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Dabrafenib Mesylate

Class: Antineoplastic Agents
Chemical Name: N - [3 - [5 - (2 - amino - 4 - pyrimidinyl) - 2 - (1,1 - dimethylethyl) - 4 - thiazolyl] - 2 - fluorophenyl] - 2,6 - difluoro - benzenesulfonamide methanesulfonate (1:1)
Molecular Formula: C23H20F3N5O2S2•CH4O3S
CAS Number: 1195768-06-9
Brands: Tafinlar

Introduction

Antineoplastic agent; an inhibitor of b-Raf serine-threonine kinase with V600E mutation (BRAF V600E).1 2 7

Uses for Dabrafenib Mesylate

Melanoma

Alone or in combination with trametinib for treatment of unresectable or metastatic melanoma in selected patients with BRAF V600E or V600K mutation1 2 5 7 (designated an orphan drug by FDA as monotherapy or when used in combination for this use).3 4

FDA-approved in vitro diagnostic test (e.g., THxID BRAF kit) required to confirm presence of BRAF V600E mutation prior to initiation of monotherapy; also required to confirm presence of BRAF V600E or V600K prior to initiation of combination therapy with trametinib.1 6

Not recommended for use in patients with wild-type BRAF melanoma; safety and efficacy not established.1 (See Tumor Promotion in Wild-Type BRAF Melanoma under Cautions.)

Dabrafenib Mesylate Dosage and Administration

General

  • Confirm presence of BRAF V600E mutation prior to initiation of monotherapy.1

  • Confirm presence of BRAF V600E or V600K mutation prior to initiation of combination therapy with trametinib.1

Administration

Oral Administration

Monotherapy: Administer orally twice daily, approximately 12 hours apart.1

Combination therapy: Administer orally twice daily; take the once-daily dose of trametinib at the same time each day either in the morning or evening with dabrafenib.1

Administer alone or in combination with trametinib at least 1 hour before or 2 hours after a meal.1

Do not open, crush, or break capsules.1

Dosage

Available as dabrafenib mesylate; dosage expressed in terms of dabrafenib.1

Adults

Melanoma
Oral

Monotherapy: 150 mg twice daily.1

Combination therapy: 150 mg twice daily when used in combination with trametinib (2 mg once daily).1

Continue therapy until disease progression or unacceptable toxicity occurs.1

Dosage Modification for Toxicity
Oral

Dosage may be reduced or therapy temporarily interrupted in patients who develop adverse effects.1 Up to 3 dosage reductions for toxicity may be made.1

If necessary, initially reduce dosage to 100 mg twice daily.1 If further dosage reduction necessary, reduce dosage to 75 mg twice daily or subsequently to 50 mg twice daily.1 For patients unable to tolerate 50 mg twice daily, permanently discontinue the drug.1

When used in combination with trametinib, dosage modification of trametinib for toxicity also may be required.1

Dosage Modification for New Primary Cutaneous Malignancies
Oral

If new primary cutaneous malignancies occur with monotherapy or dabrafenib/trametinib combination therapy, dosage modification of dabrafenib not necessary.1

Dosage Modification for New Primary Noncutaneous Malignancies
Oral

If new RAS mutation-positive, noncutaneous malignancies occur with monotherapy or dabrafenib/trametinib combination therapy, permanently discontinue dabrafenib.1

Dosage Modification for Febrile Drug Reactions
Oral

Fever of 38.5–40°C with monotherapy or dabrafenib/trametinib combination therapy: Interrupt dabrafenib therapy until fever resolves; resume therapy at same or reduced dosage.1

Fever >40°C or fever with complications (e.g., rigors, hypotension, dehydration, renal failure) with monotherapy or dabrafenib/trametinib combination therapy: Permanently discontinue dabrafenib.1 Alternatively, withhold drug until fever resolves; resume therapy with reduced dosage.1

Dosage Modification for Dermatologic Effects
Oral

Intolerable grade 2 skin toxicity: Withhold dabrafenib for up to 3 weeks.1 If improvement observed within 3 weeks, resume therapy at reduced dosage.1 If no improvement observed within 3 weeks, permanently discontinue the drug.1

Grade 3 or 4 skin toxicity: Withhold dabrafenib for up to 3 weeks.1 If improvement observed within 3 weeks, resume therapy at reduced dosage.1 If no improvement observed within 3 weeks, permanently discontinue the drug.1

