- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK, netupitant (Ro 67-3189) / Helsinn, Otsuka
Journal, CINV: New options and controversies in the management of chemotherapy-induced nausea and vomiting. (Pubmed Central) - May 15, 2019
Newer therapeutic options for the management of CINV are equivalent to standard-of-care regimens in terms of efficacy and toxicity. While the NK receptor antagonist rolapitant and a product combining palonosetron and netupitant have potential advantages over standard therapy in terms of convenience or pharmacologic properties, their relatively high costs must be considered.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK, netupitant (Ro 67-3189) / Helsinn, Otsuka
Journal: The latest consensus on antiemetics. (Pubmed Central) - Apr 30, 2019
Guidelines recommend a combination of a 5-HT3-receptor antagonist, dexamethasone, and an NK1-receptor antagonist in HEC and carboplatin-based chemotherapy. The addition of olanzapine can be useful in cisplatin-based and anthracycline-cyclophosphamide-based chemotherapy in particular if the main problem is nausea.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Retrospective data, Review, Journal, CINV: Meta-analysis of safety and efficacy of rolapitant, NK-1 receptor antagonist for prevention of chemotherapy-induced nausea and vomiting. (Pubmed Central) - Apr 26, 2019
Moreover, rates of complete protection were significantly higher with rolapitant 180mg than with placebo in the overall, acute, and delayed phases (OR = 1.52, 95% CI [1.3, 1.76]), OR = 1.24, 95% CI [1.04, 1.49], and OR = 1.5, 95% CI [1.29, 1.75]), respectively. In conclusion, rolapitant in combination with a 5-HT3 receptor antagonist and dexamethasone is well tolerated and more effective than 5-HT3 receptor antagonist plus dexamethasone for the prevention of CINV.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Clinical, PK/PD data, Journal: Pharmacokinetics of Rolapitant in Patients With Mild to Moderate Hepatic Impairment. (Pubmed Central) - Apr 19, 2019
Rolapitant was well tolerated in all groups, without serious adverse events. Pharmacokinetic differences between healthy subjects and those with mild or moderate hepatic impairment are unlikely to pose a safety risk and do not warrant predefined dosage adjustment in the presence of hepatic impairment.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Clinical, PK/PD data, Journal: Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects. (Pubmed Central) - Mar 27, 2019
No clinically significant interaction was observed between rolapitant and substrates of CYP2C9, CYP2C19, CYP2B6, or CYP2C8. CYP2D6 substrate drugs with a narrow therapeutic index may require monitoring for adverse reactions if given concomitantly with rolapitant.
- |||||||||| Review, Journal, CINV: Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting. (Pubmed Central) - Oct 18, 2018
To examine pharmacologic and clinical characteristics of neurokinin 1 (NK)-receptor antagonists (RAs) for preventing chemotherapy-induced nausea and vomiting (CINV) following highly or moderately emetogenic chemotherapy, a literature search was performed for clinical studies in patients at risk of CINV with any approved NK RAs in the title or abstract: aprepitant (capsules or oral suspension), HTX019 (intravenous [IV] aprepitant), fosaprepitant (IV aprepitant prodrug), rolapitant (tablets or IV), and fixed-dose tablets combining netupitant or fosnetupi-tant (IV netupitant prodrug) with the 5-hydroxytryptamine type 3 (5HT) RA palonosetron (oral or IV)...Adding an NK RA to 5HT RA and dexamethasone significantly improves CINV control vs the two-drug regimen. Newer NK RAs offer more formulation options, higher acute-phase plasma levels, or improved tolerability, and increase clinicians' opportunities to maximize benefits of this important class of antiemetics.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK, netupitant (Ro 67-3189) / Helsinn, Otsuka
Review, Journal, CINV: Recent Advances in Preventing Chemotherapy-Induced Nausea and Vomiting. (Pubmed Central) - Jun 22, 2018
The US Food and Drug Administration has recently approved new therapies for prevention of CINV, including the neurokinin-1 (NK1) receptor antagonist rolapitant and the fixed-dose combination of the second-generation 5-hydroxytryptamine type 3 receptor antagonist palonosetron with the novel NK1 receptor antagonist netupitant...This article will address changes in CINV guidelines over the past 5 years and provide updates on recently approved agents and agents that are expected to be approved, based on published phase III trials. It will also explore other factors affecting optimal CINV control, including the role of patient-related risk factors and the role of physician adherence to antiemetic guidelines in reducing the residual risk of CINV.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Clinical, Review, Journal: Recent developments in the clinical pharmacology of rolapitant: subanalyses in specific populations. (Pubmed Central) - Jun 14, 2018
In addition, we show that rolapitant has efficacy in the control of CINV in specific age groups of patients receiving chemotherapy (<65 and ≥65 years of age). Overall, the safety profile of rolapitant in these specific patient populations was consistent with that observed in primary analyses of phase 3 trials.
- |||||||||| Journal: Prevention of chemotherapy-induced nausea: the role of neurokinin-1 (NK1) receptor antagonists. (Pubmed Central) - Oct 20, 2017
Aprepitant has not shown consistent superiority over a two-drug (ondansetron-dexamethasone) combination in nausea control after cisplatin- or anthracycline-cyclophosphamide (AC)-based highly emetogenic chemotherapy (HEC)...The potential impact of the new NK1RAs rolapitant and netupitant (oral fixed combination with palonosetron, as NEPA) in CIN prophylaxis is discussed...Recently, NK1RAs have been challenged by olanzapine, with olanzapine showing superior efficacy in nausea prevention after HEC. Fixed antiemetic combinations (such as NEPA) or new antiemetics with a long half-life that may be given once per chemotherapy cycle (rolapitant or NEPA) may improve patient compliance with antiemetic treatment.
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Enrollment open, Monotherapy, Compliance: Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) - Oct 11, 2017
P2, N=160, Recruiting,
Fixed antiemetic combinations (such as NEPA) or new antiemetics with a long half-life that may be given once per chemotherapy cycle (rolapitant or NEPA) may improve patient compliance with antiemetic treatment. Not yet recruiting --> Recruiting
- |||||||||| Varubi (rolapitant oral) / TerSera Therap, GSK
Enrollment open, Trial initiation date, Trial primary completion date: Rolapitant Hydrochloride in Preventing Nausea/Vomiting in Patients With Sarcoma Receiving Chemotherapy (clinicaltrials.gov) - Oct 13, 2016
P2, N=91, Recruiting,
Addition of rolapitant to 5-HT3RA and dexamethasone therapy significantly improved CR, no nausea, no emesis, and CP in pts with GI/CRC receiving emetogenic chemotherapy. Not yet recruiting --> Recruiting | Initiation date: Jul 2016 --> Oct 2016 | Trial primary completion date: Jul 2019 --> Oct 2019
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