Rozlytrek Dosage

Generic name: ENTRECTINIB 100mg
Dosage form: capsule
Drug class: Multikinase inhibitors

Medically reviewed by Drugs.com. Last updated on Nov 20, 2024.

Patient Selection

Select patients for the treatment of metastatic NSCLC with ROZLYTREK based on the presence of ROS1 rearrangement(s) in tumor or plasma specimens. Testing using plasma specimens is only appropriate for patients for whom tumor tissue is not available for testing.
Information on FDA-approved tests for the detection of ROS1 rearrangement(s) in NSCLC is available at http://www.fda.gov/CompanionDiagnostics.
Select patients for treatment of locally advanced or metastatic solid tumors with ROZLYTREK based on the presence of a NTRK gene fusion in tumor or plasma specimens. Testing using plasma specimens is only appropriate for patients for whom tumor tissue is not available for testing.
Information on FDA-approved tests for the detection of NTRK gene fusion(s) in solid tumors is available at http://www.fda.gov/CompanionDiagnostics.

Recommended Evaluation and Testing Before Initiating ROZLYTREK

Before initiating ROZLYTREK, evaluate:

left ventricular ejection fraction (LVEF)
serum uric acid levels
QT interval and electrolytes

ROZLYTREK Dosage Form Overview

The physician should prescribe the most appropriate dosage form of ROZLYTREK according to the dose required and patient needs.

ROZLYTREK is available in two dosage forms, and can be administered either as capsules swallowed whole, capsules made into an oral suspension (or for enteral tube administration) and as oral pellets swallowed with soft food.

ROZLYTREK Capsules 100 mg and 200 mg

Whole capsules: For patients who can swallow whole capsules and whose doses are multiples of 100 mg.
Capsules prepared as an oral suspension:
- For patients who have difficulty or are unable to swallow capsules or who require enteral administration (e.g., gastric or nasogastric tube)..
- For dose increments of 10 mg, only use capsules prepared as a suspension.

ROZLYTREK Oral Pellets 50 mg per packet

Pellets sprinkled on one or more spoonfuls of soft food:
- For patients who have difficulty or are unable to swallow capsules but can swallow soft food and whose doses are multiples of 50 mg..
- Do not use pellets for preparation of suspension.
- Do not attempt to use partial quantities of pellets from 50 mg pellet packets to prepare a dose.
- Do not use the pellet formulation for enteral tube administration as the pellets may clog the tube.

ROZLYTREK Administration Overview

Administer ROZLYTREK capsules, capsules prepared as a suspension, or pellets once daily, with or without food.
If a dose of ROZYTREK is missed, make up that dose unless the next dose is due within 12 hours.
If vomiting occurs immediately after taking a dose of ROZLYTREK, repeat that dose.

ROZLYTREK Recommended Dosage for ROS1-Positive Non-Small Cell Lung Cancer

The recommended dosage of ROZLYTREK is 600 mg orally once daily with or without food until disease progression or unacceptable toxicity.

ROZLYTREK Recommended Dosage for NTRK Gene Fusion-Positive Solid Tumors

The recommended dosages of ROZLYTREK for the treatment of adult and pediatric patients with NTRK Gene Fusion-Positive Solid Tumors are provided in Table 1.

Administer the recommended dosage of ROZLYTREK capsules and oral pellets with or without food until disease progression or unacceptable toxicity.

Sprinkle ROZLYTREK oral pellets on one or more spoonfuls of soft food as a vehicle.

Table 1. Recommended dosage for Adults and Pediatric patients for the Treatment of NTRK Gene Fusion-Positive Solid Tumors
Patient Population	Recommended Dosage of ROZLYTREK	Duration of Treatment
* To enable dosing increments of 10 mg, capsules prepared as an oral suspension must be used.
Adults Pediatric patients with BSA ≥ 1.51 m2:	600 mg orally once daily	Until disease progression or unacceptable toxicity.
Pediatric patients > 6 months:	see Table 2
Pediatric patients > 1 month to ≤ 6 months:	250 mg/m2 orally once daily*

The recommended dosages of ROZLYTREK for the treatment of pediatric patients older than 6 months with NTRK Gene Fusion-Positive Solid Tumors is provided in Table 2.

Table 2. Recommended dosage for Pediatric Patients Older than 6 Months for the Treatment of NTRK Gene Fusion-Positive Solid Tumors
Body Surface Area (BSA)*	Recommended Dosage Orally Once Daily
* BSA categories and recommended dosage above are based on closely matching exposures to a target dose of 300 mg/m2 † To enable dosing increments of 10 mg, capsules prepared as an oral suspension must be used.
≤0.50 m2	300 mg/m2†
0.51 to 0.80 m2	200 mg
0.81 to 1.10 m2	300 mg
1.11 to 1.50 m2	400 mg
≥ 1.51 m2	600 mg

ROZLYTREK Dosage Modifications for Adverse Reactions

The recommended dosage reductions of ROZLYTREK for the management of adverse reactions for adults and pediatric patients are provided in Table 3.

