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A review of oral kallikrein inhibitor berotralstat for hereditary angioedema. 口服钾化肽抑制剂贝曲司他治疗遗传性血管性水肿的研究进展。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-02-01 DOI: 10.1358/dot.2022.58.2.3369191
YingYu Gao, Jacqueline Hwang, Gloria Hwang, Timothy Craig
{"title":"A review of oral kallikrein inhibitor berotralstat for hereditary angioedema.","authors":"YingYu Gao,&nbsp;Jacqueline Hwang,&nbsp;Gloria Hwang,&nbsp;Timothy Craig","doi":"10.1358/dot.2022.58.2.3369191","DOIUrl":"https://doi.org/10.1358/dot.2022.58.2.3369191","url":null,"abstract":"<p><p>Orladeyo, a once-daily oral formulation of berotralstat (formerly BCX-7353), is a novel oral small-molecule drug developed by BioCryst Pharmaceuticals for the prevention of hereditary angioedema (HAE) attacks. It was first approved by the U.S. Food and Drug Administration (FDA) in 2020, and in 2021 also gained approval for marketing in Japan and the European Union. Preclinical and phase I studies showed promising efficacy and safety, and several multicenter international Angioedema Prophylaxis (APeX) phase II and III trials have since been initiated to further evaluate berotralstat. The ongoing phase III APeX-2 trial showed a 67% reduction in HAE attacks at the standard 150-mg dosing. Mild to moderate gastrointestinal side effects are most commonly seen and minimal serious adverse effects have been reported. Other first-line therapies for HAE prophylaxis rely on burdensome subcutaneous or intravenous routes. Thus far berotralstat has shown to be effective and well tolerated for HAE prophylaxis with the convenience of once-daily oral dosing.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39940953","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Research progress in overcoming ibrutinib drug resistance. 克服伊鲁替尼耐药性的研究进展。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-02-01 DOI: 10.1358/dot.2022.58.2.3360405
Xiang-Yu Ma, Min Zhao, Yi-Dong Li, Yanglu Chen, Liuya Wei, Zhe-Sheng Chen
{"title":"Research progress in overcoming ibrutinib drug resistance.","authors":"Xiang-Yu Ma,&nbsp;Min Zhao,&nbsp;Yi-Dong Li,&nbsp;Yanglu Chen,&nbsp;Liuya Wei,&nbsp;Zhe-Sheng Chen","doi":"10.1358/dot.2022.58.2.3360405","DOIUrl":"https://doi.org/10.1358/dot.2022.58.2.3360405","url":null,"abstract":"<p><p>Ibrutinib, an oral small-molecule targeted drug, has been the first Bruton tyrosine kinase (BTK) inhibitor in the world to be approved for the market. It works by regulating cell proliferation, apoptosis and migration, and has been proven to exhibit high efficacy and good safety in the treatment of B-cell lymphomas, including chronic lymphocytic leukemia or small lymphocytic lymphoma and mantle cell lymphoma. However, some patients inevitably have drug resistance and disease recurrence, resulting in a poor prognosis. This article serves as a clinical reference by summarizing the related literature on ibrutinib resistance inhibitors.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39940956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An update on dapagliflozin for chronic kidney disease. 达格列净治疗慢性肾病的最新进展
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-02-01 DOI: 10.1358/dot.2022.58.2.3369188
Michael S Kelly
{"title":"An update on dapagliflozin for chronic kidney disease.","authors":"Michael S Kelly","doi":"10.1358/dot.2022.58.2.3369188","DOIUrl":"https://doi.org/10.1358/dot.2022.58.2.3369188","url":null,"abstract":"<p><p>Dapagliflozin is an oral agent for type 2 diabetes mellitus (T2DM) belonging to the sodium/glucose cotransporter 2 inhibitor (SGLT2-I) class of antihyperglycemic medications. In clinical trials, dapagliflozin has also been shown to reduce cardiovascular and major renal events. In the DAPA-CKD trial, dapagliflozin significantly reduced the composite renal outcome in patients with chronic kidney disease (CKD). Dapagliflozin represents a new pharmacologic option for reducing CKD progression in patients with and without diabetes.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39940954","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Loteprednol etabonate: a formulation for short-term use in inflammatory flares in dry eye disease. 来替诺依他巴酸:一种用于干眼病炎症发作的短期制剂。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-02-01 DOI: 10.1358/dot.2022.58.2.3367993
