Tafinlar

— THERAPEUTIC CATEGORIES —
  • CNS cancers
  • Melanoma and other skin cancers
  • Pancreatic, thyroid, and other endocrine cancers
  • Respiratory and thoracic cancers
  • Solid tumors
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

    • Tafinlar Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Dabrafenib 50mg, 75mg; caps.

    Pharmacological Class

    Kinase inhibitor.

    See Also

      How Supplied

      Caps—120; Tabs for oral susp—210

      Manufacturer

      Novartis Pharmaceuticals Corp

      Generic Availability

      NO

      Mechanism of Action

      Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

      Tafinlar Indications

      Indications

      In combination with trametinib for the treatment of pediatric patients with low-grade glioma (LGG) with a BRAF V600E mutation who require systemic therapy.

      Limitations of Use

      Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition. Not for treatment of wild-type BRAF solid tumors.

      Tafinlar Dosage and Administration

      Adult

      ≥18yrs: not established.

      Children

      <1yrs or <8kg: not established. Confirm presence of BRAF V600E mutation prior to initiation. Use caps or tabs for oral susp based on the ability to swallow and body weight. Swallow caps whole (do not use caps if <26kg). For oral susp: disperse tabs in water until fully dissolved; may administer via cup, oral dosing syringe, or feeding tube. Take at least 1hr before or 2hrs after a meal. In combination with trametinib (for caps): 1–<18yrs (26–37kg): 75mg twice daily (approx. 12hrs apart); (38–50kg): 100mg twice daily; (≥51kg): 150mg twice daily. In combination with trametinib (tabs for oral susp): 1–<18yrs (8–9kg): 20mg twice daily; (10–13kg): 30mg twice daily; (14–17kg):40mg twice daily; (18–21kg): 50mg twice daily; (22–25kg): 60mg twice daily; (26–29kg): 70mg twice daily; (30–33mg): 80mg twice daily; (34–37kg): 90mg twice daily; (38–41kg): 100mg twice daily; (42–45kg): 110mg twice daily; (46–50kg): 130mg twice daily; (≥51kg): 150mg twice daily. Continue until disease progression or unacceptable toxicity. Dose modifications: see full labeling.

      Tafinlar Contraindications

      Not Applicable

      Tafinlar Boxed Warnings

      Not Applicable

      Tafinlar Warnings/Precautions

      Warnings/Precautions

      See full labeling for trametinib prior to starting combination therapy. Increased incidence of new cutaneous malignancies; perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for non-cutaneous malignancies; permanently discontinue if RAS mutation-positive malignancy occurs. Permanently discontinue for all Grade 4 or any persistent Grade 3 hemorrhagic events. Risk of cardiomyopathy with trametinib; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for symptomatic cardiomyopathy or asymptomatic LV dysfunction of >20% from baseline that is below institutional LLN. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Monitor for uveitis; if occurs, withhold and treat as clinically indicated; permanently discontinue for persistent Grade ≥2 lasting >6wks. G6PD deficiency: monitor for hemolytic anemia. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise to use effective non-hormonal contraception (females of reproductive potential) or use of condoms (males w. female partners) during and for ≥2wks after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2wks after last dose).

      Tafinlar Pharmacokinetics

      Absorption

      Median time to peak plasma concentration (Tmax): 2 hours.

      Mean absolute bioavailability: 95% (caps); 76% (tabs for oral susp).

      Distribution

      Plasma protein bound: 99.7%.

      Apparent volume of distribution: 70.3 L.

      Metabolism

      CYP2C8, CYP3A4. 

      Elimination

      Fecal (71%), renal (23%). 

      Half-life: 8 hours.

      Apparent clearance: 17 L/h after a single dose and 34 L/h after twice-daily dosing for 2 weeks.

      Tafinlar Interactions

      Interactions

      Avoid concomitant strong CYP3A4 or CYP2C8 inhibitors (eg, ketoconazole, gemfibrozil); if unavoidable, monitor closely. May antagonize effects of CYP3A4, CYP2C8, CYP2C9, CYP2C19, CYP2B6 substrates (eg, midazolam, warfarin, dexamethasone, hormonal contraceptives); consider alternatives or monitor.