Table 3. Recommended Dose Reductions for ROZLYTREK for the Management of Adverse Reactions
Starting Dose once daily	First dose reduction	Second dose reduction
* To enable dosing increments of 10 mg, capsules prepared as an oral suspension must be used.
250 mg/m2 or 300 mg/m2	Reduce the once daily dose to two thirds of the starting dose*	Reduce the once daily dose to one third of the starting dose*	Permanently discontinue ROZLYTREK in patients who are unable to tolerate ROZLYTREK after two dose reductions.
200 mg	150 mg once daily	100 mg once daily
300 mg	200 mg once daily	100 mg once daily
400 mg	300 mg once daily	200 mg once daily
600 mg	400 mg once daily	200 mg once daily

Table 4 provides the ROZLYTREK recommended dosage modifications for the management of adverse reactions.

Table 4. ROZLYTREK Dosage Modifications for the Management of Adverse Reactions
Adverse Reaction	Severity*	Dosage Modification
* Severity as defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.0.
Congestive Heart Failure	Grade 2 or 3	Withhold ROZLYTREK until recovered to less than or equal to Grade 1. Resume at reduced dose.
Congestive Heart Failure	Grade 4	Permanently discontinue ROZLYTREK.
Central Nervous System Effects	Intolerable Grade 2	Withhold ROZLYTREK until recovery to less than or equal to Grade 1 or to baseline. Resume at same dose or reduced dose, as clinically appropriate.
	Grade 3	Withhold ROZLYTREK until recovery to less than or equal to Grade 1 or to baseline. Resume at reduced dose.
	Grade 4	Permanently discontinue ROZLYTREK.
Hepatotoxicity	Grade 3	Withhold ROZLYTREK until recovery to less than or equal to Grade 1 or to baseline. Resume at same dose if resolution occurs within 4 weeks. Permanently discontinue if adverse reaction does not resolve within 4 weeks. Resume at a reduced dose for recurrent Grade 3 events that resolve within 4 weeks.
	Grade 4	Withhold ROZLYTREK until recovery to less than or equal to Grade 1 or to baseline. Resume at reduced dose if resolution occurs within 4 weeks. Permanently discontinue if adverse reaction does not resolve within 4 weeks. Permanently discontinue for recurrent Grade 4 events.
	ALT or AST greater than 3 times ULN with concurrent total bilirubin greater than 1.5 times ULN (in the absence of cholestasis or hemolysis).	Permanently discontinue ROZLYTREK.
Hyperuricemia	Symptomatic or Grade 4	Initiate urate-lowering medication. Withhold ROZLYTREK until improvement of signs or symptoms. Resume ROZLYTREK at same or reduced dose.
QT Interval Prolongation	QTc greater than 500 ms	Withhold ROZLYTREK until QTc interval recovers to baseline. Resume at same dose if factors that cause QT prolongation are identified and corrected. Resume at reduced dose if other factors that cause QT prolongation are not identified.
QT Interval Prolongation	Torsade de pointes; polymorphic ventricular tachycardia; signs/symptoms of serious arrhythmia	Permanently discontinue ROZLYTREK.
Vision Disorders	Grade 2 or above	Withhold ROZLYTREK until improvement or stabilization. Resume at same dose or reduced dose, as clinically appropriate.
Anemia or Neutropenia	Grade 3 or 4	Withhold ROZLYTREK until recovery to less than or equal to Grade 2. Resume at the same dose or reduced dose, as clinically appropriate.
Other Adverse Reactions	Grade 3 or 4	Withhold ROZLYTREK until adverse reaction resolves or improves to recovery or improvement to Grade 1 or baseline. Resume at the same or reduced dose if resolution occurs within 4 weeks. Permanently discontinue if adverse reaction does not resolve within 4 weeks. Permanently discontinue for recurrent Grade 4 events.

ROZLYTREK Dosage Modifications for Drug Interactions

Moderate and Strong CYP3A Inhibitors

Adults and Pediatric Patients 2 Years and Older

Avoid coadministration of ROZLYTREK with moderate or strong CYP3A inhibitors. If coadministration cannot be avoided, reduce the ROZLYTREK dose as shown in Table 5 and limit coadministration to 14 days or less.

