Discovery of the Macrocycle (9E)-15-(2-(Pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a Potent Inhibitor of Janus Kinase 2/Fms-LikeTyrosine Kinase-3 (JAK2/FLT3) for the Treatment of Rheumatoid Arthritis

2012 ◽  
Vol 55 (6) ◽  
pp. 2623-2640 ◽  
Author(s):  
Anthony D. William ◽  
Angeline C.-H. Lee ◽  
Anders Poulsen ◽  
Kee Chuan Goh ◽  
Babita Madan ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Potent Inhibitor ◽  
Janus Kinase ◽  
Janus Kinase 2

scholarly journals A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis

2011 ◽  
Vol 13 (2) ◽  
pp. R68 ◽  
Author(s):  
Kristine L Stump ◽  
Lily D Lu ◽  
Pawel Dobrzanski ◽  
Cynthia Serdikoff ◽  
Diane E Gingrich ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Mouse Models ◽  
Janus Kinase ◽  
Janus Kinase 2 ◽  
Active Inhibitor ◽  
Orally Active

scholarly journals Effect of janus kinase inhibitors and methotrexate combination on malignancy in patients with rheumatoid arthritis: a systematic review and meta-analysis of randomized controlled trials

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Vinod Solipuram ◽  
Akhila Mohan ◽  
Roshniben Patel ◽  
Ruoning Ni
Keyword(s):  
Rheumatoid Arthritis ◽  
Combination Therapy ◽  
Randomized Controlled Trials ◽  
Random Effect ◽  
Janus Kinase ◽  
Controlled Trials ◽  
Randomized Controlled ◽  
Increased Risk ◽  
Significant Difference ◽  
Risk Of Malignancy

Abstract Background Rheumatoid arthritis (RA) is a systemic autoimmune disease. The combination therapy of methotrexate (MTX) and Janus kinase inhibitor (JAKi) is commonly used. Patients with RA are at increased risk of malignancy, however, it remains unclear whether the combination therapy is associated with a higher risk. Objective To assess the malignancy risk among patients with RA receiving combination therapy of JAKi and MTX compared to MTX alone. Methods PubMed, Cochrane and Embase were thoroughly searched for randomized controlled trials (RCTs) in patients with RA receiving JAKi and MTX, from inception to July 2020. Primary endpoints were malignancy events, Non melanomatous skin cancer (NMSC) and malignancy excluding NMSC and secondary endpoints were serious adverse events (SAE), deaths. Risk ratio (RR) and 95% CI were calculated using the Mantel–Haenszel random-effect method. Results 659 publications were screened and 13 RCTs with a total of 6911 patients were included in the analysis. There was no statistically significant difference in malignancy [RR = 1.42; 95% CI (0.59, 3.41)], neither NMSC [RR = 1.44 (0.36, 5.76)] nor malignancies excluding NMSC [RR = 1.12 (0.40, 3.13)]. No statistically significant difference between the two groups for SAE [RR = 1.15 (0.90, 1.47)] and deaths [RR = 1.99 (0.75, 5.27)] was found. Conclusion The adjunction of JAKi to MTX is not associated with an increased risk of malignancy when compared to MTX alone. There is no increased risk of SAE and deaths when compared to MTX alone in patients with RA.

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