Linker Information
General Information of This Linker
| Linker ID |
LIN0NGGBZ
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| Linker Name |
Mc-hydrazide linker
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Uncleavable
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| Structure |
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| Formula |
C13H19N3O4
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| Isosmiles |
CCC(NNC(CCCCCN1C(C=CC1=O)=O)=O)=O
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| InChI |
InChI=1S/C13H19N3O4/c1-2-10(17)14-15-11(18)6-4-3-5-9-16-12(19)7-8-13(16)20/h7-8H,2-6,9H2,1H3,(H,14,17)(H,15,18)
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| InChIKey |
CSPPELAPTMKZAF-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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281.312
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Polar area
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95.58
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Complexity
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387.7542476
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xlogp Value
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0.0292
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Heavy Count
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20
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Rot Bonds
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7
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Hbond acc
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4
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Hbond Donor
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2
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Lupartumab amadotin [Phase 1 (discontinued)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Inclusion requires age ≥18, ECOG 0-1, life expectancy ≥12 weeks, measurable advanced solid tumors (C4.4a+), and adequate organ function. Exclusion covers recent anticancer therapy (<4 weeks), active skin toxicity, psoriasis, unhealed wounds, serious cardiac/liver disease, CNS metastasis (unless stable >3 months), HIV/HBV/HCV, CKD (GFR <50), recent major surgery, pregnancy, or other high-risk conditions affecting compliance.
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| Administration Dosage |
Starting dose is 0.15mg/kg intravenous (I.V.) administration every 21 days.
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| Related Clinical Trial | |||||
| NCT Number | NCT02134197 | Clinical Status | PHASE1 | ||
| Clinical Description |
An Open-label Phase I Dose-escalation Study to Evaluate the Safety, Tolerability, Maximum Tolerated Dose, Pharmacokinetics, and Pharmacodynamics of the Anti-C4.4a Antibody Drug Conjugate BAY1129980 in Subjects With Advanced Solid Tumors Known to Express C4.4a
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| Primary Endpoint |
The study determines the maximum tolerated dose (MTD) of BAY1129980, defined as the highest dose with <20% DLT incidence during Cycle 1 or the maximum administered dose. Safety is assessed via adverse events (AE) monitoring over 2 years.
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| Other Endpoint |
Key evaluations include baseline C4.4a tumor expression via IHC, RECIST 1.1-assessed tumor response, BAY1129980 plasma concentration (AUC 0-tlast), and antidrug antibody titers over 2 years.
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