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Background <p>Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by synovial inflammation and joint damage. Over the past two decades, treatment has expanded from conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) to include biologic (bDMARDs) and targeted synthetic DMARDs (tsDMARDs). Despite differences in structure and mechanism, these therapies also exhibit distinct pharmacokinetic (PK) properties that directly affect personalized clinical use.</p> Area covered <p>This review aims to systematically compare the analysis of absorption, distribution, metabolism, and excretion (ADME) profiles of small-molecule drugs and biologics used in RA. The PK profiles of key agents—including methotrexate, Janus kinase inhibitors, tumor necrosis factor inhibitors, interleukin-6 blockers, and co-stimulatory modulators—were discussed, and these parameters (e.g. time to reach maximum plasma or serum concentration, volume of distribution, clearance, half-life) were linked to clinical decisions. The review also explored immunogenicity concerns associated with biologics, the role of anti-drug antibodies, and therapeutic drug monitoring. Finally, we presented a patient-centered treatment matrix that aligns PK properties with individual patient scenarios and discussed future directions, including biosimilar development, low-molecular-weight biologics, and artificial intelligence-based PK modeling platforms.</p> Expert opinion <p>PK is a powerful yet underutilized tool for individualizing RA treatment. Differences in ADME properties between small molecules and biologics affect dosing flexibility, adherence, monitoring, and safety, especially in complex cases such as organ dysfunction, pregnancy, or immunocompromised states. As new therapies emerge and healthcare advances toward precision medicine, integrating PK-based insights into clinical algorithms will be critical for optimizing therapeutic outcomes and formulation development. Linking mechanistic understanding with real-world PK is the next frontier in rational RA drug selection and optimization.</p>

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Pharmacokinetic distinctions between small molecules and biologics in treating rheumatoid arthritis: implications for personalized therapeutic strategies and formulation development

  • 期刊论文

  • 发表日期：

    2025年10月23日

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  • Seung-Hyun Jeong,
  • Ji-Hun Jang,
  • Yong-Bok Lee

摘要

Background

Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by synovial inflammation and joint damage. Over the past two decades, treatment has expanded from conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) to include biologic (bDMARDs) and targeted synthetic DMARDs (tsDMARDs). Despite differences in structure and mechanism, these therapies also exhibit distinct pharmacokinetic (PK) properties that directly affect personalized clinical use.

Area covered

This review aims to systematically compare the analysis of absorption, distribution, metabolism, and excretion (ADME) profiles of small-molecule drugs and biologics used in RA. The PK profiles of key agents—including methotrexate, Janus kinase inhibitors, tumor necrosis factor inhibitors, interleukin-6 blockers, and co-stimulatory modulators—were discussed, and these parameters (e.g. time to reach maximum plasma or serum concentration, volume of distribution, clearance, half-life) were linked to clinical decisions. The review also explored immunogenicity concerns associated with biologics, the role of anti-drug antibodies, and therapeutic drug monitoring. Finally, we presented a patient-centered treatment matrix that aligns PK properties with individual patient scenarios and discussed future directions, including biosimilar development, low-molecular-weight biologics, and artificial intelligence-based PK modeling platforms.

Expert opinion

PK is a powerful yet underutilized tool for individualizing RA treatment. Differences in ADME properties between small molecules and biologics affect dosing flexibility, adherence, monitoring, and safety, especially in complex cases such as organ dysfunction, pregnancy, or immunocompromised states. As new therapies emerge and healthcare advances toward precision medicine, integrating PK-based insights into clinical algorithms will be critical for optimizing therapeutic outcomes and formulation development. Linking mechanistic understanding with real-world PK is the next frontier in rational RA drug selection and optimization.