Olanib150 mg

Olanib is a poly (ADP-ribose) polymerase (PARP) inhibitor approved for several BRCA-mutated or homologous-recombination-deficient (HRD) cancers, most often as maintenance therapy after response to chemotherapy. Indications are classified below by strength of evidence.

FDA-Approved / Established Uses

• Ovarian cancer: First-line maintenance treatment of BRCA-mutated advanced epithelial ovarian, fallopian tube, or primary peritoneal cancer in patients who have achieved a complete or partial response to first-line platinum-based chemotherapy; maintenance treatment of BRCA-mutated recurrent ovarian cancer in response to platinum-based chemotherapy.
• Ovarian cancer (combination/adjunct use): First-line maintenance treatment of HRD-positive advanced ovarian cancer, used in combination with bevacizumab, in patients responding to first-line platinum-based chemotherapy plus bevacizumab.
• Breast cancer: Adjuvant treatment of germline BRCA-mutated, HER2-negative high-risk early breast cancer after neoadjuvant or adjuvant chemotherapy; treatment of germline BRCA-mutated, HER2-negative metastatic breast cancer in patients previously treated with chemotherapy (hormone-receptor-positive disease requires prior endocrine therapy or is considered ineligible for it).
• Pancreatic cancer: First-line maintenance treatment of germline BRCA-mutated metastatic pancreatic adenocarcinoma in patients whose disease has not progressed on at least 16 weeks of first-line platinum-based chemotherapy.
• Prostate cancer: Treatment of germline or somatic homologous-recombination-repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC) that has progressed after prior treatment with enzalutamide or abiraterone.
• Prostate cancer (combination use): Treatment of BRCA-mutated mCRPC, used in combination with abiraterone and prednisone/prednisolone.

All indications require documented BRCA mutation, HRR gene mutation, or HRD status (confirmed by an approved companion diagnostic test) unless otherwise specified. Use of Olanib outside these confirmed biomarker settings is not supported by current evidence.

Each film-coated tablet contains Olaparib as the active pharmaceutical ingredient, commonly available in strengths of 100 mg and 150 mg. Tablet formulations also contain standard pharmaceutical excipients (fillers, binders, and coating agents) that do not affect the therapeutic action of Olaparib.

Olanib is an orally administered, first-in-class poly (ADP-ribose) polymerase (PARP) inhibitor used in the treatment of certain BRCA-mutated and homologous-recombination-deficient cancers. It works by blocking DNA repair enzymes in cancer cells that already have impaired DNA-repair capacity, leading to selective cancer-cell death (a mechanism known as "synthetic lethality").

Olanib is used mainly as maintenance therapy or later-line treatment in ovarian, breast, pancreatic, and prostate cancers, either alone or in combination with other agents such as bevacizumab or abiraterone/prednisone, depending on the specific approved indication.

Antineoplastic agent — Poly (ADP-ribose) polymerase (PARP) inhibitor

Olaparib inhibits PARP enzymes (PARP1, PARP2, and PARP3), which are involved in repairing single-strand DNA breaks. Inhibition of PARP causes persistent DNA damage and trapping of PARP-DNA complexes at replication forks.

In cells with a pre-existing defect in homologous recombination repair (e.g., BRCA1/BRCA2 mutations or other HRD status), the additional DNA damage caused by Olaparib cannot be repaired, leading to accumulation of DNA double-strand breaks, cell-cycle arrest, and cancer-cell death. This selective toxicity toward HRD/BRCA-mutated cells, while sparing most normal cells, is called synthetic lethality.

Olaparib is absorbed orally, extensively metabolized in the liver mainly by the CYP3A enzyme system, and eliminated predominantly through metabolism, with excretion in both urine and feces.

Take Olanib tablets whole, with a glass of water, with or without food. Do not chew, crush, dissolve, or split the tablets. Try to take each dose at the same times each day, roughly 12 hours apart, to maintain steady drug levels.

If a dose is missed, take the next dose at its regularly scheduled time; do not take an extra dose to make up for the missed one. If vomiting occurs after a dose, do not take a replacement dose — simply continue with the next scheduled dose.

Olanib tablets and capsules are not interchangeable milligram-for-milligram; only take the formulation and strength prescribed.

The most clinically significant interactions with Olanib involve drugs that affect the CYP3A enzyme system, which is responsible for metabolizing Olanib.

• Strong or moderate CYP3A inhibitors (e.g., itraconazole, ketoconazole, clarithromycin, certain protease inhibitors such as ritonavir, and grapefruit/grapefruit juice for strong inhibition; fluconazole and similar agents for moderate inhibition): These can significantly raise Olanib blood levels, increasing the risk of toxicity. Concomitant use should be avoided; if unavoidable, the physician will reduce the Olanib dose.
• Strong or moderate CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort for strong induction; efavirenz and similar agents for moderate induction): These can substantially lower Olanib blood levels, reducing its effectiveness. Concomitant use should be avoided where possible; alternative agents should be considered.

Patients should inform their physician of all prescription drugs, over-the-counter medicines, and herbal supplements they are taking before and during treatment with Olanib.

Side effects of Olanib range from common, generally manageable effects to rare but serious reactions requiring urgent medical attention.

