Target Information
General Information of This Target
Target ID | PATR0EGDKN |
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Target Name | DNA topoisomerase 1 (TOP1) |
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Gene Name | TOP1 |
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Gene ID | ||||||
Synonym | DNA topoisomerase I |
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Sequence |
MSGDHLHNDSQIEADFRLNDSHKHKDKHKDREHRHKEHKKEKDREKSKHSNSEHKDSEKK
HKEKEKTKHKDGSSEKHKDKHKDRDKEKRKEEKVRASGDAKIKKEKENGFSSPPQIKDEP EDDGYFVPPKEDIKPLKRPRDEDDADYKPKKIKTEDTKKEKKRKLEEEEDGKLKKPKNKD KDKKVPEPDNKKKKPKKEEEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKF YYDGKVMKLSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERIANFKIEPPGL FRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHKWKEVRHDNKVTWLVSWTENI QGSIKYIMLNPSSRIKGEKDWQKYETARRLKKCVDKIRNQYREDWKSKEMKVRQRAVALY FIDKLALRAGNEKEEGETADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNK VPVEKRVFKNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTKIDAKKEQLAD ARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMKLEVQATDREENKQIALGTSK LNYLDPRITVAWCKKWGVPIEKIYNKTQREKFAWAIDMADEDYEF Click to Show/Hide
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Family | the type IB topoisomerase family |
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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.
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Uniprot Entry | ||||||
HGNC ID | ||||||
KEGG ID |
Full List of The ADC Related to This Target
Approved
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
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
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
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
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
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
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
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