Lynparza

— THERAPEUTIC CATEGORIES —
  • Breast cancer
  • Gynecologic cancers
  • Pancreatic, thyroid, and other endocrine cancers
  • Prostate and other male cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Lynparza Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Olaparib 100mg, 150mg; tabs.

    Pharmacological Class

    Poly (ADP-ribose) polymerase (PARP) inhibitor.

    See Also

      How Supplied

      Tabs—60, 120

      Manufacturer

      AstraZeneca Pharmaceuticals

      Generic Availability

      NO

      Mechanism of Action

      Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes, resulting in DNA damage and cancer cell death.

      Lynparza Indications

      Indications

      Adjuvant treatment of deleterious or suspected deleterious germline BRCA-mutated, HER2-negative (as detected by an FDA-approved test) high risk early breast cancer in adults who have been treated with neoadjuvant or adjuvant chemotherapy. Treatment of deleterious or suspected deleterious germline BRCA-mutated, HER2-negative (as detected by an FDA-approved test) metastatic breast cancer in adults who have been treated with chemotherapy in the neoadjuvant, adjuvant, or metastatic setting (patients with HR-positive breast cancer should have been treated with prior endocrine therapy or be considered inappropriate for endocrine therapy).

      Lynparza Dosage and Administration

      Adult

      Swallow whole. 300mg twice daily. Early breast cancer: continue for a total of 1yr, or until disease recurrence or unacceptable toxicity. Metastatic breast cancer: continue until disease progression or unacceptable toxicity. Dose adjustments for adverse reactions: reduce to 250mg twice daily; may further reduce to 200mg twice daily. Concomitant strong or moderate CYP3A inhibitors (if unavoidable): reduce olaparib dose to 100mg twice daily (with strong inhibitors) or 150mg twice daily (with moderate inhibitors). Moderate renal impairment (CrCl 31–50mL/min): reduce to 200mg twice daily.

      Children

      Not established.

      Lynparza Contraindications

      Not Applicable

      Lynparza Boxed Warnings

      Not Applicable

      Lynparza Warnings/Precautions

      Warnings/Precautions

      Do not start therapy until recovery from hematological toxicity due to previous chemotherapy (CTCAE Grade ≤1). Monitor CBC for cytopenia at baseline and monthly thereafter during therapy or weekly until recovery (for prolonged hematological toxicities). Discontinue if myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) is confirmed. Interrupt therapy and evaluate if new or worsening respiratory symptoms occur; discontinue and treat if pneumonitis is confirmed. Monitor for venous thrombosis, pulmonary embolism; treat appropriately. Mild renal impairment: monitor closely. Severe hepatic or severe renal impairment or ESRD (CrCl ≤30mL/min): not studied. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 6 months after the last dose. Males (w. female partners) should use effective contraception and do not donate sperm during and for 3 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).

      Lynparza Pharmacokinetics

      Absorption

      • Median time to peak plasma concentration: 1.5 hours.

      Distribution

      • Mean apparent volume of distribution: 158 ± 136 L.

      • ~82% protein bound in vitro.

      Metabolism

      • CYP3A4.

      Elimination

      • Renal (44%), fecal (42%). Half-life: 14.9 ± 8.2 hours.

      Lynparza Interactions

      Interactions

      Increased myelosuppressive toxicity with concomitant other myelosuppressive anticancer agents, including DNA damaging agents. Avoid concomitant strong CYP3A inhibitors (eg, itraconazole) and moderate CYP3A inhibitors (eg, fluconazole); if unavoidable, reduce dose (see Adults). Avoid grapefruit, grapefruit juice, Seville oranges, and Seville orange juice. Avoid concomitant strong CYP3A inducers (eg, rifampicin) and moderate CYP3A inducers (eg, efavirenz); if unavoidable, be aware of potential for decreased efficacy.

      Lynparza Adverse Reactions

      Adverse Reactions

      Nausea, fatigue, asthenia, anemia, vomiting, diarrhea, decreased appetite, headache, neutropenia, dysgeusia, cough, dyspnea, dizziness, dyspepsia, leukopenia, thrombocytopenia, upper abdominal pain. In combination with bevacizumab or abiraterone and prednisone or prednisolone: also lymphopenia, UTI.

