生物活性

• 描述Milbemycin oxime is a veterinary drug from the group of milbemycins, used as a broad spectrum antiparasitic. Absorption of actives was rapid at levels that provide the minimum effective doses of 2.5 mg/kg and 0.5 mg/kg of afoxolaner and milbemycin oxime, respectively. The pharmacokinetic profile for the combination of afoxolaner and milbemycin oxime supports the rapid onset and a sustained efficacy for afoxolaner against ectoparasites and the known endoparasitic activity of milbemycin oxime^[3]. Afoxolaner/milbemycin oxime soft chewables were shown to be safe when administered repeatedly at up to 5× the maximum exposure dose in dogs as young as 8 weeks of age^[4]. The efficacy of the afoxolaner plus milbemycin oxime combination was ≥98% against T. canis, ≥95.8% against T. leonina, and 90.2% against A. braziliense. Efficacy of the combination against A. caninum was 99.7%, while the efficacy of milbemycin oxime alone was 99.6% and the efficacy of afoxolaner alone was 2.1%. Thus, the high efficacy of the afoxolaner plus milbemycin oxime chewables against a broad range of canine intestinal nematode infections^[5]. Moreover, monthly administrations of NexGard Spectra® (the oral milbemycin oxime/afoxolaner combination) provided 100% preventive efficacy against canine thelaziosis^[6].
• 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
  NCT03554616	Malaria Anaem... more >>ia Collapse <<	Not Applicable	Not yet recruiting	October 31, 2021	Tanzania ... more >> District Misungwi Not yet recruiting Misungwi, Mwanza, Tanzania Collapse <<
  NCT00999700	Squamous Cell Carcinoma of the... more >> Head and Neck Collapse <<	Phase 3	Active, not recruiting	December 2021	Italy ... more >> Ospedale Civile Ss. Antonio E Biagio Alessandria, Italy Ausl Della Valle D' Aosta Aosta, Italy Policlinico S. Orsola-Malpighi Bologna, Italy Asl 8 - Ospedale Businco Cagliari, Italy A.S.O. S. Croce E Carle Cuneo, Italy, 12100 Irccs - Aou S. Martino - Oncology Genoa, Italy Irccs - Aou San Martino - Radiotherapy Genoa, Italy Asl 3 Genovese Genova, Italy E.O. Ospedali Galliera Genova, Italy Azienda Ospedaliera Villa Scassi - Asl3 Italy, Italy Istituto Nazionale Dei Tumori Milano, Italy Azienda Ospedaliero Universitaria Di Modena Modena, Italy Ospedale S. Giacomo Novi Ligure (al), Italy Azienda Ospedaliero-Universitaria Di Parma Parma, Italy Azienda Ospedaliera Ospedali Riuniti Di Fano Pesaro, Italy Arcispedale S. Maria Nuova Reggio Emilia, Italy Irccs Centro Di Riferimento Oncologico Di Basilicata (Crob) Rionero in Vulture (pz), Italy Ospedale S. Filippo Neri Roma, Italy Ospedale S. Paolo Savona, Italy A.O. Universitaria S. Giovanni Battista-Molinette Di Torino Torino (to) Turin, Italy A.O. Universitaria S. Giovanni Battista-Molinette Di Torino Turin, Italy Collapse <<

• 参考文献

• [1] Christie BL, Raines JA. Effect of an Otic Milbemycin Oxime Formulation on Tegastes acroporanus Infesting Corals. J Aquat Anim Health. 2016 Dec;28(4):235-239.

  [2] Lebon W, Tielemans E, et al. Monthly administrations of milbemycin oxime plus afoxolaner chewable tablets to prevent Angiostrongylus vasorum infection in dogs. Parasit Vectors. 2016 Sep 2;9(1):485.

  [3] Letendre L, Harriman J, Drag M, Mullins A, Malinski T, Rehbein S. The intravenous and oral pharmacokinetics of afoxolaner and milbemycin oxime when used as a combination chewable parasiticide for dogs. J Vet Pharmacol Ther. 2017;40(1):35‐43

  [4] Drag M, Saik J, Harriman J, Letendre L, Yoon S, Larsen D. Safety evaluation of orally administered afoxolaner and milbemycin oxime in eight-week-old dogs. J Vet Pharmacol Ther. 2017;40(5):447‐453

  [5] Fankhauser R, Hamel D, Dorr P, et al. Efficacy of oral afoxolaner plus milbemycin oxime chewables against induced gastrointestinal nematode infections in dogs. Vet Parasitol. 2016;225:117‐122

  [6] Lebon W, Guillot J, Álvarez MJ, et al. Prevention of canine ocular thelaziosis (Thelazia callipaeda) with a combination of milbemycin oxime and afoxolaner (Nexgard Spectra®) in endemic areas in France and Spain. Prévention de la thélaziose oculaire canine (Thelazia callipaeda) avec une association de milbémycine oxime et d’afoxolaner (Nexgard Spectra®) dans les zones d’endémie en France et en Espagne. Parasite. 2019;26:1

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