Safety, Tolerability, and Pharmacodynamics of the ADAMTS‐5 Nanobody M6495: Two Phase 1, Single‐Center, Double‐Blind, Randomized, Placebo‐Controlled Studies in Healthy Subjects and Patients With Osteoarthritis.

Objective: To assess the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple injections of M6495, a disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS‐5) nanobody, in healthy volunteers and patients with osteoarthritis. Methods: Two randomized, placebo...

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Publicado en:ACR Open Rheumatology Vol. 6; no. 4; pp. 205 - 214
Autores principales: Bihlet, Asger Reinstrup, Balchen, Torben, Goteti, Kosalaram, Sonne, Jesper, Ladel, Christoph, Karsdal, Morten Asser, Ona, Victor, Moreau, Flavie, Waterhouse, Roseann, Bay‐Jensen, Anne‐Christine, Guehring, Hans
Formato: research tables/charts randomized controlled trial Journal Article
Publicado: Wiley-Blackwell Apr2024
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Apr2024
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        10.1002/acr2.11610
        176608721
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        atl: Safety, Tolerability, and Pharmacodynamics of the ADAMTS‐5 Nanobody M6495: Two Phase 1, Single‐Center, Double‐Blind, Randomized, Placebo‐Controlled Studies in Healthy Subjects and Patients With Osteoarthritis.
      aug:
        au:
          Bihlet, Asger Reinstrup
          Balchen, Torben
          Goteti, Kosalaram
          Sonne, Jesper
          Ladel, Christoph
          Karsdal, Morten Asser
          Ona, Victor
          Moreau, Flavie
          Waterhouse, Roseann
          Bay‐Jensen, Anne‐Christine
          Guehring, Hans
        affil: Nordic Bioscience Clinical Development, Herlev, Denmark
      sug:
        subj:
          Osteoarthritis Drug Therapy
          Immunoglobulins Administration and Dosage
          Immunoglobulins Pharmacodynamics
          Immunoglobulins Pharmacokinetics
          Patient Safety Evaluation
          Drug Tolerance Evaluation
          Antirheumatic Agents Therapeutic Use
          Injections
          Human
          Male
          Female
          Middle Age
          Aged
          Randomized Controlled Trials
          Double-Blind Studies
          Placebos
          Metalloproteins
          Clinical Assessment Tools
          Pain Measurement
          Adverse Drug Event
          Random Assignment
          Drug Monitoring
          Biological Markers Blood
          Biological Assay
          Descriptive Statistics
          Immune System
          Funding Source
          Middle Aged: 45-64 years
          Aged: 65+ years
          Male
          Female
      ab: Objective: To assess the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of single and multiple injections of M6495, a disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS‐5) nanobody, in healthy volunteers and patients with osteoarthritis. Methods: Two randomized, placebo‐controlled, double‐blind studies were performed. Study 1 enrolled 54 healthy male volunteers who received one subcutaneous (s.c.) injection of M6495 (1‐300 mg) or placebo (ratio 2:1), evaluating safety, PK, and PD as changes in the serum aggrecan fragment alanine‐arginine‐glycine‐serine (ARGS). Study 2 enrolled 32 patients with osteoarthritis with Kellgren–Lawrence grades 2 to 4 and pain greater than or equal to 40 on the Western Ontario and McMaster Universities Arthritis Index pain subscale at screening and evaluated the safety, PK, and PD of three doses every two weeks (75‐300 mg per dose) or six once‐weekly M6495 s.c. doses (300 mg) or placebo (ratio 3:1) over 106 days' follow‐up. Results: M6495 in single and multiple doses of less than or equal to 300 mg s.c. weekly was well tolerated with no clinically significant changes in any safety parameter. Adverse events more frequently reported in the M6495 groups were mostly mild cases of injection site reactions, myalgia, and nausea, which resolved after treatment cessation. The elimination half‐life of single s.c. doses of M6495 ranged from 79 to 267 hours. M6495 administration substantially reduced serum ARGS levels, indicative of target engagement and indicating disease‐modifying potential of M6495. Conclusion: Treatment with M6495 in single and multiple doses up to and including 300 mg s.c. was found to be well tolerated and adequately safe for further clinical evaluation of potential disease‐modifying effects.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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