Target Information

General Information of This Target (ID: PATR0JHCHU)
Target Name
DNA topoisomerase 2-alpha (TOP2A)
Gene Name
TOP2A
Gene ID
7153
Synonym
TOP2A; TOP2; DNA topoisomerase II, alpha isozyme
Sequence
MEVSPLQPVNENMQVNKIKKNEDAKKRLSVERIYQKKTQLEHILLRPDTYIGSVELVTQQ
MWVYDEDVGINYREVTFVPGLYKIFDEILVNAADNKQRDPKMSCIRVTIDPENNLISIWN
NGKGIPVVEHKVEKMYVPALIFGQLLTSSNYDDDEKKVTGGRNGYGAKLCNIFSTKFTVE
TASREYKKMFKQTWMDNMGRAGEMELKPFNGEDYTCITFQPDLSKFKMQSLDKDIVALMV
RRAYDIAGSTKDVKVFLNGNKLPVKGFRSYVDMYLKDKLDETGNSLKVIHEQVNHRWEVC
LTMSEKGFQQISFVNSIATSKGGRHVDYVADQIVTKLVDVVKKKNKGGVAVKAHQVKNHM
WIFVNALIENPTFDSQTKENMTLQPKSFGSTCQLSEKFIKAAIGCGIVESILNWVKFKAQ
VQLNKKCSAVKHNRIKGIPKLDDANDAGGRNSTECTLILTEGDSAKTLAVSGLGVVGRDK
YGVFPLRGKILNVREASHKQIMENAEINNIIKIVGLQYKKNYEDEDSLKTLRYGKIMIMT
DQDQDGSHIKGLLINFIHHNWPSLLRHRFLEEFITPIVKVSKNKQEMAFYSLPEFEEWKS
STPNHKKWKVKYYKGLGTSTSKEAKEYFADMKRHRIQFKYSGPEDDAAISLAFSKKQIDD
RKEWLTNFMEDRRQRKLLGLPEDYLYGQTTTYLTYNDFINKELILFSNSDNERSIPSMVD
GLKPGQRKVLFTCFKRNDKREVKVAQLAGSVAEMSSYHHGEMSLMMTIINLAQNFVGSNN
LNLLQPIGQFGTRLHGGKDSASPRYIFTMLSSLARLLFPPKDDHTLKFLYDDNQRVEPEW
YIPIIPMVLINGAEGIGTGWSCKIPNFDVREIVNNIRRLMDGEEPLPMLPSYKNFKGTIE
ELAPNQYVISGEVAILNSTTIEISELPVRTWTQTYKEQVLEPMLNGTEKTPPLITDYREY
HTDTTVKFVVKMTEEKLAEAERVGLHKVFKLQTSLTCNSMVLFDHVGCLKKYDTVLDILR
DFFELRLKYYGLRKEWLLGMLGAESAKLNNQARFILEKIDGKIIIENKPKKELIKVLIQR
GYDSDPVKAWKEAQQKVPDEEENEESDNEKETEKSDSVTDSGPTFNYLLDMPLWYLTKEK
KDELCRLRNEKEQELDTLKRKSPSDLWKEDLATFIEELEAVEAKEKQDEQVGLPGKGGKA
KGKKTQMAEVLPSPRGQRVIPRITIEMKAEAEKKNKKKIKNENTEGSPQEDGVELEGLKQ
RLEKKQKREPGTKTKKQTTLAFKPIKKGKKRNPWSDSESDRSSDESNFDVPPRETEPRRA
ATKTKFTMDLDSDEDFSDFDEKTDDEDFVPSDASPPKTKTSPKLSNKELKPQKSVVSDLE
ADDVKGSVPLSSSPPATHFPDETEITNPVPKKNVTVKKTAAKSQSSTSTTGAKKRAAPKG
TKRDPALNSGVSQKPDPAKTKNRRKRKPSTSDDSDSNFEKIVSKAVTSKKSKGESDDFHM
DFDSAVAPRAKSVRAKKPIKYLEESDEDDLF

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Family
the type II topoisomerase family
Function
Key decatenating enzyme that alters DNA topology by binding to two double-stranded DNA molecules, generating a double-stranded break in one of the strands, passing the intact strand through the broken strand, and religating the broken strand. May play a role in regulating the period length of BMAL1 transcriptional oscillation.

