Lodenafil carbonate

近日，吉利德科学（Gilead Sciences）宣布其新型HIV抗病毒药衣壳抑制剂Lenacapavir (Sunlenca) 获得了在欧洲委员会（EC）的上市许可，用于联合其他抗逆转录病毒药物治疗多重耐药HIV感染的成人患者。Lenacapavir是一种具有多阶段作用机制的”first-in-class”衣壳抑制剂，是第一个旨在实现超长效治疗，即半年注射一次的HIV药物。虽然其被EC批准的指征具有很强限定性（多耐药情况下），并且需要与其他口服药物同时使用，而不是单一的每6个月注射一次，但是Lenacapavir的上市依然是HIV治疗领域的一个巨大突破。HIV与AIDSHIV即人类免疫缺陷病毒，于1983年被首次发现并命名为淋巴腺病相关病毒（LAV），后更名为人类免疫缺陷病毒或艾滋病病毒（HIV），感染后会导致获得性免疫缺陷综合征（AIDS），即通常所讲的艾滋。HIV是一种RNA逆转录病毒，由被膜、圆锥形衣壳核心、逆转录酶以及其RNA四个部分组成，其会通过膜上的两种糖蛋白gp120和gp41与其人体主要受体CD4+T细胞进行吸附融合，从而穿入细胞膜，并以其RNA为模板，通过逆转录酶合成单链DNA，继而在DNA聚合酶的作用下合成双链DNA。再通过后续的整合、转录、翻译形成多肽链，多肽链经历病毒蛋白酶的蛋白水解加工，其蛋白质和RNA于细胞膜上进行组装出芽，以此完成病毒在体内的复制过程（图1）。 图 1 HIV复制过程（图片来源：参考文献1）实际上，HIV感染本身并不会导致病人死亡，但其会对人体免疫系统进行攻击，在HIV相关免疫缺陷的情况下，感染者往往会并发心血管疾病及诸多恶性疾病，对感染者的生存造成了极大影响。HIV治疗历史距1983年首次发现病毒，历时四年时间，齐多夫定于1987年3月19日获批上市，成为首个抗艾滋病药物。凭借其确切的疗效，时至今日，齐多夫定也是重要的抗艾药物，且为“鸡尾酒疗法”最基本的成分之一。目前针对HIV的治疗，最有效的疗法即为“鸡尾酒疗法”，又称为高效抗逆转录病毒治疗，即通过使用三种或三种以上的抗病毒药物对艾滋病进行治疗，此种方法通过采用药物组合方案，以实现最大可能的益处、耐受性和依从性，并降低耐药发展的风险。经典的抗艾滋病药物可分为六类： 1. 核苷逆转录酶抑制剂 (NRTIs)：与病毒脱氧核苷酸结构类似，与其竞争性结合病毒逆转录酶，从而抑制逆转录酶的作用，阻碍病毒合成。其代表药物有齐多夫定、扎西他滨、司他夫定、拉米夫定、恩曲他滨等。2. 非核苷逆转录酶抑制剂 (NNRTIs)：与核苷逆转录酶抑制剂不用，此类药物是通过与HIV逆转录酶聚合位点附近的疏水口袋结合而发挥作用。其代表药物有奈韦拉平、依法韦伦和地拉韦啶等。3. 蛋白酶抑制剂 (PI)：通过抑制蛋白酶活性，使得蛋白前体不能裂解，从而无法形成成熟病毒体。其代表药物有沙奎那韦、利托那韦、氨普瑞那韦、洛匹那韦、福沙普列那韦、替普拉那韦等。4. 融合抑制剂 (FIs)：以N-HR或C-HR为靶点，抑制HIV的融合活性，从而阻止病毒进入宿主细胞内。其代表药物有恩夫韦地。5. 整合酶抑制剂 (INIs)：此类药物通过竞争性结合于整合酶的活化位点，从而抑制整合酶活性，导致病毒不能整合入宿主细胞，从而阻断病毒的复制过程。其代表药物有雷特格韦。6. 共受体抑制剂 (CRIs)：代表药物马拉韦罗，是一类CCR5拮抗剂，通过抑制CCR5辅助受体与病毒膜上糖蛋白gp120的结合从而导致病毒无法进入宿主细胞，阻断复制过程。图2 经典的抗逆转录病毒药物（图片来源：参考文献3）尽管“鸡尾酒”疗法成效显著，但艾滋病之外的其他副作用、耐药问题也逐渐显露。更重要的是，长效制剂才是接近治愈目标的全新途径。闪耀新星：衣壳抑制剂Lenacapavir，是一种first-in-class的长效HIV抑制剂，也是一款具有多阶段作用机制的首创衣壳抑制剂，主要通过稳定HIV遗传物质和必需酶的锥形外壳并由此防止感染细胞中衣壳的分解来抑制HIV-1的复制。由于其作用和机制区别于经典的抗艾滋病药物，故目前对其他类别的抗艾滋病药物没有已知的交叉耐药性。lenacapavir以前称为GS-6207或GS-CA2，它的发展源自PF-3450074（PF74）的优化，PF74是一种围绕苯丙氨酸核心构建的拟肽化合物，在氨基和羧酸端分别用吲哚-3-乙酸和苯胺部分封端（图3）。PF74可干扰衣壳的组装和拆卸，并与HIV-1辅因子Nup153和CPSF6结合，从而达到抑制HIV复制的目的。 图 3 发展中的代表性组装和拆卸抑制剂的结合位点的位置（图片来源：参考文献3）本次EC批准Lenacapavir是基于一项双盲、安慰剂对照的全球多中心II/III期CAPELLA研究数据，旨在评估Lenacapavir与优化背景治疗方案联合用于既往接受过多次治疗、多重耐药HIV患者的疗效与安全性。结果显示，在显著未满足医疗需求的患者人群中，83%（n=30/36）接受优化背景方案的基础上加用Lenacapavir的受试者在第52周时达到不可检测的病毒载量（<50拷贝/mL）。此外，CAPELLA受试者的CD4计数平均增加83个细胞/µL。在安全性方面，试验过程中未出现与Lenacapavir相关的严重不良事件。此次Lenacapavir在欧洲获批上市，适用于欧盟所有 27 个成员国，以及挪威、冰岛和列支敦士登。值得一提的是，去年12月，由于药物溶液与硼硅酸盐玻璃小瓶之间的相容性问题，Lenacapavir多达10项临床试验被FDA叫停。今年5月，FDA解除了Lenacapavir的相关临床搁置。2022年7月，FDA接受了Lenacapavir重新提交的NDA申请，处方药用户费用法案 (PDUFA) 的行动日期指定为2022年12月27日。展  望自 1987 年首个抗 HIV 药物齐多夫定上市，到“鸡尾酒”疗法的诞生使艾滋病得到了有效的控制。如今，寻求长效、治愈抗艾药物成为未来治疗的方向。除了Lenacapavir，还有多款新机制抗HIV新药也取得了研发进展。ImmunityBio公司研发的IL-15超级激动剂N803，能够诱导NK细胞和CD8+T细胞增殖分化，从而杀伤被感染HIV的细胞，其Ⅰ期临床试验表明使用N-803的参与者在治疗后长达六个月的时间里，血液中的 HIV 感染细胞显着减少，且未见显著不良事件。莫德纳的艾滋病mRNA疫苗：mRNA-1574和mRNA-1644，利用mRNA技术激发针对HIV的中和抗体，从而使人体免疫系统对HIV产生抵抗作用。目前两者均投入临床试验，且在Ⅰ期中取得了较好的安全性和有效性。医克生物的治疗用艾滋病核酸注射液，可通过诱导人体产生光谱中和抗体作用抵御HIV，目前已获得临床试验默示许可。抗逆转录病毒疗法（ART）虽然可以控制HIV的复制，但并不能治愈艾滋病，它仍然深深困扰着感染者，带给感染者无尽的痛苦。可我们仍相信随着新靶点药物和疫苗的不断探索，有朝一日，我们一定能够做到预防甚至治愈这个潜藏在人体中的恶魔。 【参考文献】1. De Clercq E. Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int J Antimicrob Agents.2009;33(4):307-320.doi:10.1016/j.ijantimicag.2008.10.0102. Kovacs L, Kress T C, Belin de Chantemèle E J. HIV, combination antiretroviral therapy, and vascular diseases in men and women[J]. Basic to Translational Science.2022; 7(4): 410-421.doi:10.1016/j.jacbts.2021.10.0173. Menéndez-Arias L, Delgado R. Update and latest advances in antiretroviral therapy. Trends Pharmacol Sci. 2022;43(1):16-29. doi: 10.1016/j.tips.2021.10.004声明：本文观点仅代表作者本人，不代表药智网立场，欢迎在留言区交流补充；如需转载，请务必注明文章作者和来源。如涉及作品内容、版权和其它问题，请在本平台留言，我们将在第一时间删除。责任编辑 | 琉  璃排版设计 | 惜  姌媒体合作 | 17316793441（微信号：18323856316）投稿爆料 | 17783467842（同微信）转载授权 | 18523380183（同微信）发现“分享”和“赞”了吗，戳我看看吧

