| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IL-23 7.1 pM (Kd)
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|---|---|
| ln Vivo |
Icotrokinra (0.03-10 mg/kg; po; once daily for 7 days) reduces the colon weight-to-length ratio and alleviates weight loss in rats with TNBS-induced colitis [1]. Icotrokinra (1-30 mg/kg; po; twice daily for 3 days) blocks IL-23-induced upregulation of IL-17A and IL-22 at doses greater than 10 mg/kg in a rat skin inflammation model [ 1].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following oral administration of 200 mg icotramycin, the mean maximum plasma concentration (Cmax) was 3.62 ng/mL, and the total systemic exposure (AUC0-inf) was 44.8 ng*h/mL. The median time to reach maximum plasma concentration (Tmax) was 2 hours, ranging from 0.25 to 8 hours. The oral bioavailability of this drug is low, estimated at 0.1% to 0.3% in animal studies. Food significantly affects its absorption—concomitant administration with a high-fat meal reduces AUC by 43% and Cmax by 59%; therefore, it must be taken on an empty stomach, at least 30 minutes before a meal. The primary route of excretion for icotramycin is feces. Approximately 37% to 81% of the oral dose is excreted unchanged in feces within 24 hours. Renal excretion is negligible, with only 0.001% of the dose excreted unchanged in urine. Following oral administration, icotrokinra achieved a steady-state apparent volume of distribution of 92,800 L. Preclinical data showed that the drug freely distributes to disease-associated tissues, including the skin, joints, and gastrointestinal tract. In monkey models, icotrokinra's tissue distribution (tissue/plasma ratio of 45.8% to 156%) was significantly higher than that of injectable IL-23 monoclonal antibody [risankizumab]. Following oral administration, icotrokinra's apparent clearance was 6550 L/h. Metabolism / Metabolites As a peptide, icotrokinra is converted into smaller peptides through nonspecific peptide catabolism. Biological Half-Life The median elimination half-life of icotrokinra is 12 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Currently, there is no information regarding the use of icotramycin during lactation. However, due to its high molecular weight of 1898 Daltons, very little is likely excreted into breast milk, and as a peptide drug, it is likely to be digested in the infant's gastrointestinal tract, making it unlikely to reach clinically significant concentrations in the infant's serum. If the mother needs to use icotramycin, this is not a reason to discontinue breastfeeding. Until more data becomes available, icotramycin should be used with caution during lactation, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Protein Binding Itraconazole binds to 52% of plasma proteins. In vitro characterization showed that the drug preferentially binds to human serum albumin compared to α-1 acid glycoprotein. |
| References | |
| Additional Infomation |
Icotrokinra is a first-in-class, orally administered, targeted peptide interleukin-23 (IL-23) receptor antagonist. Discovered and developed jointly by Protagonist and Johnson & Johnson, it provides a novel oral treatment option for patients with plaque psoriasis requiring systemic therapy. Icotrokinra received FDA approval in March 2026 for the treatment of moderate to severe plaque psoriasis.
Drug Indication Icotrokinra is indicated for the treatment of moderate to severe plaque psoriasis in adults and children aged 12 years and older who weigh at least 40 kg and are eligible for systemic therapy or phototherapy. Mechanism of Action Icotrokinra is a first-in-class targeted oral peptide that selectively binds to the IL-23 receptor (IL-23R) with high affinity, having a dissociation constant of 7 pM. This drug antagonizes the binding of IL-23 by blocking the IL-23 receptor. IL-23 is a naturally occurring cytokine involved in inflammatory and immune responses. This antagonistic effect inhibits the release of IL-23/IL-23R-dependent pro-inflammatory cytokines, which are fundamental to the inflammatory response in moderate to severe plaque psoriasis. Pharmacodynamics Compared to pre-treatment levels, icotramycin reduced serum levels of pro-inflammatory cytokines, including IL-17A, IL-17F, IL-19, IL-22, and β-defensin-2. Exploratory analyses also showed decreased expression of mRNAs associated with the IL-23/Th17 pathway and psoriasis, such as IL-17A, IL-17F, IL-19, IL-22, IL-23A, and DEFB4A, in skin lesion biopsies compared to baseline. Like other drugs affecting the immune system, icotramycin may increase the risk of infection, including relapse of latent tuberculosis. Patients should be closely monitored for signs and symptoms throughout treatment. |
