Target Information

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 5 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	Trastuzumab rezetecan	Trastuzumab	ERBB2	SHR9265	Mc-Gly-Gly-Phe-Gly	[1]
ADC Info	Datopotamab deruxtecan	Datopotamab	TACSTD2	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[2]
ADC Info	Sacituzumab govitecan	Sacituzumab	TACSTD2	Active metabolite of irinotecan SN38	CL2A	[3]
ADC Info	Sacituzumab tirumotecan	Sacituzumab	TACSTD2	KL610023	Pyrimidine-CL2A-carbonate	[4]
ADC Info	Trastuzumab deruxtecan	Trastuzumab	ERBB2	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[5]

Phase 3

Click To Hide/Show 20 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	ABBV-400	Telisotuzumab	MET	DNA topoisomerase-I inhibitor	Valine-alanine linker
ADC Info	BL-B01D1	SI-B001	ERBB3; EGFR	Camptothecin analogue ED04	Gly-Mal-Gly-Gly-Phe-Gly	[6]
ADC Info	BL-M07D1	Trastuzumab	ERBB2	Camptothecin analogue ED04	Cathepsin B cleavable linker	[7]
ADC Info	DB-1303	Trastuzumab	ERBB2	P1003	Mc-Gly-Gly-Phe-Gly	[8]
ADC Info	ESG-401	A humanized IgG1 monoclonal antibody	TACSTD2	Active metabolite of irinotecan SN38	A proprietary stable-cleavable linker	[9]
ADC Info	FDA-018	A humanized monoclonal antibody against human Trop-2	TACSTD2	Active metabolite of irinotecan SN38	An acid-cleavable linker	[10]
ADC Info	GQ-1005	Undisclosed	ERBB2	DX-8951 derivative (DXd)	Stable linker	[11]
ADC Info	HS-20089	Undisclosed	VTCN1	DNA topoisomerase-I inhibitor	Undisclosed	[12]
ADC Info	HS-20093	Risvutatug	CD276	Exatecan derivative (HS-9265)	Maleimide tetrapeptide linker	[13]
ADC Info	IBI-343	A fully humanized anti-CLDN18.2 monoclonal antibody	CLDN18.2	Exatecan	Synaffix linker	[14]
ADC Info	IBI-354	Trastuzumab	ERBB2	DX-8951 derivative (DXd)	PODS-CHX-A"-DTPA	[15]
ADC Info	Ifinatamab deruxtecan	Ifinatamab	CD276	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[16]
ADC Info	JSKN-003	Anbenitamab	HER2 ECD2; HER2 ECD4	DX-8951 derivative (DXd)	DBCO-PEG4-Mc-Gly-Gly-Phe-Gly	[17]
ADC Info	Patritumab deruxtecan	Patritumab	ERBB3	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[18]
ADC Info	PRO1184	Rinatabart	FOLR1	Exatecan	Cys-11 ADC linker	[19]
ADC Info	SHR-A1904	A humanized IgG1 monoclonal antibody targeting CLDN18.2	CLDN18.2	SHR9265	Mc-Gly-Gly-Phe-Gly	[20]
ADC Info	SHR-A2009	Ruzaltatug	ERBB3	9106-IM-2	Mc-Gly-Gly-Phe-Gly	[21]
ADC Info	SHR-A2102	Undisclosed	NECTIN4	9106-IM-2	Mc-Gly-Gly-Phe-Gly	[22]
ADC Info	SYS6010	Undisclosed	EGFR	JS-1	GGFG	[23]
ADC Info	YL-201	Undisclosed	CD276	YL0010014	Tumor microenviroment activable tripeptide linker	[24]

Phase 2/3

Click To Hide/Show 1 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	DS-6000	Raludotatug	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[25]

Phase 2

Click To Hide/Show 4 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	HLX-43	HLX20	CD274	Camptothecin-based toxin	A cleavable linker	[26]
ADC Info	JSKN016	Undisclosed	ERBB3; TACSTD2	DNA topoisomerase-I inhibitor	Undisclosed
ADC Info	SHR-A1921	Tizetatug	TACSTD2	SHR9265	Mc-Gly-Gly-Phe-Gly	[27]
ADC Info	TQB2102	Undisclosed	HER2 ECD2; HER2 ECD4	2-DDDX-d	Mc-Gly-Gly-Phe-Gly	[28]

Phase 2 (Terminated)

Click To Hide/Show 1 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	Labetuzumab govitecan	Labetuzumab	CEACAM5	Active metabolite of irinotecan SN38	CL2A	[29]

