Pub Date : 2021-02-26DOI: 10.1002/9783527826872.index
{"title":"Index","authors":"","doi":"10.1002/9783527826872.index","DOIUrl":"https://doi.org/10.1002/9783527826872.index","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"117162331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-07DOI: 10.1002/9783527814695.ch5
A. Baruch, D. Maclean
{"title":"Discovery of Etelcalcetide for the Treatment of Secondary Hyperparathyroidism in Patients with Chronic Kidney Disease","authors":"A. Baruch, D. Maclean","doi":"10.1002/9783527814695.ch5","DOIUrl":"https://doi.org/10.1002/9783527814695.ch5","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"54 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126626649","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-07DOI: 10.1002/9783527814695.ch7
A. Chan, P. Brunetta, P. Chin
{"title":"Ocrelizumab: A New Generation of anti‐CD20 mAbfor Treatment of Multiple Sclerosis","authors":"A. Chan, P. Brunetta, P. Chin","doi":"10.1002/9783527814695.ch7","DOIUrl":"https://doi.org/10.1002/9783527814695.ch7","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134004327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch2
A. Ritzén, L. David
{"title":"Physicochemical Parameters of Recently Approved Oral Drugs","authors":"A. Ritzén, L. David","doi":"10.1002/9783527814695.ch2","DOIUrl":"https://doi.org/10.1002/9783527814695.ch2","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"163 ","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133911891","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch6
A. Tsuruoka, Y. Funahashi, J. Matsui, T. Matsushima
{"title":"Development of Lenvatinib Mesylate, an Angiogenesis Inhibitor TargetingVEGFandFGFReceptors","authors":"A. Tsuruoka, Y. Funahashi, J. Matsui, T. Matsushima","doi":"10.1002/9783527814695.ch6","DOIUrl":"https://doi.org/10.1002/9783527814695.ch6","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"17 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133592657","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch9
W. Fairbrother, J. Leverson, D. Sampath, A. Souers
{"title":"Discovery and Development of Venetoclax, a Selective Antagonist ofBCL‐2","authors":"W. Fairbrother, J. Leverson, D. Sampath, A. Souers","doi":"10.1002/9783527814695.ch9","DOIUrl":"https://doi.org/10.1002/9783527814695.ch9","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121537358","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch3
Caroline Denevault-Sabourin, F. Bryden, M. Viaud-Massuard, Nicolas Joubert
{"title":"Antibody–Drug Conjugates: Empowering Antibodies for the Fight Against Cancer","authors":"Caroline Denevault-Sabourin, F. Bryden, M. Viaud-Massuard, Nicolas Joubert","doi":"10.1002/9783527814695.ch3","DOIUrl":"https://doi.org/10.1002/9783527814695.ch3","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115607987","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch1
F. Brunel, Fa Liu, J. Mayer
The growing importance of peptide drugs within the pharmacopoeia has become evident over the past several decades. Among the factors that have contributed to this trend is the recognition that peptide ligands regulate a multitude of physiological pathways and are often suitable for therapeutic applications, in either their native or modified form. In addition, certain attributes that are unique to peptides, such as their high selectivity, potency, and lack of toxicity, have ultimately become appreciated. The alternative means of drugging peptide receptors through target‐directed screening or rational design of orally available small molecules have, with few exceptions, proved unproductive. Mimicking the activity of a peptide agonist is highly challenging, particularly in the case of Class II G‐protein‐coupled receptor (GPCR) targets. Successful examples have typically involved receptor antagonists such as neurokinin, angiotensin, endothelin, and orexin. These lessons have increasingly led drug discovery scientists to consider peptides as legitimate drug candidates, rather than leads or proof‐of‐concept models for small‐molecule programs. Peptide medicinal chemists have also had to confront and overcome shortcomings such as rapid metabolism, clearance, production costs, and limited alternative delivery options. In the present chapter, we highlight the role of peptides in therapeutic areas such as metabolic disease, where peptides have been well established, as well as in areas where their impact has been minor, but now rapidly expanding. We also emphasize examples where time‐extension strategies and alternative delivery routes have helped establish and strengthen the position of peptide drugs in competitive markets. Finally, we explore two novel trends in peptide drug discovery, macrocyclic and cell‐penetrating peptides, both of which may expand future opportunities for peptide therapeutics. Trends in Peptide Therapeutics Florence M. Brunel, Fa Liu, and John P. Mayer