NEW YORK , June 22, 2022 /PRNewswire/ -- As per Zion Market Research study, The global erectile dysfunction drugs market reached nearly USD 3.64 billion in 2021 and is projected to expand with a compound annual growth rate (CAGR) of approximately 6.9 percent over the forecast period to grow by about USD 5.94 billion by 2028. Key Industry Insights & Finding of the Erectile Dysfunction Drugs Market Reports: As per the analysis shared by our research analyst, the Erectile Dysfunction Drugs Market is expected to grow annually at a CAGR of around 6.9 % (2022-2028). Through the primary research, it was established that the Erectile Dysfunction Drugs Market was valued approximately USD 3.64 Billion in 2021 and is projected to reach to roughly USD 5.94 Billion by 2028. This is mainly due to the expanding senior population and superior healthcare infrastructure, as per a Rural Health Information Center report released in April 2019 stated that there are more than 46 million older persons in the United States, with that figure predicted to climb to about 90 million by 2050. ED is particularly frequent in men over the age of 40, the rise in the elderly male population is predicted to increase the number of individuals suffering from it. Erectile dysfunction drugs are majorly sold in developed and emerging economies; however, the percentage of their sale is less in low- and middle-income countries. Zion Market Research published the latest report titled as "Erectile Dysfunction Drugs Market By Therapeutics (Existing Drugs, Tadalafil, Sildenafil Citrate Vardenafil, Udenafil, Stendra/Spedra, Lodenafil Carbonate, Mirodenafil Pipeline Drugs, Apomorphine, Alprostadil, Topiglan, Gene Therapy, And Melanocortin Activators), And By Region – Global And Regional Industry Overview, Market Intelligence, Comprehensive Analysis, Historical Data, And Forecasts 2022 – 2028." into their research database. Erectile Dysfunction Drugs Market : Overview Erectile dysfunction is the incapability to attain and maintain a hard erection for sexual activity. Having problems with erection isn't usually a reason for fear. However, if erectile dysfunction is a long-term condition, it can create stress, lower self-esteem, and lead to marital issues. Problems obtaining or maintaining an erection can be a symptom of a more serious underlying health issue, as well as a possible risk for cardiovascular disease. To treat such conditions several drugs are available on the market that can help to maintain the erection during sexual intercourse. With a change in lifestyle and increased stress conditions need for these drugs is on the rise. Get a Free Sample Report with All Related Graphs & Charts (with COVID 19 Impact Analysis): Our Free Sample Report Includes: 2022 Updated Report Introduction, Overview, and In-depth industry analysis COVID-19 Pandemic Outbreak Impact Analysis Included 190 + Pages Research Report (Inclusion of Updated Research) Provide Chapter-wise guidance on Request 2022 Updated Regional Analysis with Graphical Representation of Size, Share & Trends Includes Updated List of tables & figures Updated Report Includes Top Market Players with their Business Strategy, Sales Volume, and Revenue Analysis Zion Market Research methodology Industry Dynamics: Erectile Dysfunction Drugs Market : Growth Drivers Growth in embracing poor lifestyle choices may boost the