      Tafinlar Adverse Reactions

      Adverse Reactions

      Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome; skin toxicity (may be serious). In combination with trametinib: also chills, fatigue, rash, nausea, vomiting, diarrhea, myalgia, dry skin, decreased appetite, edema, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia, musculoskeletal pain.

      Tafinlar Clinical Trials

      See Literature

      Tafinlar Note

      Not Applicable

      Tafinlar Patient Counseling

      See Literature

      Tafinlar Generic Name & Formulations

      Legal Class

      Rx

      General Description

      Dabrafenib 50mg, 75mg; caps.

      Pharmacological Class

      Kinase inhibitor.

      See Also

        How Supplied

        Caps—120

        Manufacturer

        Novartis Pharmaceuticals Corp

        Generic Availability

        NO

        Mechanism of Action

        Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

        Tafinlar Indications

        Indications

        Treatment of unresectable or metastatic melanoma as monotherapy in patients with BRAF V600E mutation, or in combination with trametinib in patients with BRAF V600E or V600K mutations, as detected by an FDA-approved test. In combination with trametinib for the adjuvant treatment of melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and lymph node involvement, following complete resection.

        Limitations of Use

        Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition. Not for treatment of wild-type BRAF solid tumors.

        Tafinlar Dosage and Administration

        Adult

        Confirm presence of BRAF V600E or V600K mutation prior to initiation. Swallow caps whole. Take at least 1hr before or 2hrs after a meal. Monotherapy or in combination with trametinib: 150mg twice daily (approx. 12hrs apart); continue until disease progression or unacceptable toxicity. Adjuvant treatment with trametinib: 150mg twice daily (approx. 12hrs apart); continue until disease recurrence or unacceptable toxicity for up to 1 year. Dose modifications: see full labeling.

        Children

        Not established.

        Tafinlar Contraindications

        Not Applicable

        Tafinlar Boxed Warnings

        Not Applicable

        Tafinlar Warnings/Precautions

        Warnings/Precautions

        See full labeling for trametinib prior to starting combination therapy. Increased incidence of new cutaneous malignancies; perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for non-cutaneous malignancies; permanently discontinue if RAS mutation-positive malignancy occurs. Permanently discontinue for all Grade 4 or any persistent Grade 3 hemorrhagic events. Risk of cardiomyopathy with trametinib; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for symptomatic cardiomyopathy or asymptomatic LV dysfunction of >20% from baseline that is below institutional LLN. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Monitor for uveitis; if occurs, withhold and treat as clinically indicated; permanently discontinue for persistent Grade ≥2 lasting >6wks. G6PD deficiency: monitor for hemolytic anemia. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise to use effective non-hormonal contraception (females of reproductive potential) or use of condoms (males w. female partners) during and for ≥2wks after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2wks after last dose).

        Tafinlar Pharmacokinetics

        Absorption

        Median time to peak plasma concentration (Tmax): 2 hours.

        Mean absolute bioavailability: 95% (caps); 76% (tabs for oral susp).

        Distribution

        Plasma protein bound: 99.7%.

        Apparent volume of distribution: 70.3 L.

        Metabolism

        CYP2C8, CYP3A4. 

        Elimination

        Fecal (71%), renal (23%). 

        Half-life: 8 hours.

        Apparent clearance: 17 L/h after a single dose and 34 L/h after twice-daily dosing for 2 weeks.

        Tafinlar Interactions

        Interactions

        Avoid concomitant strong CYP3A4 or CYP2C8 inhibitors (eg, ketoconazole, gemfibrozil); if unavoidable, monitor closely. May antagonize effects of CYP3A4, CYP2C8, CYP2C9, CYP2C19, CYP2B6 substrates (eg, midazolam, warfarin, dexamethasone, hormonal contraceptives); consider alternatives or monitor.

