Linker Information
General Information of This Linker
| Linker ID |
LIN0OUTRX
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| Linker Name |
Formyl-Gly-Glu
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| Linker Type |
Flexible reactive (thiol) linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C9H13BrN2O6
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| Isosmiles |
O=C(O)CCC(NC(=O)CNC(=O)CBr)C(=O)O
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| InChI |
InChI=1S/C9H13BrN2O6/c10-3-6(13)11-4-7(14)12-5(9(17)18)1-2-8(15)16/h5H,1-4H2,(H,11,13)(H,12,14)(H,15,16)(H,17,18)
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| InChIKey |
LLODMEXPRFSSOV-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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325.115
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Polar area
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132.8
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Complexity
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18
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xlogp Value
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-1.0683
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Heavy Count
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18
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Rot Bonds
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8
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Hbond acc
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4
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Hbond Donor
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4
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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
ABBV-154 [Phase 2 (discontinued)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Eligible participants must have a BMI between 18.0 and 29.9 kg/m2. Key exclusions include use of medications/supplements within 2 weeks (or 5 half-lives), prior exposure to similar biologic therapies, and history of significant medical conditions (e.g., epilepsy, cardiac/respiratory/neurologic disorders, or uncontrolled illnesses).
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| Related Clinical Trial | |||||
| NCT Number | NCT05556226 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1 Study in Healthy Subjects to Evaluate the Relative Bioavailability of ABBV-154
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| Primary Endpoint |
This study evaluates the pharmacokinetic profile of the investigational drug over approximately 58 days, measuring key parameters including Cmax, Tmax, terminal elimination rate constant (beta), half-life (t1/2), and AUC values (AUCt and AUC∞). Safety is assessed through adverse event monitoring for approximately 72 days, with investigators determining causality between reported AEs and study treatment.
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| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Patients Enrolled |
Comprehensive efficacy assessments focused on joint count improvements, composite disease activity scores, and patient-reported outcomes to evaluate treatment response, disease control, and functional status in this biologic-refractory RA population.
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| Related Clinical Trial | |||||
| NCT Number | NCT04888585 | Clinical Status | PHASE2 | ||
| Clinical Description |
A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of ABBV-154 in Subjects With Moderately to Severely Active Rheumatoid Arthritis With Inadequate Response to Biologic and/or Targeted Synthetic Disease-Modifying Anti-Rheumatic Drugs (b/tsDMARDs)
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| Primary Endpoint |
The primary endpoint was achieving ACR50 response at Week 12, defined as ≥50% improvement in tender/swollen joint counts and ≥50% improvement in 3 of 5 additional measures including physician/patient global assessments, pain score, HAQ-DI, and hsCRP. Secondary endpoints included changes in DAS28 and CDAI scores, with lower scores indicating improvement, as well as ACR20/70 responses, low disease activity (DAS28 ≤3.2 or CDAI ≤10), clinical remission (DAS28 <2.6 or CDAI ≤2.8), and HAQ-DI improvement from baseline.
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| Other Endpoint |
Key inclusion criteria required confirmed RA diagnosis per 2010 ACR/EULAR criteria with ≥6 swollen/tender joints at baseline, inadequate response to prior biologics/tsDMARDs, and stable MTX dose. Exclusion criteria included prior discontinuation of adalimumab due to intolerance/toxicity.
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| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Patients Enrolled |
The study evaluated disease stability under glucocorticoid tapering by measuring flare events, steroid exposure reduction, and sustained remission in this recurrent PMR population.
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| Related Clinical Trial | |||||
| NCT Number | NCT04972968 | Clinical Status | PHASE2 | ||
| Clinical Description |
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Dose-Ranging Study to Evaluate the Safety and Efficacy of ABBV-154 in Subjects With Polymyalgia Rheumatica (PMR) Dependent on Glucocorticoid Treatment
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| Primary Endpoint |
The primary endpoint was time to PMR flare (requiring glucocorticoid dose increase) from first dose through Week 52. Secondary endpoints included flare-free status rates, cumulative glucocorticoid dose, and dose changes from baseline by Week 24.
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| Other Endpoint |
Eligible participants required confirmed PMR diagnosis per 2012 EULAR/ACR criteria with ≥2 prior flares, stable prednisone use, and willingness to follow protocol tapering. Key exclusions included prior TNF antagonist treatment or concurrent immunomodulators beyond prednisone/hydroxychloroquine.
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| Experiment 4 Reporting the Activity Date of This ADC | [4] | ||||
| Patients Enrolled |
The study aimed to demonstrate mucosal healing and sustained clinical remission in moderate-to-severe CD patients refractory to multiple biologics, using comprehensive endoscopic and symptom-based assessments.
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| Related Clinical Trial | |||||
| NCT Number | NCT05068284 | Clinical Status | PHASE2 | ||
| Clinical Description |
A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of ABBV-154 in Subjects With Moderately to Severely Active Crohn's Disease (CD): AIM-CD
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| Primary Endpoint |
The primary endpoint was endoscopic response (SES-CD reduction >50% or ≥2-point decrease in isolated ileal disease) at Week 12. Secondary endoscopic and clinical endpoints included SES-CD response at Week 40 and clinical remission (CDAI <150 or stool frequency/abdominal pain criteria) at Weeks 12 and 40.
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| Other Endpoint |
Eligible participants required confirmed CD diagnosis ≥3 months, CDAI 220-450, and SES-CD ≥6 (≥4 for isolated ileal disease), with prior biologic failure/intolerance. Key exclusion was prior adalimumab intolerance.
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| Experiment 5 Reporting the Activity Date of This ADC | [5] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04888585 | Clinical Status | Phase 2 | ||
| Clinical Description |
A randomized, double-blind, placebo-controlled study to evaluate the safety and efficacy of ABBV-154 in subjects with moderately to severely active rheumatoid arthritis with inadequate response to biologic and/or targeted synthetic disease-modifying anti-rheumatic drugs (b/tsdmards).
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| Experiment 6 Reporting the Activity Date of This ADC | [6] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04972968 | Clinical Status | Phase 2 | ||
| Clinical Description |
A phase 2, randomized, double-blind, placebo-controlled, dose-ranging study to evaluate the safety and efficacy of ABBV-154 in subjects with polymyalgia rheumatica (PMR) dependent on glucocorticoid treatment.
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| Experiment 7 Reporting the Activity Date of This ADC | [7] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05068284 | Clinical Status | Phase 2 | ||
| Clinical Description |
A randomized, double-blind, placebo-controlled study to evaluate the safety and efficacy of ABBV-154 in subjects with moderately to severely active crohn's disease (CD): aim-cd.
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| Experiment 8 Reporting the Activity Date of This ADC | [8] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05556226 | Clinical Status | Phase 1 | ||
| Clinical Description |
A phase 1 study in healthy subjects to evaluate the relative bioavailability of ABBV-154.
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References