market growth over the forecast period. With the surge in the adoption of a bad lifestyle, diabetes, obesity, and cardiovascular disease are on the rise, which in turn leads to problems like ED as people become older. The present lifestyle of youth in many emerging countries is very stressful resulting in increased alcoholism, smoking, and fast food or ready-to-eat food consumption. Due to these factors, overall health and fitness are getting compromised which in turn increases the chances of ED. Furthermore, as the senior population grows, so does the number of ED patients, which is a significant driver of the global erectile dysfunction drugs market throughout the projection period. Erectile Dysfunction Drugs Market : Restraints Low awareness and side effects associated with erectile dysfunction drugs may hinder the market growth. Erectile dysfunction drugs are majorly sold in developed and emerging economies; however, the percentage of their sale is less in low- and middle-income countries. This is mainly due to less knowledge about these types of medication, low buying power, and less willingness to adopt such kinds of medications in lifestyle. Furthermore, side effects associated with these drugs such as headache, upset stomach, flushing, nasal congestion, vision problems, dizziness, diarrhea, and rash also contribute to the slow growth of the market. Directly Purchase a Copy of the Report @ Global Erectile Dysfunction Drugs Market : Opportunities Increased pharmaceutical manufacturing in emerging countries is likely to offer better growth opportunities for market expansion. In the last couple of years, major and emerging brands in pharmaceutical industries have increased their investments in emerging countries like India, China, Africa, and major Middle East countries. This has significantly lowered the cost of medicine along with the supply and the distribution of drugs within the countries which is expected to offer significance. Furthermore, increased investments in advertisements are also likely to contribute significantly to the expansion of the global erectile dysfunction drugs market. Global Erectile Dysfunction Drugs Market : Challenges An increase in the availability of counterfeit erectile dysfunction medicines poses a major challenge to the market expansion. The expanding manufacture of generic erectile dysfunction pharmaceuticals, as well as the growing availability of bogus erectile dysfunction drugs, are two important challenges for the market. Consumers typically choose lower-cost generic erectile dysfunction pills over more expensive blockbuster kinds due to the profitable marketing of counterfeit erectile dysfunction drugs at considerably cheaper prices than either patented or generic pharmaceuticals. Aside from that, when patents on blockbuster pharmaceuticals expire, new generic equivalents are entering the market, generally at inexpensive rates. Global Erectile Dysfunction Drugs Market : Segmentation The global erectile dysfunction market is categorized based on therapeutics and region. By therapeutics, the global erectile dysfunction market is bifurcated into Existing drugs, Tadalafil, Sildenafil Citrate Vardenafil, Udenafil, Stendra/Spedra, Lodenafil Carbonate, Mirodenafil Pipeline drugs, Apomorphine, Alprostadil, Topiglan, Gene Therapy, and Melanocortin Activators. Get More Insight before [email protected] : List of Key Players of Erectile Dysfunction Drugs Market : Eli Lilly & Co. Pfizer Dong-A Pharmaceutical Co. Ltd Bayer AG Meda Pharmaceuticals