| Molecular Formula |
C90H120N20O22S2
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|---|---|
| Molecular Weight |
1898.17
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| Exact Mass |
1896.833
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| CAS # |
2763602-16-8
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| PubChem CID |
162462321
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
20
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
134
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| Complexity |
4100
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| Defined Atom Stereocenter Count |
12
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| SMILES |
N(C1(CCOCC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@H](C(=O)N(C)CC(=O)N)CC1=CN=CC=C1)C(=O)[C@@H](NC(=O)[C@@H](NC(C1C(SSC([C@@H](C(N[C@H](C(=O)NC([C@H](O)C)C(=O)N[C@@H](CC2=CNC3=C(C=CC=C23)C)C(=O)N[C@@H](CCCCNC(=O)C)C(=O)N1)CC(=O)N)=O)NC(=O)C)(C)C)(C)C)=O)CC1C=CC(OCCN)=CC=1)CC1C=CC2C=CC=CC=2C=1
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| InChi Key |
IVFNYXYPMJQSGF-QMRCQSNESA-N
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| InChi Code |
InChI=1S/C90H120N20O22S2/c1-48-16-14-20-59-57(46-97-72(48)59)42-64-79(122)99-60(21-12-13-34-96-50(3)112)77(120)108-75(89(7,8)134-133-88(5,6)74(98-51(4)113)84(127)104-66(44-69(93)115)81(124)107-73(49(2)111)83(126)102-64)85(128)103-62(39-52-23-26-58(27-24-52)132-37-32-91)78(121)100-63(40-53-22-25-55-18-10-11-19-56(55)38-53)82(125)109-90(30-35-131-36-31-90)87(130)106-61(28-29-71(117)118)76(119)101-65(43-68(92)114)80(123)105-67(41-54-17-15-33-95-45-54)86(129)110(9)47-70(94)116/h10-11,14-20,22-27,33,38,45-46,49,60-67,73-75,97,111H,12-13,21,28-32,34-37,39-44,47,91H2,1-9H3,(H2,92,114)(H2,93,115)(H2,94,116)(H,96,112)(H,98,113)(H,99,122)(H,100,121)(H,101,119)(H,102,126)(H,103,128)(H,104,127)(H,105,123)(H,106,130)(H,107,124)(H,108,120)(H,109,125)(H,117,118)/t49-,60+,61+,62+,63+,64+,65+,66+,67+,73+,74-,75-/m1/s1
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| Chemical Name |
(4S)-4-[[4-[[(2S)-2-[[(2S)-2-[[(4R,7S,10S,13S,16S,19R)-19-acetamido-7-(4-acetamidobutyl)-16-(2-amino-2-oxoethyl)-13-[(1R)-1-hydroxyethyl]-3,3,20,20-tetramethyl-10-[(7-methyl-1H-indol-3-yl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-[4-(2-aminoethoxy)phenyl]propanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]oxane-4-carbonyl]amino]-5-[[(2S)-4-amino-1-[[(2S)-1-[(2-amino-2-oxoethyl)-methylamino]-1-oxo-3-pyridin-3-ylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-oxopentanoic acid
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| Synonyms |
JNJ-77242113; JNJ-2113; PN-235
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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 Note: (1). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL (~52.68 mM; with ultrasonication)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5268 mL | 2.6341 mL | 5.2682 mL | |
| 5 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | |
| 10 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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/NCT06295692
Conditions:Generalized Pustular Psoriasis|Erythrodermic PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT07196748
Conditions:Colitis, UlcerativeLink: https://clinicaltrials.gov/ct2/show/NCT07196722
Conditions:Crohn Disease
Title:A Study to Evaluate the Efficacy and Safety of JNJ-77242113 (Icotrokinra) in Biologic-naïve Participants With Active Psoriatic Arthritis
Status:Active, not recruiting
updateDate:2026-05-08
Ctid:NCT06878404
Link: https://clinicaltrials.gov/ct2/show/NCT06878404
Conditions:Arthritis, PsoriaticLink: https://clinicaltrials.gov/ct2/show/NCT06807424
Conditions:Arthritis, PsoriaticLink: https://clinicaltrials.gov/ct2/show/NCT05357755
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06049017
Conditions:Colitis, UlcerativeLink: https://clinicaltrials.gov/ct2/show/NCT06095115
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06934226
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06095102
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06143878
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT06220604
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT05223868
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT05364554
Conditions:Plaque PsoriasisLink: https://clinicaltrials.gov/ct2/show/NCT05062200
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05703841
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04621630
Conditions:Healthy VolunteersProducts are for research use only; We do not sell to patients
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