Phase 1/2

Click To Hide/Show 24 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	9MW-2921	Undisclosed	TACSTD2	DNA topoisomerase-I inhibitor	Undisclosed	[30]
ADC Info	AMT-116	Undisclosed	CD44v9	KL610023	Hydrolysable linker
ADC Info	AMT-253	A humanized MUC18-targeting IgG1 antibody	MCAM	Exatecan	T1000
ADC Info	AZD5335	Undisclosed	FOLR1	AZ14170132	Mal-PEG8-Val-Ala	[31]
ADC Info	AZD8205	Puxitatug	VTCN1	AZ0132	Mal-PEG8-Val-Ala	[32]
ADC Info	AZD-9829	Undisclosed	IL3RA	AZ14170132	Undisclosed
ADC Info	BL-M02D1	hu4D3	TACSTD2	Camptothecin analogue ED04	Cathepsin B cleavable linker	[33]
ADC Info	DB-1305	Undisclosed	TACSTD2	P1003	Mc-Gly-Gly-Phe-Gly	[34]
ADC Info	DB-1310	A humanized anti-HER3 IgG1 monoclonal antibody	ERBB3	P1021	Maleimide tetrapeptide-based cleavable linker	[35]
ADC Info	DB-1311	Undisclosed	CD276	P1021	Maleimide tetrapeptide-based cleavable linker	[36]
ADC Info	DB-1419	Undisclosed	CD276; CD274	P1003	Undisclosed
ADC Info	DS-3939a	Gatipotuzumab	MUC1	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[37]
ADC Info	GEN-1286	Undisclosed	MET; EGFR	Exatecan	Cys-11 ADC linker
ADC Info	GQ-1010	Undisclosed	TACSTD2	Camptothecin analogue	A cleavable open-ring linker	[11]
ADC Info	IBI-129	Undisclosed	CD276	Undisclosed	Undisclosed	[38]
ADC Info	M-9140	Undisclosed	CEACAM5	Exatecan	Mal-glucuronide-PABC	[39]
ADC Info	MHB-036C	Undisclosed	TACSTD2	MH30010008	Stable cleavable linker	[40]
ADC Info	MHB-088C	Undisclosed	CD276	DNA topoisomerase I inhibitor	Protease- hydrolyzable linker	[41]
ADC Info	OBI-992	R4702	TACSTD2	Exatecan	Mal-PEG24-Val-Ala-PABC	[42]
ADC Info	PRO-1160	Undisclosed	CD70	Exatecan	Cys-11 ADC linker	[43]
ADC Info	TUB-030	Undisclosed	TPBG	Exatecan	A cleavable linker	[44]
ADC Info	TUB-040	A humanized, Fc-silenced IgG1 antibody targeting Napi2b	SLC34A2	Exatecan	P5 (PEG24)-Val-Cit-PABC	[44]
ADC Info	XNW-27011	Undisclosed	CLDN18.2	YL0010014	Tumor microenviroment activable tripeptide linker	[45]
ADC Info	YL-205	An anti-NaPi2b humanized monoclonal antibody	SLC34A2	YL0010014	Tumor microenviroment activable tripeptide linker

