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Rucaparib: Drug information

Rucaparib: Drug information
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For additional information see "Rucaparib: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Rubraca
Pharmacologic Category
  • Antineoplastic Agent, PARP Inhibitor
Dosing: Adult

Dosage guidance:

Safety: Do not initiate treatment until after hematologic recovery (to grade 1 or lower) from prior chemotherapy.

Clinical considerations: Rucaparib is associated with a moderate or high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Ref). Select patients for ovarian cancer maintenance treatment based on the presence of a deleterious BRCA mutation (germline and/or somatic). Select patients for advanced prostate cancer treatment based on the presence of a deleterious BRCA mutation (germline and/or somatic) in plasma specimen; if plasma specimen has a negative result, consider further genomic testing using tumor specimen as clinically indicated.

Ovarian cancer, recurrent, BRCA mutated, maintenance therapy

Ovarian cancer, recurrent, BRCA mutated, maintenance therapy: Oral: 600 mg twice daily until disease progression or unacceptable toxicity (Ref).

Guideline recommendations: Newly diagnosed stage III to IV epithelial ovarian cancer (off-label population) in complete or partial response to first-line platinum-based chemotherapy: Oral: 600 mg twice daily for 2 years; consider longer durations in select individuals based on a discussion of risk (Ref).

Pancreatic cancer, locally advanced or metastatic, germline BRCA2 mutated, maintenance therapy

Pancreatic cancer, locally advanced or metastatic, germline BRCA2 mutated, maintenance therapy (off-label use): Oral: 600 mg twice daily until disease progression or unacceptable toxicity (Ref).

Prostate cancer, metastatic, castration resistant, BRCA mutated

Prostate cancer, metastatic, castration resistant, BRCA mutated: Oral: 600 mg twice daily until disease progression or unacceptable toxicity (Ref). Patients should also receive a gonadotropin-releasing hormone analog or have had bilateral orchiectomy.

Missed doses: If a dose is missed, administer the next dose at its scheduled time. Do not repeat or replace a vomited dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Note: Kidney function estimated by the Cockcroft-Gault method.

CrCl ≥30 mL/minute at baseline: No dosage adjustment is necessary.

CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Hemodialysis: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Liver Impairment: Adult

Mild to moderate impairment (total bilirubin ≤3 times ULN or AST > ULN): No dosage adjustment is necessary.

Severe impairment (total bilirubin >3 times ULN and any AST): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Adjustment for Toxicity: Adult

Consider therapy interruption or dose reduction if adverse events occur.

Rucaparib Recommended Dose Modifications For Adverse Reactions

Dose reduction

Dose

Starting dose

600 mg twice daily

First dose reduction

500 mg twice daily

Second dose reduction

400 mg twice daily

Third dose reduction

300 mg twice daily

Discontinue rucaparib if unable to tolerate 300 mg twice daily (ASCO [Tew 2020]).

Hematologic toxicity:

Prolonged hematologic toxicity (>4 weeks): Interrupt treatment or reduce the dose; monitor blood counts weekly until recovery.

Anemia (Ref):

Hemoglobin <8 mg/dL and/or requiring a blood transfusion for symptom relief: Monitor.

Repeated anemia: Reduce rucaparib dose to avoid multiple transfusions.

Neutropenia (grade 4 lasting ≥5 to 7 days or associated with fever): Withhold rucaparib until recovery of infection and granulocyte count, then reinitiate with the rucaparib dose reduced. WBC growth factor support may be used while rucaparib is withheld for neutropenia; however, growth factors are not indicated during daily rucaparib dosing (Ref).

Thrombocytopenia: Persistent thrombocytopenia or significant bleeding despite dose reduction: Discontinue rucaparib (Ref).

Secondary myelodysplastic syndrome/acute myeloid leukemia (confirmed): Discontinue rucaparib.

Nonhematologic toxicity:

GI toxicity: Persistent nausea requiring daily antiemetics, resulting in performance status reduction and/or resulting in >5% weight loss: Consider rucaparib dose reduction (Ref).

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.

