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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.
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 higher than with granisetron and dexamethasone alone, a statistically significant difference. An intravenous emulsion approved in 2017 was withdrawn after anaphylaxis reports.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.
Selective, competitive substance P/NK1 receptor antagonist with a half-life of about seven days, so one oral dose covers the delayed phase; unlike aprepitant it does not inhibit CYP3A4.
1.Rolapitant slips into a pocket on its target.
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| Region | Year | Indication |
|---|---|---|
| US | 2015 | Prevention of delayed nausea and vomiting with emetogenic chemotherapy, in combination with other antiemetics |
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Query 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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