Rucaza Rucaparib Tablets

Chinese Name: Rucaparib Tablets

English Name: Rucaparib Tablets

Brand Names: Rubraca, Rucaza

Other Names: Rucaparib

Dosage Form: Film-coated tablets

Specifications: 200 mg × 60 tablets/box; 300 mg × 60 tablets/box

Manufacturer: Intas Pharmaceuticals Pvt. Ltd.

1. Composition

Active Ingredient: Rucaparib camsylate (equivalent to 200 mg, 250 mg, or 300 mg of rucaparib)

Excipients: Microcrystalline cellulose, sodium starch glycolate, colloidal silicon dioxide, magnesium stearate; film coating contains polyvinyl alcohol, titanium dioxide, polyethylene glycol, and talc. Tablet colors: 200 mg (white), 250 mg (pale yellow), 300 mg (blue).

2. Indications

2.1 Ovarian Cancer

Maintenance Treatment: Indicated for adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who have achieved a complete or partial response to platinum-based chemotherapy and harbor a deleterious BRCA mutation (germline and/or somatic).

Later-line Treatment: Indicated for adult patients with epithelial ovarian, fallopian tube, or primary peritoneal cancer who have received ≥2 prior chemotherapy regimens and harbor a deleterious BRCA mutation (germline and/or somatic).

2.2 Prostate Cancer

Indicated for adult patients with metastatic castration-resistant prostate cancer (mCRPC) who harbor a deleterious BRCA mutation (germline and/or somatic) and have previously received androgen receptor-directed therapy.

3. Dosage and Administration

3.1 Recommended Dosage

Standard dose: 600 mg (two 300 mg tablets) orally twice daily (approximately 12 hours apart); may be taken with or without food.

Duration of treatment: Until disease progression or unacceptable toxicity.

Prostate cancer: Must be administered concomitantly with a GnRH analogue or following bilateral orchiectomy.

3.2 Management of Missed Doses/Vomiting

Missed dose: Do not take a replacement dose; take the next dose at the scheduled time.

Vomiting: Do not take a replacement dose; take the next dose as scheduled.

3.3 Dose Modification (Adverse Reactions)

Dose modification regimen |

First dose reduction: 500 mg (two 250 mg tablets) twice daily

Second dose reduction: 400 mg (two 200 mg tablets) twice daily

Third dose reduction: 300 mg (one 300 mg tablet) twice daily

Intolerance: Permanently discontinue treatment

3.4 Special Populations

Hepatic impairment: No adjustment needed for mild impairment (Child-Pugh A); use with caution in moderate to severe impairment (Child-Pugh B/C).

Renal impairment: No adjustment needed for mild to moderate impairment (CrCl 30–89 mL/min); no data available for severe impairment (CrCl <30 mL/min).

Elderly: No dose adjustment required for patients ≥65 years of age.

4. Contraindications

Contraindicated in patients with hypersensitivity to rucaparib or any excipients.

5. Warnings and Precautions

5.1 Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML)

Risk: Rare but fatal; incidence <1%.

Monitoring: Complete blood count (CBC) at baseline and monthly; withhold treatment and perform bone marrow examination in cases of prolonged cytopenia (>4 weeks).

Management: Permanently discontinue treatment upon confirmed diagnosis of MDS/AML.

5.2 Hematologic Toxicity

Common: Anemia, neutropenia, thrombocytopenia.

Monitoring: Monthly CBC; withhold treatment for Grade 1/2 toxicity until recovery, then resume at a reduced dose; discontinue treatment for Grade ≥3 toxicity.

5.3 Embryo-Fetal Toxicity

Risk: May cause fetal harm

Contraception: Effective contraception required for women during treatment and for 6 months after discontinuation; for men, during treatment and for 3 months after discontinuation

Pregnancy: Contraindicated in pregnant women; discontinue breastfeeding

5.4 Gastrointestinal Toxicity

Common: Nausea, vomiting, diarrhea, constipation, abdominal pain

Management: Symptomatic treatment with antiemetics/antidiarrheals; reduce dose or discontinue drug in severe cases

5.5 Hepatotoxicity

Common: Elevated ALT/AST (mostly Grade 1–2)

Monitoring: Check liver function at baseline and monthly for the first 3 months of treatment; thereafter, every 3 months

Management: For elevations ≥Grade 3, withhold drug until recovery, then resume at a reduced dose

6. Adverse Reactions

6.1 Common Adverse Reactions (≥20%)

Digestive system: Nausea (77%), vomiting (46%), diarrhea (34%), constipation (33%), abdominal pain (22%)

Hematologic system: Anemia (50%), neutropenia (26%), thrombocytopenia (21%)

Systemic symptoms: Asthenia/fatigue (65%), decreased appetite (37%)

Other: Elevated AST/ALT (34%), taste disturbance (25%), rash (21%)

6.2 Serious Adverse Reactions (≥2%)

Anemia (9%), neutropenia (7%), thrombocytopenia (4%), pneumonia (3%), febrile neutropenia (2%)

7. Drug Interactions

CYP3A inhibitors (ketoconazole, itraconazole, clarithromycin): Increase rucaparib plasma concentrations; avoid co-administration

CYP3A inducers (rifampin, phenytoin, carbamazepine): Decrease rucaparib plasma concentrations; avoid co-administration

P-gp substrates (digoxin): Rucaparib increases their plasma concentrations; monitor and adjust dosage

8. Pharmacological Action

Mechanism of action: An oral PARP-1/2/3 inhibitor that blocks DNA damage repair; tumors with BRCA mutations exhibit DNA repair defects, leading to cancer cell death.

Pharmacokinetics: Rapid oral absorption (Tmax 1.5–2 h), absolute bioavailability 54%; steady-state volume of distribution 208 L, protein binding 70%; metabolized by CYP3A4, half-life 17–19 h; 70% excreted via feces and 30% via urine.

9. Storage

Room temperature: 20–25°C (68–77°F); 15–30°C permissible for short-term transport.

Store in a sealed container in a dry place, protected from light; keep out of reach of children.

11. Shelf Life

24 months

Specifications

Product Name: Rucaparib 200 mg/300 mg × 60 Tablets (Rucaza)