Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0NNKAQ
ADC Name
Ifinatamab deruxtecan
Synonyms
DS 7300; DS-7300; DS-7300a; DS7300
   Click to Show/Hide
Organization
Daiichi Sankyo Co., Ltd.
Drug Status
Phase 2
Indication
In total 5 Indication(s)
Non-small cell lung cancer [ICD11:2C25]
Phase 2
Small cell lung cancer [ICD11:2C25]
Phase 2
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 2
Esophageal squamous cell carcinoma [ICD11:2B71]
Phase 1
Hormone refractory prostate cancer [ICD11:2C82]
Phase 1
Drug-to-Antibody Ratio
6
Structure
Antibody Name
Ifinatamab
  Antibody Info 
Antigen Name
CD276 antigen (CD276)
  Antigen Info 
Payload Name
DX-8951 derivative (DXd)
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
Mc-Gly-Gly-Phe-Gly
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Deruxtecan
Puchem SID
461454123 , 472421681 , 476000798
ChEBI ID
CHEMBL5095331
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type NCT Number Clinical Status Clinical Trial Description
Undisclosed  NCT05280470
Phase 2
A phase 2, multicenter, randomized, open-label study of DS-7300a, a B7-H3 antibody drug conjugate (ADC), in subjects with pretreated extensive-stage small cell lung cancer (ES-SCLC).
Undisclosed  NCT04145622
Phase 1/2
Phase 1/2, two-part, multicenter first-in-human study of DS-7300a in subjects with advanced solid malignant tumors.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Small cell lung cancer PDX model (PDX: CTG-2093)
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.36
nM
MFE-280 cells
Endometrial adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.37
nM
Rh41 cells
Alveolar rhabdomyosarcoma
Half Maximal Inhibitory Concentration (IC50) 
0.55
nM
CCRF-CEM cells
T acute lymphoblastic leukemia
Undisclosed  . .
CCRF-CEM cells
T acute lymphoblastic leukemia
Full List of Activity Data of This Antibody-drug Conjugate
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]
Related Clinical Trial
NCT Number NCT05280470  Clinical Status Phase 2
Clinical Description A phase 2, multicenter, randomized, open-label study of DS-7300a, a B7-H3 antibody drug conjugate (ADC), in subjects with pretreated extensive-stage small cell lung cancer (ES-SCLC).
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT04145622  Clinical Status Phase 1/2
Clinical Description Phase 1/2, two-part, multicenter first-in-human study of DS-7300a in subjects with advanced solid malignant tumors.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 26) High CD276 expression (CD276+++)
Method Description
PDX studies CTG-2093, CTG-0166, CTG-0820, and CTG-1061 studies were performed by Champions Oncology, Inc. Models were established by inoculating tumor fragments derived from patients with small cell lung cancer (SCLC), nonsmall cell lung cancer (NSCLC), head and neck cancer, and bladder cancer, respectively, which were maintained in host mice, subcutaneously into female Hsd: Athymic Nude-Foxn1nu mice.Group assignment was carried out when the tumor volume reached approximately 100 to 300 mm3. The tumor-bearing mice were treated with DS-7300a or relevant controls intravenously on days 0 and 14.

   Click to Show/Hide
In Vivo Model Small cell lung cancer PDX model (PDX: CTG-2093)
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.36 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7304a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model Endometrial adenocarcinoma MFE-280 cells CVCL_1405
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.37 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7303a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model Alveolar rhabdomyosarcoma Rh41 cells CVCL_2176
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.55 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7302a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model T acute lymphoblastic leukemia CCRF-CEM cells CVCL_0207
Experiment 4 Reporting the Activity Date of This ADC [3]
Method Description
In vivo The target specificity and species cross-reactivity of DS-7300a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model T acute lymphoblastic leukemia CCRF-CEM cells CVCL_0207
References
Ref 1 A Phase 2, Multicenter, Randomized, Open-label Study of DS-7300a, a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC), NCT05280470
Ref 2 Phase I/II, Two-Part, Multicenter First-in-Human Study of DS-7300a in Subjects With Advanced Solid Malignant Tumors, NCT04145622
Ref 3 DS-7300a, a DNA Topoisomerase I Inhibitor, DXd-Based Antibody-Drug Conjugate Targeting B7-H3, Exerts Potent Antitumor Activities in Preclinical Models. Mol Cancer Ther. 2022 Apr 1;21(4):635-646.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.