在过去的几十年里，肽类药物在药典中的重要性越来越明显。促成这一趋势的因素之一是人们认识到肽配体调节多种生理途径，并且通常适合于治疗应用，无论是天然形式还是修饰形式。此外，多肽特有的某些特性，如其高选择性、效力和无毒性，最终得到了人们的重视。除了少数例外，通过靶向筛选或合理设计口服小分子给肽受体用药的替代方法被证明是无效的。模拟肽激动剂的活性是极具挑战性的，特别是在II类G蛋白偶联受体(GPCR)靶点的情况下。成功的例子通常涉及受体拮抗剂，如神经激肽、血管紧张素、内皮素和食欲素。这些经验教训越来越多地引导药物发现科学家将多肽视为合法的候选药物，而不是小分子项目的先导或概念证明模型。多肽药物化学家还必须面对和克服诸如快速代谢、清除、生产成本和有限的替代递送选择等缺点。在本章中，我们强调多肽在代谢疾病等治疗领域的作用，在这些领域，多肽已经很好地建立起来，以及在它们的影响较小但现在迅速扩大的领域。我们还强调了一些例子，在这些例子中，延长时间策略和替代递送路线有助于在竞争激烈的市场中建立和加强多肽药物的地位。最后，我们探讨了肽药物发现的两个新趋势，大环肽和细胞穿透肽，这两者都可能扩大肽治疗的未来机会。肽治疗的趋势Florence M. Brunel, Fa Liu, and John P. Mayer
{"title":"Trends in Peptide Therapeutics","authors":"F. Brunel, Fa Liu, J. Mayer","doi":"10.1002/9783527814695.ch1","DOIUrl":"https://doi.org/10.1002/9783527814695.ch1","url":null,"abstract":"The growing importance of peptide drugs within the pharmacopoeia has become evident over the past several decades. Among the factors that have contributed to this trend is the recognition that peptide ligands regulate a multitude of physiological pathways and are often suitable for therapeutic applications, in either their native or modified form. In addition, certain attributes that are unique to peptides, such as their high selectivity, potency, and lack of toxicity, have ultimately become appreciated. The alternative means of drugging peptide receptors through target‐directed screening or rational design of orally available small molecules have, with few exceptions, proved unproductive. Mimicking the activity of a peptide agonist is highly challenging, particularly in the case of Class II G‐protein‐coupled receptor (GPCR) targets. Successful examples have typically involved receptor antagonists such as neurokinin, angiotensin, endothelin, and orexin. These lessons have increasingly led drug discovery scientists to consider peptides as legitimate drug candidates, rather than leads or proof‐of‐concept models for small‐molecule programs. Peptide medicinal chemists have also had to confront and overcome shortcomings such as rapid metabolism, clearance, production costs, and limited alternative delivery options. In the present chapter, we highlight the role of peptides in therapeutic areas such as metabolic disease, where peptides have been well established, as well as in areas where their impact has been minor, but now rapidly expanding. We also emphasize examples where time‐extension strategies and alternative delivery routes have helped establish and strengthen the position of peptide drugs in competitive markets. Finally, we explore two novel trends in peptide drug discovery, macrocyclic and cell‐penetrating peptides, both of which may expand future opportunities for peptide therapeutics. Trends in Peptide Therapeutics Florence M. Brunel, Fa Liu, and John P. Mayer","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"124409011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch4
M. Jacobson, W. Childers, M. Abou-Gharbia
{"title":"Dopamine D\u0000 2\u0000 Partial Agonists – Discovery, Evolution, and Therapeutic Potential","authors":"M. Jacobson, W. Childers, M. Abou-Gharbia","doi":"10.1002/9783527814695.ch4","DOIUrl":"https://doi.org/10.1002/9783527814695.ch4","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"52 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121471772","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-19DOI: 10.1002/9783527814695.ch8
B. Golding
{"title":"The Story of Rucaparib (Rubraca)","authors":"B. Golding","doi":"10.1002/9783527814695.ch8","DOIUrl":"https://doi.org/10.1002/9783527814695.ch8","url":null,"abstract":"","PeriodicalId":362351,"journal":{"name":"Successful Drug Discovery","volume":"26 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126123009","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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