Dosage Modification for Cardiac Effects
Oral

Asymptomatic decrease in left ventricular ejection fraction (LVEF) from baseline of ≥10% and to a level below institution-specific lower limits of normal: Dosage modification of dabrafenib not necessary.1

Symptomatic CHF or decrease in LVEF from baseline >20% and to a level below institution-specific lower limits of normal: Withhold dabrafenib therapy.1 If improvement observed, resume therapy at the same dosage.1

Dosage Modification for Hemorrhage
Oral

Grade 3 hemorrhagic events: Withhold dabrafenib therapy.1 If improvement observed, resume therapy at reduced dosage.1 If no improvement observed, permanently discontinue the drug.1

Grade 4 hemorrhagic events: Permanently discontinue dabrafenib.1

Dosage Modification for Venous Thromboembolism
Oral

Uncomplicated DVT or PE: Dosage modification of dabrafenib not recommended.1

Life-threatening PE: Permanently discontinue dabrafenib.1

Dosage Modification for Ocular Effects
Oral

Grade 2 or 3 retinal pigment epithelial detachment or retinal vein occlusion with dabrafenib/trametinib combination therapy: Dosage modification of dabrafenib not recommended.1

Uveitis and iritis with monotherapy or dabrafenib/trametinib combination therapy: Interrupt dabrafenib therapy for up to 6 weeks.1 If improvement to grade 0 or 1 observed within 6 weeks, resume therapy at the same dosage.1 If improvement not observed within 6 weeks, permanently discontinue the drug.1

Dosage Modification for Pulmonary Effects
Oral

Interstitial lung disease or pneumonitis: Dosage modification of dabrafenib not needed.1

Dosage Modification for Other Toxicity
Oral

Intolerable grade 2 or any grade 3 adverse reaction: Interrupt therapy until adverse reaction resolves to grade 1 or less; resume therapy at reduced dosage.1 If no improvement observed, permanently discontinue dabrafenib.1

First occurrence any grade 4 adverse reaction: Permanently discontinue dabrafenib.1 Alternatively, withhold drug until adverse reaction resolves to grade 1 or less; resume at reduced dosage.1

Intolerable grade 2 or any grade 3 or 4 adverse reaction in patients receiving 50 mg twice daily: Permanently discontinue dabrafenib.1

Recurrent grade 4 adverse reaction: Permanently discontinue dabrafenib.1

Special Populations

Hepatic Impairment

Mild hepatic impairment: Dosage adjustment not necessary.1

Moderate to severe hepatic impairment: Appropriate dosage not established.1

Renal Impairment

Mild or moderate renal impairment: Dosage adjustment not necessary.1

Severe renal impairment: Appropriate dosage not established.1

Cautions for Dabrafenib Mesylate

Contraindications

  • Manufacturer states none known.1

Warnings/Precautions

Combination Therapy

When combination therapy with dabrafenib includes use of trametinib, cautions, precautions, and contraindications of trametinib also must be considered.1

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenic and embryotoxic in animals.1

Advise female patients of childbearing potential to use highly effective, nonhormonal contraception during treatment and for at least 2 weeks following discontinuance of monotherapy or for 4 months following dabrafenib/trametinib combination therapy.1 11 (See Specific Drugs under Interactions.)

If used during pregnancy, inform patient of potential fetal hazard.1

New Primary Cutaneous Malignancies

Cutaneous malignancies may occur with dabrafenib alone or when used in combination with trametinib.1

Increased incidence of cutaneous squamous cell carcinoma, keratoacanthoma, and melanoma reported with dabrafenib alone.1 In clinical trials, median time to first cutaneous squamous cell carcinoma or keratoacanthoma 9 weeks.1

Increased incidence of basal cell carcinoma reported with dabrafenib/trametinib combination therapy.1

Perform dermatologic evaluations prior to initiation of dabrafenib monotherapy or dabrafenib/trametinib combination therapy, every 2 months during therapy, and for up to 6 months following discontinuance of dabrafenib.1

New Primary Noncutaneous Malignancies

Noncutaneous malignancies may occur with dabrafenib alone or when used in combination with trametinib.1

