Rolapitant
Rolapitant (Varubi) is a long-lasting anti-sickness tablet taken once before chemotherapy, alongside a 5-HT3 blocker and dexamethasone, to prevent nausea and vomiting in the days after treatment.
Overview
Rolapitant was approved by the FDA in September 2015 in combination with other antiemetics for prevention of delayed nausea and vomiting with initial and repeat courses of emetogenic chemotherapy including highly emetogenic regimens, on three phase 3 trials (two in cisplatin-based and one in moderately emetogenic chemotherapy) in which complete response in the delayed phase was significantly higher than with granisetron and dexamethasone alone. An intravenous emulsion approved in 2017 was withdrawn after anaphylaxis reports. Its long half-life and lack of CYP3A4 inhibition avoid the dexamethasone dose adjustment required with aprepitant, but it inhibits CYP2D6 and BCRP, so thioridazine is contraindicated and irinotecan and methotrexate exposure may rise. Marketed in the US by TerSera.
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 2015 | Prevention of delayed nausea and vomiting with emetogenic chemotherapy, in combination with other antiemetics |
Trials
topRecruiting now (live from ClinicalTrials.gov)
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Latest papers
topQuery for this drug: (TITLE:"Rolapitant" OR ABSTRACT:"Rolapitant" OR TITLE:"Varubi" OR ABSTRACT:"Varubi" OR TITLE:"Varuby" OR ABSTRACT:"Varuby") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Rolapitant, not a curated reading list.
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