Vivus Inc. Apricus Biosciences. Key questions answered in this report: What are the growth rate forecast and market size for Erectile Dysfunction Drugs Market ? What are the key driving factors propelling the Erectile Dysfunction Drugs Market forward? What are the most important companies in the Erectile Dysfunction Drugs Market Industry? What segments does the Erectile Dysfunction Drugs Market cover? How can I receive a free copy of the Erectile Dysfunction Drugs Market sample report and company profiles? Report Scope: Free Brochure: Recent Developments May 2020, Metuchen Pharmaceuticals, L.L.C., a privately owned biopharmaceutical aimed at defining, developing, gaining, and commercializing revolutionary therapeutics for male sexual health conditions, and Neurotrope, Inc. ("Neurotrope") officially revealed that the two firms have decided to enter into a concise merger agreement within which Metuchen and Neurotrope, Inc. will unite in an all-stock purchase arising in a newly formed partnership firm ("Petros"). Petros is anticipated to become a Nasdaq-listed corporation specializing in men's health. Regional Dominance: North America is projected to lead the global market over the forecast period. North America is likely to dominate the global erectile dysfunction drugs market. This is mainly due to the expanding senior population and superior healthcare infrastructure, as per a Rural Health Information Center report released in April 2019 stated that there are more than 46 million older persons in the United States, with that figure predicted to climb to about 90 million by 2050. When the last of the baby boom cohorts reach 65, the number of older individuals is predicted to climb by roughly 18 million between 2020 and 2030. Because ED is particularly frequent in men over the age of 40, the rise in the elderly male population is predicted to increase the number of individuals suffering from it. The domination of these countries is due to the availability of numerous ED medicines by OTC and internet outlets. The National Institute of Diabetes and Digestive and Kidney Diseases stated roughly 30 million men in the United States suffer from ED. Furthermore, the United States has the greatest rate of self-reported ED. As a result, rising ED prevalence in the US is likely to fuel market growth throughout the projection period. Global Erectile Dysfunction Drugs Market is segmented as follows: Erectile Dysfunction Drugs Market : By Therapeutics Type Outlook (2022-2028) Existing drugs Tadalafil Sildenafil Citrate Vardenafil Udenafil Stendra/Spedra Lodenafil Carbonate Mirodenafil Pipeline drugs Apomorphine Alprostadil Topiglan Gene Therapy Melanocortin Activators Erectile Dysfunction Drugs Market : By Region Outlook (2022-2028) North America The U.S. Canada Europe France The UK Spain Germany Italy Rest of Europe Asia Pacific China Japan India South Korea Southeast Asia Rest of Asia Pacific Latin America Brazil Mexico Rest of Latin America Middle East & Africa GCC South Africa Rest of Middle East & Africa Press Release For Erectile Dysfunction Drugs Market : Browse Other Related Research Reports from Zion Market Research Medical Enzyme Technology Market - Global Industry Analysis : The global Medical Enzyme Technology market accrued earnings worth approximately 4.5(USD Billion) in 2020 and is predicted to gain revenue of about 6.7(USD Billion) by 2028, is set to record a CAGR of nearly 6.2% over the period from 2021 to 2028. 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