KRAS mutation-positive pancreatic adenocarcinoma, recurrent NRAS mutation-positive colorectal carcinoma, head and neck carcinoma, and glioblastoma have occurred in patients receiving dabrafenib/trametinib combination therapy.1

Monitor patients receiving dabrafenib/trametinib combination therapy closely for signs or symptoms of new noncutaneous malignancies prior to initiation, during treatment, and following discontinuance of therapy.1 If a RAS mutation-positive noncutaneous malignancy occurs, permanently discontinue dabrafenib.1

Tumor Promotion in Wild-Type BRAF Melanoma

In vitro evidence of increased cell proliferation in BRAF wild-type cells exposed to BRAF inhibitors.1

Confirm BRAF V600E mutation prior to initiating dabrafenib alone; confirm V600E or V600K mutation prior to initiating combination therapy with trametinib; not recommended in patients with wild-type BRAF melanoma.1

Hemorrhage

Hemorrhage (sometimes fatal), including intracranial or GI hemorrhage, has occurred during dabrafenib/trametinib combination therapy.1 Increased incidence and severity of hemorrhagic events observed during combination therapy compared with dabrafenib alone.1

Dosage modification or treatment discontinuance may be necessary if grade 3 or 4 hemorrhagic events occur.1 (See Dosage Modification for Toxicity under Dosage and Administration.)

Venous Thromboembolism

Venous thromboembolism (VTE) has occurred during dabrafenib/trametinib combination therapy.1 Increased incidence of DVT or PE (sometimes fatal) observed during such combination therapy compared with dabrafenib alone.1

Advise patients to immediately seek medical care if they develop symptoms of DVT or PE (e.g., shortness of breath, chest pain, arm or leg swelling).1 Dosage modification or treatment discontinuance may be necessary if DVT or PE occurs.1 (See Dosage Modification for Toxicity under Dosage and Administration.)

Febrile Drug Reactions

Serious febrile drug reactions (including fever accompanied by hypotension, rigors/chills, dehydration, or renal failure) reported with dabrafenib alone or in combination with trametinib.1 Increased incidence and severity of pyrexia observed during dabrafenib/trametinib combination therapy compared with dabrafenib alone.1

For fever ≥38.5°C or other serious febrile reactions, interrupt treatment and evaluate patient for manifestations of infection.1 Dosage modification or treatment discontinuance may be necessary.1 (See Dosage Modification for Toxicity under Dosage and Administration.)

May use prophylactic antipyretics when resuming dabrafenib following adverse febrile reactions.1

Hyperglycemia

Hyperglycemia requiring increased dosage or initiation of insulin or oral hypoglycemic agents reported in patients receiving dabrafenib monotherapy.1 Hyperglycemia also occurred in patients receiving dabrafenib/trametinib combination therapy.1

Monitor serum glucose concentrations in patients with preexisting diabetes or hyperglycemia, as clinically appropriate.1 Also evaluate patients for manifestations of severe hyperglycemia (e.g., excessive thirst, increased volume/frequency of urination).1

Dermatologic Effects

Serious dermatologic toxicity reported in patients receiving dabrafenib/trametinib combination therapy.1

Monitor patients receiving dabrafenib monotherapy or combination therapy for dermatologic toxicity and secondary infections.1 (See Dosage Modification for Toxicity under Dosage and Administration.)

Ocular Effects

Retinal pigment epithelial detachments reported during dabrafenib/trametinib combination therapy.1

Perform ophthalmologic evaluation if patient reports vision loss or visual disturbances and compare with baseline measurements, if available.1

If retinal pigment epithelial detachment or retinal vein occlusion is diagnosed, no dosage modification of dabrafenib necessary.1

Uveitis, including iritis, reported with dabrafenib alone or in combination with trametinib. 1 If uveitis occurs, symptomatic treatment with ophthalmic corticosteroid or mydriatic preparations may be required.1

Monitor patients for signs and symptoms of uveitis (e.g., vision change, photophobia, eye pain).1

Hemolytic Anemia

Potential risk of hemolytic anemia in patients with glucose-6-phosphate dehydrogenase (G-6-PD) deficiency.1

Closely monitor patients with G-6-PD deficiency for hemolytic anemia.1

Specific Populations

Pregnancy

Category D.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Fertility

Potential for impaired spermatogenesis with dabrafenib.1 Advise male patients to seek counseling on fertility/family planning options prior to therapy initiation.1