      Lynparza Clinical Trials

      See Literature

      Lynparza Note

      Not Applicable

      Lynparza Patient Counseling

      See Literature

      Lynparza Generic Name & Formulations

      Legal Class

      Rx

      General Description

      Olaparib 100mg, 150mg; tabs.

      Pharmacological Class

      Poly (ADP-ribose) polymerase (PARP) inhibitor.

      See Also

        How Supplied

        Tabs—60, 120

        Manufacturer

        AstraZeneca Pharmaceuticals

        Generic Availability

        NO

        Mechanism of Action

        Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes, resulting in DNA damage and cancer cell death.

        Lynparza Indications

        Indications

        First-line maintenance treatment of deleterious or suspected deleterious germline or somatic BRCA-mutated (as detected by an FDA-approved test) advanced epithelial ovarian, fallopian tube or primary peritoneal cancer, in adults who are in complete or partial response to first-line platinum-based chemotherapy. In combination with bevacizumab for the first-line maintenance treatment of advanced epithelial ovarian, fallopian tube or primary peritoneal cancer, in adults who are in complete or partial response to first-line platinum-based chemotherapy and whose cancer is associated with homologous recombination deficiency (HRD)-positive status defined by either a deleterious or suspected deleterious BRCA mutation, and/or genomic instability (as detected by an FDA-approved test). Maintenance treatment of recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, in adults who are in complete or partial response to platinum-based chemotherapy. Treatment of deleterious or suspected deleterious germline BRCA-mutated (as detected by an FDA-approved test) advanced ovarian cancer in adults who have been treated with ≥3 prior lines of chemotherapy.

        Lynparza Dosage and Administration

        Adult

        Swallow whole. 300mg twice daily. First-line maintenance of BRCA-mutated or HRD-positive advanced ovarian: continue until disease progression, unacceptable toxicity, or completion of 2yrs of treatment. Discontinue if complete response at 2yrs; may treat beyond 2yrs in those with evidence of disease if provider can derive further benefit from continuous treatment. Others: continue until disease progression or unacceptable toxicity. In combination with bevacizumab: give bevacizumab (15mg/kg every 3 weeks) for total of 15 months (refer to respective product labeling for details). Dose adjustments for adverse reactions: reduce to 250mg twice daily; may further reduce to 200mg twice daily. Concomitant strong or moderate CYP3A inhibitors (if unavoidable): reduce olaparib dose to 100mg twice daily (with strong inhibitors) or 150mg twice daily (with moderate inhibitors). Moderate renal impairment (CrCl 31–50mL/min): reduce to 200mg twice daily.

        Children

        Not established.

        Lynparza Contraindications

        Not Applicable

        Lynparza Boxed Warnings

        Not Applicable

        Lynparza Warnings/Precautions

        Warnings/Precautions

        Do not start therapy until recovery from hematological toxicity due to previous chemotherapy (CTCAE Grade ≤1). Monitor CBC for cytopenia at baseline and monthly thereafter during therapy or weekly until recovery (for prolonged hematological toxicities). Discontinue if myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) is confirmed. Interrupt therapy and evaluate if new or worsening respiratory symptoms occur; discontinue and treat if pneumonitis is confirmed. Monitor for venous thrombosis, pulmonary embolism; treat appropriately. Mild renal impairment: monitor closely. Severe hepatic or severe renal impairment or ESRD (CrCl ≤30mL/min): not studied. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 6 months after the last dose. Males (w. female partners) should use effective contraception and do not donate sperm during and for 3 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).

        Lynparza Pharmacokinetics

        Absorption

        • Median time to peak plasma concentration: 1.5 hours.

        Distribution

        • Mean apparent volume of distribution: 158 ± 136 L.

        • ~82% protein bound in vitro.

        Metabolism

        • CYP3A4.

        Elimination

        • Renal (44%), fecal (42%). Half-life: 14.9 ± 8.2 hours.

        Lynparza Interactions

        Interactions

        Increased myelosuppressive toxicity with concomitant other myelosuppressive anticancer agents, including DNA damaging agents. Avoid concomitant strong CYP3A inhibitors (eg, itraconazole) and moderate CYP3A inhibitors (eg, fluconazole); if unavoidable, reduce dose (see Adults). Avoid grapefruit, grapefruit juice, Seville oranges, and Seville orange juice. Avoid concomitant strong CYP3A inducers (eg, rifampicin) and moderate CYP3A inducers (eg, efavirenz); if unavoidable, be aware of potential for decreased efficacy.

