Rucaparib Camsylate CAS No. 1859053-21-6

Pharmaceutical Use

• Therapeutic Area: Oncology

• Primary Indications: Ovarian cancer, prostate cancer, and other solid tumors with BRCA mutations

• Mechanism of Action: PARP enzyme inhibition → impaired DNA repair → synthetic lethality in BRCA-mutated cells

• Route of Administration: Oral (capsules or tablets)

• Clinical Status: Approved as the free base (rucaparib) under the brand name Rubraca®. The camsylate salt is used for formulation stability and improved physicochemical properties during drug development and manufacturing.

Pharmacology and Mechanism of Action

• Drug Class: PARP Inhibitor

• Mechanism: Rucaparib inhibits the PARP enzymes (primarily PARP-1, PARP-2, and PARP-3), which are involved in DNA repair, particularly the repair of single-strand breaks.

• Synthetic Lethality: In cancer cells with deficient Homologous Recombination Repair (HRR) pathways—such as those with BRCA1 or BRCA2 mutations—the inhibition of PARP leads to an accumulation of DNA damage that the cancer cell cannot repair. This synthetic lethality causes selective cancer cell death while sparing healthy cells with functional HRR.

Clinical Use and Indications

Rucaparib is approved under the brand name Rubraca® for the treatment of:

• Ovarian Cancer:

  • Maintenance Treatment: For adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy.

  • Treatment of Advanced Cancer: For adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated epithelial ovarian, fallopian tube, or primary peritoneal cancer who have been treated with two or more chemotherapies.

• Prostate Cancer:

  • Treatment of mCRPC: For adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor-directed therapy and a taxane-based chemotherapy.

Chemical and Structural Information

• Name: Rucaparib camsylate

• Synonyms: Rucaparib camphorsulfonate, CO-338, PF-1367338-BW

• Chemical Class: Poly(ADP-ribose) polymerase (PARP) inhibitor (antineoplastic agent)

• Structural Features: Contains fluorophenyl and sulfonate groups, enhancing water solubility and stability.

• Salt Form: Camsylate (camphorsulfonate) salt of rucaparib

Chemical Features

• Appearance: White to off-white crystalline powder

• Solubility: Freely soluble in water and DMSO; limited solubility in nonpolar solvents

• Melting Point: Around 200–210 °C (varies by polymorph)

• Storage: Stable under dry, dark conditions at room temperature. Temperature: -20°C (Shelf Life: 2 Years). Use as soon as possible after dissolution.

Important Safety Information

• Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): Occurred in patients exposed to Rucaparib, and can be fatal. Patients should be monitored for hematological toxicity.

• Embryo-Fetal Toxicity: Can cause fetal harm. Women of childbearing potential should use effective contraception.

• Other Common Adverse Reactions: Include nausea, fatigue, asthenia, vomiting, anemia, abdominal pain, dysgeusia (altered taste), constipation, decreased appetite, diarrhea, thrombocytopenia, and dyspnea.

Product Documents

• Safety Data Sheet (SDS)
• Certificate of Analysis
• Product Brochure
• Technical Data Sheet