David M Paton
{"title":"Loteprednol etabonate: a formulation for short-term use in inflammatory flares in dry eye disease.","authors":"David M Paton","doi":"10.1358/dot.2022.58.2.3367993","DOIUrl":"https://doi.org/10.1358/dot.2022.58.2.3367993","url":null,"abstract":"<p><p>Loteprednol etabonate is a soft corticosteroid that is rapidly deactivated after reaching the general circulation, displaying good local activity and a high therapeutic index without inducing systemic side effects. In 2021, Kala Pharmaceuticals launched Eysuvis (loteprednol etabonate ophthalmic suspension) 0.25% in the U.S. for the short-term (up to 2 weeks) treatment of the signs and symptoms of dry eye disease. Approval by the Food and Drug Administration (FDA) was based on results from one phase II trial and three phase III trials showing Eysuvis significantly improved both the signs and symptoms of dry eye disease and was well tolerated. Eysuvis is a novel loteprednol etabonate nanosuspension formulation developed by Kala using its AMPPLIFY mucus-penetrating particle (MPP) drug delivery technology. Use of this MPP formulation results in enhanced penetration of loteprednol etabonate into target tissue on the ocular surface. Eysuvis is the first FDA-approved ocular corticosteroid indicated for dry eye disease.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39940955","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
Estetrol and drospirenone: a novel oral contraceptive. 炔雌醇和屈螺酮:一种新型口服避孕药。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-01-01 DOI: 10.1358/dot.2022.58.1.3353167
David M Paton
{"title":"Estetrol and drospirenone: a novel oral contraceptive.","authors":"David M Paton","doi":"10.1358/dot.2022.58.1.3353167","DOIUrl":"https://doi.org/10.1358/dot.2022.58.1.3353167","url":null,"abstract":"<p><p>Estetrol (E₄) is a natural human estrogen produced during human pregnancy in the fetal liver with a unique mechanism of action that displays tissue-selective activity, and behaves as a natural selective estrogen receptor modulator. E₄ acts as an estrogen agonist on the vagina, the uterus and the endometrium, and also shows bone-sparing activity. Its mechanism of action results in neutral impact on endocrine, metabolic and hemostatic parameters, compared with other oral contraceptives. In 2021, Health Canada approved the combination 15 mg E₄/3 mg drospirenone (DRSP), the first and only combined oral contraceptive based on the native estrogen E₄, which has been synthesized from plant-based sources. Shortly afterwards, the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) also approved the combination 14.2 mg E₄/3 mg DRSP as a female contraceptive.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39756899","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Telitacicept, a novel humanized, recombinant TACI-Fc fusion protein, for the treatment of systemic lupus erythematosus. Telitacicept是一种新的人源化重组TACI-Fc融合蛋白，用于治疗系统性红斑狼疮。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-01-01 DOI: 10.1358/dot.2022.58.1.3352743
Yong Fan, Dai Gao, Zhuoli Zhang