>10%:

Cardiovascular: Peripheral edema (12%)

Dermatologic: Skin rash (45%)

Endocrine & metabolic: Increased serum cholesterol (39%)

Gastrointestinal: Constipation (39%), decreased appetite (23%), diarrhea (34%; grades 3/4: 2%), dysgeusia (33%), dyspepsia (12%), nausea (79%; grades 3/4: 2%), stomatitis (28%; grades 3/4: <1%), vomiting (37%; grades 3/4: 4%)

Hematologic & oncologic: Anemia (41%; grades 3/4: 26%), leukopenia (39%; grades 3/4: 3%), lymphocytopenia (33%; grades 3/4: 7%), neutropenia (22%; grades 3/4: 8%), thrombocytopenia (35%; grades 3/4: 6%)

Hepatic: Increased serum alanine aminotransferase (67%), increased serum alkaline phosphatase (39%), increased serum aspartate aminotransferase (59%)

Nervous system: Asthenia (≤74%), depression (15%), dizziness (15%), fatigue (≤74%), headache (22%), insomnia (19%)

Renal: Increased serum creatinine (96%)

Respiratory: Dyspnea (17%), nasopharyngitis (≤29%), upper respiratory tract infection (≤29%)

Miscellaneous: Fever (15%)

1% to 10%: Hematologic & oncologic: Acute myelocytic leukemia (≤7%), myelodysplastic syndrome (≤7%)

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Secondary malignancy: Myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) has been reported (rarely) in patients receiving rucaparib; may be potentially fatal. Some cases have occurred during or within 28 days following treatment. The duration of therapy prior to diagnosis of MDS/AML ranged from ~1 month to ~72 months. The cases were typical of secondary MDS or cancer-therapy related AML and all patients had received prior chemotherapy with platinum agents and/or other DNA-damaging medications. In a metastatic castration-resistant prostate cancer trial, MDS/AML was not observed, regardless of homologous recombination deficiency mutation. If prolonged hematologic toxicity occurs and blood counts do not recover to ≤ grade 1 after 4 weeks or if MDS/AML is suspected, further hematology evaluation (including bone marrow and cytogenetic analyses) is necessary.

Other warnings/precautions:

BRCA-mutation status: Select patients for maintenance treatment of recurrent ovarian cancer based on the presence of a deleterious BRCA mutation (germline and/or somatic). Select patients with metastatic castration-resistant prostate cancer for therapy based on the presence of a deleterious BRCA mutation (germline and/or somatic) in plasma specimen; if plasma specimen has a negative result, consider further genomic testing using tumor specimen as clinically indicated (a negative plasma specimen does not mean the tumor is negative for BRCA mutation). Information on approved tests for the detection of BRCA mutations may be found at http://www.fda.gov/companiondiagnostics.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Rubraca: 200 mg [contains fd&c blue #1 (brill blue) aluminum lake, fd&c blue #2 (indigo carm) aluminum lake]

Rubraca: 250 mg, 300 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Rubraca Oral)

200 mg (per each): $173.70

250 mg (per each): $173.70

300 mg (per each): $173.70

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer orally twice daily (~12 hours apart) with or without food. Do not repeat a vomited dose.

Rucaparib is associated with a moderate or high emetic potential; antiemetics are recommended to prevent nausea and vomiting (Ref).

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2024) list; however, it may meet the criteria for a hazardous drug. Rucaparib may cause carcinogenicity, teratogenicity, potential genotoxicity, and has a structural or toxicity profile similar to existing hazardous agents.

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Ovarian cancer, recurrent, BRCA-mutated, maintenance therapy: Maintenance treatment of deleterious BRCA mutation (germline and/or somatic)–associated recurrent ovarian cancer (epithelial, fallopian tube, or primary peritoneal) in adults who are in complete or partial response to platinum-based chemotherapy.

Prostate cancer, metastatic, castration-resistant, BRCA-mutated: Treatment of deleterious BRCA mutation (germline and/or somatic)-associated (as detected by an approved test) metastatic castration-resistant prostate cancer in adults who have been treated with androgen receptor-directed therapy and a taxane-based chemotherapy.

Use: Off-Label: Adult

Pancreatic cancer, locally advanced or metastatic, germline BRCA2-mutated, maintenance therapy

Medication Safety Issues

Sound-alike/look-alike issues:

Rucaparib may be confused with niraparib, olaparib, regorafenib, ripretinib, ruxolitinib, talazoparib.

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).

