Mekinist Dosage

Generic name: TRAMETINIB DIMETHYL SULFOXIDE .5mg
Dosage form: tablet, film coated
Drug class: Multikinase inhibitors

Medically reviewed by Drugs.com. Last updated on Jul 11, 2024.

Patient Selection

Melanoma

Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to initiation of treatment with MEKINIST as a single agent or in combination with dabrafenib [see Clinical Studies (14.1, 14.2)].
Information on FDA-approved tests for the detection of BRAF V600 mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics.

NSCLC

Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.3)].
Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

ATC

Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.4)]. An FDA-approved test for the detection of BRAF V600E mutation in ATC is not currently available.

Solid Tumors

Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.6)]. An FDA-approved test for the detection of BRAF V600E mutation in solid tumors other than melanoma and NSCLC is not currently available.

Low-Grade Glioma

Confirm the presence of BRAF V600E mutation in tumor specimens prior to initiation of treatment with MEKINIST and dabrafenib [see Clinical Studies (14.7)]. An FDA-approved test for the detection of BRAF V600E mutation in LGG is not currently available.

Recommended Dosage

MEKINIST Tablets

Adult Patients

The recommended dosage for MEKINIST tablets in adult patients is 2 mg orally taken once daily [see Dosage and Administration (2.3)].

Pediatric Patients

The recommended dosage for MEKINIST tablets in pediatric patients who weigh at least 26 kg is based on body weight (Table 1) [see Dosage and Administration (2.3)]. A recommended dosage of MEKINIST tablets has not been established in patients who weigh less than 26 kg.

Table 1. Recommended Dosage for MEKINIST Tablets in Pediatric Patients (Weight-based)
Body Weight	Recommended Dosage
26 to 37 kg	1 mg orally once daily
38 to 50 kg	1.5 mg orally once daily
51 kg or greater	2 mg orally once daily

MEKINIST for Oral Solution

The recommended dosage for MEKINIST for oral solution is based on body weight (Table 2) [see Dosage and Administration (2.3)].

Table 2. Recommended Dosage for MEKINIST for Oral Solution (Weight-based)
Body Weight	Recommended Dosage Total Volume of Oral Solution Once Daily (Trametinib Content)
8 kg	0.3 mg (6 mL)
9 kg	0.35 mg (7 mL)
10 kg	0.35 mg (7 mL)
11 kg	0.4 mg (8 mL)
12 to 13 kg	0.45 mg (9 mL)
14 to 17 kg	0.55 mg (11 mL)
18 to 21 kg	0.7 mg (14 mL)
22 to 25 kg	0.85 mg (17 mL)
26 to 29 kg	0.9 mg (18 mL)
30 to 33 kg	1 mg (20 mL)
34 to 37 kg	1.15 mg (23 mL)
38 to 41 kg	1.25 mg (25 mL)
42 to 45 kg	1.4 mg (28 mL)
46 to 50 kg	1.6 mg (32 mL)
≥ 51 kg	2 mg (40 mL)

The recommended duration of treatment for patients with unresectable or metastatic melanoma or solid tumors, metastatic NSCLC, or locally advanced or metastatic anaplastic thyroid cancer is until disease progression or unacceptable toxicity.
The recommended duration of treatment in the adjuvant melanoma setting is until disease recurrence or unacceptable toxicity for up to 1 year.
The recommended duration of treatment for pediatric patients with LGG is until disease progression or until unacceptable toxicity.

Refer to the dabrafenib prescribing information for recommended dabrafenib dosing information.

Administration

Take MEKINIST at the same time each day, approximately 24 hours apart.
Take MEKINIST at least 1 hour before or 2 hours after a meal [see Clinical Pharmacology (12.3)].
Do not take a missed dose of MEKINIST within 12 hours of the next dose of MEKINIST.
If vomiting occurs after MEKINIST administration, do not take an additional dose. Take the next dose at its scheduled time.

MEKINIST Tablets

Do not crush or break MEKINIST tablets.

MEKINIST for Oral Solution

MEKINIST for oral solution is intended for administration by a caregiver. Prior to use of the oral solution, ensure caregivers receive training on proper dosing and administration of MEKINIST for oral solution.

Preparation and Administration

To prepare MEKINIST for oral solution, tap the bottle until powder flows freely. Add 90 mL distilled or purified water to the powder in the bottle and invert or gently shake the bottle with re-attached cap for up to 5 minutes until powder is fully dissolved yielding a clear solution. Separate the bottle adapter from the oral syringe. Insert bottle adapter into bottle neck after reconstitution of the solution. Write the discard after date. Once reconstituted, MEKINIST for oral solution can be used for 35 days.
The final concentration of the solution is 0.05 mg/mL.
Administer MEKINIST for oral solution from an oral syringe or feeding tube (4 French gauge or larger).
After reconstitution, store in original bottle below 25°C (77°F) and do not freeze.

Dosage Modifications for Adverse Reactions

Dose reductions for adverse reactions associated with MEKINIST are presented in Tables 3 and 4.

Table 3. Recommended Dosage Reductions for MEKINIST Tablets for Adverse Reactions
Recommended Dosage	1 mg orally once daily	1.5 mg orally once daily	2 mg orally once daily
First dose reduction	0.5 mg orally once daily	1 mg orally once daily	1.5 mg orally once daily
Second dose reduction	N/A	0.5 mg orally once daily	1 mg orally once daily
Subsequent modification	Permanently discontinue MEKINIST tablets if unable to tolerate a maximum of two dose reductions.

