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Computational Biology and Bioinformatics in Anti-SARS-CoV-2 Drug Development
Published in Debmalya Barh, Kenneth Lundstrom, COVID-19, 2022
Traditional structure-based drug discovery applies the computational ligand-receptor–binding modeling and virtual screening, whereas the stability of the resulting ligand-protein complexes is confirmed by molecular dynamics simulation. All potentially druggable SARS-CoV-2 proteins were subjected to these analyses, and the number of computational studies dedicated to finding potential drugs targeting these proteins is mounting. For example, Hosseini et al. conducted molecular docking and virtual screening of 1,615 FDA-approved drugs on the binding pocket of SARS-CoV-2 Mpro, PLpro, and RdRp proteins [127]. The authors used AutoDock Vina, Glide, and rDock followed by MD simulation using GROMACS on the top inhibitors and identified six novel ligands as potential inhibitors against SARS-CoV-2, such as antiemetics rolapitant and ondansetron for Mpro; labetalol and levomefolic acid for PLpro; and leucal and antifungal natamycin for RdRp [127]. Chourasia et al. investigated in silico binding of epigallocatechin gallate (EGCG), and other catechins to SARS-CoV-2 proteins and identified papain-like protease protein (PLPro) as a binding partner [128].
Main Classes of Drugs
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
AntiemeticAprepitantChlorpromazineDexamethasoneDimenhydrinateDiphenhydramineDomperidoneDronabinolDroperidolGranisetronHaloperidolMarihuanaMeclizineMetoclopramideNabiloneOndansetronPalonosetronPerphenazineProchlorperazineRolapitantScopolamineTrimethobenzamide
Neurokinin-1 receptor antagonists: review of their role for the prevention of chemotherapy-induced nausea and vomiting in adults
Published in Expert Review of Clinical Pharmacology, 2019
Meinolf Karthaus, Xaver Schiel, Christina H. Ruhlmann, Luigi Celio
Rolapitant was approved by the FDA in 2015 [93] and by the EMA in 2017 [94] in combination with a 5-HT3RA and dexamethasone for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy. In a global, randomized, double-blind phase 3 trial, 1369 chemotherapy-naive patients received either one oral dose of rolapitant or placebo 1–2 h before administration of MEC or AC regimens [95]. All patients also received granisetron and dexamethasone. Prophylaxis with a rolapitant-based regimen was superior to control in the CR rate in the delayed and overall phases. CR rates in the acute phase were similar in both arms. The incidence of AEs was similar in the rolapitant and control groups.
The safety of rolapitant for the treatment of nausea and vomiting associated with chemotherapy
Published in Expert Opinion on Drug Safety, 2019
While the new antiemetic agents have provided improved control of CINV, they have been relatively well tolerated by patients with few serious toxicities [2–4, 6–9]. Constipation may occur in patients using the 5HT3 receptor antagonists [2], local infusion-site reactions, and rare systemic reactions may occur with some of the NK-1 receptor antagonists [4,6], dexamethasone may induce transient insomnia [3], and mild sedation may occur with the use of olanzapine [7–9]. The purpose of this review is to review the NK-1 receptor antagonists with specific focus on the safety of the NK-1 receptor antagonist Rolapitant for the treatment of nausea and vomiting associated with chemotherapy.
Pharmacokinetics and pharmacodynamics of dextromethorphan: clinical and forensic aspects
Published in Drug Metabolism Reviews, 2020
Ana Rita Silva, Ricardo Jorge Dinis-Oliveira
Rolapitant is a potent selective and competitive substance P/neurokinin-1 (NK-1) receptor antagonist indicated in combination with other antiemetic agents in adults for the prevention of delayed chemotherapy-induced nausea and vomiting. In vivo rolapitant moderately inhibits CYP2D6 for at least seven days after one 180 mg dose, but the relevance of this finding is yet to be fully clarified (Glass et al. 2019). Nevertheless, a significant increase of DXM systemic exposure with clinical relevance was reported after a single oral dose of rolapitant 180 mg (Wang et al. 2019).