IL-13 Inhibitor

Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.

Lebrikizumab (TNX-650) is an IgG4 humanized anti-interleukin-13 (IL-13) mAb with anti-itch effects that specifically binds to IL-13 in a non-receptor binding domain and inhibits its function. Lebrikizumab inhibits the IL-13 driven Th2 inflammatory response and blocks the signaling of IL-4Rα/IL-13Rα1. Lebrikizumab can be used for the research of asthma, atopic dermatitis and neuroinflammatory diseases.

Tilrekimig (PF-07275315) is a monoclonal antibody targeting human interleukin-4 (IL-4), interleukin-13 (IL-13) and thymic stromal lymphopoietin (TSLP). Tilrekimig can be used in the research of allergic and inflammatory diseases, such as asthma and atopic dermatitis.

TSLP-IN-1 is a potent thymic stromal lymphopoietin (TSLP) inhibitor. TSLP-IN-1 disrupts TSLP-TSLPR protein-protein interaction, and downregulates IL-4 and IL-13. TSLP-IN-1 can be used for the research of inflammation diseases, such as skin disease, asthma, and allergies.

BP79 is a potent TSLP receptor inhibitor. BP79 disrupts TSLP-mediated ternary complex formation, blocks TSLPR-IL7Rα co-localization, binds and stabilizes TSLPR, and inhibits phosphorylated STAT3/6. BP79 suppresses immune cell infiltration, secretion of IL-13, IL-4. BP79 can be used for the research of inflammation diseases, such as atopic dermatitis, allergic asthma, and allergic rhinitis.

Pyrrothiogatain is a transcription factor GATA3 inhibitor with an IC₅₀ of 54.7 μM. Pyrrothiogatain inhibits the DNA-binding activity of GATA3 and inhibits the T helper 2 (Th2) cell differentiation and expression of Th2 cytokines. Pyrrothiogatain shows anti-infection effect by inhibiting ACE2 expression. Pyrrothiogatain can be used for the researches of inflammation, immunology, infection and cancer, such as colon cancer and SARS-CoV-2 infection.

Tralokinumab (CAT354) is a humanized IgG4 monoclonal antibody that specifically binds to and neutralizes IL-13. Tralokinumab can be used in the research of diseases such as asthma, atopic dermatitis, and pulmonary fibrosis.

Lunsekimig (SAR443765) is a nanobody composed of 5 VH domains that targets both TSLP and IL-13. Lunsekimig blocks the functional effects of TSLP and IL-13, inhibits related inflammatory signals, and improves lung function associated with type 2 inflammation. Lunsekimig can be used in research on asthma and type 2 inflammation.

Stapokibart (CM310) is a humanized monoclonal antibody targeting IL-4Rα (K_D values of 0.25 nM, 1.50 nM, and 2.75 nM for human, cynomolgus monkey, and rat IL-4Rα, respectively). Stapokibart effectively blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart reduces IL-4 and IL-13 mRNA, inhibits CD23 upregulation, and inhibits IL-4 and IL-13-induced STAT6 activation. Stapokibart improves inflammation (airway inflammation, rhinitis, dermatitis).

CAN10 is is a humanized monoclonal antibody inhibitor targeting interleukin 1RAP (IL1RAP). CAN10 blocks IL-1, IL-33, and IL-36 signalling by targeting IL1RAP, preventing downstream proinflammatory and profibrotic responses. CAN10 reduces dermal and pulmonary fibrosis. CAN10 can be used for the research of immune system diseases, such as systemic sclerosis.

Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma.

Atinvicitinib is an orally active and selective JAK1 inhibitor. Atinvicitinib blocks signaling of JAK1-dependent pruritogenic and pro-inflammatory cytokines, including those in the IL-31, IL-4, and IL-13 pathways. Atinvicitinib can be used for the researches of pruritus associated with allergic dermatitis and canine atopic dermatitis.

Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targeting ICOSL. Prezalumab inhibits T cell activation and related immune responses by binding to ICOSL and blocking the interaction between ICOS and ICOSL. Prezalumab can be used in the research of autoimmune diseases and inflammatory diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002).

Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC₅₀s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis).

Gypenoside A is an orally active triterpenoid compound that can be isolated from Gynostemma pentaphyllum. Gypenoside A has anti-inflammatory and antioxidant activities. Gypenoside A also has a certain protective effect on cardiomyocytes and can inhibit apoptosis. Gypenoside A can be used in the research of cardiovascular diseases and inflammation-related diseases.

Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.

Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.

(±)-Praeruptorin A, a coumarin compound, is the main bioactive component in Peucedani Radix. As a calcium channel blocker, (±)-Praeruptorin A exhibits great antihypertensive effects. In addition, (±)-Praeruptorin A also has the effects of relaxing vascular smooth muscle, inhibiting airway inflammation and airway hyperresponsiveness. (±)-Praeruptorin A can be used for the research of allergic asthma, hypertension and other diseases.

SM-17 is a human monoclonal antibody targeting IL-17RB. SM-17 binds to human IL-17RB, inhibits the dimerization of IL-17RA/IL-17RB, blocks IL-25-induced phosphorylation of ERK1/2 and STAT5, and suppresses Th2-mediated inflammatory responses. SM-17 inhibits the secretion of IL-5, IL-9, IL-13 and IL-4, impairs the proliferation/expansion of ILC2 and Th2 cells, and restores filaggrin expression. SM-17 reduces immune cell infiltration, epidermal hyperplasia, goblet cell hyperplasia, collagen deposition, ear swelling and scratching behavior in animal models. SM-17 can be used in research related to atopic dermatitis and allergic asthma.

JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC₅₀ values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC₅₀s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).