Synthesis of TNF inhibitor, flurbiprofen and an i-Pr analogue in enantioenriched forms by copper-catalyzed propargylic substitution with Grignard reagents

2021 ◽  
Author(s):  
Yuji Takashima ◽  
Yukari Isogawa ◽  
Atsuki Tsuboi ◽  
Narihito Ogawa ◽  
Yuichi Kobayashi
Keyword(s):  
Tumor Necrosis Factor ◽  
Substitution Reaction ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Inhibitor ◽  
Grignard Reagents ◽  
Tnf Inhibitor ◽  
Factor Inhibitor ◽  
Propargylic Substitution ◽  
Necrosis Factor

The copper-catalyzed substitution reaction of 5-(TBDPS-oxy)-1-(TMS)pent-1-yn-3-yl phosphate with [3-(cyclopentyloxy)-4-methoxyphenyl]MgBr, followed by several transformations, afforded the tumor necrosis factor inhibitor possessing a Ph-acetylene moiety. The inhibitor was also synthesized from 5-(TBDPS-oxy)-1-(Ph)pent-1-yn-3-yl...

scholarly journals Switch rates and total cost associated with apremilast and biologics in biologic-naive patients with psoriatic arthritis

2021 ◽  
Author(s):  
David L Kaplan ◽  
Brian L Ung ◽  
Corey Pelletier ◽  
Chuka Udeze ◽  
Ibrahim Khilfeh ◽  
...  
Keyword(s):  
Psoriatic Arthritis ◽  
Tumor Necrosis Factor ◽  
Real World ◽  
Tumor Necrosis ◽  
Claims Data ◽  
Tumor Necrosis Factor Inhibitor ◽  
Total Cost ◽  
Factor Inhibitor ◽  
Treatment Data ◽  
Necrosis Factor

Aim: Real-world treatment data for psoriatic arthritis are limited. We evaluated switch rates, adherence, and costs for patients initiating apremilast versus tumor necrosis factor inhibitor (TNFi) and interleukin inhibitor (ILi) among biologic-naive psoriatic arthritis patients. Materials & methods: This retrospective analysis used IBM MarketScan claims data to assess treatment switches, adherence and costs. Results: Twelve-month switch rates were significantly lower for apremilast versus TNFi (15.5% vs 26.6%; p < 0.0001) and similar to ILi (15.5% vs 14.0%; p = 0.71). Apremilast initiators had lower total costs versus TNFi and ILi (US$39,854 vs US$57,243 and US$65,687; p < 0.05) and adherence was slightly lower versus TNFi and higher versus ILi. Conclusion: Biologic-naive apremilast initiators had lower switch rates versus TNFi initiators and lower total costs versus TNFi or ILi initiators.

Effectiveness of a second biologic after failure of a non-tumor necrosis factor inhibitor as first biologic in rheumatoid arthritis

2021 ◽  
pp. jrheum.201467
Author(s):  
Katerina Chatzidionysiou ◽  
Merete Lund Hetland ◽  
Thomas Frisell ◽  
Daniela Di Giuseppe ◽  
Karin Hellgren ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Tumor Necrosis Factor ◽  
Disease Activity ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Inhibitor ◽  
Primary Response ◽  
Low Disease Activity ◽  
Factor Inhibitor ◽  
Disease Modifying ◽  
Necrosis Factor

Objective In Rheumatoid Arthritis (RA), evidence regarding the effectiveness of a second biologic Disease Modifying Anti-Rheumatic Drugs (bDMARDs) in patients whose first ever bDMARD was a non-tumor-necrosis-factor-inhibitor (TNFi) bDMARD is limited. The objective of this study was therefore to assess the outcome of the second bDMARD (non-TNFi [rituximab, abatacept or tocilizumab, separately] and TNFi) after failure of a non-TNFi bDMARD as first bDMARD. Methods We identified RA patients from the five Nordic biologics registers started treatment with a non-TNFi as first ever bDMARD but switched to a second bDMARD. For the second bDMARD, we assessed survival-on-drug (at 6 and 12 months), and primary response (at 6 months). Results We included 620 patients starting a second bDMARD (ABA 86, RTX 40, TCZ 67 and TNFi 427) following failure of a first non-TNFI bDMARD. At 6 and 12 months after start of their second bDMARD, around 70% and 50%, respectively, remained on treatment, and at 6 months less than one third of patients were still on their second bDMARD and had reached low disease activity or remission according to DAS28. For those patients whose second bMDARD was a TNFI, the corresponding proportion was slightly higher (40%). Conclusion The survival-on-drug and primary response of a second bDMARD in RA patients switching due to failure of a non-TNFi bDMARD as first bDMARD is modest. Some patients may benefit from TNFi when used after failure of a non-TNFi as first bDMARD.

Effects of Tumor Necrosis Factor Inhibitor on Stress-Shielded Tendons

Orthopedics ◽  
2016 ◽  
Vol 40 (1) ◽  
pp. 49-55 ◽  
Author(s):  
Kang Chen ◽  
Ping Li ◽  
Huakun Zhao ◽  
Xiaoyan Yan ◽  
Yanhong Ma
Keyword(s):  
Tumor Necrosis Factor ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Inhibitor ◽  
Factor Inhibitor ◽  
Necrosis Factor
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