Linker Information

General Information of This Linker
Linker ID
LIN0GOSDZ
Linker Name
Tetraxetan
Linker Type
Chelating agent
Antibody-Linker Relation
Uncleavable
Structure
Formula
C16H28N4O8
Isosmiles
C1CN(CCN(CCN(CCN1CC(=O)O)CC(=O)O)CC(=O)O)CC(=O)O
PubChem CID
121841
InChI
InChI=1S/C16H28N4O8/c21-13(22)9-17-1-2-18(10-14(23)24)5-6-20(12-16(27)28)8-7-19(4-3-17)11-15(25)26/h1-12H2,(H,21,22)(H,23,24)(H,25,26)(H,27,28)
InChIKey
WDLRUFUQRNWCPK-UHFFFAOYSA-N
IUPAC Name
2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid
Pharmaceutical Properties
Molecule Weight
404.42
Polar area
162
Complexity
447
xlogp Value
-10.6
Heavy Count
28
Rot Bonds
8
Hbond acc
12
Hbond Donor
4
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Rosopatamab tetraxetan [Clinical candidate]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
9.38% (breast cancer)
0.00% (gastric cancer)
Patients Enrolled
Unresectable, locally advanced or metastatic breast cancer or gastric cancer refractory to standard therapy.
Administration Dosage
Intravenously over 60 to 90 minutes at 0.05, 0.10, 0.20, 0.30, 0.40, 0.50, 0.60, 0.75, or 0.90 mg/kg every 3 weeks.
Related Clinical Trial
NCT Number NCT02576548  Clinical Status Phase 1
Clinical Description
A phase 1/2 multicenter, open-label, dose-escalation, and dose-expansion study to evaluate the safety, pharmacokinetics, immunogencity, and antitumor activity of MEDI4276 in subjects with select HER2-expressing advanced solid tumors.
Primary Endpoint
In patients with breast cancer,ORR=9.38% (N=3/32),DOR=4.20-10.20 months. In the 0.05 to 0.40 mg/kg cohort,PFS=1.3-2.0 months. In the 0.50 to 0.75 mg/kg cohort,PFS=4.60-15.40 months. median overall survival (OS)=19.10 months (range 0.80-30.60, 95% CI 9.6-NA).
Other Endpoint
No objective responses in patients with gastric cancer,median PFS=1.80 months (range 0-10.7, 95% CI,1.3-3.0),median OS=6.50 months (range 2.80-16.30, 95% CI, 3.10-16.30).
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT00070837  Clinical Status Phase 1
Clinical Description
A phase 1/2 dose escalation trial of multiple doses of mLN2704 (DM1 conjugated monoclonal antibody mLN591) in subjects with metastatic androgen-independent prostate cancer.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT00052000  Clinical Status Phase 1
Clinical Description
Phase 1 dose-escalation study of intravenous CMD-193 in subjects with advanced malignant solid tumors.
References
Ref 1 First-in-Human, Phase 1 Dose-Escalation Study of Biparatopic Anti-HER2 Antibody-Drug Conjugate MEDI4276 in Patients with HER2-positive Advanced Breast or Gastric Cancer. Mol Cancer Ther. 2021 Aug;20(8):1442-1453.
Ref 2 Phase 1/2 multiple ascending dose trial of the prostate-specific membrane antigen-targeted antibody drug conjugate MLN2704 in metastatic castration-resistant prostate cancer. Urol Oncol. 2016 Dec;34(12):530.e15-530.e21.
Ref 3 A Trial of MLN2704 in Subjects With Metastatic Androgen Independent Prostate Cancer; NCT00052000

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