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| Targets |
Lomedeucitinib targets tyrosine kinase 2 (TYK2), a member of the Janus kinase (JAK) family of intracellular tyrosine kinases. TYK2 is involved in cytokine signaling pathways, particularly those mediated by IL-12, IL-23, and type I interferons. Inhibition of TYK2 suppresses downstream STAT phosphorylation and pro-inflammatory cytokine production, providing therapeutic benefit in autoimmune and inflammatory diseases.
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| ln Vitro |
Lomedeucitinib shows potent in vitro inhibition of TYK2-mediated signaling. It significantly inhibits IFNα production downstream of IL-12/TYK2 activation with an IC₅₀ of 0.047 μM. The compound exhibits selectivity for TYK2 over other JAK family members, which may confer an improved safety profile by reducing JAK1/JAK2/JAK3-related toxicities.
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| ln Vivo |
Lomedeucitinib has been evaluated for in vivo efficacy in clinical trials for moderate-to-severe psoriasis. As a selective TYK2 inhibitor, it suppresses the IL-23/Th17 axis and reduces skin inflammation in psoriasis patients. Clinical studies have demonstrated its effectiveness and safety profile in the treatment of plaque psoriasis.
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| Enzyme Assay |
Non-cell-based binding assays for Lomedeucitinib typically involve kinase activity assays measuring TYK2 inhibition. A typical protocol includes: incubating recombinant TYK2 kinase domain with ATP and a peptide substrate, adding Lomedeucitinib at various concentrations, and measuring kinase activity by detecting phosphorylated substrate using fluorescence, luminescence, or radiometric detection. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for Lomedeucitinib typically involve cytokine-stimulated cell lines or primary cells. A representative protocol includes: culturing cells (e.g., PBMCs or T cells), stimulating with IL-12 or IFNα, treating with Lomedeucitinib at various concentrations (0.001–10 μM), measuring STAT phosphorylation by phospho-flow cytometry or Western blot, and assessing cytokine production (e.g., IFNγ, IL-17) by ELISA.
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| Animal Protocol |
In vivo animal studies with Lomedeucitinib have been conducted in preclinical models of psoriasis and other inflammatory diseases. A representative protocol includes: administering the compound via oral gavage to mouse models of psoriasis (e.g., imiquimod-induced or IL-23-induced models), monitoring skin inflammation, measuring cytokine levels in skin and serum, and performing histopathological analysis of skin lesions.
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| ADME/Pharmacokinetics |
Lomedeucitinib is an orally bioavailable TYK2 inhibitor. While detailed PK parameters are not fully reported in the available literature, typical PK properties of TYK2 inhibitors include oral bioavailability of 30–70%, half-life of 6–12 hours, moderate volume of distribution, and metabolism primarily via CYP450 enzymes. The compound is designed for once-daily oral administration in clinical settings.
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| Toxicity/Toxicokinetics |
Lomedeucitinib has been evaluated for safety in clinical trials. As a selective TYK2 inhibitor, it is expected to have a more favorable safety profile than pan-JAK inhibitors, with reduced risk of hematologic toxicity, infections, and lipid abnormalities. However, comprehensive toxicology data are available from clinical studies, with the compound being investigated in clinical trial NCT05730725 for moderate-to-severe psoriasis.
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| References | |
| Additional Infomation |
Lomedeucitinib is a small molecule drug. The International Nonproprietary Name (INN) prefix "-citinib" in its name indicates that lomedeucitinib is a Janus kinase inhibitor. Lomedeucitinib is currently being investigated in the clinical trial NCT05730725 (a study evaluating the efficacy and safety of BMS-986322 in patients with moderate to severe psoriasis). The monoisotope molecular weight of lomedeucitinib is 419.15 Da.
Lomedeucitinib (BMS-986322, CAS 2328068-29-5) is an investigational drug for the treatment of inflammatory diseases, particularly plaque psoriasis. The compound is being developed as a selective TYK2 inhibitor with the potential to provide effective anti-inflammatory activity with improved safety compared to non-selective JAK inhibitors. It represents a promising therapeutic approach for autoimmune and inflammatory conditions. |
| Exact Mass |
419.146
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| CAS # |
2328068-29-5
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| PubChem CID |
138620496
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
765
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[2H]C([2H])([2H])NC(=O)C1=NN=C(C=C1NC2=C(C=CC=N2)S(=O)(=O)C)NC(=O)[C@@H]3CC34CC4
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| InChi Key |
VWIVBQZLVAGLMH-ASGODXDTSA-N
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| InChi Code |
InChI=1S/C18H20N6O4S/c1-19-17(26)14-11(21-15-12(29(2,27)28)4-3-7-20-15)8-13(23-24-14)22-16(25)10-9-18(10)5-6-18/h3-4,7-8,10H,5-6,9H2,1-2H3,(H,19,26)(H2,20,21,22,23,25)/t10-/m0/s1/i1D3
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| Chemical Name |
4-[(3-methylsulfonyl-2-pyridinyl)amino]-6-[[(2R)-spiro[2.2]pentane-2-carbonyl]amino]-N-(trideuteriomethyl)pyridazine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT05730725
Conditions:PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06088264
Conditions:Healthy Male ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT05615012
Conditions:Healthy Participants
Title:A Study to Investigate the Interaction of BMS-986322 and a Combined Oral Hormonal Contraceptive (Ethinyl Estradiol EE/Norethindrone NET) in Healthy Female Participants
Status:Completed
updateDate:2023-08-18
Ctid:NCT05579574
Link: https://clinicaltrials.gov/ct2/show/NCT05579574
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT05546151
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT04175925
Conditions:Healthy ParticipantsProducts are for research use only; We do not sell to patients
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