        Lynparza Adverse Reactions

        Adverse Reactions

        Nausea, fatigue, asthenia, anemia, vomiting, diarrhea, decreased appetite, headache, neutropenia, dysgeusia, cough, dyspnea, dizziness, dyspepsia, leukopenia, thrombocytopenia, upper abdominal pain. In combination with bevacizumab or abiraterone and prednisone or prednisolone: also lymphopenia, UTI.

        Lynparza Clinical Trials

        See Literature

        Lynparza Note

        Not Applicable

        Lynparza Patient Counseling

        See Literature

        Lynparza Generic Name & Formulations

        Legal Class

        Rx

        General Description

        Olaparib 100mg, 150mg; tabs.

        Pharmacological Class

        Poly (ADP-ribose) polymerase (PARP) inhibitor.

        See Also

          How Supplied

          Tabs—60, 120

          Manufacturer

          AstraZeneca Pharmaceuticals

          Generic Availability

          NO

          Mechanism of Action

          Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes, resulting in DNA damage and cancer cell death.

          Lynparza Indications

          Indications

          First-line maintenance treatment of deleterious or suspected deleterious germline BRCA-mutated (as detected by an FDA-approved test) metastatic pancreatic adenocarcinoma in adults whose disease has not progressed on at least 16 weeks of a first-line platinum-based chemotherapy regimen.

          Lynparza Dosage and Administration

          Adult

          Swallow whole. 300mg twice daily. Continue until disease progression or unacceptable toxicity. Dose adjustments for adverse reactions: reduce to 250mg twice daily; may further reduce to 200mg twice daily. Concomitant strong or moderate CYP3A inhibitors (if unavoidable): reduce olaparib dose to 100mg twice daily (with strong inhibitors) or 150mg twice daily (with moderate inhibitors). Moderate renal impairment (CrCl 31–50mL/min): reduce to 200mg twice daily.

          Children

          Not established.

          Lynparza Contraindications

          Not Applicable

          Lynparza Boxed Warnings

          Not Applicable

          Lynparza Warnings/Precautions

          Warnings/Precautions

          Do not start therapy until recovery from hematological toxicity due to previous chemotherapy (CTCAE Grade ≤1). Monitor CBC for cytopenia at baseline and monthly thereafter during therapy or weekly until recovery (for prolonged hematological toxicities). Discontinue if myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) is confirmed. Interrupt therapy and evaluate if new or worsening respiratory symptoms occur; discontinue and treat if pneumonitis is confirmed. Monitor for venous thrombosis, pulmonary embolism; treat appropriately. Mild renal impairment: monitor closely. Severe hepatic or severe renal impairment or ESRD (CrCl ≤30mL/min): not studied. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 6 months after the last dose. Males (w. female partners) should use effective contraception and do not donate sperm during and for 3 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).

          Lynparza Pharmacokinetics

          Absorption

          • Median time to peak plasma concentration: 1.5 hours.

          Distribution

          • Mean apparent volume of distribution: 158 ± 136 L.

          • ~82% protein bound in vitro.

          Metabolism

          • CYP3A4.

          Elimination

          • Renal (44%), fecal (42%). Half-life: 14.9 ± 8.2 hours.

          Lynparza Interactions

          Interactions

          Increased myelosuppressive toxicity with concomitant other myelosuppressive anticancer agents, including DNA damaging agents. Avoid concomitant strong CYP3A inhibitors (eg, itraconazole) and moderate CYP3A inhibitors (eg, fluconazole); if unavoidable, reduce dose (see Adults). Avoid grapefruit, grapefruit juice, Seville oranges, and Seville orange juice. Avoid concomitant strong CYP3A inducers (eg, rifampicin) and moderate CYP3A inducers (eg, efavirenz); if unavoidable, be aware of potential for decreased efficacy.

          Lynparza Adverse Reactions

          Adverse Reactions

          Nausea, fatigue, asthenia, anemia, vomiting, diarrhea, decreased appetite, headache, neutropenia, dysgeusia, cough, dyspnea, dizziness, dyspepsia, leukopenia, thrombocytopenia, upper abdominal pain. In combination with bevacizumab or abiraterone and prednisone or prednisolone: also lymphopenia, UTI.

