ArticleACR open rheumatology2025
Safety, Tolerability, Efficacy, Pharmacokinetics, and Pharmacodynamics of Afimetoran, a Toll-Like Receptor 7 and 8 Inhibitor, in Patients With Cutaneous Lupus Erythematosus: A Phase 1b Randomized, Double-Blind, Placebo-Controlled Study.
Article in ACR open rheumatology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT04493541 (A Phase 1b Randomized, Double-blind, Placebo-controlled Study to Assess the Safety and Pharmacokinetics of BMS-986256 in Participants With Active Cutaneous Lupus Erythematosus), which is not on this map. Cited by 9 papers.
What it found
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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.
A Phase 1b Randomized, Double-blind, Placebo-controlled Study to Assess the Safety and Pharmacokinetics of BMS-986256 in Participants With Active Cutaneous Lupus Erythematosus
Who cites it
9 citing papers in PubMed.
- Enpatoran, a first-in-class, selective, orally administered toll-like receptor 7/8 inhibitor, in systemic and cutaneous lupus erythematosus: results from a randomised, placebo-controlled phase Ib study.Lupus science & medicine · 2025Trial
- The SLC15A4-TASL complex is essential for lupus development in mice.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Innate immunity: current understandings and future perspectives.Signal transduction and targeted therapy · 2026Review
- TLR7 in systemic lupus erythematosus: genetics and emerging therapies.Nature reviews. Rheumatology · 2026Review
- Natural products and dietary bioactives as antiviral agents against herpesviruses: molecular mechanisms, immunomodulatory actions, and nutritional perspectives.Archives of microbiology · 2026Review
- TLR7 and TLR9 have overlapping but distinct roles in systemic lupus erythematosus and Sjögren's disease.Frontiers in immunology · 2026Review
- The Type I Interferon Axis in Systemic Autoimmune Diseases: From Molecular Pathways to Targeted Therapy.Biomolecules · 2025Review
- Structural and immunological impacts of TOLLIP nsSNPs: A computational biology approach to drug discovery and immune system modulation.PloS one · 2025Article
- Targeting TLR Signaling Cascades in Systemic Lupus Erythematosus and Rheumatoid Arthritis: An Update.Biomedicines · 2024Article
Corrections and comments
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Authors and funding
14 authors.
Funding
Abstract
objectiveThere is an unmet need for safe and effective oral treatments for cutaneous lupus erythematosus (CLE). Afimetoran is an investigational, first-in-class, orally bioavailable, selective small molecule inhibitor of Toll-like receptors (TLRs) 7 and 8. We investigated the safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics of afimetoran in patients with CLE.
methodsIn this Phase 1b, randomized, double-blind, placebo-controlled study (NCT04493541), patients with CLE received afimetoran (30 mg once daily) or a placebo, in addition to select background medications, over 16 weeks. Safety and tolerability were mainly reported through adverse events (AEs). Pharmacokinetics were determined using plasma concentration-time data. Pharmacodynamic biomarkers and efficacy (CLE Disease Area and Severity Index-Activity [CLASI-A] scores) were exploratory end points.
resultsThirteen patients were randomized (afimetoran, n = 8; placebo, n = 5), and 12 patients completed treatment (1 discontinued afimetoran [COVID-19 infection]). Afimetoran demonstrated a favorable safety profile compared with placebo (patients with AEs: 62.5% vs 80.0%), with mainly mild-to-moderate AEs. Plasma concentrations exceeded the projected targeted 24-hour 90% inhibition concentration, supporting once- daily dosing. Pharmacodynamic analyses showed a rapid response to afimetoran by week 1 maintained throughout and beyond treatment, with reduced expression of TLR7/8 pathway-associated cytokines. All patients who received afimetoran had a change in the interferon-1 gene signature (P < 0.0001) at week 16, with five of eight patients demonstrating a >50% improvement in CLASI-A scores.
conclusionThese findings support afimetoran's potential as a once daily oral treatment for patients with CLE and suggest a possibly substantial therapeutic benefit, warranting further clinical investigation of afimetoran for lupus.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.