{"title":"Telitacicept, a novel humanized, recombinant TACI-Fc fusion protein, for the treatment of systemic lupus erythematosus.","authors":"Yong Fan,&nbsp;Dai Gao,&nbsp;Zhuoli Zhang","doi":"10.1358/dot.2022.58.1.3352743","DOIUrl":"https://doi.org/10.1358/dot.2022.58.1.3352743","url":null,"abstract":"<p><p>Systemic lupus erythematosus (SLE) is a chronic autoimmune disease, in which aberrant immune cells and proinflammatory mediators act as key players in the pathogenesis of the disease. Telitacicept (RC-18) is a novel, recombinant fusion protein, consisting of transmembrane activator and calcium modulator and cyclophilin ligand interactor (TACI) and the Fc portion of human immunoglobulin G (IgG) (TACI-Fc). It was designed to inhibit the activity of two target cytokines, the B-cell lymphocyte stimulator (BLyS, also known as the B-cell activation factor [BAFF]) and a proliferation-inducing ligand (APRIL), both of which are involved in B cell-mediated autoimmune diseases. In Chinese patients with moderate to severe SLE, subcutaneous telitacicept (80, 160 and 240 mg) in combination with standard therapy was associated with clinical benefit and appeared to be well tolerated. On March 9, 2021, the Chinese National Medical Products Administration (NMPA) granted telitacicept conditional marketing approval for the treatment of adult patients with active, autoantibody-positive SLE. Additionally, on April 15, 2020, the U.S. Food and Drug Administration (FDA) granted fast track designation to telitacicept for the treatment of SLE. Here, we provide a comprehensive review of the preclinical and clinical activity of telitacicept in SLE.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39756901","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 16
Ofatumumab for relapsing forms of multiple sclerosis. Ofatumumab用于多发性硬化症复发。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-01-01 DOI: 10.1358/dot.2022.58.1.3353168
Alberto Gajofatto, Riccardo Orlandi
{"title":"Ofatumumab for relapsing forms of multiple sclerosis.","authors":"Alberto Gajofatto,&nbsp;Riccardo Orlandi","doi":"10.1358/dot.2022.58.1.3353168","DOIUrl":"https://doi.org/10.1358/dot.2022.58.1.3353168","url":null,"abstract":"<p><p>In recent years, B cells have been extensively studied as a therapeutic target in multiple sclerosis (MS). Particularly, anti-CD20 monoclonal antibodies (MAbs) such as rituximab or ocrelizumab have proven to be effective in treating various forms of MS. Ofatumumab, a second-generation anti-CD20 IgG1κ fully human MAb, binds to a different, membrane-proximal epitope of CD20 compared with other anti-CD20 MAbs, thus ensuring a slower dissociation rate. This results in dose-dependent B-cell depletion mainly exerted through a mechanism of complement-dependent cytotoxicity. The repletion kinetic is faster than that of rituximab or ocrelizumab. Ofatumumab is the first approved drug for relapsing forms of MS that is administered via subcutaneous injection every 4 weeks. Two phase II and two phase III clinical trials have shown that it is effective in reducing the annualized relapse rate and clinical disability worsening, as well as in suppressing magnetic resonance imaging (MRI) disease activity. The safety profile of the drug has proven to be favorable, with good tolerability and low immunogenic risk. Moreover, the subcutaneous injection grants an easier way of administration. The current evidence on ofatumumab efficacy and safety is reviewed in the present article.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39756900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
An update on tenapanor to treat hyperphosphatemia. 泰纳帕诺治疗高磷血症的最新进展。
IF 1.8 4区 医学
Drugs of today Pub Date : 2022-01-01 DOI: 10.1358/dot.2022.58.1.3343689
Giuseppe Cianciolo, Simona Barbuto, Francesca Iacovella, Gaetano La Manna, Andrea Galassi, Paola Ciceri, Mario Cozzolino
