Antibody ID	ANI0XJJLY
Antibody Name	Pertuzumab
Brand Name	PERJETA
Organization	Genentech, Inc.; Roche Holding AG
Indication	Ovarian cancer; Gastric cancer; Breast cancer; Prostate cancer
Approval Date	Jun. 2012
Synonyms	rhuMAB 2C4; PERTUZUMAB-ZZXF; RG-1273; RHUMAB 2C4; RHUMAB-2C4    Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)					Antigen Info
ChEMBI ID	CHEMBL2007641
PDB ID	1l7i , 1s78 , 4llu , 4llw , 4lly
DrugBank ID	DB06366
Drug Central ID	4957
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	EVQLVESGGGLVQPGGSLRLSCAASGFTFTDYTMDWVRQAPGKGLEWVADVNPNSGGSIY NQRFKGRFTLSVDRSKNTLYLQMNSLRAEDTAVYYCARNLGPSFYFDYWGQGTLVTVSSA STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ QGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Varible Domain	EVQLVESGGGLVQPGGSLRLSCAASGFTFTDYTMDWVRQAPGKGLEWVADVNPNSGGSIY NQRFKGRFTLSVDRSKNTLYLQMNSLRAEDTAVYYCARNLGPSFYFDYWGQGTLVTVSS     Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTH     Click to Show/Hide
Heavy Chain CDR 1	GFTFTDYT     Click to Show/Hide
Heavy Chain CDR 2	VNPNSGGS     Click to Show/Hide
Heavy Chain CDR 3	ARNLGPSFYFDY     Click to Show/Hide
Light Chain Sequence	DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQKPGKAPKLLIYSASYRYTGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQYYIYPYTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain Varible Domain	DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQKPGKAPKLLIYSASYRYTGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQYYIYPYTFGQGTKVEIK     Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain CDR 1	QDVSIG     Click to Show/Hide
Light Chain CDR 2	SAS     Click to Show/Hide
Light Chain CDR 3	QQYYIYPYT     Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	7.10%
Patients Enrolled	Patients have HER2-expressing or amplified solid tumors.
Administration Dosage	0.60 mg/kg administered Q2 weeks.
Related Clinical Trial
NCT Number	NCT04460456	Clinical Status	Phase 1
Clinical Description	A phase 1/1b, open-label, dose escalation and expansion study of SBT6050 alone and in combination with PD-1 inhibitors in subjects with advanced solid tumors expressing HER2.
Experiment 2 Reporting the Activity Date of This ADC					[2]
Related Clinical Trial
NCT Number	NCT05091528	Clinical Status	Phase 1
Clinical Description	An open-label, phase 1/2, dose-escalation and expansion study of SBT6050 combined with other HER2-directed therapies in subjects with pretreated unresectable locally advanced and/or metastatic HER2-expressing or HER2-amplified cancers.

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 30)	High HER2 expression (HER2+++)
Method Description	BT474 human breast carcinomas fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); pertuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.00% (Day 22)	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 3 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.00% (Day 22)	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 10 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.19 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Adult hepatocellular carcinoma	SNU-182 cells		CVCL_0090
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.20% (Day 22)	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (XI) conjugate at 3 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.40% (Day 22)	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (XI) conjugate at 10 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.50 pM	High HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57.00 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 5 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric carcinoma	NCC-StC-K140 cells		CVCL_3055
Experiment 7 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.58 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC202 cells		CVCL_2062
Experiment 8 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.82 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma of no special type	UACC-812 cells		CVCL_1781
Experiment 9 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.86 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 10 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.99 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 11 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.11 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1419 cells		CVCL_1251
Experiment 12 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC2218 cells		CVCL_1263
Experiment 13 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast carcinoma	MDA-MB-175-VII cells		CVCL_1400
Experiment 14 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.69 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074
Experiment 15 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.59 nM	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 16 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.40 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC2157 cells		CVCL_1261
Experiment 17 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.72 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.26 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.51 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.95 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Ref 1	A Phase I Pharmacokinetic (PK) and Safety Study of Trph-222 in Patients with Relapsed/Refractory B-Cell Non-Hodgkin Lymphoma (R/R NHL): Dose-Escalation Results. 2020 Dec 7.
Ref 2	An Open-label, Phase 1/2, Dose-escalation and Expansion Study of SBT6050 Combined With Other HER2-directed Therapies in Subjects With Pretreated Unresectable Locally Advanced and/or Metastatic HER2-expressing or HER2-amplified Cancers, NCT05091528
Ref 3	Neodegrader conjugates; 2021-10-07.
Ref 4	Linkers for use in antibody drug conjugates; 2023-03-16.
Ref 5	Ligand-drug conjugate of exatecan analogue, preparation method therefor and application thereof; 2020-04-02.