Phase 1

Click To Hide/Show 42 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	ABBV-706	Undisclosed	SEZ6	DNA topoisomerase-I inhibitor	Valine-alanine linker
ADC Info	ABBV-969	A anti-PSMA/STEAP1 IgG1 antibody	FOLH1; STEAP1	DNA topoisomerase-I inhibitor	Undisclosed
ADC Info	ADRX-0405	Undisclosed	STEAP1	DNA topoisomerase-I inhibitor	Undisclosed	[46]
ADC Info	AMT-562	Ab562	ERBB3	Exatecan	T800	[47]
ADC Info	AMT-676	Undisclosed	CDH17	Exatecan	Polylysine modified protease sensitive peptide linker	[48]
ADC Info	AZD9592	Tilatamig	EGFR; MET	AZ0132	Mal-PEG8-Val-Ala	[49]
ADC Info	BAT8006	Undisclosed	FOLR1	Exatecan	Cleavable linker	[50]
ADC Info	BAT8007	Undisclosed	NECTIN4	Exatecan	Cleavable but systemically stable linker	[51]
ADC Info	BAT8008	Undisclosed	TACSTD2	Exatecan	Enzymatically cleavable linker	[52]
ADC Info	BAT8009	Undisclosed	CD276	Exatecan	Cleavable linker	[53]
ADC Info	BAT8010	Undisclosed	ERBB2	Exatecan	Cleavable linker	[54]
ADC Info	BG-C9074	Undisclosed	VTCN1	DNA topoisomerase-I inhibitor	Undisclosed	[55]
ADC Info	BL-M05D1	Undisclosed	CLDN18.2	Camptothecin analogue ED04	Undisclosed	[56]
ADC Info	BL-M08D1	Undisclosed	TACSTD2	Camptothecin analogue ED04	Gly-Mal-Gly-Gly-Phe-Gly	[56]
ADC Info	BL-M11D1	Gemtuzumab	CD33	Camptothecin analogue ED04	Gly-Mal-Gly-Gly-Phe-Gly	[57]
ADC Info	CUSP06	A humanized anti-CDH6 IgG1 mAb	CDH6	Exatecan	T1000	[58]
ADC Info	CX-2051	Undisclosed	EPCAM	Camptothecin analog	Cleavable linker	[59]
ADC Info	DAC-1002	Undisclosed	TACSTD2	CPT113	CrossConju linker	[60]
ADC Info	DM001	Undisclosed	TACSTD2; EGFR	BCPT02	Hydrophilic, protease-cleavable linker	[61]
ADC Info	DM002	Undisclosed	ERBB3; MUC1	BCPT02	Hydrophilic, protease-cleavable linker	[62]
ADC Info	DM005	Undisclosed	MET; EGFR	BCPT02	Hydrophilic, protease-cleavable linker
ADC Info	DXC-006	DXA006	NCAM1	CPT113	Cleavable peptidyl linker	[63]
ADC Info	FDA-022	Trastuzumab	ERBB2	DX-8951 derivative (DXd)	Mc-Val-Ala-PABC double self-immolative linker	[64]
ADC Info	FZ-AD004	Undisclosed	TACSTD2	DX-8951 derivative (DXd)	Mc-Val-Ala-PABC double self-immolative linker	[65]
ADC Info	HBM9033	Undisclosed	MSLN	Undisclosed	Undisclosed	[66]
ADC Info	HLX-42	A highly specific humanized IgG1 anti-EGFR	EGFR	DNA topoisomerase-I inhibitor	Undisclosed	[67]
ADC Info	IBI-3001	IBI-334	EGFR; CD276	Exatecan	Undisclosed
ADC Info	IBI-3005	Undisclosed	EGFR; ERBB3	Camptothecin analog	Undisclosed
ADC Info	IPH-4502	Undisclosed	NECTIN4	Exatecan	Cleavable hydrophilic linker
ADC Info	LY-4052031	A human IgG1 Fc-silent monoclonal Nectin-4 antibody	NECTIN4	LSN3889710	Cleavable peptide linker
ADC Info	LY-4170156	Fc-silent FR specific humanized IgG1 antibody	FOLR1	Exatecan	Mal-Polysarcosine10-Val-Ala-PABC	[68]
ADC Info	PHN-010	Undisclosed	Undisclosed	DNA topoisomerase-I inhibitor	Undisclosed	[69]
ADC Info	SAR-445953	Tusamitamab	CEACAM5	7-aminomethyl-10,11-methylenedioxycamptothecin (AMDCPT)	Undisclosed
ADC Info	SHR-1826	A humanized c-MET-directed IgG2 monoclonal antibody	MET	9106-IM-2	Mc-Gly-Gly-Phe-Gly
ADC Info	SHR-4849	SHR-2495	DLL3	9106-IM-2	Mc-Gly-Gly-Phe-Gly
ADC Info	SHR-A1912	SHR-1920	CD79B	SHR9265	Mc-Gly-Gly-Phe-Gly	[70]
ADC Info	SKB-315	Undisclosed	CLDN18.2	Topoisomerase I inhibitor	Stable linker	[71]
ADC Info	TQB2103	A humanized anti-CLDN18.2 IgG1 monoclonal antibody	CLDN18.2	2-DDDX-d	Mc-Gly-Gly-Phe-Gly	[72]
ADC Info	YL-202	An anti-HER3 IgG1 monoclonal antibody	ERBB3	YL0010014	Tumor microenviroment activable tripeptide linker	[73]
ADC Info	YL-211	Undisclosed	MET	YL0010014	Tumor microenviroment activable tripeptide linker
ADC Info	ZL-1310	Undisclosed	DLL3	YL0010014	Tumor microenviroment activable tripeptide linker	[74]
ADC Info	ZW191	Humanized Anti-FOLR1 IgG1 mAb	FOLR1	ZD06519	Mc-Gly-Gly-Phe-Gly-AM	[75]

Phase 1 (Terminated)

Click To Hide/Show 1 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	DS-6157a	Undisclosed	GPR20	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[76]

