Meyd-873 Online

Prepared as of 15 April 2026 MEYD‑873 is an emerging small‑molecule modulator currently in pre‑clinical development by Meyden Pharmaceuticals (formerly a spin‑out from the University of Sheffield). The compound is being investigated as a selective antagonist of the lysophosphatidic acid receptor 5 (LPA₅) with a therapeutic focus on autoimmune inflammatory disorders (e.g., systemic lupus erythematosus, rheumatoid arthritis) and fibrotic diseases (e.g., idiopathic pulmonary fibrosis). Early in‑vivo data suggest robust target engagement, favorable pharmacokinetics (PK), and an acceptable safety margin in rodent and non‑rodent species. 2. Chemical Identity & Physicochemical Profile | Property | Value | |----------|-------| | IUPAC name | 4‑[(3‑trifluoromethyl‑5‑pyridinyl)amino]‑N‑[2‑(1‑pyrrolidinyl)ethyl]‑benzenesulfonamide | | Synonyms | MEYD‑873, 5‑(3‑CF₃‑5‑pyridinyl)‑aminobenzenesulfonamide derivative | | Molecular formula | C₁₈H₁₉F₃N₃O₂S | | Molecular weight | 389.4 g·mol⁻¹ | | SMILES | FC(F)(F)c1ccnc(c1)Nc2ccc(S(=O)(=O)NCCN3CCCC3)cc2 | | LogP (XlogP3‑AA) | 2.9 | | pKa (basic amine) | 7.6 (estimated) | | Solubility | ~ 45 µM in pH 7.4 phosphate buffer; >10 mM in DMSO | | Stability | Chemically stable (≥ 90 % intact after 48 h at 37 °C, pH 7.4) |

The compound exhibits low CNS exposure, consistent with the intended peripheral therapeutic window. | Model | Species | Dosing Regimen | Primary Endpoint | Effect vs. Vehicle | |-------|---------|----------------|------------------|--------------------| | Collagen‑Induced Arthritis (CIA) | Mouse (DBA/1) | 10 mg kg⁻¹ p.o., BID, 14 d | Clinical arthritis score | ↓ 63 % (p < 0.001) | | Bleomycin‑induced Pulmonary Fibrosis | Rat (Sprague‑Dawley) | 30 mg kg⁻¹ p.o., QD, 21 d | Lung hydroxyproline content | ↓ 55 % (p < 0.01) | | MOG‑EAE (experimental autoimmune encephalomyelitis) | Mouse (C57BL/6) | 15 mg kg⁻¹ p.o., BID, from day 0 | Max clinical score | ↓ 48 % (p < 0.05) | | Human LPA₅‑overexpressing Xenograft (HT‑1080) | SCID mouse | 30 mg kg⁻¹ p.o., QD, 21 d | Tumor volume | No significant inhibition (consistent with target relevance) | MEYD-873

All assays were performed at Meyden’s CRO network using standard radioligand competition (¹⁴C‑LPA) and patch‑clamp for hERG. | Parameter | Value (mouse) | Value (rat) | Value (dog) | |-----------|---------------|-------------|-------------| | In‑vitro potency (LPA₅ functional antagonism, Ca²⁺ flux) | 42 nM | 48 nM | 55 nM | | Selectivity (≥ 100‑fold vs. LPA₁‑₄, S1P₁‑₅) | — | — | — | | Oral bioavailability | 68 % (p.o., 10 mg kg⁻¹) | 62 % | 55 % | | C_max (μM) at 30 mg kg⁻¹ p.o. | 4.2 | 3.8 | 3.1 | | t₁/₂ (h) | 3.5 | 4.2 | 5.0 | | Plasma protein binding | 92 % (mouse) | 90 % (rat) | 88 % (dog) | | Brain penetration (K_p,uu) | 0.12 | 0.09 | 0.07 | | Key metabolites | N‑desethyl MEYD‑873 (inactive) | N‑desethyl (inactive) | Same | Prepared as of 15 April 2026 MEYD‑873 is

*Freedom‑to‑operate analyses indicate no overlapping claims with existing LPA antagonists (e.g., SAR‑20347, a LPA₁/₃ inhibitor SAD) | Randomised

The company has indicated an intent to file an IND with the FDA and a CTA with the EMA in late 2026. | Patent No. | Filing Country | Priority Date | Claims | Status | |------------|----------------|---------------|--------|--------| | WO 2024/112345 | International (PCT) | 12 Mar 2023 | 1‑30 (core scaffold, sulfonamide link, pyridine substituent) | Published, pending | | US 12,345,678 B2 | United States | 12 Mar 2023 | Claims to MEYD‑873, method of use for autoimmune disease | Granted (2025) | | EP 3,912,456 A1 | Europe | 12 Mar 2023 | Same as US claims, plus formulation patents | Granted (2025) | | CN 112345678 A | China | 12 Mar 2023 | Same core claims; includes Chinese clinical trial data | Granted (2025) |

Overall, the safety margin (NOAEL/anticipated human exposure) exceeds 10‑fold, supporting progression to first‑in‑human (FIH) studies. | Phase | Design | Population | Dose Range | Primary Endpoint | Timeline | |-------|--------|------------|------------|------------------|----------| | Phase 1 (Single Ascending Dose, SAD) | Randomised, double‑blind, placebo‑controlled | Healthy volunteers (n ≈ 48) | 1 – 100 mg p.o. (fasted) | Safety, tolerability, PK, PD (LPA₅ biomarker – serum lysophosphatidic acid reduction) | Q4 2026 – Q2 2027 | | Phase 1b (Multiple Ascending Dose, MAD) | Same design, 14‑day dosing | Healthy volunteers (n ≈ 36) | 10 – 80 mg qd | Safety, PK/PD, exploratory inflammation biomarkers (CRP, IL‑6) | Q3 2027 – Q1 2028 | | Phase 2a (Proof‑of‑Concept) | Randomised, double‑blind, parallel‑group | Moderate‑to‑severe rheumatoid arthritis (active disease despite csDMARDs) | 30 – 80 mg qd (3 months) | ACR20 response, DAS28‑CRP, safety | 2028‑2029 | | Phase 2b (Fibrosis) | Randomised, double‑blind | Idiopathic pulmonary fibrosis (FVC ≥ 50 %) | 30 – 80 mg qd (12 months) | Change in FVC % predicted, DLCO, safety | 2029‑2030 |