Ramatroban for chemoprophylaxis and treatment of COVID-19: David takes on Goliath.
Ramatroban for chemoprophylaxis and treatment of COVID-19: David takes on Goliath.
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DOI：
10.1080/14728222.2022.2031975
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发表时间：
2022-01
影响因子：
5.8
通讯作者：
Gupta A
中科院分区：
文献类型：
--
作者：
Chiang KC;Rizk JG;Nelson DJ;Krishnamurti L;Subbian S;Imig JD;Khan I;Reddy ST;Gupta A
在COVID-19肺炎中，脂肪酸水平和脂质介质大量增加，环氧合酶代谢物占主导地位，特别是肺中的TxB2、PGE2、PGD2和体循环中的TxA2代谢物11-脱氢-TxB2。虽然TxA2刺激血栓烷前列腺素（TP）受体，但11-脱氢-TxB2是PGD2的DP2（以前称为CRTh2）受体的完全激动剂。使用雷马曲班（一种TxA2/TP和PGD2/DP2受体的双重受体拮抗剂）的轶事经验表明，急性呼吸窘迫和低氧血症的症状迅速缓解，同时避免住院治疗。支持TxA2/TP受体和PGD2/DP2受体在引起与低氧血症、适应不良免疫反应和血栓炎症相关的快速进行性肺损伤中的作用的证据进行了讨论。本文提出了关于TxA2/TP和PGD2/DP2受体信号传导的双重拮抗作用作为COVID-19治疗方法的创新观点。本文研究了雷马曲班，一种用于急性和长期COVID-19的抗血小板，免疫调节剂和抗纤维化剂。Ramatroban是TP和DP2受体的双重阻断剂，已在呼吸功能障碍、动脉粥样硬化、血栓形成和脓毒症的动物模型中证明了疗效，以及快速缓解COVID-19肺炎中呼吸困难和低氧血症的初步证据。Ramatroban值得研究，作为一种有前途的抗血栓和免疫调节剂，用于化学预防和治疗。
In COVID-19 pneumonia, there is a massive increase in fatty acid levels and lipid mediators with a predominance of cyclooxygenase metabolites, notably TxB2 ⪢ PGE2 > PGD2 in the lungs, and 11-dehydro-TxB2, a TxA2 metabolite, in the systemic circulation. While TxA2 stimulates thromboxane prostanoid (TP) receptors, 11-dehydro-TxB2 is a full agonist of DP2 (formerly known as the CRTh2) receptors for PGD2. Anecdotal experience of using ramatroban, a dual receptor antagonist of the TxA2/TP and PGD2/DP2 receptors, demonstrated rapid symptomatic relief from acute respiratory distress and hypoxemia while avoiding hospitalization. Evidence supporting the role of TxA2/TP receptors and PGD2/DP2 receptors in causing rapidly progressive lung injury associated with hypoxemia, a maladaptive immune response and thromboinflammation is discussed. An innovative perspective on the dual antagonism of TxA2/TP and PGD2/DP2 receptor signaling as a therapeutic approach in COVID-19 is presented. This paper examines ramatroban an anti-platelet, immunomodulator, and antifibrotic agent for acute and long-haul COVID-19. Ramatroban, a dual blocker of TP and DP2 receptors, has demonstrated efficacy in animal models of respiratory dysfunction, atherosclerosis, thrombosis, and sepsis, as well as preliminary evidence for rapid relief from dyspnea and hypoxemia in COVID-19 pneumonia. Ramatroban merits investigation as a promising antithrombotic and immunomodulatory agent for chemoprophylaxis and treatment.
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DOI：
10.3904/kjim.2011.26.1.8
发表时间：
2011-03
期刊：
The Korean journal of internal medicine
影响因子：
--
作者：
Arima M;Fukuda T
通讯作者：
Fukuda T
影响因子：
20.3
作者：
Bombeli, T;Karsan, A;Harlan, JM
通讯作者：
Harlan, JM
影响因子：
56.9
作者：
Broggi, Achille;Ghosh, Sreya;Zanoni, Ivan
通讯作者：
Zanoni, Ivan
影响因子：
8.2
作者：
Abadpour, Shadab;Tyrberg, Bjorn;Winzell, Maria Sorhede
通讯作者：
Winzell, Maria Sorhede
影响因子：
3.7
作者：
Chakraborty, Raja;Bhullar, Rajinder P.;Chelikani, Prashen
通讯作者：
Chelikani, Prashen