Investigative

Click To Hide/Show 162 ADC Related to This Stage

ADC Info	ADC Name	Antibody	Antigen	Payload	Linker	Ref
ADC Info	40H3-CL2A-SN38	Anti-EGFR mAb 40H3	EGFR	Active metabolite of irinotecan SN38	CL2A	[77]
ADC Info	40H3-Deruxtecan	Anti-EGFR mAb 40H3	EGFR	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[77]
ADC Info	7MW-3711	Undisclosed	CD276	Topoisomerase I inhibitor	Undisclosed	[78]
ADC Info	A7R-ADC-SN38	Anti-IL7R mAb A7R	IL7R	Active metabolite of irinotecan SN38	Mal-PEG12-carbamate-PEG27	[79]
ADC Info	ADC1-1	Cofetuzumab	PTK7	ADC 1-1 payload	ADC 1-1 linker	[80]
ADC Info	ADC1-11	Cofetuzumab	PTK7	ADC 1-11 payload	ADC 1-11 linker	[80]
ADC Info	ADC1-12	Cofetuzumab	PTK7	ADC 1-12 payload	ADC 1-12 linker	[80]
ADC Info	ADC1-2	Cofetuzumab	PTK7	ADC 1-2 payload	ADC 1-2 linker	[80]
ADC Info	ADC1-4	Cofetuzumab	PTK7	ADC 1-4 payload	ADC 1-4 linker	[80]
ADC Info	ADC2-10	Trastuzumab	ERBB2	ADC 2-10 payload	ADC 2-10 linker	[80]
ADC Info	ADC2-11	Trastuzumab	ERBB2	ADC 2-11 payload	ADC 2-11 linker	[80]
ADC Info	ADC2-12	Trastuzumab	ERBB2	ADC 2-12 payload	ADC 2-12 linker	[80]
ADC Info	ADC2-2	Trastuzumab	ERBB2	ADC 2-2 payload	ADC 2-2 linker	[80]
ADC Info	ADC2-22	Trastuzumab	ERBB2	ADC 2-22 payload	ADC 2-22 linker	[80]
ADC Info	ADC2-23	Trastuzumab	ERBB2	ADC 2-23 payload	ADC 2-23 linker	[80]
ADC Info	ADC2-24	Trastuzumab	ERBB2	ADC 2-24 payload	ADC 2-24 linker	[80]
ADC Info	ADC2-25	Trastuzumab	ERBB2	ADC 2-25 payload	ADC 2-25 linker	[80]
ADC Info	ADC2-26	Trastuzumab	ERBB2	ADC 2-26 payload	ADC 2-26 linker	[80]
ADC Info	ADC2-27	Trastuzumab	ERBB2	ADC 2-27 payload	ADC 2-27 linker	[80]
ADC Info	ADC2-29	Trastuzumab	ERBB2	ADC 2-29 payload	ADC 2-29 linker	[80]
ADC Info	ADC2-30	Trastuzumab	ERBB2	ADC 2-30 payload	ADC 2-30 linker	[80]
ADC Info	ADC2-31	Trastuzumab	ERBB2	ADC 2-31 payload	ADC 2-31 linker	[80]
ADC Info	ADC2-32	Trastuzumab	ERBB2	ADC 2-32 payload	ADC 2-32 linker	[80]
ADC Info	ADC2-33	Trastuzumab	ERBB2	ADC 2-33 payload	ADC 2-33 linker	[80]
ADC Info	ADC2-34	Trastuzumab	ERBB2	ADC 2-34 payload	ADC 2-34 linker	[80]
ADC Info	ADC2-35	Trastuzumab	ERBB2	ADC 2-35 payload	ADC 2-35 linker	[80]
ADC Info	ADC2-36-1	Trastuzumab	ERBB2	ADC 2-36-1 payload	ADC 2-36-1 linker	[80]
ADC Info	ADC2-36-2	Trastuzumab	ERBB2	ADC 2-36-2 payload	ADC 2-36-2 linker	[80]
ADC Info	ADC2-37	Trastuzumab	ERBB2	ADC 2-37 payload	ADC 2-37 linker	[80]
ADC Info	ADC2-38	Trastuzumab	ERBB2	ADC 2-38 payload	ADC 2-38 linker	[80]
ADC Info	ADC2-39	Trastuzumab	ERBB2	ADC 2-39 payload	ADC 2-39 linker	[80]
ADC Info	ADC2-4	Trastuzumab	ERBB2	ADC 2-4 payload	ADC 2-4 linker	[80]
ADC Info	ADC2-40	Trastuzumab	ERBB2	ADC 2-40 payload	ADC 2-40 linker	[80]
ADC Info	ADC2-41	Trastuzumab	ERBB2	ADC 2-41 payload	ADC 2-41 linker	[80]