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Uniprot Entry
TOP2A_HUMAN
HGNC ID
HGNC:11989
KEGG ID
hsa:7153
Full List of The ADC Related to This Target
Phase 2 (discontinued)
Click To Hide/Show 1 ADC Related to This Stage
ADC Name Antibody Antigen Payload Linker ADC Info
SGN-15
CBR96
Lewis Y
Doxorubicin
Acid-labile linker
ADC Info
Phase 1/2 (discontinued)
Click To Hide/Show 3 ADC Related to This Stage
ADC Name Antibody Antigen Payload Linker ADC Info
NBE-002
HuXBR1-402
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
LPETG-Gly5-EDA
ADC Info
SO-N102
Anti-CLDN18.2 antibody
Claudin-18.2 (CLDN18.2)
PNU-159682
Pentaglycine-EDA uncleavable linker
ADC Info
Milatuzumab doxorubicin
Milatuzumab
HLA class II histocompatibility antigen gamma chain (CD74)
Doxorubicin
SMCC-hydrazide
ADC Info
Investigative
Click To Hide/Show 34 ADC Related to This Stage
ADC Name Antibody Antigen Payload Linker ADC Info
CAC10-Gly5-PNU [1]
Brentuximab
Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)
PNU-159682
Gly5
ADC Info
Tras-Gly5-EDA-Pnu [1]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Gly5-EDA
ADC Info
HuXBR1-402-G5-PNU [2]
Anti-ROR1 mAb huXBR1-402
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
Gly5-FITC
ADC Info
Tras-Gly5-EDA-Dox [1]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
Doxorubicin
Gly5-EDA
ADC Info
Tras-Gly5-EDA-Nemo [1]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
Nemorubicin
Gly5-EDA
ADC Info
Tras-Gly3-Vakl-Cit-PAB-PNU-159682 [1]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Gly3-vcPAB
ADC Info
Alb-DMBA-SIL-DOX [3]
Alb
Albumin (ALB)
Doxorubicin
DMBA-SIL
ADC Info
Trastuzumab-PNU-159682 Antibody-Drug Conjugate [4]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
Trastuzumab-BCN-HydraSpace-Val-Cit-PABC-PNU-159682 [5]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
BCN-HydraSpace-Val-Cit-PABC
ADC Info
Trastuzumab-G5-PNU [1]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Gly5-FITC
ADC Info
Anti-CD22-NMS249 [6]
Pinatuzumab
B-cell receptor CD22 (CD22)
PNU-159682
Mc-Val-Cit-PAB-DEA
ADC Info
Anti-CD8-idarubicin conjugate [7]
Anti-CD8 (Ly-2.1) mAb
T-cell surface glycoprotein CD8 alpha chain (CD8A); T-cell surface glycoprotein CD8 alpha chain (CD8A)
Idarubicin
Undisclosed
ADC Info
MAb-DMBA-SIL-Dox [3]
Cetuximab
Epidermal growth factor receptor (EGFR)
Doxorubicin
DMBA-SIL
ADC Info
Cetuximab-Val-Cit-Dox [8]
Cetuximab
Epidermal growth factor receptor (EGFR)
Doxorubicin
Mc-Val-Cit-PABC
ADC Info
NV102 [9]
Undisclosed
B-lymphocyte antigen CD19 (CD19)
Doxorubicin
Undisclosed
ADC Info
NV101 [10]
Undisclosed
CD99 antigen (CD99)
Doxorubicin
Undisclosed
ADC Info
CytSCA208 [11]
CA208
Pregnancy-specific beta-1-glycoprotein 2 (PSG2)
Cytorhodin S
Undisclosed
ADC Info
Trastuzumab-PC4AP-DOX [12]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
Doxorubicin
Photocaged C4AP
ADC Info
Trastuzumab-PNUEDAGly5 [13]
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
LPETG-Gly5-EDA
ADC Info
Brentuximab-PNUEDAGly5 [13]
Brentuximab
Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)
PNU-159682
LPETG-Gly5-EDA
ADC Info
WO2007011968A2 cAC10-17 [14]
Brentuximab
Tumor necrosis factor receptor superfamily member 8 (TNFRSF8)
Doxorubicin
WO2007011968A2_cAC10-17 linker
ADC Info
WO2007011968A2 c1F6-17 [14]
Anti-CD70 mAb c1F6
CD70 antigen (CD70)
Doxorubicin
WO2007011968A2_c1F6-17 linker
ADC Info
PDL1-Dox ADC [15]
Atezolizumab
Programmed cell death 1 ligand 1 (PD-L1)
Doxorubicin
Undisclosed
ADC Info
HCD46-19 [16]
Anti-CD46 mAb
Membrane cofactor protein (CD46)
PNU-159682
Hydrophilic cleavable linker 19
ADC Info
HuIgG1-19 [16]
Undisclosed
Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (HER3)
PNU-159682
Hydrophilic cleavable linker 19
ADC Info
HCD46-25 [16]
Anti-CD46 mAb
Membrane cofactor protein (CD46)
PNU-159682
Alternative linker without basic amines linker 25
ADC Info
HuIgG1-25 [16]
Undisclosed
Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (HER3)
PNU-159682
Alternative linker without basic amines linker 25
ADC Info
HCD46-26 [16]
Anti-CD46 mAb
Membrane cofactor protein (CD46)
PNU-159682
Maleimide based noncleavable linker 26
ADC Info
HuIgG1-26 [16]
Undisclosed
Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (HER3)
PNU-159682
Maleimide based noncleavable linker 26
ADC Info
HCD46-29 [16]
Anti-CD46 mAb
Membrane cofactor protein (CD46)
PNU-159682
PNU-thiazole cleavable linker 29
ADC Info
HuIgG1-29 [16]
Undisclosed
Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (HER3)
PNU-159682
PNU-thiazole cleavable linker 29
ADC Info
B12-PEG-G2-DOX [17]
B12
Envelope glycoprotein gp160 (env)
Cis-aconityl-doxorubicin
B12-PEG-G2-DOX linker
ADC Info
B12-PEG-G4-DOX [17]
B12
Envelope glycoprotein gp160 (env)
Cis-aconityl-doxorubicin
B12-PEG-G4-DOX linker
ADC Info
B12-PEG-G5-DOX [17]
B12
Envelope glycoprotein gp160 (env)
Cis-aconityl-doxorubicin
B12-PEG-G5-DOX linker
ADC Info
Investigative(Terminated)
Click To Hide/Show 2 ADC Related to This Stage
ADC Name Antibody Antigen Payload Linker ADC Info
Monoclonal antibody 1H10-doxorubicin conjugate [18]
IH10
Tubulin alpha 1B (TUBA1B)
Doxorubicin
Dextran
ADC Info
Anti-Laminin receptor monoclonal antibody-liposomal doxorubicin conjugate [19]
Anti-laminin receptor IgM
Small ribosomal subunit protein uS2 (RPSA)
Doxorubicin
Disulfide bond linker
ADC Info
Investigative
Click To Hide/Show 67 ADC Related to This Stage
ADC Name Antibody Antigen Payload Linker ADC Info
ZA202500202A D04-Y180/F404-LP32 [20]
D04-Y180/F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-L-Cysteic acid-PEG4-Gly
ADC Info
ZA202500202A D04-F404-LP32 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-L-Cysteic acid-PEG4-Gly
ADC Info
ZA202500202A D04-F404-LP31 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-L-Cysteic acid-PEG4 (OH)
ADC Info
ZA202500202A D04-F404-LP30 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-PEG4-Gly (NH2)
ADC Info
ZA202500202A D04-F404-LP28 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-sidechain PEG12
ADC Info
ZA202500202A D04-F404-LP27 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-sidechain PEG12-EDA
ADC Info
ZA202500202A D04-F404-LP26 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-PEG4-EDA
ADC Info
ZA202500202A D04-F404-LP25 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-PEG4-Gly
ADC Info
ZA202500202A D04-F404-LP24 [20]
D04-F404
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-PEG4
ADC Info
EGFR-EDV-RRM1 [21]
Undisclosed
Epidermal growth factor receptor (EGFR)
Doxorubicin
Undisclosed
ADC Info
PD0721-DOX ADC [22]
PD0721
Epidermal growth factor receptor variant III (EGFRvIII)
Doxorubicin
dextran T-10
ADC Info
WO2024140927A1-ADC-E (DAR6) [23]
mAb-A
Receptor tyrosine-protein kinase erbB-2 (HER2)
Doxorubicin
Succinimidyl-4- (N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
ADC Info
WO2024140927A1-ADC-E (DAR2) [23]
mAb-A
Receptor tyrosine-protein kinase erbB-2 (HER2)
Doxorubicin
Succinimidyl-4- (N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
ADC Info
WO2024140927A1-ADC-G (DAR2) [23]
mAb-D
Vascular endothelial growth factor A (VEGFA)
Doxorubicin
Succinimidyl-4- (N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
ADC Info
WO2024140927A1-ADC-I (DAR2) [23]
mAb-E
B-lymphocyte antigen CD20 (MS4A1)
Doxorubicin
Succinimidyl-4- (N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
ADC Info
WO2020252015A1 ADCLP-24 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nAA-PEG4
ADC Info
WO2020252015A1 ADCLP-25 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nnAA-PEG4-Gly
ADC Info
WO2020252015A1 ADCLP-28 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-nAA-sidechain PEG12
ADC Info
WO2020252015A1 ADCLP-29 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-PEG4
ADC Info
WO2020252015A1 ADCLP-30 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-PEG4-Gly (OH)
ADC Info
WO2020252015A1 ADCLP-31 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-L-Cysteic acid-PEG4 (OH)
ADC Info
WO2020252015A1 ADCLP-32 [24]
mAb42
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
PNU-159682
DBCO-L-Cysteic acid-PEG4-Gly
ADC Info
CN106714844B ADC-101 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-101-linker
ADC Info
CN106714844B ADC-102 [25]
10F4v3 HC A118C
B-cell receptor CD22 (CD22)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-103 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-103-linker
ADC Info
