Malignant Melanoma. Mol Cancer Ther. 2018 Jan;17(1):150-160. doi: 10.1158/1535-7163.MCT-17-0354. Epub 2017 Nov 13.
Ref 32 Immunoregulation by IL-7R-targeting antibody-drug conjugates: overcoming steroid-resistance in cancer and autoimmune disease. Sci Rep. 2017 Sep 6;7(1):10735. doi: 10.1038/s41598-017-11255-4.
Ref 33 ZW191, a novel FRa-targeting antibody drug conjugate bearing a topoisomerase 1 inhibitor payload. Cancer Res (2023) 83 (7_Supplement): 2641.
Ref 34 ZW220, a novel NaPi2b-targeting antibody drug conjugate bearing a topoisomerase 1 inhibitor payload. Cancer Res (2023) 83 (7_Supplement): 1533.
Ref 35 An innovative site-specific dual-payload antibody drug conjugate (dpADC) combining a novel Topo1 inhibitor and an immune agonist delivers a strong immunogenic cell death (ICD) and antitumor response in vitro and in vivo. Cancer Res (2023) 83 (7_Supplement): 2640.
Ref 36 HER2-targeted DEP SN-38 ADC outperforms in HER2+ human cancer model (ASX announcement); 2023
Ref 37 Expanded precision medicine capabilities for strengthening oncology drug development at Daiichi Sankyo; 2021
Ref 38 Xiling yuan pharmaceutical company product pipeline
Ref 39 The preclinical pharmacology of PRO1102, a novel exatecan-based HER2-directed antibody-drug conjugate with robust anti-tumor activity. Cancer Res (2022) 82 (12_Supplement): 1758.
Ref 40 STRO-003 is a novel ROR1-targeted ADC for breast and lung cancer. Journal for ImmunoTherapy of Cancer 2022;10:doi: 10.1136/jitc-2022-SITC2022.1191.
Ref 41 CUSP06/AMT-707, a new CDH6-targeting antibody-drug conjugate, demonstrates potent antitumor activity in preclinical models. Cancer Res (2023) 83 (7_Supplement): 6320.
Ref 42 HMBD-501 - a novel Fc engineered, exatecan-based next generation HER3 targeting antibody drug conjugate shows robust efficacy and tolerability in pre-clinical solid tumor models. Cancer Res (2023) 83 (7_Supplement): 2660.
Ref 43 Nanovalent pharmaceuticals product pipeline
Ref 44 ADC review NV103
Ref 45 An investigational next generation ADC (DAN-311) is highly effective in HER2-low breast cancer models. Cancer Res (2022) 82 (4_Supplement): P2-13-09.
Ref 46 Preclinical development of a B7-H3-targeting ADC with a novel DNA topoisomerase I inhibitor for solid tumors. Cancer Res (2023) 83 (7_Supplement): 2967.
Ref 47 DB-1310, a novel Her3 targeting antibody-drug conjugate, exhibits therapeutic efficacy for solid tumors. Cancer Res (2023) 83 (7_Supplement): 1884.
Ref 48 Introduction to basic information on ADC drug AMB-101
Ref 49 Development of Novel Antibody-Camptothecin Conjugates. Mol Cancer Ther. 2021 Feb;20(2):329-339.
Ref 50 Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.
Ref 51 Antibody drug conjugates, targeting cancer-expressed EGFR, exhibit potent and specific antitumor activity. Biomed Pharmacother. 2023 Jan;157:114047.
Ref 52 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34.
Ref 53 A highly stable human single-domain antibody-drug conjugate exhibits superior penetration and treatment of solid tumors. Mol Ther. 2022 Aug 3;30(8):2785-2799.
Ref 54 Modified taxols .6. preparation of water-soluble prodrugs of taxol. J Nat Prod. 1991;54(6):1607-1611.
Ref 55 Diazaborines Are a Versatile Platform to Develop ROS-Responsive Antibody Drug Conjugates*. Angew Chem Int Ed Engl. 2021 Dec 1;60(49):25914-25921. doi: 10.1002/anie.202109835. Epub 2021 Nov 5.
Ref 56 Optimal cleavable linker for antibody-SN-38 conjugates for cancer therapy: Impact of linker's stability on efficacy. Cancer Res (2012) 72 (8_Supplement): 2526.
Ref 57 Antibody-SN-38 immunoconjugates with a CL2A linker.
Ref 58 Introduction to basic information on ADC drug hA19-SN-38 antibody-drug conjugate - Immunomedics.
Ref 59 Daiichi-Sankyo showcases latest research towards creating new standards of care for patients with cancer with data at ASCO and EHA; 25 May 2023.
Ref 60 Exatecan Antibody Drug Conjugates Based on a Hydrophilic Polysarcosine Drug-Linker Platform. Pharmaceuticals (Basel). 2021 Mar 9;14(3):247. doi: 10.3390/ph14030247.
Ref 61 ZW251, a novel glypican-3-targeting antibody drug conjugate bearing a topoisomerase 1 inhibitor payload. Cancer Res (2023) 83 (7_Supplement): 2658.
Ref 62 Antibody drug conjugates; 2023-07-06.
Ref 63 Antitumor compound, and preparation method therefor and use thereof; 2022-04-07.
Ref 64 A HER2-targeted antibody-novel DNA topoisomerase I inhibitor conjugate induces durable adaptive antitumor immunity by activating dendritic cells. MAbs. 2023 Jan-Dec;15(1):2220466. doi: 10.1080/19420862.2023.2220466.
Ref 65 AMT-562, a novel HER3-targeting antibody drug conjugate, demonstrates a potential to broaden therapeutic opportunities for HER3-expressing tumors. Mol Cancer Ther. 2023 Jun 11:MCT-23-0198. doi: 10.1158/1535-7163.MCT-23-0198. Online ahead of print.
Ref 66 Antibody-Exatecan Conjugates with a Novel Self-immolative Moiety Overcome Resistance in Colon and Lung Cancer. Cancer Discov. 2023 Apr 3;13(4):950-973. doi: 10.1158/2159-8290.CD-22-1368.
Ref 67 Antibody-Assisted Delivery of a Peptide-Drug Conjugate for Targeted Cancer Therapy. Mol Pharm. 2019 Jan 7;16(1):165-172. doi: 10.1021/acs.molpharmaceut.8b00924. Epub 2018 Dec 17.
Ref 68 Camptothecin derivative and ligand-drug conjugate thereof; 2022-04-21.
Ref 69 Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematologic malignancies. Mol Cancer Ther. 2012 Jan;11(1):224-34. doi: 10.1158/1535-7163.MCT-11-0632. Epub 2011 Oct 28.
Ref 70 Anti-cdh6 antibody and anti-cdh6 antibody-drug conjugate.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.