        Tafinlar Adverse Reactions

        Adverse Reactions

        Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome; skin toxicity (may be serious). In combination with trametinib: also chills, fatigue, rash, nausea, vomiting, diarrhea, myalgia, dry skin, decreased appetite, edema, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia, musculoskeletal pain.

        Tafinlar Clinical Trials

        See Literature

        Tafinlar Note

        Not Applicable

        Tafinlar Patient Counseling

        See Literature

        Tafinlar Generic Name & Formulations

        Legal Class

        Rx

        General Description

        Dabrafenib 50mg, 75mg; caps.

        Pharmacological Class

        Kinase inhibitor.

        See Also

          How Supplied

          Caps—120

          Manufacturer

          Novartis Pharmaceuticals Corp

          Generic Availability

          NO

          Mechanism of Action

          Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

          Tafinlar Indications

          Indications

          In combination with trametinib for the treatment of locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options.

          Limitations of Use

          Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition. Not for treatment of wild-type BRAF solid tumors.

          Tafinlar Dosage and Administration

          Adult

          Confirm presence of BRAF V600E mutation prior to initiation. Swallow caps whole. Take at least 1hr before or 2hrs after a meal. In combination with trametinib: 150mg twice daily (approx. 12hrs apart); continue until disease recurrence or unacceptable toxicity. Dose modifications: see full labeling.

          Children

          Not established.

          Tafinlar Contraindications

          Not Applicable

          Tafinlar Boxed Warnings

          Not Applicable

          Tafinlar Warnings/Precautions

          Warnings/Precautions

          See full labeling for trametinib prior to starting combination therapy. Increased incidence of new cutaneous malignancies; perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for non-cutaneous malignancies; permanently discontinue if RAS mutation-positive malignancy occurs. Permanently discontinue for all Grade 4 or any persistent Grade 3 hemorrhagic events. Risk of cardiomyopathy with trametinib; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for symptomatic cardiomyopathy or asymptomatic LV dysfunction of >20% from baseline that is below institutional LLN. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Monitor for uveitis; if occurs, withhold and treat as clinically indicated; permanently discontinue for persistent Grade ≥2 lasting >6wks. G6PD deficiency: monitor for hemolytic anemia. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise to use effective non-hormonal contraception (females of reproductive potential) or use of condoms (males w. female partners) during and for ≥2wks after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2wks after last dose).

          Tafinlar Pharmacokinetics

          Absorption

          Median time to peak plasma concentration (Tmax): 2 hours.

          Mean absolute bioavailability: 95% (caps); 76% (tabs for oral susp).

          Distribution

          Plasma protein bound: 99.7%.

          Apparent volume of distribution: 70.3 L.

          Metabolism

          CYP2C8, CYP3A4. 

          Elimination

          Fecal (71%), renal (23%). 

          Half-life: 8 hours.

          Apparent clearance: 17 L/h after a single dose and 34 L/h after twice-daily dosing for 2 weeks.

          Tafinlar Interactions

          Interactions

          Avoid concomitant strong CYP3A4 or CYP2C8 inhibitors (eg, ketoconazole, gemfibrozil); if unavoidable, monitor closely. May antagonize effects of CYP3A4, CYP2C8, CYP2C9, CYP2C19, CYP2B6 substrates (eg, midazolam, warfarin, dexamethasone, hormonal contraceptives); consider alternatives or monitor.

          Tafinlar Adverse Reactions

          Adverse Reactions

          Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome; skin toxicity (may be serious). In combination with trametinib: also chills, fatigue, rash, nausea, vomiting, diarrhea, myalgia, dry skin, decreased appetite, edema, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia, musculoskeletal pain.

          Tafinlar Clinical Trials

          See Literature

          Tafinlar Note

          Not Applicable

          Tafinlar Patient Counseling

          See Literature

          Tafinlar Generic Name & Formulations

          Legal Class

          Rx

          General Description

          Dabrafenib 50mg, 75mg; caps.