Potential for impaired fertility with trametinib.1 Advise female patients of childbearing potential that dabrafenib/trametinib combination therapy may result in impaired fertility.1

Lactation

Not known whether distributed into milk; discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

No substantial differences in safety and efficacy of dabrafenib monotherapy in those ≥65 years of age relative to younger adults.1

Insufficient experience with dabrafenib/trametinib combination therapy in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1

Hepatic Impairment

Not studied in patients with hepatic impairment; possible increased exposure in moderate to severe hepatic impairment.1

Renal Impairment

Not studied in patients with renal impairment.1

Common Adverse Effects

Monotherapy: Hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, palmar-plantar erythrodysesthesia syndrome (hand-foot syndrome), hyperglycemia, hypophosphatemia.1

Combination therapy with trametinib: Pyrexia, chills, fatigue, rash, nausea, vomiting, diarrhea, abdominal pain, peripheral edema, cough, headache, arthralgia, night sweats, decreased appetite, constipation, myalgia.1

Interactions for Dabrafenib Mesylate

Metabolized by CYP 3A4 and 2C8; inducer of CYP 3A4 and 2C9; in vitro data show dabrafenib as inducer of CYP 3A4 and 2B6; possible inducer of other CYP 2C isoenzymes.1

Substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP); moderate inhibitor of BCRP in vitro.1

Inhibits organic anion-transporting polypeptides (OATP) 1B1 and 1B3; also inhibits organic anion transporters (OAT) 1 and 3 in vitro.1

May induce uridine diphosphate glucuronosyltransferase (UGT).1

Drugs Affecting Hepatic Microsomal Enzymes

Potent inhibitors of CYP 3A4 or 2C8: Potential pharmacokinetic interaction (increased dabrafenib concentrations).1 Alternative therapy to potent inhibitors of CYP 3A4 or 2C8 recommended.1 If concomitant use unavoidable, monitor patients closely for dabrafenib-associated adverse reactions.1

Potent inducers of CYP 3A4 or 2C8: Potential pharmacokinetic interaction (decreased dabrafenib concentrations).1 Alternative therapy to potent inducers of CYP 3A4 or 2C8 recommended.1 If concomitant use unavoidable, monitor patients closely for reduced dabrafenib efficacy.1

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP 3A4, 2B6, 2C8, 2C9: Potential pharmacokinetic interaction (decreased concentrations of substrate drug).1 Alternative therapy to substrate drug recommended.1 If concomitant use is unavoidable, monitor for reduced efficacy of substrate drug.1

Drugs Metabolized by Uridine Diphosphate-glucuronosyltransferase

Substrates of UGT: Potential pharmacokinetic interaction (decreased concentrations of substrate drug).1 Consider alternative therapy to substrate drug.1 If concomitant use is unavoidable, monitor for reduced efficacy of substrate drug.1

Specific Drugs

Drug

Interaction

Comments

Antacids

Possible decreased dabrafenib concentrations; effect on dabrafenib efficacy unknown1

Anticonvulsants (carbamazepine, phenobarbital, phenytoin)

Possible decreased dabrafenib concentrations1

Monitor closely for reduced dabrafenib efficacy1

Clarithromycin

Possible increased dabrafenib concentrations1

Monitor closely for dabrafenib-associated adverse effects1

Dexamethasone

Possible decreased dexamethasone concentrations and reduced efficacy1

Alternative therapy to dexamethasone recommended; if concomitant use unavoidable, monitor closely for reduced dexamethasone efficacy1

Gemfibrozil

Possible increased dabrafenib concentrations1

Use alternative to gemfibrozil; if concomitant use unavoidable, monitor closely for dabrafenib-associated adverse effects1

Histamine H2-receptor antagonists

Possible decreased dabrafenib concentrations; effect on dabrafenib efficacy unknown1

Hormonal contraceptives

Possible decreased estrogen/progestin concentrations and reduced efficacy1

Advise females of childbearing potential to use alternative nonhormonal contraception during and for 2 weeks after discontinuing dabrafenib monotherapy or for 4 months after last dose of dabrafenib/trametinib combination therapy1

If concomitant use unavoidable, monitor closely for reduced hormonal contraceptive efficacy1