Metabolism/Transport Effects

Substrate of BCRP, CYP1A2 (Minor), CYP2D6 (Minor), CYP3A4 (Minor), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP, CYP1A2 (Moderate), CYP2C19 (Weak), CYP2C9 (Weak), CYP3A4 (Weak), OATP1B1/1B3;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

5-Aminosalicylic Acid Derivatives: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Agomelatine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Agomelatine. Risk C: Monitor

Alosetron: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Alosetron. Management: Avoid concomitant use of alosetron and moderate CYP1A2 inhibitors whenever possible. If combined use is necessary, monitor for increased alosetron effects/toxicities. Risk D: Consider Therapy Modification

Alpelisib: BCRP/ABCG2 Inhibitors may increase serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider Therapy Modification

ALPRAZolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of ALPRAZolam. Risk C: Monitor

Anagrelide: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Anagrelide. CYP1A2 Inhibitors (Moderate) may increase active metabolite exposure of Anagrelide. Risk C: Monitor

Antithyroid Agents: Myelosuppressive Agents may increase neutropenic effects of Antithyroid Agents. Risk C: Monitor

Atogepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Atogepant. Management: For episodic migraine, the recommended atogepant dose is 10 mg or 30 mg once daily if given with OATP1B1/1B3 inhibitors. For chronic migraine, the recommended atogepant dose is 30 mg once daily with OATP1B1/1B3 inhibitors. Risk D: Consider Therapy Modification

Atrasentan: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Atrasentan. Risk X: Avoid

BCG (Intravesical): Myelosuppressive Agents may decrease therapeutic effects of BCG (Intravesical). Myelosuppressive Agents may increase adverse/toxic effects of BCG (Intravesical). Risk X: Avoid

Bendamustine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Bendamustine. Management: Consider alternatives to moderate CYP1A2 inhibitors during therapy with bendamustine due to the potential for increased bendamustine plasma concentrations and increased bendamustine toxicity. Risk D: Consider Therapy Modification

Brincidofovir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Brincidofovir. Management: Consider alternatives to OATP1B/1B3 inhibitors in patients treated with brincidofovir. If coadministration is required, administer OATP1B1/1B3 inhibitors at least 3 hours after brincidofovir and increase monitoring for brincidofovir adverse reactions. Risk D: Consider Therapy Modification

Caffeine and Caffeine Containing Products: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Caffeine and Caffeine Containing Products. Risk C: Monitor

CarBAMazepine: CYP3A4 Inhibitors (Weak) may increase serum concentration of CarBAMazepine. Risk C: Monitor

Chloramphenicol (Ophthalmic): May increase adverse/toxic effects of Myelosuppressive Agents. Risk C: Monitor

Chloramphenicol (Systemic): Myelosuppressive Agents may increase myelosuppressive effects of Chloramphenicol (Systemic). Risk X: Avoid

Cladribine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk X: Avoid

CloBAZam: CYP2C19 Inhibitors (Weak) may increase serum concentration of CloBAZam. CYP2C19 Inhibitors (Weak) may increase active metabolite exposure of CloBAZam. Risk C: Monitor

ClomiPRAMINE: CYP1A2 Inhibitors (Moderate) may increase serum concentration of ClomiPRAMINE. Risk C: Monitor

CloZAPine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of CloZAPine. Risk C: Monitor

CloZAPine: Myelosuppressive Agents may increase adverse/toxic effects of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor

CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor

Deferiprone: Myelosuppressive Agents may increase neutropenic effects of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider Therapy Modification

Diazoxide Choline: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Diazoxide Choline. Risk C: Monitor

Dofetilide: CYP3A4 Inhibitors (Weak) may increase serum concentration of Dofetilide. Risk C: Monitor

DULoxetine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of DULoxetine. Risk C: Monitor

Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Risk X: Avoid

Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elagolix. Risk X: Avoid

Elbasvir and Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid

Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with OATP1B1/1B3 inhibitors and monitor patients for increased eluxadoline effects/toxicities. Risk D: Consider Therapy Modification

Fexinidazole: Myelosuppressive Agents may increase myelosuppressive effects of Fexinidazole. Risk X: Avoid

Fezolinetant: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Fezolinetant. Risk X: Avoid

Finerenone: CYP3A4 Inhibitors (Weak) may increase serum concentration of Finerenone. Risk C: Monitor

Flibanserin: CYP3A4 Inhibitors (Weak) may increase serum concentration of Flibanserin. Risk C: Monitor

Fosphenytoin-Phenytoin: CYP2C19 Inhibitors (Weak) may increase serum concentration of Fosphenytoin-Phenytoin. Risk C: Monitor

Ixabepilone: CYP3A4 Inhibitors (Weak) may increase serum concentration of Ixabepilone. Risk C: Monitor

Lemborexant: CYP3A4 Inhibitors (Weak) may increase serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider Therapy Modification

Linezolid: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Lomitapide: CYP3A4 Inhibitors (Weak) may increase serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Risk D: Consider Therapy Modification

