生物活性

• 描述Fexofenadine HCl is the acid metabolite of terfenadine (Seldane). fexofenadine HCl has no significant effect on QTc(corrected QT interval), even at doses > 10-fold higher than that is efficacious for SAR(seasonal allergic rhinitis) ^[3]. Fexofenadine is a highly specific, H1-receptor antagonist with a safety profile similar to placebo. Fexofenadine has a high margin of safety and is also well tolerated in subjects with renal or hepatic impairment, in children and the elderly. The recommended dose of fexofenadine HC1 is 120 mg daily for SAR (either as 120 mg once daily or 60 mg twice daily) or 180 mg once daily for CIU^[4]. Fexofenadine is highly selective for peripheral H(1)-receptors and does not cross the blood-brain barrier. Fexofenadine has also been shown to have a favorable effect on nasal congestion. This therapeutic advantage might be related to its significant antiallergic properties, ie, the demonstrated ability of fexofenadine to blunt the inflammatory effects of preformed and de novo synthesized mediators at clinically relevant doses in vivo and in vitro^[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
  NCT01375790	Aging	Phase 3	Completed	-	Spain ... more >> Albada Centre Socio Sanitari Parc Taulí Sabadell, Babadell, Spain, 08208 Ballesol Badalona Badalona, Barcelona, Spain, 08911 Ballesol Barberà Barberà del Vallès, Barcelona, Spain, 08210 Residència Allegra Sabadell, Barcelona, Spain, 08203 Residència Poble Nou Barcelona, Spain, 08005 Ballesol Fabra i Puig Barcelona, Spain, 08016 Ballesol Almogàvers Barcelona, Spain, 08018 Residència Mapfre Quavitae Barcelona, Spain, 08025 Residència AMMA Horta Barcelona, Spain, 08035 Residència Collserola (Mutuam) Barcelona, Spain, 08035 Collapse <<
  NCT02796898	Prostate Cancer ... more >> Rising Prostate Specific Antigen (PSA) Collapse <<	Phase 1 Phase 2	Recruiting	December 31, 2019	United States, New Jersey ... more >> AdvanceMed Research Completed Lawrence, New Jersey, United States, 08648 United States, New York Montefiore Medical Center- Montefiore Medical Park Not yet recruiting Bronx, New York, United States, 10461 Contact: Gartrell Benjamin, MD    718-405-8404    bgartrel@montefiore.org    Eastchester Center for Cancer Care Recruiting Bronx, New York, United States, 10469 Contact: Carmen Vicuna    718-732-4078    cvicuna@nycancer.com    AccuMed Research Associates Recruiting Garden City, New York, United States, 11530-1664 Contact: Tammi Allegra, RN    516-746-2190    tallegra.accumedresearch@gmail.com    United States, Pennsylvania MidLantic Urology Recruiting Bala-Cynwyd, Pennsylvania, United States, 19004 Contact: Cheryl A Zinar, RN, BSN    610-667-0458       Principal Investigator: Laurence H Belkoff, DO Collapse <<
  NCT00078195	Hay Fever Hyp... more >>ersensitivity Allergy Rhinitis Collapse <<	Phase 2	Completed	-	United States, Iowa ... more >> University of Iowa Iowa City, Iowa, United States, 52242 United States, Nebraska Creighton University Omaha, Nebraska, United States, 68131 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53705 Collapse <<

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• 参考文献

• [1] Corcostegui R, Labeaga L, et al. Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D. 2005;6(6):371-84.

  [2] Petri N, Tannergren C, et al. Transport characteristics of fexofenadine in the Caco-2 cell model. Pharm Res. 2004 Aug;21(8):1398-404.

  [3] Pratt CM, Mason J, Russell T, Reynolds R, Ahlbrandt R. Cardiovascular safety of fexofenadine HCl. Am J Cardiol. 1999 May 15;83(10):1451-4

  [4] Mason J, Reynolds R, Rao N. The systemic safety of fexofenadine HCl. Clin Exp Allergy. 1999 Jul;29 Suppl 3:163-70; discussion 171-3

  [5] Meeves SG, Appajosyula S. Efficacy and safety profile of fexofenadine HCl: a unique therapeutic option in H1-receptor antagonist treatment. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S69-77

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