Note: Rucaparib is associated with a moderate or high emetic potential; antiemetics are recommended to prevent nausea and vomiting (ASCO [Hesketh 2020]). Do not initiate treatment until after hematologic recovery (to grade 1 or lower) from prior chemotherapy. 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: Oral: 600 mg twice daily until disease progression or unacceptable toxicity (Coleman 2017; Ledermann 2020).
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 (ASCO [Tew 2022]).
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 (Reiss 2021).
Prostate cancer, metastatic, castration resistant, BRCA-mutated: Oral: 600 mg twice daily until disease progression or unacceptable toxicity (Abida 2000; Fizazi 2023). 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.
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).
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).
Consider therapy interruption or dose reduction if adverse events occur.
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 (ASCO [Tew 2020]):
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 (ASCO (Tew 2020]).
Thrombocytopenia: Persistent thrombocytopenia or significant bleeding despite dose reduction: Discontinue rucaparib (ASCO [Tew 2020]).
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 (ASCO [Tew 2020]).
Refer to adult dosing.
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%)
There are no contraindications listed in the manufacturer's labeling.
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.
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
No
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.
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 (ASCO [Hesketh 2020]).
This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Rucaparib may cause carcinogenicity, teratogenicity, reproductive toxicity, and potential genotoxicity.
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 2016; 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.
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.
Pancreatic cancer, locally advanced or metastatic, germline BRCA2-mutated, maintenance therapy
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).
Substrate of BCRP/ABCG2, CYP1A2 (minor), CYP2D6 (minor), CYP3A4 (minor), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP/ABCG2, CYP1A2 (moderate), CYP2C19 (weak), CYP2C9 (weak), CYP3A4 (weak), OATP1B1/1B3 (SLCO1B1/1B3)
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 enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Agomelatine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Agomelatine. Risk C: Monitor therapy
Alosetron: CYP1A2 Inhibitors (Moderate) may increase the 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 the 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 the serum concentration of ALPRAZolam. Risk C: Monitor therapy
Anagrelide: CYP1A2 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Anagrelide. CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Anagrelide. Risk C: Monitor therapy
Antithyroid Agents: Myelosuppressive Agents may enhance the neutropenic effect of Antithyroid Agents. Risk C: Monitor therapy
Atogepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the 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
BCG (Intravesical): Myelosuppressive Agents may enhance the adverse/toxic effect of BCG (Intravesical). Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination
Bendamustine: CYP1A2 Inhibitors (Moderate) may increase the 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
Berotralstat: BCRP/ABCG2 Inhibitors may increase the serum concentration of Berotralstat. Management: Decrease the berotralstat dose to 110 mg daily when combined with BCRP inhibitors. Risk D: Consider therapy modification
Brincidofovir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the 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 the serum concentration of Caffeine and Caffeine Containing Products. Risk C: Monitor therapy
CarBAMazepine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of CarBAMazepine. Risk C: Monitor therapy
Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Risk C: Monitor therapy
Chloramphenicol (Systemic): Myelosuppressive Agents may enhance the myelosuppressive effect of Chloramphenicol (Systemic). Risk X: Avoid combination
Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk X: Avoid combination
CloBAZam: CYP2C19 Inhibitors (Weak) may increase serum concentrations of the active metabolite(s) of CloBAZam. CYP2C19 Inhibitors (Weak) may increase the serum concentration of CloBAZam. Risk C: Monitor therapy
ClomiPRAMINE: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ClomiPRAMINE. Risk C: Monitor therapy
CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor therapy
CloZAPine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of CloZAPine. Risk C: Monitor therapy
CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect 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
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Risk C: Monitor therapy
DULoxetine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of DULoxetine. Risk C: Monitor therapy
Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Risk X: Avoid combination
Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Risk X: Avoid combination
Elbasvir and Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid combination
Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the 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 enhance the myelosuppressive effect of Fexinidazole. Risk X: Avoid combination
Fezolinetant: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Fezolinetant. Risk X: Avoid combination
Finerenone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Finerenone. Risk C: Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Risk C: Monitor therapy
Fosphenytoin-Phenytoin: CYP2C19 Inhibitors (Weak) may increase the serum concentration of Fosphenytoin-Phenytoin. Risk C: Monitor therapy
Ixabepilone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ixabepilone. Risk C: Monitor therapy
Lemborexant: CYP3A4 Inhibitors (Weak) may increase the 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 enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the 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 the serum concentration of Mavacamten. Management: Start mavacamten at 5 mg/day if stable on a weak CYP2C19 inhibitor. For those stable on mavacamten who are initiating a weak CYP2C19 inhibitor, reduce mavacamten dose by one dose level. Risk D: Consider therapy modification
Melatonin: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Melatonin. Risk C: Monitor therapy
Midazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Midazolam. Risk C: Monitor therapy
Momelotinib: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Momelotinib. Risk C: Monitor therapy
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Risk C: Monitor therapy
OLANZapine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of OLANZapine. Risk C: Monitor therapy
Olaparib: Myelosuppressive Agents may enhance the myelosuppressive effect of Olaparib. Risk C: Monitor therapy
PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
Pentoxifylline: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Pentoxifylline. Risk C: Monitor therapy
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Risk X: Avoid combination
Pirfenidone: CYP1A2 Inhibitors (Moderate) may increase the 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 the serum concentration of Pomalidomide. Risk C: Monitor therapy
Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Propranolol: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Propranolol. Risk C: Monitor therapy
Ramelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramelteon. Risk C: Monitor therapy
Ramosetron: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Ramosetron. Risk C: Monitor therapy
Rasagiline: CYP1A2 Inhibitors (Moderate) may increase the 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 the serum concentration of Resmetirom. Risk X: Avoid combination
Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Risk X: Avoid combination
Ropeginterferon Alfa-2b: Myelosuppressive Agents may enhance the myelosuppressive effect 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 the serum concentration of ROPINIRole. Risk C: Monitor therapy
ROPivacaine: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of ROPivacaine. Risk C: Monitor therapy
Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentrations of the active metabolite(s) of Simvastatin. CYP3A4 Inhibitors (Weak) may increase the serum concentration of Simvastatin. Risk C: Monitor therapy
Sirolimus (Conventional): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy
Sirolimus (Protein Bound): CYP3A4 Inhibitors (Weak) may increase the 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 the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Risk C: Monitor therapy
Tasimelteon: CYP1A2 Inhibitors (Moderate) may increase the serum concentration of Tasimelteon. Risk C: Monitor therapy
Taurursodiol: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Taurursodiol. Risk X: Avoid combination
Theophylline Derivatives: CYP1A2 Inhibitors (Moderate) may increase the 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 the serum concentration of TiZANidine. Management: If combined use cannot be avoided, initiate tizanidine in adults at 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Risk D: Consider therapy modification
TOLBUTamide: CYP2C9 Inhibitors (Weak) may increase the serum concentration of TOLBUTamide. Risk C: Monitor therapy
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Risk C: Monitor therapy
Ubrogepant: Rucaparib may increase the 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 (eg, warfarin): CYP2C9 Inhibitors (Weak) may increase the serum concentration of Vitamin K Antagonists. Risk C: Monitor therapy
Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Risk X: Avoid combination
Zavegepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Zavegepant. Risk X: Avoid combination
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.
Based on the mechanism of action and data from animal reproduction studies, in utero exposure to rucaparib may cause fetal harm.
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.
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.
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.
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.
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