Mavacamten: CYP2C19 Inhibitors (Weak) may increase serum concentration of Mavacamten. Management: Start mavacamten at 5 mg/day if stable on a weak CYP2C19 inhibitor, and reduce the mavacamten dose by one dose level if initiating a weak CYP2C19 inhibitor. Avoid initiating weak CYP2C19 inhibitors in patients on mavacamten 2.5 mg/day. Risk D: Consider Therapy Modification

Melatonin: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Melatonin. Risk C: Monitor

Midazolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of Midazolam. Risk C: Monitor

Momelotinib: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Momelotinib. Risk C: Monitor

NiMODipine: CYP3A4 Inhibitors (Weak) may increase serum concentration of NiMODipine. Risk C: Monitor

OLANZapine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of OLANZapine. Risk C: Monitor

Olaparib: Myelosuppressive Agents may increase myelosuppressive effects of Olaparib. Risk C: Monitor

PAZOPanib: BCRP/ABCG2 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid

Pentoxifylline: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Pentoxifylline. Risk C: Monitor

Pimozide: CYP3A4 Inhibitors (Weak) may increase serum concentration of Pimozide. Risk X: Avoid

Pirfenidone: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Pirfenidone. Management: Avoid concomitant use of pirfenidone and moderate CYP1A2 inhibitors whenever possible. If combined, decrease the pirfenidone dose to 1,602 mg per day (534 mg three times daily) and monitor for increased pirfenidone toxicities. Risk D: Consider Therapy Modification

Pomalidomide: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Pomalidomide. Risk C: Monitor

Promazine: May increase myelosuppressive effects of Myelosuppressive Agents. Risk C: Monitor

Propranolol: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Propranolol. Risk C: Monitor

Ramelteon: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Ramelteon. Risk C: Monitor

Ramosetron: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Ramosetron. Risk C: Monitor

Rasagiline: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Rasagiline. Management: Limit rasagiline dose to 0.5 mg once daily in patients taking moderate CYP1A2 inhibitors. Risk D: Consider Therapy Modification

Resmetirom: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Resmetirom. Risk X: Avoid

Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase active metabolite exposure of Revefenacin. Risk X: Avoid

Ropeginterferon Alfa-2b: Myelosuppressive Agents may increase myelosuppressive effects of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider Therapy Modification

ROPINIRole: CYP1A2 Inhibitors (Moderate) may increase serum concentration of ROPINIRole. Risk C: Monitor

ROPivacaine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of ROPivacaine. Risk C: Monitor

Seladelpar: BCRP/ABCG2 Inhibitors may increase serum concentration of Seladelpar. Risk C: Monitor

Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentration of Simvastatin. CYP3A4 Inhibitors (Weak) may increase active metabolite exposure of Simvastatin. Risk C: Monitor

Sirolimus (Conventional): CYP3A4 Inhibitors (Weak) may increase serum concentration of Sirolimus (Conventional). Risk C: Monitor

Sirolimus (Protein Bound): CYP3A4 Inhibitors (Weak) may increase serum concentration of Sirolimus (Protein Bound). Management: Reduce the dose of protein bound sirolimus to 56 mg/m2 when used concomitantly with a weak CYP3A4 inhibitor. Risk D: Consider Therapy Modification

Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor

Talazoparib: BCRP/ABCG2 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor

Tasimelteon: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Tasimelteon. Risk C: Monitor

Taurursodiol: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Taurursodiol. Risk X: Avoid

Theophylline Derivatives: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Theophylline Derivatives. Management: Consider avoidance of this combination. If coadministration is necessary, monitor for increased theophylline serum concentrations and toxicities when combined. Theophylline dose reductions will likely be required. Risk D: Consider Therapy Modification

TiZANidine: CYP1A2 Inhibitors (Moderate) may increase serum concentration of TiZANidine. Management: Avoid the use of tizanidine with moderate CYP1A2 inhibitors when possible. If combined, monitor closely for increased tizanidine toxicities (eg, hypotension, bradycardia, drowsiness). Tizanidine dose reduction or discontinuation may be necessary. Risk D: Consider Therapy Modification

TOLBUTamide: CYP2C9 Inhibitors (Weak) may increase serum concentration of TOLBUTamide. Risk C: Monitor

Topotecan: BCRP/ABCG2 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid

Triazolam: CYP3A4 Inhibitors (Weak) may increase serum concentration of Triazolam. Risk C: Monitor

Ubrogepant: Rucaparib may increase serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with rucaparib. Risk D: Consider Therapy Modification

Vitamin K Antagonists: CYP2C9 Inhibitors (Weak) may increase serum concentration of Vitamin K Antagonists. Risk C: Monitor

Vorasidenib: CYP1A2 Inhibitors (Moderate) may increase serum concentration of Vorasidenib. Management: Avoid concurrent use with moderate CYP1A2 inhibitors when possible. If combined use cannot be avoided, monitor for evidence of adverse effects and adjust vorasidenib dose accordingly if necessary. Risk D: Consider Therapy Modification

Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Voxilaprevir. Risk X: Avoid

Zavegepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentration of Zavegepant. Risk X: Avoid

Reproductive Considerations

Evaluate pregnancy status prior to use in patients who could become pregnant.