Ketoconazole

Possible increased dabrafenib concentrations1

Use alternative to ketoconazole; if concomitant use unavoidable, monitor closely for dabrafenib-associated adverse effects1

Midazolam

Decreased midazolam concentrations1

Use alternative to midazolam; if concomitant use unavoidable, monitor closely for reduced midazolam efficacy1

Nefazodone

Possible increased dabrafenib concentrations1

Use alternative to nefazodone; if concomitant use unavoidable, monitor closely for dabrafenib-associated adverse effects1

Proton-pump inhibitors

Possible decreased dabrafenib concentrations; effect on dabrafenib efficacy unknown1

Rifampin

Possible decreased dabrafenib concentrations1

Use alternative to rifampin; if concomitant use unavoidable, monitor closely for reduced dabrafenib efficacy1

St. John’s wort (Hypericum perforatum)

Possible decreased dabrafenib concentrations1

Use alternative to St. John's wort; if concomitant use unavoidable, monitor closely for reduced dabrafenib efficacy1

Trametinib

Increased AUC of dabrafenib and desmethyl-dabrafenib; pharmacokinetic interactions not considered clinically relevant 1

Warfarin

Decreased warfarin concentrations1

Monitor INR frequently in patients receiving warfarin during initiation or discontinuance of dabrafenib1

Dabrafenib Mesylate Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability 95%.1

Following oral administration, peak plasma concentrations attained after approximately 2 hours.1 8

Desmethyl metabolite may be reabsorbed from the gut.1

Food

High-fat meal decreased peak plasma concentrations and AUC by 51 and 31%, respectively; also delayed median time to peak plasma concentrations by 3.6 hours.1 8

Distribution

Extent

Not known if distributed into milk.1

Plasma Protein Binding

99.7%.1

Elimination

Metabolism

Principally mediated by CYP3A4 and 2C8 to form hydroxy-dabrafenib.1 Hydroxy metabolite further metabolized via CYP3A4 to form carboxy-dabrafenib.1 Carboxy metabolite further metabolized to desmethyl-dabrafenib via decarboxylation.1 Hydroxy and desmethyl metabolites likely contribute to clinical activity.1

Elimination Route

Fecal (71%) and urinary (23%) excretion.1

Half-life

8 hours.1

Special Populations

Formal pharmacokinetic study not performed in patients with hepatic impairment; population analysis indicates no clinically important pharmacokinetic changes in patients with mild hepatic impairment.1 No data available in patients with moderate to severe hepatic impairment; systemic exposure may be increased in these patients.1

Formal pharmacokinetic study not performed in patients with renal impairment; population analysis indicates no clinically important pharmacokinetic changes in patients with mild or moderate renal impairment.1 No data available in patients with severe renal impairment.1

Clinically important pharmacokinetic differences based on age, gender, or weight not observed.1

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).1

Actions

  • Potent inhibitor of b-Raf serine-threonine kinase with V600E mutation (BRAF V600E);1 7 8 also shows some in vitro activity against kinases with BRAF mutations V600K and V600D.1 10

  • Approximately 50% of cutaneous melanomas carry a BRAF mutation; substitution of glutamic acid for valine at codon 600 (BRAF V600E) is the most common BRAF mutation.2 9

  • Mutation of BRAF V600E activates the mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinase (ERK) signal transduction pathway, which enhances cell proliferation and tumor progression (e.g., metastasis).1 9

  • Paradoxical activation of MAPK and increased cell proliferation observed in BRAF wild-type cells exposed to b-Raf serine-threonine kinase inhibitors.1

  • Dabrafenib/trametinib combination therapy targets 2 different tyrosine kinases in the MAPK/ERK pathway.1 Combination therapy resulted in greater growth inhibition of melanoma cell lines and prolonged inhibition of tumor growth in melanoma xenografts testing positive for BRAF V600 mutations in vitro.1

Advice to Patients

  • Importance of advising patient to read the manufacturer's medication guide before beginning treatment and each time the prescription is refilled.1

  • Importance of taking dabrafenib exactly as prescribed and of not altering the dosage or discontinuing therapy unless advised to do so by clinician.1

  • Importance of taking dabrafenib at least 1 hour before or 2 hours after a meal and of not opening, crushing, or breaking the capsules.1

