生物活性

• 描述Loxoprofen (LOX) is a non-selective cyclooxygenase inhibitor that is widely used for the treatment of pain and inflammation caused by chronic and transitory conditions. In addition, LOX can also be converted into an inactive hydroxylated metabolite (OH-LOXs) by cytochrome P450 (CYP) ^[3]. Loxoprofen (Loxonin(®), Loxonin(®) Pap, Loxonin(®) Tape) is a prodrug-type NSAID that is available in several formulations, including 60 mg tablets, 100 mg hydrogel patches and 50 or 100 mg tape. Loxoprofen is a useful analgesic option for patients with pain and inflammation, with topical loxoprofen potentially reducing the risk of gastrointestinal, cardiovascular and renal complications associated with oral NSAID use^[4]. The uptake of loxoprofen into Caco-2 cells was pH- and concentration-dependent, and was described by a Michaelis-Menten equation with passive diffusion (Km : 4.8 mm, Vmax : 142 nmol/mg protein/30 s, and Kd : 2.2 μl/mg protein/30 s). Transport of loxoprofen in Caco-2 cells is, at least in part, mediated by a proton-dependent transport system^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02384928	Sciatica Inte... more >>rvertebral Disc Displacement Collapse <<	Not Applicable	Completed	-	Korea, Republic of ... more >> Jaseng Hospital of Korean Medicine Seoul, Gangnam-Gu, Korea, Republic of, 135-896 Collapse <<
  NCT03386149	Lumbar Disc Herniation	Phase 3	Recruiting	September 30, 2018	Korea, Republic of ... more >> Dongguk University Bundang Oriental Hospital Recruiting Seongnam, Gyeonggi, Korea, Republic of, 13601 Contact: Eun-Jung Kim, PhD., KMD    +82317103751    hanijjung@naver.com    Daegu Korean Medicine Hospital of Daegu Haany University Recruiting Daegu, Korea, Republic of, 42158 Contact: I-Rang Choi, B.S    +82537702324    soongood88@dhu.ac.kr    Kyunghee University Medical Center Recruiting Seoul, Korea, Republic of, 02447 Contact: Sae-Rom Jeon, B.S.    +821050478756    sr9213@naver.com    Kyung Hee University Hospital at Gangdong Recruiting Seoul, Korea, Republic of, 05278 Contact: Bonhyuk Goo, M.S., KMD    +8224406099    goobh99@naver.com Collapse <<
  NCT02467504	Rheumatoid Arthritis	Phase 2	Unknown	June 2017	China, Beijing ... more >> Department of Rheumatology and Immunology, Peking University People's Hospital Recruiting Beijing, Beijing, China, 100044 Contact: Xiaoying Zhang, MD    +8613810001444    xiaoying19880307@163.com Collapse <<

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• 参考文献

• [1] Hiroshima Y, Kato T, Tajima K. Regression of diffuse large B-cell lymphoma in sphenoid and ethmoid sinuses following treatment with loxoprofen. Leuk Lymphoma. 2016;57(3):721-3.

  [2] Kanda A, Ebihara S, et al. Loxoprofen sodium suppresses mouse tumor growth by inhibiting vascular endothelial growth factor. Acta Oncol. 2003;42(1):62-70.

  [3] Paudel S, Shrestha A, Cho P, et al. Assessing Drug Interaction and Pharmacokinetics of Loxoprofen in Mice Treated with CYP3A Modulators. Pharmaceutics. 2019;11(9):479. Published 2019 Sep 16

  [4] Greig SL, Garnock-Jones KP. Loxoprofen: A Review in Pain and Inflammation. Clin Drug Investig. 2016;36(9):771-781

  [5] Narumi K, Kobayashi M, Kondo A, et al. Characterization of loxoprofen transport in Caco-2 cells: the involvement of a proton-dependent transport system in the intestinal transport of loxoprofen. Biopharm Drug Dispos. 2016;37(8):447-455

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