Payload Information

General Information of This Payload
Payload ID
PAY0EXXSU
Name
Differentiated TLR-9 agonist (T-CpG)
Synonyms
Differentiated TLR-9 agonist (T-CpG)
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Target Toll-like receptor 9 (TLR9)
 Target Info 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
TAC-001 [Phase 1/2]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Key inclusion: Histologically/cytologically confirmed solid tumors, ECOG PS 0-1, and adequate organ function
Administration Dosage
TAC-001 Single-Agent Dose-Escalation Cohorts
Related Clinical Trial
NCT Number NCT05399654  Phase Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2, Open Label, Dose Escalation and Expansion Study of TAC-001 in Patients With Select Advanced or Metastatic Solid Tumors
Primary Endpoint
Primary objectives include determining the RP2D of TAC-001 monotherapy in advanced/metastatic solid tumors [2 years], and evaluating preliminary efficacy through ORR (CR+PR), duration of response, and clinical benefit rate per RECIST 1.1/iRECIST [2 years].
Other Endpoint
Secondary endpoints assess safety (AE/SAE/irAE incidence via CTCAE v5.0 [2 years]), pharmacokinetics (Cmax, Tmax, AUC, half-life, clearance [2 years]), and immunogenicity (ADA incidence [2 years]).
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT05399654  Phase Status Phase 1/2
Clinical Description
A phase 1/2, open label, dose escalation and expansion study of TAC-001 in patients with select advanced or metastatic solid tumors.
Trastuzumab-MCC-CpG conjugate [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.27 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
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)
0.43 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model Esophageal adenocarcinoma OE19 cells CVCL_1622
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2 -)
Method Description
Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 A Dose Escalation and Expansion Study of TAC-001 in Patients With Select Advanced or Metastatic Solid Tumors
Ref 2 A Phase 1/2, Open Label, Dose Escalation and Expansion Study of TAC-001 in Patients With Select Advanced or Metastatic Solid Tumors, NCT05399654
Ref 3 Antibody conjugates for targeted delivery of Toll-like receptor 9 agonist to the tumor tissue. PLoS One. 2023 Mar 13;18(3):e0282831. doi: 10.1371/journal.pone.0282831. eCollection 2023.