ADC Info	ADC2-42	Trastuzumab	ERBB2	ADC 2-42 payload	ADC 2-42 linker	[80]
ADC Info	ADC2-42-RO	Trastuzumab	ERBB2	ADC 2-42-RO payload	ADC 2-42-RO linker	[80]
ADC Info	ADC2-43	Trastuzumab	ERBB2	ADC 2-43 payload	ADC 2-43 linker	[80]
ADC Info	ADC2-44	Trastuzumab	ERBB2	ADC 2-44 payload	ADC 2-44 linker	[80]
ADC Info	ADC2-45	Trastuzumab	ERBB2	ADC 2-45 payload	ADC 2-45 linker	[80]
ADC Info	ADC2-46	Trastuzumab	ERBB2	ADC 2-46 payload	ADC 2-46 linker	[80]
ADC Info	ADC2-47	Trastuzumab	ERBB2	ADC 2-47 payload	ADC 2-47 linker	[80]
ADC Info	ADC2-48	Trastuzumab	ERBB2	ADC 2-48 payload	ADC 2-48 linker	[80]
ADC Info	ADC2-49	Trastuzumab	ERBB2	ADC 2-49 payload	ADC 2-49 linker	[80]
ADC Info	ADC2-50	Trastuzumab	ERBB2	ADC 2-50 payload	ADC 2-50 linker	[80]
ADC Info	ADC2-51	Trastuzumab	ERBB2	ADC 2-51 payload	ADC 2-51 linker	[80]
ADC Info	ADC2-53	Trastuzumab	ERBB2	ADC 2-53 payload	ADC 2-53 linker	[80]
ADC Info	ADC2-54	Trastuzumab	ERBB2	ADC 2-54 payload	ADC 2-54 linker	[80]
ADC Info	ADC2-55	Trastuzumab	ERBB2	ADC 2-55 payload	ADC 2-55 linker	[80]
ADC Info	ADC2-56	Trastuzumab	ERBB2	ADC 2-56 payload	ADC 2-56 linker	[80]
ADC Info	ADC2-57	Trastuzumab	ERBB2	ADC 2-57 payload	ADC 2-57 linker	[80]
ADC Info	ADC2-58	Trastuzumab	ERBB2	ADC 2-58 payload	ADC 2-58 linker	[80]
ADC Info	ADC2-59	Trastuzumab	ERBB2	ADC 2-59 payload	ADC 2-59 linker	[80]
ADC Info	ADC2-60	Trastuzumab	ERBB2	ADC 2-60 payload	ADC 2-60 linker	[80]
ADC Info	ADC2-61	Trastuzumab	ERBB2	ADC 2-61 payload	ADC 2-61 linker	[80]
ADC Info	ADC2-6-2	Trastuzumab	ERBB2	ADC 2-6-2 payload	ADC 2-6-2 linker	[80]
ADC Info	ADC-2-62-1	Trastuzumab	ERBB2	ADC 2-62-1 payload	ADC 2-62-1 linker	[80]
ADC Info	ADC-2-62-2	Trastuzumab	ERBB2	ADC 2-62-2 payload	ADC 2-62-2 linker	[80]
ADC Info	ADC-2-63-1	Trastuzumab	ERBB2	ADC 2-63-1 payload	ADC 2-63-1 linker	[80]
ADC Info	ADC-2-63-2	Trastuzumab	ERBB2	ADC 2-63-2 payload	ADC 2-63-2 linker	[80]
ADC Info	ADC-2-64-1	Trastuzumab	ERBB2	ADC 2-64-1 payload	ADC 2-64-1 linker	[80]
ADC Info	ADC-2-64-2	Trastuzumab	ERBB2	ADC 2-64-2 payload	ADC 2-64-2 linker	[80]
ADC Info	ADC-2-65-1	Trastuzumab	ERBB2	ADC 2-65-1 payload	ADC 2-65-1 linker	[80]
ADC Info	ADC-2-65-2	Trastuzumab	ERBB2	ADC 2-65-2 payload	ADC 2-65-2 linker	[80]
ADC Info	ADC2-7-2	Trastuzumab	ERBB2	ADC 2-7-2 payload	ADC 2-7-2 linker	[80]
ADC Info	ADC2-9-1	Trastuzumab	ERBB2	ADC 2-9-1 payload	ADC 2-9-1 linker	[80]
ADC Info	ADC2-9-2	Trastuzumab	ERBB2	ADC 2-9-2 payload	ADC 2-9-2 linker	[80]
ADC Info	ADC2-A	Trastuzumab	ERBB2	ADC 2-A payload	ADC 2-A linker	[80]
ADC Info	ADC2-B	Trastuzumab	ERBB2	ADC 2-B payload	ADC 2-B linker	[80]
ADC Info	ADC3-1	Trastuzumab	ERBB2	ADC 3-1 payload	ADC 3-1 linker	[80]
ADC Info	ADC3-10	Patritumab	ERBB3	ADC 3-10 payload	ADC 3-10 linker	[80]
