Varubi (rolapitant oral) / TerSera Therap, GSK 
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  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Journal:  Overcoming amphotericin B resistance in Candida auris using the antiemetic drug rolapitant. (Pubmed Central) -  Nov 6, 2024   
    Moreover, rolapitant enhanced the in vivo activity of AmB in a mouse model of disseminated C. auris infection, as the combination reduced the fungal burden in murine kidneys by ~1 log (~90%) colony forming units. Our findings warrant further investigation of using rolapitant to overcome AmB resistance in C. auris and other fungal species.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Journal:  Rolapitant treats lung cancer by targeting deubiquitinase OTUD3. (Pubmed Central) -  Apr 1, 2024   
    Our findings warrant further investigation of using rolapitant to overcome AmB resistance in C. auris and other fungal species. In summary, the present study identifies Rolapitant as a novel inhibitor of deubiquitinase OTUD3 and establishes that the OTUD3-GRP78 axis is a potential therapeutic target for lung cancer.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, netupitant (Ro 67-3189) / Helsinn, Otsuka
    Prophylactic Neurokinin-1 Receptor Antagonist Use Pre- and Post- Choosing Wisely Initiative among Women with Breast Cancer (Hall 2-3) -  Nov 4, 2023 - Abstract #SABCS2023SABCS_1865;    
    Continued statewide or local educational efforts for dissemination of CW recommendations are needed to facilitate appropriate prophylactic use of NK1-RAs. Adjusted* Interrupted Time Series Segmented Regression Analysis of Prophylactic NK1-RA use among women with breast cancer before and after the Choosing Wisely initiative *Adjusted for insurance, health plan type, age, comorbidity, and emetic risk
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Rezonic (casopitant) / GSK
    Journal:  Homology modeling, virtual screening, molecular docking, and ADME approaches to identify a potent agent targeting NK2R protein. (Pubmed Central) -  Oct 31, 2023   
    The evaluation of the in silico ADME profile, solubility, and permeability of the ligand molecules has revealed that the small molecules are potentially nontoxic and have the chance of exhibiting biological activity after oral administration. Further experimental studies (in vitro and in vivo assays) are required to evaluate the effectiveness of these inhibitors as therapeutic targets.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Emend intravenous (fosaprepitant) / Merck (MSD), Ono Pharma, netupitant (Ro 67-3189) / Helsinn, Otsuka
    Predictors of Neurokinin-Receptor Antagonist (NK1-RA) Overuse Among Women with Breast Cancer () -  Mar 9, 2023 - Abstract #ISPOR2023ISPOR_748;    
    Variability in NK1-RAs overuse was driven by certain patient and healthcare related factors. Continued education about these recommendations is important to achieve value-based cancer care.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Trial completion, Enrollment change, Trial completion date, Trial primary completion date, Monotherapy, Compliance:  Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) -  Dec 14, 2022   
    P2,  N=47, Completed, 
    Continued education about these recommendations is important to achieve value-based cancer care. Suspended --> Completed | N=160 --> 47 | Trial completion date: Apr 2023 --> Jun 2022 | Trial primary completion date: Mar 2023 --> May 2022
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Journal:  Morphological and Skeletal Abnormalities Induced by Rolapitant: An Antiemetic Agent. (Pubmed Central) -  Sep 23, 2022   
    Conclusion Rolapitant is toxic when taken in large doses and for an extended period. As a result, rolapitant should be taken only when a valid diagnosis has been established and only at the recommended dose, not at a larger dose or for an extended period of time.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Procoralan (ivabradine) / Amgen, Servier, Ono Pharma
    FDA event, Journal:  Virtual Screening for FDA-Approved Drugs That Selectively Inhibit Arginase Type 1 and 2. (Pubmed Central) -  Sep 3, 2022   
    The partial validation also favors the idea that the other half of the top 30 potential drugs could be used in therapeutic settings. The three categories greatly expand the selectivity of arginase inhibition.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Varubi (Twitter) -  Jan 14, 2022   
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Retrospective data, Review, Journal:  Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis. (Pubmed Central) -  Dec 16, 2021   
    For people receiving HEC, synthesised evidence does not suggest one superior treatment for prevention and control of chemotherapy-induced nausea and vomiting.  For people receiving MEC, synthesised evidence does not suggest superiority for treatments including both NK₁ and 5-HT₃ inhibitors when compared to treatments including 5-HT₃ inhibitors only. Rather, the results of our NMA suggest that the choice of 5-HT₃ inhibitor may have an impact on treatment efficacy in preventing CINV.  When interpreting the results of this systematic review, it is important for the reader to understand that NMAs are no substitute for direct head-to-head comparisons, and that results of our NMA do not necessarily rule out differences that could be clinically relevant for some individuals.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Review, Journal:  The next generation of antiemetics for the management of postoperative nausea and vomiting. (Pubmed Central) -  Jun 2, 2021   
