beta-aminoarteether maleate (SM934) / Shanghai Inst. of Materia Medica, Jiangsu ZuoYou Medicine - LARVOL DELTA

Safety and Efficacy of SM934 Compared to Placebo in Adult Subjects With Active Systemic Lupus Erythematosus (clinicaltrials.gov) - P2 | N=32 | Completed | Sponsor: RenJi Hospital | Unknown status ➔ Completed | N=48 ➔ 32 | Trial completion date: Dec 2020 ➔ Oct 2023 | Trial primary completion date: Dec 2020 ➔ Oct 2023

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Immunology • Inflammatory Arthritis • Lupus • Systemic Lupus Erythematosus

Artemisinin analog SM934 alleviates epithelial barrier dysfunction via inhibiting apoptosis and caspase-1-mediated pyroptosis in experimental colitis. (PubMed, Front Pharmacol) - "Moreover, SM934 interdicted pyroptosis via blocking the transduction of mitogen-activated protein kinase (MAPK) and nuclear factor-kB (NF-kB) signaling pathways. In conclusion, SM934 protected TNBS-induced colitis against intestinal barrier disruption by inhibiting the apoptosis and pyroptosis of epithelial cells via the NLRP3/NF-κB/MAPK signal axis, and intestinal barrier protection in company with an anti-inflammatory strategy might yield greater benefits in IBD treatment."

Journal • Gastroenterology • Gastrointestinal Disorder • Immune Modulation • Immunology • Inflammation • Inflammatory Bowel Disease • Oncology • HMGB1 • IL18 • NLRP3 • TNFA

Artemisinin derivative SM934 in the treatment of autoimmune and inflammatory diseases: therapeutic effects and molecular mechanisms. (PubMed, Acta Pharmacol Sin) - "Here, we summarize the immunomodulatory effects, anti-inflammatory, anti-oxidative and anti-fibrosis activities of SM934 in disease-relevant animal models and present the probable pharmacological mechanisms involved in its therapeutic efficacy. This review also delineates a typical example of natural product-based drug discovery, which might further vitalize natural product exploration and development in pharmacotherapy."

Journal • Review • CNS Disorders • Dry Eye Disease • Fibrosis • Gastroenterology • Gastrointestinal Disorder • Genetic Disorders • Glomerulonephritis • Hematological Disorders • Immune Modulation • Immunology • Infectious Disease • Inflammation • Inflammatory Arthritis • Inflammatory Bowel Disease • Lupus • Multiple Sclerosis • Oncology • Ophthalmology • Renal Disease • Rheumatoid Arthritis • Rheumatology • Systemic Lupus Erythematosus

Artemisinin analogue SM934 protects against lupus-associated antiphospholipid syndrome via activation of Nrf2 and its targets. (PubMed, Sci China Life Sci) - "Among others, we interpreted in present work that both anti-inflammatory and antioxidative effects of SM934 is closely correlated with the enhancement of Nrf2 signaling and expression of its targets. Collectively, our finding confirmed that therapeutic strategy simultaneously exerting antioxidant and anti-inflammatory efficacy provide a novel feasible remedy for treating APSN-LN."

Journal • Complement-mediated Rare Disorders • Genetic Disorders • Glomerulonephritis • Hematological Disorders • Immunology • Inflammation • Inflammatory Arthritis • Lupus • Lupus Nephritis • Nephrology • Renal Disease • Systemic Lupus Erythematosus

The artemisinin analog SM934 alleviates dry eye disease in rodent models by regulating TLR4/NF-κB/NLRP3 signaling. (PubMed, Acta Pharmacol Sin) - "In LPS-treated RAW 264.7 cells, we demonstrated that pretreatment with SM934 (10 μM) impeded the upregulation of TLR4 and downstream NF-κB/NLRP3 signaling proteins. Collectively, artemisinin analog SM934 exerts therapeutic benefits on DED by simultaneously reserving the structural integrity of ocular surface and preventing the corneal and conjunctival inflammation, suggested a further application of SM934 in ophthalmic therapy, especially for DED."

Journal • Preclinical • Dry Eye Disease • Immunology • Ocular Inflammation • Ophthalmology • IL10 • IL6 • MYD88 • TLR4

Novel use for old drugs: The emerging role of artemisinin and its derivatives in fibrosis. (PubMed, Pharmacol Res) - "The present review summarizes the related studies on artemisinin treatment in fibrosis and elucidates the underlying mechanisms. We believe that this review can explain the potential anti-fibrotic value of artemisinin, outlining its potential use in the development of a safe and effective therapeutic method to alleviate fibrosis in the future."

Journal • Review • Fibrosis • Immunology • Infectious Disease • Oncology

A novel derivative of artemisinin inhibits cell proliferation and metastasis via down-regulation of cathepsin K in breast cancer. (PubMed, Eur J Pharmacol) - "Moreover, pathway enrichment was performed to understand the mechanism of action that Cathepsin K could adjust apoptosis regulator Bcl-X, and knockdown of Cathepsin K by SM934-Testosterone resulted in the reduction of Bcl-xL, which has been reported to be related to the proliferation and metastasis of cells. Collectively, SM934-Testosterone inhibited proliferation and metastasis ability of breast cancer cells via inhibiting the expression of Cathepsin K followed by the inhibition of Bcl-xL."

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