ArticleClinical pharmacokinetics2021
Pharmacokinetics and Exposure-Response Relationship of Teprotumumab, an Insulin-Like Growth Factor-1 Receptor-Blocking Antibody, in Thyroid Eye Disease.
Article in Clinical pharmacokinetics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers, 2 of them syntheses that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 2 syntheses or guidelines pooled it, 25 citations in OpenAlex.
- Comparative efficacy and safety of rituximab, tocilizumab, and teprotumumab in Graves' orbitopathy: a systematic review and meta-analysis.Eye (London, England) · 2025Pooled it
- The Efficacy and Safety of Teprotumumab in Thyroid Eye Disease: Evidence from Randomized Controlled Trials.International journal of clinical practice · 2023Pooled it
- Thyroid eye disease with teprotumumab-related hyperglycemia associated with increased growth hormone secretion.JCEM case reports · 2026Article
- Innovative Clinical Pharmacology, Modeling, and Simulation Strategies for Accelerating Rare Disease Drug Development.Journal of clinical pharmacology · 2026Review
- Marked and reversible circulating insulin-like growth factor-1 elevation during teprotumumab N01 treatment for thyroid eye disease with limited correspondence to glycemic changes.Frontiers in endocrinology · 2026Article
- Article
- Teprotumumab for Thyroid Eye Disease: Mechanism, Clinical Efficacy, and Current Challenges.Antibodies (Basel, Switzerland) · 2025Review
- Thyroid-related orbitopathy: clinical overview, novel medical treatments and the role of orbital surgery.International ophthalmology · 2025Review
- Targeting the Neonatal Fc Receptor in Autoimmune Diseases: Pipeline and Progress.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2025Review
- The Relevance and Potential Role of Orbital Fat in Inflammatory Orbital Diseases: Implications for Diagnosis and Treatment.Ophthalmology and therapy · 2025Review
- Teprotumumab-trbw as a Novel Monoclonal Antibody for Thyroid Eye Disease: A Literature Review.Cureus · 2023Review
- Teprotumumab: A Review in Thyroid Eye Disease.Drugs · 2022Review
- Extending IGF-1 Receptor Inhibition Beyond Thyroid Eye Disease: A Scoping Review of Teprotumumab Administration in Pretibial Myxedema.AACE endocrinology and diabetesReview
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectiveThyroid eye disease (TED) is characterized by inflammation/expansion of orbital tissues, proptosis, and diplopia. Teprotumumab is the first US Food and Drug Administration-approved therapy for TED, administered as an initial intravenous infusion of 10 mg/kg followed by 20 mg/kg every 3 weeks for an additional seven infusions. The objective of this article is to discuss the pharmacokinetics and exposure-response profile for teprotumumab in patients with TED.
methodsA population pharmacokinetic analysis was performed to characterize pharmacokinetics and select dosing in patients with TED. Exposure-response was evaluated for efficacy (proptosis response, clinical activity score categorical response, and diplopia response) and safety (hyperglycemia, muscle spasms, and hearing impairment) parameters.
resultsTeprotumumab pharmacokinetics was linear in patients with TED, with low systemic clearance (0.334 L/day), low volume of distribution (3.9 and 4.2 L for the central and peripheral compartment, respectively), and a long elimination half-life (19.9 days). The approved dosing regimen provided > 20 µg/mL for > 90% insulin-like growth factor 1 receptor saturation throughout the dosing interval. Model-predicted mean (± standard deviation) steady-state area under the concentration-time curve, peak, and trough concentrations in patients with TED were 131 (± 30.9) mg∙h/mL, 643 (± 130) µg/mL, and 157 (± 50.6) µg/mL, respectively. Female patients had a 15% higher steady-state peak concentration but a similar steady-state area under the concentration-time curve vs male patients. No other covariates affected teprotumumab pharmacokinetics. No meaningful correlations between teprotumumab exposures and efficacy or safety parameters were observed.
conclusionsTeprotumumab pharmacokinetics was well characterized in patients with TED, and generally consistent with other IgG1 antibodies. Efficacy was consistent across the exposure range with a well-tolerated safety profile supporting the current dose regimen for patients with TED.
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Registered trials
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