    Newer antiemetics have been introduced that may have improved safety profiles, longer duration of action, and better efficacy. This review aims to summarize the recent developments pertaining to these new agents and their potential application toward the management of PONV.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Trial completion date, Trial primary completion date, Monotherapy, Compliance:  Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) -  Apr 22, 2021   
    P2,  N=160, Recruiting, 
    This review aims to summarize the recent developments pertaining to these new agents and their potential application toward the management of PONV. Trial completion date: Apr 2021 --> Apr 2023 | Trial primary completion date: Mar 2021 --> Mar 2023
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Review, Journal:  Computational molecular docking and virtual screening revealed promising SARS-CoV-2 drugs. (Pubmed Central) -  Apr 13, 2021   
    The results of our analysis with some other suggested drugs indicated that chloroquine and hydroxychloroquine had high binding energy (low inhibitory effect) with all three proteins-Mpro, PLpro, and RdRp. In summary, our computational molecular docking approach and virtual screening identified some promising candidate SARS-CoV-2 inhibitors that may be considered for further clinical studies.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, netupitant (Ro 67-3189) / Helsinn, Otsuka
    [VIRTUAL] Opioid toxicity from cytochrome P450 related drug-drug interactions: Potential Scope of Intervention by Pharmacist () -  Dec 26, 2020 - Abstract #ASHP2020ASHP_1564;    
    It illustrates awareness in their function and metabolism with co-administered medications, allowing for better treatment outcomes and preventing toxic opioid levels. Consequently, pharmacists have the opportunity in practical settings to improve therapy by understanding metabolism patterns commonly seen in comorbid conditions that coexist in opioid regimens.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Retrospective data, Review, Journal:  Drugs for preventing postoperative nausea and vomiting in adults after general anaesthesia: a network meta-analysis. (Pubmed Central) -  Nov 18, 2020   
    No further efficacy studies are needed as there is evidence of moderate to high certainty for seven single drugs with relevant benefit for prevention of vomiting. However, additional studies are needed to investigate potential side effects of these drugs and to examine higher-risk patient populations (e.g. individuals with diabetes and heart disease).
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Enrollment open, Monotherapy, Compliance:  Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) -  Aug 8, 2020   
    P2,  N=160, Recruiting, 
    However, additional studies are needed to investigate potential side effects of these drugs and to examine higher-risk patient populations (e.g. individuals with diabetes and heart disease). Suspended --> Recruiting
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Clinical, PK/PD data, Journal, CINV:  Population Pharmacokinetics of Rolapitant in Patients With Chemotherapy-Induced Nausea and Vomiting. (Pubmed Central) -  Aug 5, 2020   
    In summary, this validated population pharmacokinetic model satisfactorily describes pharmacokinetics of rolapitant and M19 in patients with CINV. These results support the recommendation that no dose adjustment for patient variables investigated is necessary.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Avelox (moxifloxacin) / Bayer
    Clinical, P1 data, Journal:  A Phase 1 Assessment of the QT Interval in Healthy Adults Following Exposure to Rolapitant, a Cancer Supportive Care Antiemetic. (Pubmed Central) -  Jul 16, 2020   
    At any point, the upper bound of the confidence interval for the mean difference between placebo and rolapitant was no greater than 4.4 milliseconds, and the mean difference between placebo and rolapitant was no greater than 1.7 milliseconds, suggesting an insignificant change in QTc with rolapitant. Rolapitant is safe and does not prolong the QT interval at doses up to 720 mg relative to placebo in healthy adults.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Trial completion, Enrollment change, Trial completion date, Trial primary completion date:  Rolapitant Hydrochloride in Preventing Nausea/Vomiting in Patients With Sarcoma Receiving Chemotherapy (clinicaltrials.gov) -  Jul 14, 2020   
    P2,  N=37, Completed, 
    Completed --> Terminated; Terminated per PI's request Recruiting --> Completed | N=91 --> 37 | Trial completion date: Dec 2020 --> Jul 2020 | Trial primary completion date: Dec 2020 --> Jul 2020
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Clinical, Journal:  An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant. (Pubmed Central) -  Apr 10, 2020   
    The geometric mean ratios of C and AUC were 0.99 (0.89-1.11) and 1.05 (0.92-1.19), respectively, establishing bioequivalence of the rolapitant tablet and capsule formulations. Both formulations were well tolerated, with a similar incidence of treatment-emergent adverse events in the 2 groups.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, bromocriptine / Generic mfg.
