Rucaparib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-RUCAPARIB |
|---|---|
| Type | Drug |
| Aliases | AG-014699CO-338RubracaРукапариб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | DIS-OVARIAN |
| Sources | SRC-ESMO-OVARIAN-2024 SRC-NCCN-OVARIAN-2025 |
Drug Facts
| Class | PARP1/2/3 inhibitor |
|---|---|
| Mechanism | Oral small-molecule inhibitor of poly(ADP-ribose) polymerase (PARP) 1, 2 and 3, with both catalytic inhibition and PARP-trapping activity (locks PARP onto DNA, generating replication-fork collapse during S-phase). In tumors with deficient homologous recombination repair (HRR) — most prominently BRCA1/2 mutated, but also other HRR-pathway alterations (RAD51C/D, BRIP1, PALB2, CHEK2 in some contexts) — accumulated double-strand breaks cannot be faithfully repaired, producing synthetic lethality. Pivotal trials: ARIEL3 (maintenance after platinum-sensitive recurrent ovarian — mPFS benefit greatest in BRCA-mut, then HRD-positive, then HRD-negative); TRITON2/TRITON3 (BRCA-mutant mCRPC post-AR-targeted therapy — FDA accelerated 2020, mCRPC indication subsequently restricted / partially withdrawn after confirmatory analyses). |
| Typical dosing | 600 mg PO BID continuous, with or without food. Dose modifications for cytopenias / non-hematologic AE: -1 = 500 mg BID; -2 = 400 mg BID; -3 = 300 mg BID; permanent discontinuation if recurrent G3-4 at -3. Hold for any G3-4 hematologic AE until recovery (Hb ≥9, plt ≥100, ANC ≥1.0). No formal renal adjustment for CrCl ≥30; not studied in severe renal or hepatic impairment. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Less commonly used than olaparib or niraparib in 1L maintenance (which now has both BRCA-mut and HRD-positive labels for olaparib ± bevacizumab — rucaparib's 1L ATHENA-MONO data is positive but approval restricted in some regions). Distinct creatinine-rise pattern from MATE transporter inhibition — labs may show "AKI" picture but no actual nephrotoxicity (do not stop or dose-adjust on creatinine alone; check cystatin C or renal scan if uncertain). Photosensitivity less prominent than vemurafenib but real — counsel sun protection. Baseline workup: CBC, CMP, pregnancy test. Monitor CBC weekly first month then monthly; LFTs monthly. Long- term MDS/AML surveillance with annual CBC + smear if persistent cytopenia. UA access via EAP / self-pay only.
Used By
Regimens
REG-RUCAPARIB-MAINT-OVARIAN- Rucaparib maintenance (recurrent platinum-sensitive ovarian, ARIEL3)