Antibody Information

General Information of This Antibody

Antibody ID	ANI0WHSDZ
Antibody Name	Telisotuzumab
Organization	AbbVie, Inc.; Pierre Fabre SA
Indication	Solid tumors
Synonyms	ABT-700; hz224G11 Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Hepatocyte growth factor receptor (MET)	Antigen Info
ChEMBI ID	CHEMBL3545419
DrugBank ID	DB14838
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	QVQLVQSGAEVKKPGASVKVSCKASGYIFTAYTMHWVRQAPGQGLEWMGWIKPNNGLANY AQKFQGRVTMTRDTSISTAYMELSRLRSDDTAVYYCARSEITTEFDYWGQGTLVTVSSAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDCHCPPCPAPELLGGPSVF LFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYR VVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKN QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGN VFSCSVMHEALHNHYTQKSLSLSPG Click to Show/Hide
Heavy Chain Varible Domain	QVQLVQSGAEVKKPGASVKVSCKASGYIFTAYTMHWVRQAPGQGLEWMGWIKPNNGLANY AQKFQGRVTMTRDTSISTAYMELSRLRSDDTAVYYCARSEITTEFDYWGQGTLVTVSS Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV Click to Show/Hide
Heavy Chain Constant Domain 2	APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK Click to Show/Hide
Heavy Chain Constant Domain 3	GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG Click to Show/Hide
Heavy Chain Hinge Region	EPKSCDCHCPPCP Click to Show/Hide
Heavy Chain CDR 1	GYIFTAYT Click to Show/Hide
Heavy Chain CDR 2	IKPNNGLA Click to Show/Hide
Heavy Chain CDR 3	ARSEITTEFDY Click to Show/Hide
Light Chain Sequence	DIVMTQSPDSLAVSLGERATINCKSSESVDSYANSFLHWYQQKPGQPPKLLIYRASTRES GVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQSKEDPLTFGGGTKVEIKRTVAAPSVF IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
Light Chain Varible Domain	DIVMTQSPDSLAVSLGERATINCKSSESVDSYANSFLHWYQQKPGQPPKLLIYRASTRES GVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQSKEDPLTFGGGTKVEIK Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
Light Chain CDR 1	ESVDSYANSF Click to Show/Hide
Light Chain CDR 2	RAS Click to Show/Hide
Light Chain CDR 3	QQSKEDPLT Click to Show/Hide

