Linker Information

General Information of This Linker
Linker ID
LIN0JDEBG
Linker Name
Oxime-PEG3
Linker Type
Uncleavable linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C7H17NO4
Isosmiles
NOCCOCCOCCOC
InChI
InChI=1S/C7H17NO4/c1-9-2-3-10-4-5-11-6-7-12-8/h2-8H2,1H3
InChIKey
UPZRLQLRXOQKOM-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
179.216
Polar area
62.94
Complexity
56.4385619
xlogp Value
-0.4437
Heavy Count
12
Rot Bonds
9
Hbond acc
5
Hbond Donor
1
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
ARX-517 [Phase 1]
 ADC Info 
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 NCT04662580  Clinical Status Phase 1/2
Clinical Description
A phase 1/2, multicenter, open-label, dose-escalation, and dose-expansion study to evaluate the safety, pharmacokinetics, and anti-tumor activity of ARX517, with randomized comparison to investigator's choice of treatment, in subjects with metastatic castration-resistant prostate cancer who are resistant or refractory to prior standard therapies.
Experiment 2 Reporting the Activity Date of This ADC [2]
Patients Enrolled
Major exclusions include recent chemotherapy/hormonal/radiation therapy (varies by cohort), prior taxanes or ARPIs (specific to cohorts), corticosteroid use (>10mg prednisone equivalent), active CNS metastases, other malignancies (last 2 years), QTc >480ms, lung disease (last 12 months), ocular disorders, grade ≥2 neuropathy, and proteinuria (>1g/24h). Seizure history disqualifies for apalutamide combination cohorts.

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Administration Dosage
ARX517 will be administered via intravenous (IV) infusion, with the initial treatment regimen by weight-based infusion at an interval of every 3 weeks. Other treatment regimen may be explored.
Related Clinical Trial
NCT Number NCT04662580  Clinical Status PHASE1
Clinical Description
A Phase 1, Multicenter, Open-Label, Dose-Escalation, and Dose-Expansion Study to Evaluate the Safety, Pharmacokinetics, and Anti-Tumor Activity of ARX517 as Monotherapy and in Combination With Androgen Receptor Pathway Inhibitors in Subjects With Metastatic Prostate Cancer
Primary Endpoint
The study will assess safety and tolerability of ARX517 (alone or combined with ARPIs) through adverse event incidence/severity (CTCAE v5) over 1.5 years, alongside pharmacokinetic parameters (AUC, Cmax, Ctrough) and immunogenicity (ADA incidence) over 3 years. Efficacy endpoints include overall survival (OS), PSA response rates (PSA30/50/90), and progression-free survival (PFS).

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Other Endpoint
Key inclusion criteria require males ≥18 with prostate adenocarcinoma, adequate LHRH therapy (testosterone ≤50ng/dL for mCRPC), prior treatments per cohort, documented progression (mCRPC) or high-volume metastases (mCSPC), and PSMA-positive lesions. Adequate hematologic/organ function and PSMA PET eligibility are mandatory.
References
Ref 1 A Phase 1/2, Multicenter, Open-label, Dose-escalation, and Dose-expansion Study to Evaluate the Safety, Pharmacokinetics, and Anti-tumor Activity of ARX517, With Randomized Comparison to Investigator's Choice of Treatment, in Subjects With Metastatic Castration-resistant Prostate Cancer Who Are Resistant or Refractory to Prior Standard Therapies, NCT04662580
Ref 2 ARX517/JNJ-95298177 as Monotherapy or Combination Therapy in Subjects With Metastatic Prostate Cancer