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ACS Med Chem Lett. 2017 Apr 25;8(5):582-586. doi: 10.1021/acsmedchemlett.7b00157. eCollection 2017 May 11.
2
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1
Fevipiprant, a prostaglandin D2 receptor 2 antagonist, in patients with persistent eosinophilic asthma: a single-centre, randomised, double-blind, parallel-group, placebo-controlled trial.非索罗肽，一种前列腺素 D2 受体 2 拮抗剂，在持续性嗜酸性粒细胞性哮喘患者中的应用：一项单中心、随机、双盲、平行分组、安慰剂对照试验。
Lancet Respir Med. 2016 Sep;4(9):699-707. doi: 10.1016/S2213-2600(16)30179-5. Epub 2016 Aug 5.
2
The oral CRTh2 antagonist QAW039 (fevipiprant): A phase II study in uncontrolled allergic asthma.口服CRTh2拮抗剂QAW039（非维普拉特）：一项针对未控制的过敏性哮喘的II期研究。
Pulm Pharmacol Ther. 2016 Aug;39:54-63. doi: 10.1016/j.pupt.2016.06.005. Epub 2016 Jun 21.
3
Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy.CRTh2拮抗剂LAS191859的药理学特性：长受体驻留时间转化为持久的体内疗效。
Pharmacol Res. 2016 Sep;111:208-216. doi: 10.1016/j.phrs.2016.06.014. Epub 2016 Jun 16.
4
Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo-Controlled Studies in Healthy Volunteers.福维匹坦（QAW039）的药代动力学、安全性和耐受性：两项在健康志愿者中进行的随机、1 期、安慰剂对照研究的结果。福维匹坦是一种新型的 CRTh2 受体拮抗剂。
Clin Pharmacol Drug Dev. 2016 Jul;5(4):306-13. doi: 10.1002/cpdd.244. Epub 2016 Mar 28.
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Lancet. 2016 Jul 2;388(10039):31-44. doi: 10.1016/S0140-6736(16)30307-5. Epub 2016 Apr 27.
6
Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.非维哌兰特（QAW039），一种解离缓慢的CRTh2拮抗剂，具有改善临床疗效的潜力。
Mol Pharmacol. 2016 May;89(5):593-605. doi: 10.1124/mol.115.101832. Epub 2016 Feb 25.
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Bioorg Med Chem Lett. 2014 Nov 1;24(21):5123-6. doi: 10.1016/j.bmcl.2014.08.029. Epub 2014 Aug 19.
9
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.双环杂芳基乙酸作为强效CRTh2拮抗剂的构效关系（SAR）和构动关系（SKR）I
Bioorg Med Chem Lett. 2014 Nov 1;24(21):5118-22. doi: 10.1016/j.bmcl.2014.09.005. Epub 2014 Oct 15.
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Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists.作为CRTh2拮抗剂的吡咯并哌啶酮乙酸的构效关系（SAR）和构动关系（SKR）
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发现用于治疗哮喘的强效选择性DP受体拮抗剂非维泼兰特（NVP-QAW039）。

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP Receptor Antagonist for Treatment of Asthma.

作者信息

Sandham David A, Barker Lucy, Brown Lyndon, Brown Zarin, Budd David, Charlton Steven J, Chatterjee Devnandan, Cox Brian, Dubois Gerald, Duggan Nicholas, Hall Edward, Hatto Julia, Maas Janet, Manini Jodie, Profit Rachael, Riddy Darren, Ritchie Catherine, Sohal Bindi, Shaw Duncan, Stringer Rowan, Sykes David A, Thomas Matthew, Turner Katharine L, Watson Simon J, West Ryan, Willard Elisabeth, Williams Gareth, Willis Jennifer

机构信息

Novartis Institutes for Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom.

出版信息

ACS Med Chem Lett. 2017 Apr 25;8(5):582-586. doi: 10.1021/acsmedchemlett.7b00157. eCollection 2017 May 11.

DOI:10.1021/acsmedchemlett.7b00157
PMID:28523115
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5430394/
Abstract

Further optimization of an initial DP receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1-pyrrolo[2,3-]pyridin-3-yl)acetic acid (compound , NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.

摘要

对首个DP受体拮抗剂临床候选药物NVP-QAV680的进一步优化，促成了后续分子2-(2-甲基-1-(4-(甲基磺酰基)-2-(三氟甲基)苄基)-1-吡咯并[2,3 -]吡啶-3-基)乙酸（化合物，NVP-QAW039，非维普兰特）的发现，该化合物对人嗜酸性粒细胞和Th2细胞表现出更高的效力，同时受体驻留时间更长，目前正处于重症哮喘的临床试验阶段。