Each Antibody-drug Conjugate Related to This Antibody

Full Information of The Activity Data of The ADC(s) Related to This Antibody

Telisotuzumab vedotin [Phase 3]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 12 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Objective Response Rate (ORR)	7.40%
Patients Enrolled	Advanced non-small cell lung cancer (NSCLC).
Administration Dosage	Teliso-V Q2W (1.60, 1.90, or 2.20 mg/kg, intravenous) with nivolumab (3 mg/kg, or 240 mg, or per locally approved label, intravenously).
*Related Clinical Trial*
NCT Number	NCT02099058	Clinical Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Most patients (97.30%, n=36) experienced one or more TEAE, with 23 (62.16%) reporting TEAEs grades 3 or higher. TEAEs considered possibly related to Teliso-V were reported in 78.38% (n=29) of patients; 32.43% (n=12) were grade greater than or equal to 3.
Other Endpoint	Combination therapy with Teliso-V plus nivolumab was well tolerated in patients with c-Met-+NSCLC with limited antitumor activity. The ORR was 7.40% (95% CI: 0.90-24.30), with two patients (PD-L1+, n =1; PD-L1-, n=1) having a confirmed PR.Overall, 66.67% of patients (16 of 24) had evidence of tumor size reduction; three (12.5%) reported a greater than 30% reduction in target lesion. The overall median PFS (95% CI) was 7.20 months (3.30-8.90); 7.20 months(1.50-not reached [NR]) for PD-L1 patients, 4.50 months(1.50-NR) for PD-L1- patients, and NR (2.00-NR) for PD-L1-unk patients. The objective response rate was 7.40%, with two patients having a confirmed partial response. Overall median progression-free survival was 7.20 months. Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Objective Response Rate (ORR)	23.00% (all) 28.00% (in once every 2 weeks cohorts all) 18.00% (in once every 3 weeks cohorts) 18.00% (nonsquamous NSCLC) 31.00% (in once every 2 weeks cohorts nonsquamous NSCLC) 6.00% (in once every 3 weeks cohorts nonsquamous NSCLC) 43.00% (squamous NSCLC)
Patients Enrolled	Non-small cell lung cancer (NSCLC) and c-Met H-score 150 (c-Met+) or MET amplification/exon 14 skipping mutations.
Administration Dosage	Intravenously once every 3 weeks (0.15-3.30 mg/kg) or once every 2 weeks (1.60-2.20 mg/kg).
*Related Clinical Trial*
NCT Number	NCT02099058	Clinical Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Four objective responses (ORR = 26.70%; 95% CI, 7.80-55.10) were observed in this subgroup, 3 in once every 2 weeks (ORR = 43.00%; 95% CI, 9.90-81.60), and 1 in once every 3 weeks (ORR = 13.00%; 95% CI, 0.30-52.70).
Other Endpoint	The median PFS in once every 2 weeks cohorts was 8.00 months (range, 1.20-9.10) and the median treatment duration was 19.60 weeks (range, 0.10-60.10).
Experiment 3 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Objective Response Rate (ORR)	30.55% (for all efficacy-evaluable patients) 32.10% (for EGFR-M+ patients) 52.60% (of EGFR-M+ patients, those who were c-Met high)
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
*Related Clinical Trial*
NCT Number	NCT02099058	Clinical Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	OrR for all efficacy-evaluable patients was 30.55% (11/36; 95% CI, 16.30 to 48.10), and DCR was 86.11% (31/36; 95% CI, 70.5 to 95.3). Median PFS for all efficacy-evaluable patients was 5.90 months (95% CI, 2.80 to not reached [NR]).
Other Endpoint	For EGFR-M+ patients (n = 28), ORR was 32.14% (9/28; 95% CI, 15.90 to 52.40), with one CR (3.57%) and eight PR (28.57%). DCR was 85.71% (24/28; 95% CI, 67.30 to 96.00) and median PFS was 5.90 months (95% CI, 2.80 to NR). Median PFS was 3.70 months (95% CI, 1.40 to NR) for T790M+ patients, compared with 6.80 months (95% CI, 4.30 to NR) for non-T790M+ patients. Of EGFR-M+ patients, those who were c-Met high (n = 15) had an ORR of 52.60%. Median PFS was 6.80 months for non-T790M+ and for those whose T790M status was unknown, versus 3.70 months for T790M+. Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Objective Response Rate (ORR)	30.60% (for all efficacy-evaluable patients) 32.18% (for EGFR-M+ patients) 52.60% (of EGFR-M+ patients, those who were c-Met high)