          Pharmacological Class

          Kinase inhibitor.

          See Also

            How Supplied

            Caps—120

            Manufacturer

            Novartis Pharmaceuticals Corp

            Generic Availability

            NO

            Mechanism of Action

            Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

            Tafinlar Indications

            Indications

            In combination with trametinib for the treatment of metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation, as detected by an FDA-approved test.

            Limitations of Use

            Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition. Not for treatment of wild-type BRAF solid tumors.

            Tafinlar Dosage and Administration

            Adult

            Confirm presence of BRAF V600E mutation prior to initiation. Swallow caps whole. Take at least 1hr before or 2hrs after a meal. In combination with trametinib: 150mg twice daily (approx. 12hrs apart); continue until disease recurrence or unacceptable toxicity. Dose modifications: see full labeling.

            Children

            Not established.

            Tafinlar Contraindications

            Not Applicable

            Tafinlar Boxed Warnings

            Not Applicable

            Tafinlar Warnings/Precautions

            Warnings/Precautions

            See full labeling for trametinib prior to starting combination therapy. Increased incidence of new cutaneous malignancies; perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for non-cutaneous malignancies; permanently discontinue if RAS mutation-positive malignancy occurs. Permanently discontinue for all Grade 4 or any persistent Grade 3 hemorrhagic events. Risk of cardiomyopathy with trametinib; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for symptomatic cardiomyopathy or asymptomatic LV dysfunction of >20% from baseline that is below institutional LLN. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Monitor for uveitis; if occurs, withhold and treat as clinically indicated; permanently discontinue for persistent Grade ≥2 lasting >6wks. G6PD deficiency: monitor for hemolytic anemia. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise to use effective non-hormonal contraception (females of reproductive potential) or use of condoms (males w. female partners) during and for ≥2wks after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2wks after last dose).

            Tafinlar Pharmacokinetics

            Absorption

            Median time to peak plasma concentration (Tmax): 2 hours.

            Mean absolute bioavailability: 95% (caps); 76% (tabs for oral susp).

            Distribution

            Plasma protein bound: 99.7%.

            Apparent volume of distribution: 70.3 L.

            Metabolism

            CYP2C8, CYP3A4. 

            Elimination

            Fecal (71%), renal (23%). 

            Half-life: 8 hours.

            Apparent clearance: 17 L/h after a single dose and 34 L/h after twice-daily dosing for 2 weeks.

            Tafinlar Interactions

            Interactions

            Avoid concomitant strong CYP3A4 or CYP2C8 inhibitors (eg, ketoconazole, gemfibrozil); if unavoidable, monitor closely. May antagonize effects of CYP3A4, CYP2C8, CYP2C9, CYP2C19, CYP2B6 substrates (eg, midazolam, warfarin, dexamethasone, hormonal contraceptives); consider alternatives or monitor.

            Tafinlar Adverse Reactions

            Adverse Reactions

            Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome; skin toxicity (may be serious). In combination with trametinib: also chills, fatigue, rash, nausea, vomiting, diarrhea, myalgia, dry skin, decreased appetite, edema, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia, musculoskeletal pain.

            Tafinlar Clinical Trials

            See Literature

            Tafinlar Note

            Not Applicable

            Tafinlar Patient Counseling

            See Literature

            Tafinlar Generic Name & Formulations

            Legal Class

            Rx

            General Description

            Dabrafenib 50mg, 75mg; caps.

            Pharmacological Class

            Kinase inhibitor.

            See Also

              How Supplied

              Caps—120; Tabs for oral susp—210

              Manufacturer

              Novartis Pharmaceuticals Corp

              Generic Availability

              NO

              Mechanism of Action

              Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases, such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.

              Tafinlar Indications

              Indications

              In combination with trametinib, for the treatment of unresectable or metastatic solid tumors in adult and pediatric patients with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options.

              Limitations of Use

              Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition. Not for treatment of wild-type BRAF solid tumors.

