rheumatoid arthritis

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Parecoxib (SC 69124) is an effective and selective COX-2 inhibitor.

Frentizole, an immunosuppressive agent, is an inhibitor of the Aβ-ABAD interaction

WRG-28 is a potent and selective, allosteric discoidin domain receptor 2 (ddr2) inhibitor(IC50 : 230 nM)

Y-320 is a new phenylpyrazoleanilide immunomodulator.

Bucillamine (DE019) protects against Ischemia/reperfusion injury in high-risk organ transplants and inhibits the production of VEGF. Bucillamine is an orally active sulfhydryl donor and antioxidant with antirheumatic and antiangiogenic properties. Bucillamine can be used for studies about choroidal neovascularization and rheumatoid arthritis.

Cosyntropin (acetate) stimulates the release of corticosteroids such as cortisol from the adrenal gland.

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

Anakinra (Raleukin) is a cytokine inactivator and interleukin 1 receptor antagonist that can be used to study secondary phagocytic lymphohistiocytosis and rheumatoid arthritis.

Etanercept is a fusion protein consisting of the soluble portion of the p75-tumor necrosis factor receptor (TNFR) and the Fc fragment of human IgG1 and is commonly used to treat patients with rheumatoid arthritis.[1]

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

Tocilizumab (Anti-Human IL6R) is a neutralizing antibody against human interleukin-6 receptor (IL-6R) that blocks the binding of IL-6 to IL-6R, thereby inhibiting both classical and trans signaling. It can be used to study rheumatoid arthritis and has been suggested as a possible drug for the treatment of severe COVID-19.

Infliximab is a monoclonal antibody, a human-mouse chimeric monoclonal antibody that inhibits TNF-α and prevents TNF-α from interacting with TNFR1 and TNFR2. Infliximab can be used to treat Crohn's disease and rheumatoid arthritis.

Clozic (ICI 55897) is a small molecule anti-arthritis candidate that exerts anti-inflammatory effects by reversibly inhibiting excessive proliferation of synovial cells, and can be used for mechanistic studies of rheumatoid arthritis and related inflammatory diseases.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.

Theralizumab (TGN1412) is an anti-CD28-targeting monoclonal antibody that directly stimulates T cells. Theralizumab has antitumor activity and is used for the treatment of B-cell chronic lymphocytic leukemia and rheumatoid arthritis.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

DHODH-IN-13 is an inhibitor of DHODH with IC50 of 4.3 μM for rat liver. DHODH-IN-13 can be used in studies about rheumatoid arthritis.

DHODH-IN-14 is an analog of hydroxyfuran pyrimidine A771726. DHODH-IN-14 is a dihydroorotate dehydrogenase (DHODH) inhibitor IC50 0.49 μM mouse liver DHODH. DHODH-IN-14 can be used for rheumatoid arthritis.