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
*Related Clinical Trial*
NCT Number	NCT02099058	Clinical Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Median PFS=5.90 months (95% CI, 2.80 to not reached). ORR for EGFR-M+ patients = 32.18% (n=28). EGFR-M+ patients ORR = 52.60%.
Other Endpoint	Median PFS=6.80 months for non-T790M+.
Experiment 5 Reporting the Activity Date of This ADC				[4]
Efficacy Data	Objective Response Rate (ORR)	71.70% (plus lenalidomide) 70.60% (plus pomalidomide)
Patients Enrolled	Relapsed or refractory multiple myeloma, and ECOG performance status or Zubrod score of 2 or below, received indatuximab ravtansine with lenalidomide and dexamethasone (indatuximab ravtansine plus lenalidomide) had failure of at least one previous therapy.
Administration Dosage	Intravenously on days 1, 8, and 15 of each 28-day cycle in dose of 100 mg/m² plus lenalidomide or pomalidomide and dexamethasone.
*Related Clinical Trial*
NCT Number	NCT01638936	Clinical Status	Phase 1
Clinical Description	A phase 1/2a multi-dose escalation study of BT062 in combination with lenalidomide or pomalidomide and dexamethasone in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 6 Reporting the Activity Date of This ADC				[5]
Efficacy Data	Objective Response Rate (ORR)	75.00%
Patients Enrolled	MA advanced GEC.
Administration Dosage	15 mg/kg IV, once every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT01472016	Clinical Status	Phase 1
Clinical Description	A multi-center, phase 1/1b, open-label, dose escalation study of ABT-700, a monoclonal antibody in subjects with advanced solid tumors.
Primary Endpoint	Among these patients, three achieved a partial response and one had progressive disease as best response (ORR=75.00%). The duration of disease control in responders ranged from 18-27 weeks and the median duration of response was 16.10 weeks. The median progression- free survival in MET-amplified patients was 17.90 weeks.
Experiment 7 Reporting the Activity Date of This ADC				[6]
*Related Clinical Trial*
NCT Number	NCT01915472	Clinical Status	Phase 2
Clinical Description	A phase 2 study of IMMU 130 (hmn-14-SN38 antibody drug conjugate) in patients with metastatic colorectal cancer.
Experiment 8 Reporting the Activity Date of This ADC				[7]
*Related Clinical Trial*
NCT Number	NCT01001442	Clinical Status	Phase 1/2
Clinical Description	A phase 1/2a multi-dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), safety and efficacy of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 9 Reporting the Activity Date of This ADC				[8]
Patients Enrolled	Nonsmall-cell lung cancer (NSCLC) with c-Metoverexpressing tumors (c-Met positive; immunohistochemistry membrane H-score 150).
Administration Dosage	Teliso-V was administered by intravenous (IV) infusion to groups of three to six patients who were enrolled in eight-dose cohorts for dosing at 0.15 to 3.30 mg/kg on day 1, once every 21 days, or until disease progression or unacceptable toxicity.
*Related Clinical Trial*
NCT Number	NCT02099058	Clinical Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	No formal MTD was identified.
Experiment 10 Reporting the Activity Date of This ADC				[9]
*Related Clinical Trial*
NCT Number	NCT01605318	Clinical Status	Phase 1
Clinical Description	A phase 1/2 study of once or twice weekly IMMU-130 (hMN-14-SN38, antibody-drug conjugate) in patients with colorectal cancer.
Experiment 11 Reporting the Activity Date of This ADC				[10]
*Related Clinical Trial*
NCT Number	NCT01270698	Clinical Status	Phase 1
Clinical Description	A phase 1 study of IMMU-130 (hmn-14-SN38 antibody drug conjugate) in patients with colorectal cancer.
Experiment 12 Reporting the Activity Date of This ADC				[11]
*Related Clinical Trial*
NCT Number	NCT00723359	Clinical Status	Phase 1
Clinical Description	A phase 1 dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), and safety of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.