CN106714844B ADC-104 [25]
10F4v3 HC A118C
B-cell receptor CD22 (CD22)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-105 [25]
GM15.33 HC A118C
Myeloid cell surface antigen CD33 (CD33)
PNU-159682
CN106714844B-ADC-105-linker
ADC Info
CN106714844B ADC-106 [25]
10H1.11B HC A118C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-107 [25]
7C2 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-108 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-109 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-109-linker
ADC Info
CN106714844B ADC-110 [25]
15G15.3 LC K149C
Myeloid cell surface antigen CD33 (CD33)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-111 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-112 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-113 [25]
10H1.11B HC A118C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-114 [25]
7C2 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-115 [25]
15G15.3 LC K149C
Myeloid cell surface antigen CD33 (CD33)
PNU-159682
CN106714844B-ADC-115-linker
ADC Info
CN106714844B ADC-116 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-117 [25]
6E7.N54A LC K149C
C-type lectin domain family 12 member A (CLEC12A)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-118 [25]
6E7.N54A LC K149C
C-type lectin domain family 12 member A (CLEC12A)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-119 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-119-linker
ADC Info
CN106714844B ADC-120 [25]
10F4v3 LC A149C
B-cell receptor CD22 (CD22)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-121 [25]
10H1.11.4B LC A149C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-122 [25]
10F4v3 LC A149C
B-cell receptor CD22 (CD22)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-123 [25]
10H1.11.4B LC A149C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-124 [25]
10F4v3 LC A149C
B-cell receptor CD22 (CD22)
PNU-159682
CN106714844B-ADC-124-linker
ADC Info
CN106714844B ADC-125 [25]
10H1.11.4B LC A149C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-126 [25]
10F4v3 LC A149C
B-cell receptor CD22 (CD22)
PNU-159682
CN106714844B-ADC-126-linker
ADC Info
CN106714844B ADC-127 [25]
10H1.11.4B LC A149C
Sodium-dependent phosphate transport protein 2B (SLC34A2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-128 [25]
4D5 HC A140C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-129 [25]
4D5 LC A149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-130 [25]
4D5 LC V205C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-131 [25]
4D5 HC A118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-132 [25]
4D5 LC S121C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-133 [25]
6E7.N54A LC K149C
C-type lectin domain family 12 member A (CLEC12A)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-134 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-134-linker
ADC Info
CN106714844B ADC-135 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
CN106714844B-ADC-135-linker
ADC Info
CN106714844B ADC-136 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Undisclosed
ADC Info
CN106714844B ADC-137 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Ethylmaleimide linker
ADC Info
CN106714844B ADC-138 [25]
7C2 LC K149C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Ethylmaleimide linker
ADC Info
CN106714844B ADC-139 [25]
15G15.3 LC K149C
Myeloid cell surface antigen CD33 (CD33)
PNU-159682
Ethylmaleimide linker
ADC Info
CN106714844B ADC-140 [25]
7C2 HC K118C
Receptor tyrosine-protein kinase erbB-2 (HER2)
PNU-159682
Ethylmaleimide linker
ADC Info
CN113286618A ADC-1 [26]
alpha-HMGB1Ab
High mobility group box 1 protein (HMGB1)
Doxorubicin
CN113286618A-ADC-1-linker
ADC Info
CN113286618A ADC-2 [26]
alpha-KLHAb
Hemocyanin 1 (KLH1)
Doxorubicin
Undisclosed
ADC Info
CN114450324B ADC-39 [27]
Undisclosed
Interleukin-1 beta (IL1B)
Doxorubicin
CN114450324B-ADC-39-linker
ADC Info
CN114450324B ADC-41 [27]
Undisclosed
Interleukin-1 beta (IL1B)
Doxorubicin
CN114450324B-ADC-41-linker
ADC Info
PNU-159682-P1C1TM
Undisclosed
Cellular tumor antigen p53 (TP53)
PNU-159682
Undisclosed
ADC Info
References
Ref 1 Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.
