坦尼司特,一种用于治疗哮喘和慢性阻塞性肺疾病的新型吸入性磷酸二酯酶4抑制剂。

Tanimilast, A Novel Inhaled Pde4 Inhibitor for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease.

作者信息

Facchinetti Fabrizio, Civelli Maurizio, Singh Dave, Papi Alberto, Emirova Aida, Govoni Mirco

机构信息

Corporate Pre-clinical R&D, Chiesi, Parma, Italy.

Medicines Evaluation Unit, Manchester University NHS Foundation Hospital Trust, Manchester, United Kingdom.

出版信息

Front Pharmacol. 2021 Nov 23;12:740803. doi: 10.3389/fphar.2021.740803. eCollection 2021.

Abstract

Chronic respiratory diseases are the third leading cause of death, behind cardiovascular diseases and cancer, affecting approximately 550 million of people all over the world. Most of the chronic respiratory diseases are attributable to asthma and chronic obstructive pulmonary disease (COPD) with this latter being the major cause of deaths. Despite differences in etiology and symptoms, a common feature of asthma and COPD is an underlying degree of airways inflammation. The nature and severity of this inflammation might differ between and within different respiratory conditions and pharmacological anti-inflammatory treatments are unlikely to be effective in all patients. A precision medicine approach is needed to selectively target patients to increase the chance of therapeutic success. Inhibitors of the phosphodiesterase 4 (PDE4) enzyme like the oral PDE4 inhibitor roflumilast have shown a potential to reduce inflammatory-mediated processes and the frequency of exacerbations in certain groups of COPD patients with a chronic bronchitis phenotype. However, roflumilast use is dampened by class related side effects as nausea, diarrhea, weight loss and abdominal pain, resulting in both substantial treatment discontinuation in clinical practice and withdrawal from clinical trials. This has prompted the search for PDE4 inhibitors to be given by inhalation to reduce the systemic exposure (and thus optimize the systemic safety) and maximize the therapeutic effect in the lung. Tanimilast (international non-proprietary name of CHF6001) is a novel highly potent and selective inhaled PDE4 inhibitor with proven anti-inflammatory properties in various inflammatory cells, including leukocytes derived from asthma and COPD patients, as well as in experimental rodent models of pulmonary inflammation. Inhaled tanimilast has reached phase III clinical development by showing promising pharmacodynamic results associated with a good tolerability and safety profile, with no evidence of PDE4 inhibitors class-related side effects. In this review we will discuss the main outcomes of preclinical and clinical studies conducted during tanimilast development, with particular emphasis on the characterization of the pharmacodynamic profile that led to the identification of target populations with increased therapeutic potential in inflammatory respiratory diseases.

摘要

慢性呼吸道疾病是全球第三大致死原因,仅次于心血管疾病和癌症,影响着全球约5.5亿人。大多数慢性呼吸道疾病可归因于哮喘和慢性阻塞性肺疾病(COPD),其中后者是主要死因。尽管哮喘和COPD在病因和症状上存在差异,但两者的一个共同特征是存在潜在程度的气道炎症。这种炎症的性质和严重程度在不同的呼吸道疾病之间以及同一疾病内部可能有所不同,而且药理抗炎治疗不太可能对所有患者都有效。需要一种精准医学方法来有针对性地选择患者,以增加治疗成功的机会。磷酸二酯酶4(PDE4)抑制剂,如口服PDE4抑制剂罗氟司特,已显示出在某些具有慢性支气管炎表型的COPD患者群体中,有降低炎症介导过程和加重频率的潜力。然而,罗氟司特的使用因类相关副作用如恶心、腹泻、体重减轻和腹痛而受到限制,导致临床实践中大量治疗中断以及临床试验撤药。这促使人们寻找通过吸入给药的PDE4抑制剂,以减少全身暴露(从而优化全身安全性)并最大化肺部治疗效果。他尼米司特(CHF6001的国际非专利名称)是一种新型的高效选择性吸入PDE4抑制剂,在各种炎症细胞中,包括来自哮喘和COPD患者的白细胞,以及在肺部炎症的实验啮齿动物模型中,都具有已证实的抗炎特性。吸入他尼米司特已进入III期临床开发阶段,显示出有前景的药效学结果,具有良好的耐受性和安全性,且没有PDE4抑制剂类相关副作用的证据。在本综述中,我们将讨论他尼米司特开发过程中进行的临床前和临床研究的主要结果,特别强调药效学特征的描述,这些特征有助于确定在炎症性呼吸道疾病中具有更高治疗潜力的目标人群。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/627e/8650159/b55ccd5cb479/fphar-12-740803-g001.jpg

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