  • Importance of taking a missed dose as soon as remembered, but only if it can be taken at least 6 hours prior to next scheduled dose.1

  • Importance of confirming that patient has melanoma testing positive for the BRAF V600E mutation using an FDA-approved diagnostic test prior to initiation of monotherapy.1 6

  • Importance of confirming that patient has melanoma testing positive for the BRAF V600E or V600K mutation using an FDA-approved diagnostic test prior to initiation of dabrafenib/trametinib combination therapy.1 6

  • Risk of new primary cutaneous and noncutaneous malignancies.1 Importance of contacting clinician promptly if dermatologic changes (i.e., new lesions, changes to existing lesions) or signs and/or symptoms of other malignancies occur.1

  • Risk of intracranial and GI hemorrhage with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician promptly if signs and/or symptoms of unusual bleeding or hemorrhage occur.1

  • Risk of DVT and PE with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician promptly if sudden onset of breathing difficulty, leg pain, or swelling occurs.1

  • Risk of cardiomyopathy with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician promptly if signs and/or symptoms of heart failure occur.1

  • Risk of serious febrile drug reactions.1 Increased incidence and severity of pyrexia with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician if fever occurs.1

  • Risk of skin toxicities (possibly requiring hospitalization) with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician if progressive or intolerable rash occurs.1

  • Risk of impaired glucose control in patients with diabetes resulting in need for more intensive antidiabetic treatment.1 Importance of contacting clinician if symptoms of severe hyperglycemia occur.1

  • Risk of hemolytic anemia in patients with G-6-PD deficiency.1 Importance of patients with known G-6-PD deficiency contacting clinician if manifestations of anemia or hemolysis occur.1

  • Risk of fetal harm if taken during pregnancy.1 Importance of female patients using highly effective, nonhormonal contraception during treatment, for at least 2 weeks after discontinuance of monotherapy, and for 4 months after discontinuance of dabrafenib/trametinib combination therapy.1 11 Importance of contacting clinician if pregnancy is suspected or confirmed during treatment. 1

  • Risk of serious adverse reactions in nursing infants of women receiving dabrafenib.1 Importance of discontinuing breast-feeding during therapy.1

  • Risk of impaired spermatogenesis.1 Importance of counseling male patients on fertility/family planning options prior to therapy initiation.1

  • Risk of adverse ocular effects.1 Risk of blindness with dabrafenib/trametinib combination therapy.1 Importance of contacting clinician promptly if any vision changes or other ocular effects (e.g., ocular pain, swelling, redness, blurred vision) occur.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses (e.g., diabetes).1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Dabrafenib Mesylate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

50 mg (of dabrafenib)

Tafinlar

GlaxoSmithKline

75 mg (of dabrafenib)

Tafinlar

GlaxoSmithKline

AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions August 12, 2015. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. GlaxoSmithKline. Tafinlar(dabrafenib) capsules prescribing information. Research Triangle Park, NC; 2014 Jan.

2. Hauschild A, Grob JJ, Demidov LV et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet. 2012; 380:358-65. [PubMed 22735384]

3. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD. From FDA web site.

4. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD. From FDA web site.

5. Flaherty KT, Infante JR, Daud A et al. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med. 2012; 367:1694-703. [PubMed 23020132]

6. bioMerieux. THxID BRAF kit package insert. Durham, NC. 2013 May.

7. Long GV, Trefzer U, Davies MA et al. Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial. Lancet Oncol. 2012; 13:1087-95. [PubMed 23051966]

8. Ouellet D, Grossmann KF, Limentani G et al. Effects of particle size, food, and capsule shell composition on the oral bioavailability of dabrafenib, a BRAF inhibitor, in patients with BRAF mutation-positive tumors. J Pharm Sci. 2013; :. [PubMed 23608920]

9. Jang S, Atkins MB. Which drug, and when, for patients with BRAF-mutant melanoma?. Lancet Oncol. 2013; 14:e60-9. [PubMed 23369684]

10. Gentilcore G, Madonna G, Mozzillo N et al. Effect of dabrafenib on melanoma cell lines harbouring the BRAF(V600D/R) mutations. BMC Cancer. 2013; 13:17. [PubMed 23317446]

11. GlaxoSmithKline, Research Triangle Park, NC: Personal communication.

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