Table 5. Recommended Dose Modifications of ROZYLTREK for Concomitant Use with Moderate or Strong CYP3A Inhibitors for Adults and Pediatric Patients 2 Years and Older
Starting dose*	Moderate CYP3A inhibitor	Strong CYP3A inhibitor
* For pediatric patients with a starting dose less than 200 mg, avoid coadministration with moderate or strong CYP3A inhibitors
200 mg	50 mg once daily	50 mg on alternate days
300 mg	100 mg once daily	50 mg once daily
400 mg	200 mg once daily	50 mg once daily
600 mg	200 mg once daily	100 mg once daily

After discontinuation of a strong or moderate CYP3A inhibitor for 3 to 5 elimination half-lives, resume the ROZLYTREK dose that was taken prior to initiating the CYP3A inhibitor.

ROZLYTREK Preparation and Administration Instructions

ROZLYTREK Capsules

Swallow capsules whole. Do not crush or chew the capsules.

ROZLYTREK Capsules Prepared as a Suspension for Oral or Enteral Tube Administration

It is recommended that a healthcare provider discuss with the patient or caregiver, the volume of water or milk to be added and oral suspension to withdraw, prior to administration of the first dose (see Table 6).

Table 6 provides the ROZLYTREK dose and volume of room temperature drinking water or milk required to prepare an oral suspension. Instruct patients or caregivers to carefully open capsule(s) and pour the contents into room temperature drinking water or milk to prepare an oral suspension. Let sit for 15 minutes.

Table 6. Preparation of ROZLYTREK Capsules as an Oral Suspension
Dose of ROZLYTREK to be administered	Dose needed for suspension (using 100 mg or 200 mg capsules, as appropriate)	Volume of water or milk to be added	Volume of oral suspension to withdraw and administer
20 mg	100 mg	5 mL	1 mL
30 mg	100 mg	5 mL	1.5 mL
40 mg	100 mg	5 mL	2 mL
50 mg	100 mg	5 mL	2.5 mL
60 mg	100 mg	5 mL	3 mL
70 mg	100 mg	5 mL	3.5 mL
80 mg	100 mg	5 mL	4 mL
90 mg	100 mg	5 mL	4.5 mL
100 mg	100 mg	5 mL	5 mL
110 mg	200 mg	10 mL	5.5 mL
120 mg	200 mg	10 mL	6 mL
130 mg	200 mg	10 mL	6.5 mL
140 mg	200 mg	10 mL	7 mL
150 mg	200 mg	10 mL	7.5 mL
200 mg	200 mg	10 mL	10 mL
300 mg	300 mg	15 mL	15 mL
400 mg	400 mg	20 mL	20 mL
600 mg	600 mg	30 mL	30 mL

Administer ROZLYTREK oral suspension immediately after preparation.

Discard any unused suspension if not used within 2 hours.

Instruct patients to drink water after taking the oral suspension to ensure ROZLYTREK has been completely swallowed.

Enteral Tube Administration

If enteral administration (e.g., gastric or nasogastric tube) is required, administer the oral suspension via the tube. Use an enteral tube that is 8 FR or higher to administer dosing volumes of 3 mL or higher. Instruct patients to divide dosing volumes of 3 mL or higher into at least two aliquots and flush the tube after each administration. Flush the tube with a volume of water or milk that is equal to the aliquot administered. For a dose volume of 30 mL, divide into at least three (10 mL) aliquots. The tube should be flushed with water or milk after delivering each aliquot of ROZLYTREK.

Refer to the Instructions for Use for detailed instructions on preparation and administration of ROZLYTREK capsules as an oral suspension via an enteral tube.

ROZLYTREK Oral Pellets

Sprinkle pellets on one or more spoonfuls of a soft food (e.g., applesauce, yogurt, or pudding) and take within 20 minutes of preparation. Do not crush or chew to avoid a bitter taste.

The patient should drink water after taking the pellets to ensure the drug has been completely swallowed.

Do not attempt to use partial quantities of pellets from 50 mg pellet packets to prepare a dose.

Do not use the pellet formulation for enteral tube administration as the pellets may clog the tube.

Refer to the Instructions for Use for detailed instructions on preparation and administration of ROZLYTREK oral pellets.

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Drug Status

Availability Prescription only Rx

Pregnancy & Lactation Risk data available

CSA Schedule* Not a controlled drug N/A

Approval History Drug history at FDA

User Reviews & Ratings

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Rozlytrek Dosage

Patient Selection

Recommended Evaluation and Testing Before Initiating ROZLYTREK

ROZLYTREK Dosage Form Overview

ROZLYTREK Administration Overview

ROZLYTREK Recommended Dosage for ROS1-Positive Non-Small Cell Lung Cancer

ROZLYTREK Recommended Dosage for NTRK Gene Fusion-Positive Solid Tumors

ROZLYTREK Dosage Modifications for Adverse Reactions

ROZLYTREK Dosage Modifications for Drug Interactions

ROZLYTREK Preparation and Administration Instructions

More about Rozlytrek (entrectinib)

Patient resources

Professional resources

Related treatment guides

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