Olanib 150 mg, containing Niraparib, is an oral PARP (poly ADP-ribose polymerase) inhibitor indicated for the treatment of advanced breast and ovarian cancers:

• Breast Cancer: Monotherapy for adult patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm), HER2-negative metastatic breast cancer who have previously received chemotherapy in the neoadjuvant, adjuvant, or metastatic setting. Hormone receptor-positive patients must have progressed on, or be considered inappropriate for, endocrine therapy. Germline BRCA mutation must be confirmed prior to treatment.

• Ovarian Cancer: Monotherapy for maintenance treatment of adult patients with platinum-sensitive relapsed high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer who achieved complete or partial response to prior platinum-based chemotherapy.

Mode of Action

Olanib 150 mg selectively inhibits PARP1, PARP2, and PARP3 enzymes, which are essential for DNA repair, transcription, and cell cycle regulation. By blocking PARP activity, Olanib induces accumulation of DNA damage, particularly in tumor cells deficient in BRCA or homologous recombination repair. This leads to cell death and prevents cancer progression.

Pharmacology

• Mechanism: Inhibits PARP enzymatic activity and increases formation of PARP-DNA complexes, disrupting cellular homeostasis.

• Absorption: Rapidly absorbed with oral administration; food does not significantly affect absorption.

• Metabolism: Primarily metabolized by CYP3A.

• Elimination: Excreted mainly via urine and feces.

Dosage & Administration

• Standard Dose: 600 mg daily, taken as two 150 mg tablets twice daily.

• Dose Reduction: 100 mg tablets are available for dose adjustments if required.

• Ovarian Cancer: Treatment should start within 8 weeks after completion of the final platinum-based chemotherapy dose. Patients must have recovered from prior hematologic toxicities (hemoglobin, platelet, neutrophil counts ≤ CTCAE grade 1).

Administration Tips:

• Swallow tablets whole.

• Avoid grapefruit or other CYP3A inhibitors during treatment.

• Continue treatment until disease progression or unacceptable toxicity.

Drug Interactions

• Avoid co-administration with strong CYP3A inhibitors or inducers, which may increase or decrease Olanib plasma concentration.

• Monotherapy dose is not recommended with other myelosuppressive anticancer agents, as this increases hematologic toxicity.

Contraindications

• Hypersensitivity to Olanib or any excipients in the formulation.

Side Effects

Common adverse effects include anemia, thrombocytopenia, neutropenia, fatigue, and nausea. Serious adverse reactions may include:

• Myelodysplastic syndrome (MDS)/acute myeloid leukemia (AML) – potentially fatal, monitor hematologic parameters monthly.

• Pneumonitis – interrupt treatment if suspected and discontinue if confirmed.

• Dermatitis, decreased neutrophil or platelet counts in rare cases.

Approximately 4.9% of patients permanently discontinued Olanib due to adverse events. Hematologic toxicities are the most frequent reasons for dose interruption or reduction.

Pregnancy & Lactation

• Can cause fetal harm; effective contraception is required during treatment and after discontinuation.

• Unknown excretion in breast milk; breastfeeding is not recommended during therapy.

Precautions & Warnings

• Monitor hematologic parameters, liver function, and pulmonary status regularly.

• Adjust or discontinue therapy for severe adverse events.

• Patients should be informed of potential embryo-fetal toxicity and serious hematologic effects.

Pediatric Use

• Safety and efficacy not established in pediatric patients.

Therapeutic Class

Targeted Cancer Therapy / PARP Inhibitor

Storage Conditions

Store in a dry place below 30°C, protected from light, and out of reach of children.