anti-rheumatic

Sulfapyridine (2-Sulfapyridine) is a short-acting sulfonamide antibiotic and by-product of the non-steroidal anti-inflammatory drug sulfasalazine.

Salsalate (Sasapyrine) is an orally available salicylate and non-steroidal anti-inflammatory drug (NSAID), with anti-inflammatory, analgesic and antipyretic activities.

Fenbufen (Lederfen) is a non-steroidal anti-inflammatory drug used primarily to treat inflammation in osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve backaches, sprains, and fractures. Fenbufen is available as a capsule or tablet sold with the brand names Cepal, Cinopal, Cybufen, Lederfen, and Reugast. Fenbufen acts by preventing cyclooxygenase from producing prostaglandins which can cause inflammation.

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.

Lonazolac is a nonsteroidal anti-inflammatory drug[1].

Oxaceprol (N-Acetyl-L-hydroxyproline) is an established therapeutic agent for osteoarthritis.

Tenidap (CP-66248) is a selective COX-1 and SLC26A3 inhibitor with anti-inflammatory, analgesic, and anti-rheumatic activities.

Butibufen (FF-106) is an orally active non-steroidal anti-inflammatory compound, a potential cyclooxygenase inhibitor with analgesic and antipyretic activity, and inhibits urea synthesis.Butibufen has been used in the study of rheumatic diseases.

Colchicine is an orally active natural alkaloid that acts by inhibiting microtubule polymerization (IC50 = 3 nM) and as a competitive antagonist of the α3 glycine receptor. It possesses broad anti-inflammatory, immunosuppressive, and antifibrotic activities, can inhibit NLRP3 inflammasome activation to prevent NSAID-induced small intestine injury, holds potential for gouty arthritis and rheumatoid arthritis research, and is commonly used to establish Alzheimer’s disease models.

(R)-Naproxen, an anti-inflammatory agent, has antipyretic and analgesic properties. Both the acid and its sodium salt are used in the therapy of acute gout or dysmenorrhea, musculoskeletal disorders, rheumatoid arthritis and other rheumatic.

Tiaprofenic acid D3 is a deuterium-labeled Tiaprofenic acid. Tiaprofenic acid is a nonsteroidal anti-inflammatory drug and treatment of rheumatic diseases.

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium (Miochrysin) is a potent and selective inhibitor of oncogenic PKC-ι signaling. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium exhibits potent anti-tumor activity.

Olpimedone is a compound developed for its anti-rheumatic and analgesic properties, though it was never marketed. Current information regarding olpimedone's uses is unavailable.

Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.

Oxycinchophen is a quinoline-like organic, anti-rheumatic compound. It has been used to study P- selectin antagonistic activity, DHOD inhibitory activity, and the effects of anti-inflammatory drugs on vascular smooth muscle.

Pipebuzone is an anti-inflammatory, antipyretic and analgesic drug used in the treatment of various rheumatic diseases. It is well tolerated clinically and pathologically and has a reliable anti-inflammatory effect.

FR-217840, a novel matrix metalloproteinase inhibitor, successfully suppresses joint destruction and suggest that FR217840 may have potential as a novel anti-rheumatic drug.

TAK-603 is an anti-rheumatic drug and is also anti-inflammatory compound. It selectively suppresses Th1 cytokine production and inhibits the progression of adjuvant arthritis.

AR-17048 is a potential anti-rheumatic drug.

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

1. Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects, may be used for the treatment of neurodegenerative diseases such as arthritis.

Tripdiolide has cytotoxic, and anti-rheumatic activities, it suppresses pro-inflammatory gene expression, may be effective therapy for lupus nephritis.

Piroxicam cinnamate (Cinnoxicam), a cyclooxygenase (COX) inhibitor with anti-inflammatory properties, is used to study inflammatory degenerative bone and joint diseases, rheumatic diseases, and varicocele-related oligospermia.

Cistifolin is an integrin-dependent cell adhesion blocker from the anti-rheumatic herbal drug, gravel root