ADC Info	ADC3-11	Patritumab	ERBB3	ADC 3-11 payload	ADC 3-11 linker	[80]
ADC Info	ADC3-12	Patritumab	ERBB3	ADC 3-12 payload	ADC 3-12 linker	[80]
ADC Info	ADC3-13	Patritumab	ERBB3	ADC 3-13 payload	ADC 3-13 linker	[80]
ADC Info	ADC3-14	Patritumab	ERBB3	ADC 3-14 payload	ADC 3-14 linker	[80]
ADC Info	ADC3-15	Patritumab	ERBB3	ADC 3-15 payload	ADC 3-15 linker	[80]
ADC Info	ADC3-16	Patritumab	ERBB3	ADC 3-16 payload	ADC 3-16 linker	[80]
ADC Info	ADC3-17	Patritumab	ERBB3	ADC 3-17 payload	ADC 3-17 linker	[80]
ADC Info	ADC3-18	Patritumab	ERBB3	ADC 3-18 payload	ADC 3-18 linker	[80]
ADC Info	ADC3-19	Patritumab	ERBB3	ADC 3-19 payload	ADC 3-19 linker	[80]
ADC Info	ADC3-2	Trastuzumab	ERBB2	ADC 3-2 payload	ADC 3-2 linker	[80]
ADC Info	ADC3-20	Patritumab	ERBB3	ADC 3-20 payload	ADC 3-20 linker	[80]
ADC Info	ADC3-3	Trastuzumab	ERBB2	ADC 3-3 payload	ADC 3-3 linker	[80]
ADC Info	ADC3-4	Trastuzumab	ERBB2	ADC 3-4 payload	ADC 3-4 linker	[80]
ADC Info	ADC3-5	Trastuzumab	ERBB2	ADC 3-5 payload	ADC 3-5 linker	[80]
ADC Info	ADC3-6	Patritumab	ERBB3	ADC 3-6 payload	ADC 3-6 linker	[80]
ADC Info	ADC3-7	Patritumab	ERBB3	ADC 3-7 payload	ADC 3-7 linker	[80]
ADC Info	ADC3-8	Patritumab	ERBB3	ADC 3-8 payload	ADC 3-8 linker	[80]
ADC Info	ADC3-9	Patritumab	ERBB3	ADC 3-9 payload	ADC 3-9 linker	[80]
ADC Info	ADC-C1	Patritumab	ERBB3	ADC-C1 payload	ADC-C1 linker	[80]
ADC Info	ADC-C2	Patritumab	ERBB3	ADC-C2 payload	ADC-C2 linker	[80]
ADC Info	ADC-C3	Patritumab	ERBB3	ADC-C3 payload	ADC-C3 linker	[80]
ADC Info	ADC-C4	Patritumab	ERBB3	ADC-C4 payload	ADC-C4 linker	[80]
ADC Info	ADC-C5	Patritumab	ERBB3	ADC-C5 payload	ADC-C5 linker	[80]
ADC Info	AMB-101	Undisclosed	Undisclosed	Topoisomerase I inhibitor	Undisclosed	[81]
ADC Info	CAC10-CPT-LA	Brentuximab	TNFRSF8	Methylenedioxy CPT1 (CPT1)	Mc-PEG4-Val-Lys-Gly	[82]
ADC Info	CAC10-CPT-LB	Brentuximab	TNFRSF8	Methylenedioxy CPT2 (CPT2)	Mc-PEG4-Val-Lys-Gly	[82]
ADC Info	CAC10-CPT-LC	Brentuximab	TNFRSF8	Methylenedioxy CPT2 (CPT2)	Mc-PEG8-Val-Lys-Gly	[82]
ADC Info	CAC10-DT	Brentuximab	TNFRSF8	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[82]
ADC Info	CAC10-GT	Brentuximab	TNFRSF8	Active metabolite of irinotecan SN38	CL2A	[82]
ADC Info	cot-APTEDB-SN38	Anti-EDB Ab cot	VAMP8	Active metabolite of irinotecan SN38	Mal-PEG4-Ala	[83]
ADC Info	DAN-311	Undisclosed	ERBB2	Camptothecin	Undisclosed	[84]
ADC Info	DpADC	Undisclosed	TACSTD2	Topo1 inhibitor+immune agonist	Undisclosed	[85]
ADC Info	Emab-CL2E-SN38	Epratuzumab	CD22	Active metabolite of irinotecan SN38	CL2E	[86]
ADC Info	Epratuzumab-CL2E-SN-38	Epratuzumab	CD22	Active metabolite of irinotecan SN38	CL2E	[87]
ADC Info	Epratuzumab-SN-38	Epratuzumab	CD22	Active metabolite of irinotecan SN38	CL2A	[87]