Common Side Effects

• Nausea and vomiting
• Fatigue and weakness (asthenia)
• Anemia
• Diarrhea
• Decreased appetite
• Headache and dizziness
• Altered taste (dysgeusia)
• Cough and shortness of breath
• Low blood cell counts: neutropenia, leukopenia, thrombocytopenia

Serious Side Effects (Seek Medical Attention)

• Signs of myelodysplastic syndrome/acute myeloid leukemia (unusual bruising or bleeding, prolonged fever, persistent fatigue) — see Precautions and Warnings.
• Signs of pneumonitis (new or worsening shortness of breath, cough, fever) — see Precautions and Warnings.
• Signs of blood clots (leg swelling/pain, sudden chest pain, breathlessness).
• Signs of liver injury (yellowing of skin/eyes, dark urine, severe fatigue).

Patients should report any severe or persistent side effect to their physician promptly.

Olanib can cause fetal harm and is not recommended during pregnancy. Animal studies have shown embryo-fetal toxicity and malformations at doses below the recommended human dose.

• Females of reproductive potential should use effective, non-hormonal contraception during treatment with Olanib and for at least 6 months after the final dose.
• Males with pregnant or potentially pregnant partners should use effective contraception during treatment and for at least 3 months after the final dose.
• If pregnancy occurs during treatment, the physician must be informed immediately so risks can be assessed.
• Breastfeeding is not recommended during treatment with Olanib and for at least one month after the final dose, due to the potential for serious adverse effects in a nursing infant.

Olanib should be used in pregnancy or lactation only if clearly needed and if the potential benefit justifies the potential risk to the fetus or infant; always consult a physician before use in these situations.

Treatment with Olanib requires close monitoring for the following important risks:

Myelodysplastic Syndrome / Acute Myeloid Leukemia (MDS/AML)

MDS/AML has occurred in a small percentage of patients treated with Olanib, usually more than a year after starting treatment, and has been fatal in some cases. Risk is higher in patients with prior chemotherapy or radiotherapy. Complete blood count (CBC) should be checked at baseline and monthly during treatment. If prolonged hematologic toxicity occurs, treatment should be interrupted and the patient evaluated; if MDS/AML is confirmed, Olanib should be discontinued.

Pneumonitis

Pneumonitis, including fatal cases, has been reported. Treatment should be interrupted if pneumonitis is suspected (new or worsening respiratory symptoms) and discontinued if confirmed.

Venous Thromboembolism (VTE)

Increased rates of VTE, including pulmonary embolism, have been observed, particularly in combination regimens. Patients should be monitored for signs of blood clots and managed with anticoagulation as clinically indicated.

Hepatotoxicity

Liver enzyme elevations and drug-induced liver injury have been reported. Liver function should be monitored at baseline and periodically during treatment.

Embryo-Fetal Toxicity

See Pregnancy and Lactation section for full detail on contraception requirements.

Renal Impairment

Use with caution and with dose reduction in moderate renal impairment; not recommended in severe renal impairment due to insufficient data.

There is no specific antidote for Olanib overdose. Symptoms of overdose may include worsening of known side effects such as severe nausea, vomiting, and bone marrow suppression (low blood counts).

If an overdose of Olanib is suspected, seek immediate medical attention or contact emergency services / a poison control center right away. Management is supportive and should be directed by qualified medical personnel; general measures may include close clinical monitoring and blood count surveillance. Do not attempt to manage a suspected overdose at home.

Store at room temperature (below 30°C), in the original container to protect from moisture, and away from direct light. Do not remove the desiccant if present. Keep out of reach and sight of children.

Renal Impairment

Dose reduction to 200 mg twice daily is recommended in moderate renal impairment (creatinine clearance 31–50 mL/min). Use in severe renal impairment or dialysis is not recommended due to lack of data.

Hepatic Impairment

No dose adjustment is needed in mild hepatic impairment. Olanib has not been well studied in moderate-to-severe hepatic impairment; use with caution.

Elderly Patients

No specific dose adjustment is required based on age alone, though clinical experience in patients over 65 years is more limited; monitor as for other adults.

Pediatric Patients

Safety and efficacy of Olanib have not been established in pediatric patients; see Pediatric Uses.

Duration of Olanib treatment depends on the indication: maintenance therapy in ovarian cancer is generally continued for up to 2 years or until disease progression/unacceptable toxicity (a subset of complete responders may stop at 2 years per protocol); adjuvant breast cancer treatment is typically given for 1 year; pancreatic, metastatic breast, and prostate cancer treatment is generally continued until disease progression or unacceptable toxicity. The treating oncologist determines the exact duration based on response and tolerability.

PARP (poly ADP-ribose polymerase) inhibitor; antineoplastic / targeted cancer therapy

Olaparib inhibits PARP1/2/3 enzymes and traps PARP-DNA complexes, preventing repair of single-strand DNA breaks. In cancer cells that already lack functional homologous recombination repair (e.g., BRCA1/2-mutated or HRD-positive cells), this leads to accumulated DNA damage and selective cell death — a mechanism called synthetic lethality. See Pharmacology for full detail.

The safety and efficacy of Olanib have not been established in pediatric patients. Olanib is not currently approved or recommended for use in children or adolescents outside of a clinical trial setting. Any pediatric use would be strictly under specialist oncology supervision.