              Tafinlar Dosage and Administration

              Adult

              Confirm presence of BRAF V600E mutation prior to initiation. Swallow whole. Take at least 1hr before or 2hrs after a meal. In combination with trametinib: ≥18yrs: 150mg twice daily (approx. 12hrs apart); continue until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling.

              Children

              <1yrs or <8kg: not established. Confirm presence of BRAF V600E mutation prior to initiation. Use caps or tabs for oral susp based on the ability to swallow and body weight. Swallow caps whole (do not use caps if <26kg). For oral susp: disperse tabs in water until fully dissolved; may administer via cup, oral dosing syringe, or feeding tube. Take at least 1hr before or 2hrs after a meal. In combination with trametinib (for caps): 1–<18yrs (26–37kg): 75mg twice daily (approx. 12hrs apart); (38–50kg): 100mg twice daily; (≥51kg): 150mg twice daily. In combination with trametinib (tabs for oral susp): 1–<18yrs (8–9kg): 20mg twice daily; (10–13kg): 30mg twice daily; (14–17kg):40mg twice daily; (18–21kg): 50mg twice daily; (22–25kg): 60mg twice daily; (26–29kg): 70mg twice daily; (30–33mg): 80mg twice daily; (34–37kg): 90mg twice daily; (38–41kg): 100mg twice daily; (42–45kg): 110mg twice daily; (46–50kg): 130mg twice daily; (≥51kg): 150mg twice daily. Continue until disease progression or unacceptable toxicity. Dose modifications: see full labeling.

              Tafinlar Contraindications

              Not Applicable

              Tafinlar Boxed Warnings

              Not Applicable

              Tafinlar Warnings/Precautions

              Warnings/Precautions

              See full labeling for trametinib prior to starting combination therapy. Increased incidence of new cutaneous malignancies; perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for non-cutaneous malignancies; permanently discontinue if RAS mutation-positive malignancy occurs. Permanently discontinue for all Grade 4 or any persistent Grade 3 hemorrhagic events. Risk of cardiomyopathy with trametinib; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for symptomatic cardiomyopathy or asymptomatic LV dysfunction of >20% from baseline that is below institutional LLN. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Monitor for uveitis; if occurs, withhold and treat as clinically indicated; permanently discontinue for persistent Grade ≥2 lasting >6wks. G6PD deficiency: monitor for hemolytic anemia. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise to use effective non-hormonal contraception (females of reproductive potential) or use of condoms (males w. female partners) during and for ≥2wks after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2wks after last dose).

              Tafinlar Pharmacokinetics

              Absorption

              Median time to peak plasma concentration (Tmax): 2 hours.

              Mean absolute bioavailability: 95% (caps); 76% (tabs for oral susp).

              Distribution

              Plasma protein bound: 99.7%.

              Apparent volume of distribution: 70.3 L.

              Metabolism

              CYP2C8, CYP3A4. 

              Elimination

              Fecal (71%), renal (23%). 

              Half-life: 8 hours.

              Apparent clearance: 17 L/h after a single dose and 34 L/h after twice-daily dosing for 2 weeks.

              Tafinlar Interactions

              Interactions

              Avoid concomitant strong CYP3A4 or CYP2C8 inhibitors (eg, ketoconazole, gemfibrozil); if unavoidable, monitor closely. May antagonize effects of CYP3A4, CYP2C8, CYP2C9, CYP2C19, CYP2B6 substrates (eg, midazolam, warfarin, dexamethasone, hormonal contraceptives); consider alternatives or monitor.

              Tafinlar Adverse Reactions

              Adverse Reactions

              Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome; skin toxicity (may be serious). In combination with trametinib: also chills, fatigue, rash, nausea, vomiting, diarrhea, myalgia, dry skin, decreased appetite, edema, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia, musculoskeletal pain.

              Tafinlar Clinical Trials

              See Literature

              Tafinlar Note

              Not Applicable

              Tafinlar Patient Counseling

              See Literature

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