Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TIZXC
ADC Name
A-166
Synonyms
A 166; KL-A166
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Organization
Sichuan Kelun Pharmaceutical Co., Ltd.; Fudan University; KLUS Pharma, Inc.; Levena Biopharma US, Inc.
Drug Status
NDA
Indication
In total 26 Indication(s)
HER2(+) breast cancer [ICD11:2C60-2C65]
NDA
Bladder cancer [ICD11:2C94]
Phase 2
Cervical cancer [ICD11:2C77]
Phase 2
Colon cancer [ICD11:2B90]
Phase 2
Gastric cancer [ICD11:2B72]
Phase 2
Head and neck squamous carcinoma [ICD11:2C31]
Phase 2
Hepatocellular carcinoma [ICD11:2C12]
Phase 2
HER2(+) colorectal cancer [ICD11:2B91]
Phase 2
Intrahepatic bile ducts cancer [ICD11:2C12]
Phase 2
Laryngeal cancer [ICD11:2C23]
Phase 2
Lip cancer [ICD11:2B6E]
Phase 2
Lung cancer [ICD11:2C25]
Phase 2
Malignant neoplasms of tonsil [ICD11:2B69]
Phase 2
Mucoepidermoid carcinoma [ICD11:2B6D]
Phase 2
Ovarian cancer [ICD11:2C73]
Phase 2
Pancreatic cancer [ICD11:2C10]
Phase 2
Prostate cancer [ICD11:2C82]
Phase 2
Rectal cancer [ICD11:2B92]
Phase 2
Renal cell carcinoma [ICD11:2C90]
Phase 2
Salivary gland tumor [ICD11:2E91]
Phase 2
Skin cancer [ICD11:2C30-2C37]
Phase 2
Tongue cancer [ICD11:2B62]
Phase 2
Gastroesophageal junction cancer [ICD11:2B71]
Phase 1
HER2(+) gastric cancer [ICD11:2B72]
Phase 1
Non-small cell lung cancer [ICD11:2C25]
Phase 1
Urothelial cancer [ICD11:2C9Z]
Phase 1
Drug-to-Antibody Ratio
2
Structure
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Duostatin 5
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
K-lock-Val-Cit-PABC
  Linker Info 
Conjugate Type
Site-specific conjugation through special chemical environment nucleophilic lysines.
Puchem SID
478838279 , 472221605
Drugbank ID
DB17413
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Partial Response (PR)  NCT03602079
Phase 1
A phase 1-2, FIH Study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.

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Objective Response Rate (ORR)  NCT05311397
Phase 1
A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of A166 in patients with unresectable, locally advanced or metastatic HER2-expressing solid tumors (KL166-I-01-CTP).

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Undisclosed  NCT05346328
Phase 2
An open-clinical trial phase , injection of A166 for HER2-positive patients with refractory unresectable locally advanced or metastatic breast cancer KL166-2S-001.
Undisclosed  NCT03602079
Phase 1/2
A phase 1-2, FIH study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.

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Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Partial Response (PR)
25.92%
Patients Enrolled
Locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified.
Administration Dosage
0.30, 1.20, 3.60, 4.80 mg/kg, every 3 weeks from date of enrollment until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 24 months.
Related Clinical Trial
NCT Number NCT03602079  Clinical Status Phase 1
Clinical Description A phase 1-2, FIH Study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.
Primary Endpoint
Overall incidence of ophthalmic toxicities in the 3.60 mg/kg cohort was 80% and in the 4.80 mg/kg cohort it was 83.00%. Responses were seen only at the dose levels of 3.60 mg/kg and 4.80 mg/kg. Among the 27 patients evaluable for efficacy,best response was progression of disease in 11 patients (40.74%), stable disease in 9 patients (33.33%) and partial response in 7 patients (25.92%),for the total disease control rate of 59%.

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Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
73.90% (4.8 mg/kg)
68.60% (6.0 mg/kg)
Patients Enrolled
Patients with HER2-expressing advanced solid tumours.
Administration Dosage
0.10, 0.30, 0.60, 1.20, 2.40, 3.60, 4.80 or 6.00 mg/kg Q3W.
Related Clinical Trial
NCT Number NCT05311397  Clinical Status Phase 1
Clinical Description A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of A166 in patients with unresectable, locally advanced or metastatic HER2-expressing solid tumors (KL166-I-01-CTP).
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT05346328  Clinical Status Phase 2
Clinical Description An open-clinical trial phase , injection of A166 for HER2-positive patients with refractory unresectable locally advanced or metastatic breast cancer KL166-2S-001.
Experiment 4 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT03602079  Clinical Status Phase 1/2
Clinical Description A phase 1-2, FIH study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.
References
Ref 1 A first in-human study of A166 in patients with locally advanced/metastatic solid tumors which are HER2-positive or HER2-amplified who did not respond or stopped responding to approved therapies. Journal of Clinical Oncology 38, no. 15_suppl (May 20, 2020) 1049-1049.
Ref 2 Phase I study of A166, an antibodydrug conjugate in advanced HER2-expressing solid tumours. NPJ Breast Cancer. 2023 Apr 18;9(1):28. doi: 10.1038/s41523-023-00522-5.
Ref 3 An Open-clinical Trial Phase , Injection of A166 for HER2-positive Patients With Refractory Unresectable Locally Advanced or Metastatic Breast CancerKL166-IIS-001, NCT05346328
Ref 4 A Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies, NCT03602079

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