Linker Information

General Information of This Linker
Linker ID
LIN0PWYIO
Linker Name
DOTA-P-toluene isothiocyanate
Linker Type
Chelating agent
Antibody-Linker Relation
Uncleavable
Structure
Formula
C24H33N5O8S
Isosmiles
O=C(O)CN1CCN(CC(=O)O)CCN(CC(=O)O)C(Cc2ccc(N=C=S)cc2)CN(CC(=O)O)CC1
InChI
InChI=1S/C24H33N5O8S/c30-21(31)13-26-5-6-27(14-22(32)33)9-10-29(16-24(36)37)20(12-28(8-7-26)15-23(34)35)11-18-1-3-19(4-2-18)25-17-38/h1-4,20H,5-16H2,(H,30,31)(H,32,33)(H,34,35)(H,36,37)
InChIKey
UDOPJKHABYSVIX-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
551.622
Polar area
174.52
Complexity
38
xlogp Value
-0.108
Heavy Count
38
Rot Bonds
11
Hbond acc
10
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
Lintuzumab Ac-225 [Phase 2]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
67.00%
Patients Enrolled
Patients with more than 25% of leukemic blasts must have been CD33 positive by flow cytometry.
Administration Dosage
Induction consisted of G-CSF, 300 mg/d, given D1-6, cladribine 5 mg/m2, given D2-6, cytarabine 2 ug/m2, given D2-6, and mitoxantrone 10 mg/m2, given D2-4. Lintuzumab Ac225 was administered as a single dose on either day 7, 8, or 9 with a dose of 0.25 uCi/kg, 0.50 uCi/kg, or 0.75 uCi/kg.
Related Clinical Trial
NCT Number NCT03441048  Clinical Status Phase 1
Clinical Description
A phase 1 study of lintuzumab-Ac225 in combination with CLAG-M chemotherapy in patients with relapsed/refractory acute myeloid leukemia.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT03932318  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of venetoclax and azacitidine and lintuzumab-Ac225 in patients with refractory or relapsed AML.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT03867682  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of venetoclax and lintuzumab-Ac225 in patients with refractory or relapsed AML.
Experiment 4 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT02998047  Clinical Status Phase 1
Clinical Description
A phase 1 study of lintuzumab-Ac225 in patients with refractory multiple myeloma.
Experiment 5 Reporting the Activity Date of This ADC [5]
Related Clinical Trial
NCT Number NCT02575963  Clinical Status Phase 1
Clinical Description
A phase 1/2 study of lintuzumab-Ac225 in older patients with untreated acute myeloid leukemia.
References
Ref 1 TROPION-Lung02: Datopotamab deruxtecan (Dato-DXd) plus pembrolizumab (pembro) with or without platinum chemotherapy (Pt-CT) in advanced non-small cell lung cancer (aNSCLC). J Clin Oncol. 2023 41:16_suppl, 9004-9004.
Ref 2 A Phase I/II Study of Venetoclax and Azacitidine and Lintuzumab-Ac225 in Patients With Refractory or Relapsed AML, NCT03932318
Ref 3 A Phase I/II Study of Venetoclax and Lintuzumab-Ac225 in Patients With Refractory or Relapsed AML, NCT03867682
Ref 4 A Phase I Study of Lintuzumab-Ac225 in Patients With Refractory Multiple Myeloma, NCT02998047
Ref 5 A Phase I/II Study of Lintuzumab-Ac225 in Older Patients With Untreated Acute Myeloid Leukemia, NCT02575963

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