ADC Info	H00-CPT-LA	Anti-CD30 mAb h00	TNFRSF8	Methylenedioxy CPT1 (CPT1)	Mc-PEG4-Val-Lys-Gly	[82]
ADC Info	H00-CPT-LB	Anti-CD30 mAb h00	TNFRSF8	Methylenedioxy CPT2 (CPT2)	Mc-PEG4-Val-Lys-Gly	[82]
ADC Info	H00-CPT-LC	Anti-CD30 mAb h00	TNFRSF8	Methylenedioxy CPT2 (CPT2)	Mc-PEG8-Val-Lys-Gly	[82]
ADC Info	H00-DT	Anti-CD30 mAb h00	TNFRSF8	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[82]
ADC Info	H00-GT	Anti-CD30 mAb h00	TNFRSF8	Active metabolite of irinotecan SN38	CL2A	[88]
ADC Info	H01L02-DXd	Anti-CDH6 mAb H01L02	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[89]
ADC Info	H02L02-DXd	Anti-CDH6 mAb H02L02	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[89]
ADC Info	H02L03-DXd	Anti-CDH6 mAb H02L03	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[89]
ADC Info	H04L02-DXd	Anti-CDH6 mAb H04L02	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[89]
ADC Info	HA19-SN38 antibody-drug conjugate	Anti-CD19 mAb hA19	CD19	Active metabolite of irinotecan SN38	CL2A	[90]
ADC Info	HER2 targeted DEP conjugate	Trastuzumab	ERBB2	Active metabolite of irinotecan SN38	Undisclosed	[91]
ADC Info	HLL1-CL2A-SN38	Milatuzumab	CD74	Active metabolite of irinotecan SN38	CL2A	[92]
ADC Info	HMBD-501	Undisclosed	ERBB3	Exatecan	Undisclosed	[93]
ADC Info	HPAM4-CL2A-SN38	Anti-MUC1 mAb hPAM4	MUC1	Active metabolite of irinotecan SN38	CL2A	[94]
ADC Info	IMMU-140	IMMU-114	HLA-DRA	Active metabolite of irinotecan SN38	CL2A	[95]
ADC Info	Labetuzumab-CL2E-SN-38	Labetuzumab	CEACAM5	Active metabolite of irinotecan SN38	CL2E	[87]
ADC Info	Labetuzumab-SN-38	Labetuzumab	CEACAM5	Active metabolite of irinotecan SN38	CL2A	[87]
ADC Info	Lmab-CL2A-SN38	Labetuzumab	CEACAM5	Active metabolite of irinotecan SN38	CL2E	[86]
ADC Info	M603-SN38 DAR4	Anti-5T4 mAb m603	TPBG	Active metabolite of irinotecan SN38	CL2A	[96]
ADC Info	M603-SN38 DAR6	Anti-5T4 mAb m603	TPBG	Active metabolite of irinotecan SN38	CL2A	[96]
ADC Info	M603-SN38 DAR8	Anti-5T4 mAb m603	TPBG	Active metabolite of irinotecan SN38	CL2A	[96]
ADC Info	Mil40-11 (DAR=3.8)	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mc-PEG8-Val-Ala-PABC	[97]
ADC Info	Mil40-11 (DAR=7.1)	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mc-PEG8-Val-Ala-PABC	[97]
ADC Info	Mil40-5	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mc-Val-Ala-PABC	[97]
ADC Info	Mil40-6	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mal-PEG2-Val-Ala-PABC	[97]
ADC Info	Mil40-7	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mal-PEG4-Val-Ala-PABC	[97]
ADC Info	Mil40-8	Mil40	ERBB2	Active metabolite of irinotecan SN38	Mal-PEG8-Val-Ala-PABC	[97]
ADC Info	N501-SN38	Anti-5T4 n501 (nanobody)	TPBG	Active metabolite of irinotecan SN38	CL2A	[96]