Patients who could become pregnant should use effective contraception during therapy and for 6 months after the last rucaparib dose. Patients with partners who could become pregnant or with partners who are pregnant should use effective contraception during treatment and for 3 months after the last rucaparib dose. Patients also should not donate sperm during therapy and for 3 months following the last rucaparib dose.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to rucaparib may cause fetal harm.

Breastfeeding Considerations

It is not known if rucaparib is present in breast milk. Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during treatment and for 2 weeks following the last dose.

Monitoring Parameters

BRCA mutation testing (for recurrent ovarian cancer and for metastatic castration-resistant prostate cancer). Evaluate for germline BRCA2 mutation in pancreatic cancer (off-label use). CBC at baseline and monthly thereafter, or as clinically indicated (weekly until recovery for prolonged hematologic toxicity). Further hematology evaluation (including bone marrow and cytogenetic analyses) is necessary for prolonged hematologic toxicity if blood counts do not recover to ≤ grade 1 after 4 weeks or if myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) is suspected. Evaluate pregnancy status (prior to treatment initiation in patients who could become pregnant). Monitor for signs/symptoms of MDS/AML. Monitor adherence.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Rucaparib is a poly (ADP-ribose) polymerase (PARP) enzyme inhibitor, including PARP1, PARP2, and PARP3. PARP enzymes are involved in DNA transcription, cell cycle regulation, and DNA repair. By inhibiting PARP, rucaparib may cause increased formation of PARP-DNA complexes, resulting in DNA damage, apoptosis, and cancer cell death. Increased cytotoxicity and anti-tumor activity due to rucaparib was observed in tumor cell lines deficient in BRCA1/2 and other DNA repair genes.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Cmax is increased by 20%, AUC is increased by 38%, and Tmax is delayed by 2.5 hours following a high-fat meal (~800 to 1,000 calories, including ~250 calories from carbohydrates, ~500 to 600 calories from fat, and ~150 calories from protein), as compared to fasted conditions.

Distribution: Vd: 2,300 L.

Protein binding: 70%.

Metabolism: Primarily hepatic via CYP2D6; minor pathways include CYP1A2 and CYP3A4; oxidation, N-demethylation, N-methylation, and glucuronidation are the major metabolic pathways.

Bioavailability: 36% (range: 30% to 45%).

Half-life elimination: Terminal: 26 hours.

Time to peak: 1.9 hours.

Excretion: Urine (~45%); feces (~95%).

Clearance: 44.2 L/hour.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Rubraca | Rucafas;
  • (CZ) Czech Republic: Rubraca;
  • (DE) Germany: Rubraca;
  • (ES) Spain: Rubraca;
  • (FR) France: Rubraca;
  • (GB) United Kingdom: Rubraca;
  • (HU) Hungary: Rubraca;
  • (IN) India: Bdparib | Lucaparib | Nuparp | Rucaza;
  • (IT) Italy: Rubraca;
  • (NL) Netherlands: Rubraca;
  • (PL) Poland: Rubraca;
  • (PR) Puerto Rico: Rubraca
  1. Abida W, Patnaik A, Campbell D, et al. Rucaparib in men with metastatic castration-resistant prostate cancer harboring a BRCA1 or BRCA2 gene alteration. J Clin Oncol. Published online August 14, 2020. doi:10.1200/JCO.20.01035 [PubMed 32795228]
  2. Coleman RL, Oza AM, Lorusso D, et al. Rucaparib maintenance treatment for recurrent ovarian carcinoma after response to platinum therapy (ARIEL3): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet. 2017;390(10106):1949-1961. [PubMed 28916367]
  3. Drew Y, Ledermann J, Hall G, et al. Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer. Br J Cancer. 2016;114(7):723-730. [PubMed 27002934] 10.1038/bjc.2016.41
  4. Fizazi K, Piulats JM, Reaume MN, et al; TRITON3 Investigators. Rucaparib or physician's choice in metastatic prostate cancer. N Engl J Med. 2023;388(8):719-732. doi:10.1056/NEJMoa2214676 [PubMed 36795891]
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