ABT-700 (S238C)-PBD [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	70.68% (Day 36)	Low MET expression (MET+; IHC 1+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0363)
Experiment 2 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.79% (Day 22)	High MET expression (MET+++; IHC 3+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0170)
Experiment 3 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.94% (Day 21)	Moderate MET expression (MET++; IHC 2+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0159)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.94% (Day 32)	Positive MET expression (MET +++/++)
Method Description	Mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype or ADC at 0.3 mg/kg intraperitoneally.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724

Revealed Based on the Cell Line Data

Click To Hide/Show 52 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SK-CO-1 cells		CVCL_0626
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-138MG cells		CVCL_0020
Experiment 4 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 5 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059K cells		CVCL_0401
Experiment 6 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Anaplastic astrocytoma	DBTRG-05MG cells		CVCL_1169
Experiment 7 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.90 pM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	HCC15 cells		CVCL_2057
Experiment 9 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	DLD-1 cells		CVCL_0248
Experiment 10 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 11 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 12 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 13 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gliosarcoma	SF264 cells		Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW403 cells		CVCL_0545
Experiment 15 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	SNB-19 cells		CVCL_0535
Experiment 16 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 201 cells		CVCL_1987
Experiment 17 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 7.00 pM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 18 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 19 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	RKO cells		CVCL_0504
Experiment 20 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Rectal adenocarcinoma	SW1463 cells		CVCL_1718
Experiment 21 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760
Experiment 22 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gastric adenocarcinoma	Hs 746.T cells		CVCL_0333
Experiment 23 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 24 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Pancreatic carcinoma	KP-4 cells		CVCL_1338
Experiment 25 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H820 cells		CVCL_1592
Experiment 26 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	SW900 cells		CVCL_1731
Experiment 27 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 28 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 320DM cells		CVCL_0219
Experiment 29 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW1116 cells		CVCL_0544
Experiment 30 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 31 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Cecum adenocarcinoma	LS1034 cells		CVCL_1382
Experiment 32 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	COLO 320HSR cells		CVCL_0220
Experiment 33 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Gliosarcoma	SF539 cells		CVCL_1691
Experiment 34 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	NCI-H1573 cells		CVCL_1478
Experiment 35 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 36 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High MET expression (MET+++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 37 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 38 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 39 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	T84 cells		CVCL_0555
Experiment 40 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 41 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Astrocytoma	U-118MG cells		CVCL_0633
Experiment 42 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Low MET expression (MET+)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 43 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 44 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 45 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Anaplastic astrocytoma	CHLA-03-AA cells		CVCL_U616
Experiment 46 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.45 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Primitive neuroectodermal tumor	PFSK-1 cells		CVCL_1642
Experiment 47 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 48 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.20 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	SNB-75 cells		CVCL_1706
Experiment 49 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	Caco-2 cells		CVCL_0025
Experiment 50 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292
Experiment 51 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67.00 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	A-172 cells		CVCL_0131
Experiment 52 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	141 nM	Positive MET expression (MET +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556

References

Ref 1	A Phase 1b Study of Telisotuzumab Vedotin in Combination With Nivolumab in Patients With NSCLC. JTO Clin Res Rep. 2021 Dec 4;3(1):100262.
Ref 2	Phase I Study of 2- or 3-Week Dosing of Telisotuzumab Vedotin, an Antibody-Drug Conjugate Targeting c-Met, Monotherapy in Patients with Advanced Non-Small Cell Lung Carcinoma. Clin Cancer Res. 2021 Nov 1;27(21):5781-5792.
Ref 3	Phase Ib Study of Telisotuzumab Vedotin in Combination With Erlotinib in Patients With c-Met Protein-Expressing Non-Small-Cell Lung Cancer. J Clin Oncol. 2023 Feb 10;41(5):1105-1115.
Ref 4	Indatuximab ravtansine plus dexamethasone with lenalidomide or pomalidomide in relapsed or refractory multiple myeloma: a multicentre, phase 1/2a study. Lancet Haematol. 2021 Nov;8(11):e794-e807.
Ref 5	Phase I study of ABT-700, an anti-c-Met antibody, in patients (pts) with advanced gastric or esophageal cancer (GEC). Journal of Clinical Oncology 33, no. 3_suppl (January 20, 2015) 167-167.
Ref 6	A Phase II Study of IMMU 130 (hMN-14-SN38 Antibody Drug Conjugate) in Patients With Metastatic Colorectal Cancer, NCT01915472
Ref 7	A Phase I/IIa Multi-Dose Escalation Study to Evaluate Maximum Tolerated Dose (MTD), Pharmacokinetics (PK), Safety and Efficacy of BT062 in Subjects With Relapsed or Relapsed/Refractory Multiple Myeloma, NCT01001442
Ref 8	First-in-Human Phase I, Dose-Escalation and -Expansion Study of Telisotuzumab Vedotin, an Antibody-Drug Conjugate Targeting c-Met, in Patients With Advanced Solid Tumors. J Clin Oncol. 2018 Nov 20;36(33):3298-3306.
Ref 9	A Phase I/II Study of Once or Twice Weekly IMMU-130 (hMN-14-SN38, Antibody-Drug Conjugate) in Patients With Colorectal Cancer. NCT01605318
Ref 10	A Phase I Study of IMMU-130 (hMN-14-SN38 Antibody Drug Conjugate) in Patients With Colorectal Cancer. NCT01270698
Ref 11	A Phase I Dose Escalation Study to Evaluate Maximum Tolerated Dose (MTD), Pharmacokinetics (PK), and Safety of BT062 in Subjects With Relapsed or Relapsed/Refractory Multiple Myeloma, NCT00723359
Ref 12	ANTI-cMet antibody drug conjugates and methods for their use; 2017-11-23.

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

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

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