ADC Info	NOV0712-DXd	Anti-CDH6 mAb NOV0712	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[89]
ADC Info	NV103	Undisclosed	CD99	Irinotecan	Undisclosed	[98]
ADC Info	NV104	Undisclosed	CD276	Irinotecan	Undisclosed	[99]
ADC Info	PRO-1102	Trastuzumab	ERBB2	Exatecan	Cleavable hydrophilic linker	[100]
ADC Info	Raludotatug deruxtecan	Raludotatug	CDH6	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[101]
ADC Info	ROS-responsive SN38 ADC	Rabbit derived VL single-domain Anti-ody	Undisclosed	Active metabolite of irinotecan SN38	Mal-Cyc-PEG3-DAB	[102]
ADC Info	Sacituzumab-Deruxtecan	Sacituzumab	TACSTD2	DX-8951 derivative (DXd)	Mc-Gly-Gly-Phe-Gly	[103]
ADC Info	Sacituzumab-SN-38	Sacituzumab	TACSTD2	Active metabolite of irinotecan SN38	CL2A	[87]
ADC Info	SMP-190	Undisclosed	Undisclosed	DX-8951 derivative (DXd)	Unique hydrophilic Linker	[104]
ADC Info	STRO-003	SP11285	ROR1	Exatecan	SC3417	[105]
ADC Info	Tra-Exa-PSAR0	Trastuzumab	ERBB2	Exatecan	Mal-Exa-PSAR0	[106]
ADC Info	Tra-Exa-PSAR10	Trastuzumab	ERBB2	Exatecan	Mal-Exa-PSAR10	[106]
ADC Info	Trastuzumab-L6	Trastuzumab	ERBB2	MF-6	Bridged PEG4-valine-alanine	[107]
ADC Info	Trastuzumab-T1000-exatecan	Trastuzumab	ERBB2	Exatecan	Undisclosed	[108]
ADC Info	Veltuzumab-CL2E-SN-38	Veltuzumab	MS4A1	Active metabolite of irinotecan SN38	CL2E	[87]
ADC Info	Veltuzumab-SN-38	Veltuzumab	MS4A1	Active metabolite of irinotecan SN38	CL2A	[87]
ADC Info	VL-DAB31-SN38	Rabbit derived VL single-domain Anti-ody	Undisclosed	Active metabolite of irinotecan SN38	Mal-Cyc-PEG3-DAB	[102]
ADC Info	WO2022078260A1 ADC-1	Trastuzumab	ERBB2	Ln-D9	WO2022078260A1_ADC-1 linker	[109]
ADC Info	WO2022078260A1 ADC-10	Cetuximab	EGFR	Ln-D7	WO2022078260A1_ADC-10 linker	[109]
ADC Info	WO2022078260A1 ADC-2	Trastuzumab	ERBB2	Ln-D1	WO2022078260A1_ADC-2 linker	[109]
ADC Info	WO2022078260A1 ADC-3	Trastuzumab	ERBB2	Ln-D2	WO2022078260A1_ADC-3 linker	[109]
ADC Info	WO2022078260A1 ADC-4	Trastuzumab	ERBB2	Ln-D4	WO2022078260A1_ADC-4 linker	[109]
ADC Info	WO2022078260A1 ADC-5	Trastuzumab	ERBB2	Ln-D5	WO2022078260A1_ADC-5 linker	[109]
ADC Info	WO2022078260A1 ADC-6	Trastuzumab	ERBB2	Ln-D6	WO2022078260A1_ADC-6 linker	[109]
ADC Info	WO2022078260A1 ADC-7	Trastuzumab	ERBB2	Ln-D7	WO2022078260A1_ADC-7 linker	[109]
ADC Info	WO2022078260A1 ADC-8	Trastuzumab	ERBB2	Ln-D8	WO2022078260A1_ADC-8 linker	[109]
ADC Info	WO2022078260A1 ADC-9	Cetuximab	EGFR	Ln-D2	WO2022078260A1_ADC-9 linker	[109]
ADC Info	ZW-220	Fully humanized Anti-SLC34A2 IgG1 mAb	SLC34A2	ZD06519	Mc-Gly-Gly-Phe-Gly-AM	[110]
ADC Info	ZW-251	Humanized Anti-GPC3 IgG1 mAb	GPC3	ZD06519	Mc-Gly-Gly-Phe-Gly-AM	[111]

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Target Information

Citation

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)