Ref 2 The ROR1 antibody-drug conjugate huXBR1-402-G5-PNU effectively targets ROR1+ leukemia. Blood Adv. 2021 Aug 24;5(16):3152-3162.
Ref 3 Radiation Cleaved Drug-Conjugate Linkers Enable Local Payload Release. Bioconjug Chem. 2022 Aug 17;33(8):1474-1484.
Ref 4 A novel anti-HER2 anthracycline-based antibody-drug conjugate induces adaptive anti-tumor immunity and potentiates PD-1 blockade in breast cancer. J Immunother Cancer. 2019 Jan 21;7(1):16. doi: 10.1186/s40425-018-0464-1.
Ref 5 Non-Genetic Generation of Antibody Conjugates Based on Chemoenzymatic Tyrosine Click Chemistry. Bioconjug Chem. 2021 Oct 20;32(10):2167-2172. doi: 10.1021/acs.bioconjchem.1c00351. Epub 2021 Sep 14.
Ref 6 A Novel Anti-CD22 Anthracycline-Based Antibody-Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs. Clin Cancer Res. 2015 Jul 15;21(14):3298-306. doi: 10.1158/1078-0432.CCR-14-2035. Epub 2015 Apr 3.
Ref 7 Evidence that an anthracycline-anti-CD8 immunoconjugate, idarubicin-anti-Ly-2.1, prolongs heart allograft survival in mice. Transplantation. 1993 Mar;55(3):484-90. doi: 10.1097/00007890-199303000-00006.
Ref 8 EGFR Targeted Cetuximab-Valine-Citrulline (vc)-Doxorubicin Immunoconjugates- Loaded Bovine Serum Albumin (BSA) Nanoparticles for Colorectal Tumor Therapy. Int J Nanomedicine. 2021 Mar 26;16:2443-2459. doi: 10.2147/IJN.S289228. eCollection 2021.
Ref 9 ADC review: basic information about NV102 (Doxorubicin-Anti-CD19).
Ref 10 ADC review NV101
Ref 11 Selective killing of carcinoembryonic-antigen (CEA)-producing cells in vitro by the immunoconjugate cytorhodin-S and CEA-reactive cytorhodin-S antibody CA208. Cancer Immunol Immunother. 1989;30(4):239-46. doi: 10.1007/BF01665011.
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Ref 13 Binding protein drug conjugates comprising anthracycline derivatives; 2016-06-30.
Ref 14 Beta-glucuronide-linker drug conjugates; 2007-10-25.
Ref 15 PDL-1 Antibody Drug Conjugate for Selective Chemo-Guided Immune Modulation of Cancer. Cancers (Basel). 2019 Feb 16;11(2):232. doi: 10.3390/cancers11020232.
Ref 16 Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.
Ref 17 Immune conjugate having dendron conjugated to antibody and use thereof.
Ref 18 Doxorubicin: monoclonal antibody conjugate for therapy of human cervical carcinoma. Int J Cancer. 1992 May 8;51(2):274-82. doi: 10.1002/ijc.2910510217.
Ref 19 Anti-laminin receptor antibody targeting of liposomes with encapsulated doxorubicin to human breast cancer cells in vitro. J Natl Cancer Inst. 1989 Dec 6;81(23):1794-800. doi: 10.1093/jnci/81.23.1794.
Ref 20 Anti-ROR1 antibodies and antibody conjugates, compositions comprising Anti-ROR1 antibodies or antibody conjugates, and methods of making and using Anti-ROR1 antibodies and antibody conjugates
Ref 21 Introduction to basic information on antibody-drug nanocell conjugates(EnGeneIC Pty Ltd.).
Ref 22 Preparation and evaluation of the PD0721-DOX antibody-drug conjugate targeting EGFRvIII to inhibit glioblastoma
Ref 23 Use of hydroxypropyl-β-cyclodextrin in stabilizing antibody-drug conjugate formulations
Ref 24 Immunomodulator antibody drug conjugates and uses thereof
Ref 25 Anthracycline disulfide intermediates, antibody-drug conjugates and methods
Ref 26 Antibody-drug conjugates and applications in antibody-mediated drug delivery
Ref 27 Heterobifunctional monodisperse polyethylene glycol with peptide linkers