Rolapitant
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-ROLAPITANT |
|---|---|
| Type | Drug |
| Aliases | VarubiVarubyРолапітант |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | None declared |
| Sources | SRC-ESMO-DLBCL-2024 SRC-NCCN-BCELL-2025 |
Drug Facts
| Class | Long-acting substance P / neurokinin-1 (NK1) receptor antagonist |
|---|---|
| Mechanism | Selective competitive antagonist of the substance P / NK1 receptor in CNS emetic centers (nucleus tractus solitarius, area postrema), blocking the late phase of chemotherapy-induced nausea and vomiting (CINV) mediated by substance P. Distinguishing pharmacokinetic feature is an exceptionally long terminal half-life of ~7 days (~169 hours), which provides receptor coverage across the full 5-day delayed phase from a single oral dose without need for follow-up doses on days 2-3. Approved by FDA September 2015 and EMA April 2017 for prevention of delayed CINV in adults receiving HEC or MEC. |
| Typical dosing | 180 mg PO single dose 1-2 hours before chemotherapy on day 1 only; no dose on days 2-3 (the long half-life provides 5-day coverage). Always combined with 5-HT3 antagonist (ondansetron 8-16 mg or palonosetron 0.25 mg IV) and dexamethasone (12 mg PO/IV day 1, then 8 mg days 2-4). Notable difference from aprepitant: rolapitant does NOT inhibit CYP3A4, so dexamethasone dose adjustment is NOT required. No dose adjustment for renal impairment. No adjustment for mild-moderate hepatic impairment; not studied in severe hepatic impairment (avoid). Not approved in pediatrics. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Long-acting NK1 antagonist with single-dose convenience and absent CYP3A4 interaction (no need for dexamethasone dose halving — a practical advantage when patients already take other CYP3A4 substrates). Pivotal trials: HEC1, HEC2, MEC (Rapoport, Lancet Oncol 2015) — rolapitant + ondansetron + dex superior to placebo + ondansetron + dex for delayed-phase CR (~70% vs ~57%). IV formulation withdrawn US in 2018 due to anaphylaxis signal; oral remains available. Key DDI hazard is CYP2D6 inhibition lasting up to 28 days post-dose — review concomitant medications carefully (especially tamoxifen patients, where reduced endoxifen formation is a theoretical efficacy concern). Ukraine: NOT registered; alternatives (aprepitant, fosaprepitant) widely available.
Used By
No reverse references found in the YAML corpus.