    Journal:  Human cytochrome P450 enzymes bind drugs and other substrates mainly through conformational-selection modes. (Pubmed Central) -  Mar 4, 2020   
    Binding of the P450s 2C8, 2D6, 3A4, 4A11, and 21A2 was best described by conformational-selection, and P450 2E1 appeared to fit either mode. These findings highlight the complexity of human P450-substrate interactions and that conformational-selection is a dominant feature of many of these interactions.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Journal:  Rolapitant is a reversible inhibitor of CYP2D6. (Pubmed Central) -  Feb 24, 2020   
    Given these findings, we do not see evidence that rolapitant is a mechanism based inactivator. Moreover, the reversible inhibition of CYP2D6 by rolapitant may not fully account for the moderate inhibition described in vivo.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Clinical, Journal:  Absorption, metabolism, and excretion of the antiemetic rolapitant, a selective neurokinin-1 receptor antagonist, in healthy male subjects. (Pubmed Central) -  Jan 23, 2020   
    Adverse events (AEs) were generally mild; there were no serious AEs, and no clinically significant changes in laboratory or electrocardiogram parameters were observed. The combination of rolapitant safety, its long half-life, extensive tissue distribution, and slow elimination via the hepatobiliary route (rather than renal excretion) suggest suitability that a single dose of rolapitant may provide protection against CINV beyond the first 24 h after chemotherapy administration.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Varubi IV (rolapitant IV) / TerSera Therap, GSK
    Journal:  Infusion reactions following administration of intravenous rolapitant at an academic medical center. (Pubmed Central) -  Nov 28, 2019   
    Due to the quick onset of the infusion-related hypersensitivity reactions with intravenous rolapitant, interpatient differences in pharmacokinetics or pharmacodynamics are unlikely to be the cause. An objective assessment utilizing the Naranjo Causality Scale rates these infusion-related hypersensitivity reactions as definite adverse drug reactions.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK, Imperan (metoclopramide) / Generic Mfg.
    Supportive care to control nausea and dizziness in malignant tumours: A systematic review (Exhibition area) -  Sep 17, 2019 - Abstract #ESMOAsia2019ESMO_ASIA_779;    
    The neurokinin-1 receptor rolapitant is a possible alternative [5].Legal entity responsible for the study: The first author and the last author. Funding: Has not received any funding.
  • ||||||||||  Varubi (rolapitant oral) / TerSera Therap, GSK
    Trial primary completion date:  Rolapitant Hydrochloride in Preventing Nausea/Vomiting in Patients With Sarcoma Receiving Chemotherapy (clinicaltrials.gov) -  May 24, 2019   
    P2,  N=91, Recruiting, 
    This is the highest substrate loading and productivity for the bioreduction of 3,5-BTAP by carbonyl reductase ever reported, and this method represents an efficient and cost-effective process for production of (R)-3,5-BTPE. Trial primary completion date: Oct 2019 --> Jul 2019