达拉非尼TAFINLAR(dabrafenib)

[Function and indications]
(1) Tafinlar is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma and BRAF V600E mutation detected by FDA-approved tests.
(2) Tafinlar combined with trametinib is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations detected by FDA-approved tests. The combined use is based on the demonstrated durable response rate. Improvement in disease-related symptoms and overall survival with the combination of Tafinlar and trametinib has not been demonstrated.
Limitations of use: Tafinlar is not indicated for the treatment of patients with wild-type BRAF-inhibitor therapy.
[Model and specifications]
Capsules: 50 mg, 75 mg
[Usage and dosage]
(1) Confirm the presence of BRAF V600E mutation in tumor specimens before starting treatment with Tafinlar as a single agent. Confirm the presence of BRAF V600E or V600K mutation in tumor specimens before starting treatment with Tafinlar and trametinib in combination.
(2) The recommended dose of Tafinlar is 150 mg orally twice daily as a single agent or 2 mg orally once daily in combination with trametinib. Take Tafinlar at least 1 hour before and 2 hours after meals.

[Precautions]
(1) New primary malignancies, skin and non-skin: May occur when Tafinlar is used in combination with trametinib. Monitor patients for new malignancies before and during treatment with Tafinlar, and after discontinuation of combination therapy.
(2) Tumor promotion in BRAF wild-type melanoma: Increased cell proliferation may occur with BRAF inhibitors.
(3) Bleeding: Major bleeding events may occur in patients receiving Tafinlar in combination with trametinib. Monitor for signs and symptoms of bleeding.
(4) Venous thromboembolism: Deep vein thrombosis and pulmonary embolism may occur in patients receiving Tafinlar in combination with trametinib.
(5) Cardiomyopathy: Assess LVEF before treatment with Tafinlar in combination with trametinib, 1 month after treatment, and then every 2 to 3 months thereafter.
(6) Ocular toxicity: Perform an ophthalmological evaluation for any visual disturbance.
(7) Severe febrile reactions: May occur when Tafinlar is used in combination with trametinib.
(8) Severe skin toxicity: Monitor for skin toxicity and secondary infection. Discontinue dosing for intolerable Grade 2, and Grade 3 and 4 rashes that do not improve within 3 weeks despite interruption of Tafinlar.
(9) Hyperglycemia: Monitor serum glucose levels in patients with preexisting diabetes and hyperglycemia.
(10) Glucose-6-phosphate dehydrogenase deficiency: Closely monitor for hemolytic anemia.
(11) Embryofetal toxicity: May cause fetal harm. Advise females of reproductive potential of the risk to the fetus. Tafinlar may render hormonal contraceptives ineffective and an alternative method of contraception should be used.

[Adverse Reactions]
(1) The most common adverse reactions (≥20%) to Tafinlar as a single agent are hyperkeratosis, headache, fever, arthritis, papilloma, alopecia, and palmar-plantar erythrodysesthesia syndrome.
(2) The most common adverse reactions (≥20%) for the combination of Tafinlar and trametinib include fever, chills, fatigue, rash, nausea, vomiting, diarrhea, abdominal pain, peripheral edema, cough, headache, arthralgia, night sweats, decreased appetite, constipation, and myalgia.

[Use in Pregnant Women]
(1) Breastfeeding mothers: discontinue the drug and breastfeeding.
(2) Females and males of reproductive potential: Advise female patients to use highly effective contraception during treatment and for 2 weeks after discontinuation of treatment. Advise male patients of reproductive potential of the potential risk of impaired spermatogenesis.

[Drug Interactions]
(1) Avoid co-administration of strong inhibitors of CYP3A4 and CYP2C8.
(2) Avoid co-administration of strong inducers of CYP3A4 and CYP2C8.
(3) Concomitant use of drugs that are sensitive substrates of CYP3A4, CYP2C8, CYP2C9, CYP2C19, and CYP2B6 may result in loss of efficacy of these drugs.

Note: If the drug has a new packaging, the new packaging shall prevail. The above information comes from the Internet or is translated by student volunteers from higher medical colleges (if there are any errors or omissions, please help correct them). It is only for internal discussion among medical staff and is not used as any basis for medication. For specific medication instructions, please consult your attending physician.