Table 4. Recommended Dosage Reductions for MEKINIST for Oral Solution for Adverse Reactions
Body Weight (Recommended dosage once daily)	First Dose Reduction (Administer once daily)	Second Dose Reduction (Administer once daily)
8 kg [0.3 mg (6 mL)]	0.25 mg (5 mL)	0.15 mg (3 mL)
9 kg [0.35 mg (7 mL)]	0.25 mg (5 mL)	0.2 mg (4 mL)
10 kg [0.35 mg (7 mL)]	0.25 mg (5 mL)	0.2 mg (4 mL)
11 kg [0.4 mg (8 mL)]	0.3 mg (6 mL)	0.2 mg (4 mL)
12 to 13 kg [0.45 mg (9 mL)]	0.35 mg (7 mL)	0.25 mg (5 mL)
14 to 17 kg [0.55 mg (11 mL)]	0.4 mg (8 mL)	0.3 mg (6 mL)
18 to 21 kg [0.7 mg (14 mL)]	0.55 mg (11 mL)	0.35 mg (7 mL)
22 to 25 kg [0.85 mg (17 mL)]	0.65 mg (13 mL)	0.45 mg (9 mL)
26 to 29 kg [0.9 mg (18 mL)]	0.7 mg (14 mL)	0.45 mg (9 mL)
30 to 33 kg [1 mg (20 mL)]	0.75 mg (15 mL)	0.5 mg (10 mL)
34 to 37 kg [1.15 mg (23 mL)]	0.85 mg (17 mL)	0.6 mg (12 mL)
38 to 41 kg [1.25 mg (25 mL)]	0.95 mg (19 mL)	0.65 mg (13 mL)
42 to 45 kg [1.4 mg (28 mL)]	1.05 mg (21 mL)	0.7 mg (14 mL)
46 to 50 kg [1.6 mg (32 mL)]	1.2 mg (24 mL)	0.8 mg (16 mL)
≥ 51 kg [2 mg (40 mL)]	1.5 mg (30 mL)	1 mg (20 mL)
Permanently discontinue MEKINIST for oral solution if unable to tolerate a maximum of two dose reductions.

Dosage modifications for adverse reactions associated with MEKINIST are presented in Table 5.

Table 5. Recommended Dosage Modifications for MEKINIST for Adverse Reactions
aNational Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.0. bSee Tables 3 and 4 for recommended dose reductions of MEKINIST. cDose modifications are not recommended for MEKINIST when administered with dabrafenib for the following adverse reactions of dabrafenib: non-cutaneous malignancies and uveitis. Dose modification of MEKINIST is not required for new primary cutaneous malignancies.
Severity of Adverse Reactiona	Dosage Modification for MEKINISTb
Hemorrhage [see Warnings and Precautions (5.2)]
Grade 3	Withhold MEKINIST. If improved, resume MEKINIST at lower dose. If not improved, permanently discontinue MEKINIST.
Grade 4	Permanently discontinue MEKINIST.
Venous Thromboembolic Events [see Warnings and Precautions (5.4)]
Uncomplicated deep venous thrombosis (DVT) or pulmonary embolism (PE)	Withhold MEKINIST for up to 3 weeks. If improved to Grade 0-1, resume MEKINIST at lower dose. If not improved, permanently discontinue MEKINIST.
Life-threatening PE	Permanently discontinue MEKINIST.
Cardiomyopathy [see Warnings and Precautions (5.5)]
Asymptomatic, absolute decrease in left ventricular ejection fraction (LVEF) of 10% or greater from baseline and is below institutional lower limit of normal (LLN) from pretreatment value	Withhold MEKINIST for up to 4 weeks. If improved to normal LVEF value, resume MEKINIST at lower dose. If not improved to normal LVEF value, permanently discontinue MEKINIST.
Symptomatic cardiomyopathy Absolute decrease in LVEF of greater than 20% from baseline that is below LLN	Permanently discontinue MEKINIST.
Ocular Toxicities [see Warnings and Precautions (5.6)]
Retinal pigment epithelial detachments (RPED)	Withhold MEKINIST for up to 3 weeks. If improved, resume MEKINIST at same or lower dose. If not improved, permanently discontinue MEKINIST or resume MEKINIST at lower dose.
Retinal vein occlusion (RVO)	Permanently discontinue MEKINIST.
Pulmonary [see Warnings and Precautions (5.7)]
Interstitial lung disease (ILD)/pneumonitis	Permanently discontinue MEKINIST.
Febrile Reactions [see Warnings and Precautions (5.8)]
Fever of 100.4°F to 104°F (or first symptoms in case of recurrence)	Withhold MEKINIST until fever resolves, then resume MEKINIST at same or lower dose.
Fever higher than 104°F Fever complicated by rigors, hypotension, dehydration, or renal failure	Withhold MEKINIST until febrile reactions resolve for at least 24 hours, then resume MEKINIST at lower dose. Or Permanently discontinue MEKINIST.
Skin Toxicities [see Warnings and Precautions (5.9)]
Intolerable Grade 2 Grade 3 or 4	Withhold MEKINIST for up to 3 weeks. If improved, resume MEKINIST at lower dose. If not improved, permanently discontinue MEKINIST.
Severe cutaneous adverse reactions (SCARs)	Permanently discontinue MEKINIST.
Other Adverse Reactionsc
Intolerable Grade 2 Any Grade 3	Withhold MEKINIST. If improved to Grade 0-1, resume MEKINIST at lower dose. If not improved, permanently discontinue MEKINIST.
First occurrence of any Grade 4	Withhold MEKINIST until improves to Grade 0-1, then resume MEKINIST at lower dose. Or Permanently discontinue MEKINIST.
Recurrent Grade 4	Permanently discontinue MEKINIST.