          Lynparza Clinical Trials

          See Literature

          Lynparza Note

          Not Applicable

          Lynparza Patient Counseling

          See Literature

          Lynparza Generic Name & Formulations

          Legal Class

          Rx

          General Description

          Olaparib 100mg, 150mg; tabs.

          Pharmacological Class

          Poly (ADP-ribose) polymerase (PARP) inhibitor.

          See Also

            How Supplied

            Tabs—60, 120

            Manufacturer

            AstraZeneca Pharmaceuticals

            Generic Availability

            NO

            Mechanism of Action

            Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes, resulting in DNA damage and cancer cell death.

            Lynparza Indications

            Indications

            Treatment of deleterious or suspected deleterious germline or somatic homologous recombination repair (HRR) gene-mutated (as detected by an FDA-approved test) metastatic castration-resistant prostate cancer in adults who have progressed following prior treatment with enzalutamide or abiraterone. In combination with abiraterone and prednisone or prednisolone for the treatment of deleterious or suspected deleterious BRCA-mutated (BRCAm) (as detected by an FDA-approved test) mCRPC in adults.

            Lynparza Dosage and Administration

            Adult

            Swallow whole. 300mg twice daily. Continue until disease progression or unacceptable toxicity. Should also give a GnRH analog concurrently or should have had bilateral orchiectomy. For BRCAm mCRPC: give abiraterone 1000mg once daily with prednisone or prednisolone 5mg twice daily. Dose adjustments for adverse reactions: reduce to 250mg twice daily; may further reduce to 200mg twice daily. Concomitant strong or moderate CYP3A inhibitors (if unavoidable): reduce olaparib dose to 100mg twice daily (with strong inhibitors) or 150mg twice daily (with moderate inhibitors). Moderate renal impairment (CrCl 31–50mL/min): reduce to 200mg twice daily.

            Children

            Not established.

            Lynparza Contraindications

            Not Applicable

            Lynparza Boxed Warnings

            Not Applicable

            Lynparza Warnings/Precautions

            Warnings/Precautions

            Do not start therapy until recovery from hematological toxicity due to previous chemotherapy (CTCAE Grade ≤1). Monitor CBC for cytopenia at baseline and monthly thereafter during therapy or weekly until recovery (for prolonged hematological toxicities). Discontinue if myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) is confirmed. Interrupt therapy and evaluate if new or worsening respiratory symptoms occur; discontinue and treat if pneumonitis is confirmed. Monitor for venous thrombosis, pulmonary embolism; treat appropriately. Mild renal impairment: monitor closely. Severe hepatic or severe renal impairment or ESRD (CrCl ≤30mL/min): not studied. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 6 months after the last dose. Males (w. female partners) should use effective contraception and do not donate sperm during and for 3 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).

            Lynparza Pharmacokinetics

            Absorption

            • Median time to peak plasma concentration: 1.5 hours.

            Distribution

            • Mean apparent volume of distribution: 158 ± 136 L.

            • ~82% protein bound in vitro.

            Metabolism

            • CYP3A4.

            Elimination

            • Renal (44%), fecal (42%). Half-life: 14.9 ± 8.2 hours.

            Lynparza Interactions

            Interactions

            Increased myelosuppressive toxicity with concomitant other myelosuppressive anticancer agents, including DNA damaging agents. Avoid concomitant strong CYP3A inhibitors (eg, itraconazole) and moderate CYP3A inhibitors (eg, fluconazole); if unavoidable, reduce dose (see Adults). Avoid grapefruit, grapefruit juice, Seville oranges, and Seville orange juice. Avoid concomitant strong CYP3A inducers (eg, rifampicin) and moderate CYP3A inducers (eg, efavirenz); if unavoidable, be aware of potential for decreased efficacy.

            Lynparza Adverse Reactions

            Adverse Reactions

            Nausea, fatigue, asthenia, anemia, vomiting, diarrhea, decreased appetite, headache, neutropenia, dysgeusia, cough, dyspnea, dizziness, dyspepsia, leukopenia, thrombocytopenia, upper abdominal pain. In combination with bevacizumab or abiraterone and prednisone or prednisolone: also lymphopenia, UTI.

            Lynparza Clinical Trials

            See Literature

            Lynparza Note

            Not Applicable

            Lynparza Patient Counseling

            See Literature

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