{"title":"An update on tenapanor to treat hyperphosphatemia.","authors":"Giuseppe Cianciolo,&nbsp;Simona Barbuto,&nbsp;Francesca Iacovella,&nbsp;Gaetano La Manna,&nbsp;Andrea Galassi,&nbsp;Paola Ciceri,&nbsp;Mario Cozzolino","doi":"10.1358/dot.2022.58.1.3343689","DOIUrl":"https://doi.org/10.1358/dot.2022.58.1.3343689","url":null,"abstract":"<p><p>Hyperphosphatemia is a common feature in patients with chronic kidney disease (CKD), especially in those with end-stage renal disease (ESRD). Commonly, high serum phosphate levels are observed only in later stages of CKD. The control of hyperphosphatemia plays a key role in the management of CKD patients. However, the optimal range for serum phosphate levels in CKD patients is still controversial. Currently, phosphate binders are the only medications available to reduce elevated serum phosphate levels in patients with ESRD receiving hemodialysis. Tenapanor, an inhibitor of gastrointestinal sodium/hydrogen exchanger 3 (NHE3), acts via a non-phosphate-binding mechanism, reducing paracellular phosphate transport in the intestine. Has tenapanor the potential to improve management of mineral bone disorder in CKD?</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39756902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ponesimod to treat multiple sclerosis. Ponesimod治疗多发性硬化症。
IF 1.8 4区 医学
Drugs of today Pub Date : 2021-12-01 DOI: 10.1358/dot.2021.57.12.3353166
A Ianniello, C Pozzilli
{"title":"Ponesimod to treat multiple sclerosis.","authors":"A Ianniello,&nbsp;C Pozzilli","doi":"10.1358/dot.2021.57.12.3353166","DOIUrl":"https://doi.org/10.1358/dot.2021.57.12.3353166","url":null,"abstract":"<p><p>Ponesimod (ACT-128800) is a directly bioavailable, rapidly reversible sphingosine-1-phosphate (S1P) receptor modulator, highly selective for the subtype 1 (S1P₁ receptor). It acts by blocking the egress of lymphocytes from the lymphoid organs, thus limiting the entry of autoreactive cells into the central nervous system. Unlike fingolimod, ponesimod does not require monitoring of the first dose, thanks to a 14-day uptitration regimen, which markedly reduces the incidence of cardiodynamic effects related to the initiation of therapy. Results from the OPTIMUM phase III trial demonstrated the superiority of ponesimod over teriflunomide on disease activity markers, without unexpected safety concerns. Furthermore, the drug is eliminated within 1 week of discontinuation, allowing for the reversibility of its effects. Ponesimod was recently approved in both the U.S. and E.U. for the treatment of relapsing forms of multiple sclerosis. This review summarizes the pharmacological characteristics of ponesimod and the main studies that led to its approval.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39727552","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Delgocitinib in atopic dermatitis. 德尔格西替尼治疗特应性皮炎。
IF 1.8 4区 医学
Drugs of today Pub Date : 2021-12-01 DOI: 10.1358/dot.2021.57.12.3352760
J Ho, S Molin
{"title":"Delgocitinib in atopic dermatitis.","authors":"J Ho,&nbsp;S Molin","doi":"10.1358/dot.2021.57.12.3352760","DOIUrl":"https://doi.org/10.1358/dot.2021.57.12.3352760","url":null,"abstract":"<p><p>Delgocitinib ointment is a newly approved topical medication for the treatment of atopic dermatitis (AD). AD usually has onset in early childhood and is a common, often chronic relapsing inflammatory skin condition that affects all age groups. AD has a large impact on patients' quality of life including physical health and emotional impacts. Conventional management of AD consists of phototherapy and treatments that comprise corticosteroids (both topically and systemically), topical calcineurin inhibitors (tacrolimus and pimecrolimus) or systemic immunosuppressants like ciclosporin. New targeted therapies for AD, including interleukin (IL)-4/13 inhibitors, Janus kinase (JAK) inhibitors and IL-13 inhibitors have been introduced for both topical and systemic use. In this review, we give an overview of the use of delgocitinib, the first topical JAK inhibitor to be approved for AD, including its preclinical pharmacology, pharmacokinetics and metabolism, safety, existing clinical trials and future directions.</p>","PeriodicalId":11397,"journal":{"name":"Drugs of today","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39727035","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
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