Rozlytrek

— THERAPEUTIC CATEGORIES —
  • Respiratory and thoracic cancers
  • Solid tumors

Rozlytrek Generic Name & Formulations

General Description

Entrectinib 100mg, 200mg; caps.

Pharmacological Class

Kinase inhibitor.

How Supplied

Caps 100mg—30; 200mg—90

Manufacturer

Generic Availability

NO

Rozlytrek Indications

Indications

In adults with ROS1-positive metastatic non-small cell lung cancer (NSCLC), as detected by an FDA-approved test.

Rozlytrek Dosage and Administration

Adult

Confirm presence of ROS1 rearrangement(s) in tumor specimens. Swallow whole. 600mg once daily, until disease progression or unacceptable toxicity. Avoid moderate or strong CYP3A inhibitors; if unavoidable, reduce to 200mg once daily (moderate CYP3A inhibitors); and 100mg once daily (strong CYP3A inhibitors). Dose modifications for adverse reactions: see full labeling.

Children

Not established.

Rozlytrek Contraindications

Not Applicable

Rozlytrek Boxed Warnings

Not Applicable

Rozlytrek Warnings/Precautions

Warnings/Precautions

Assess LVEF prior to initiation in those with risk factors for CHF. Withhold, reduce dose or permanently discontinue based on severity if CHF or CNS effects occur. Increased risk for fractures. Monitor LFTs (including AST/ALT) every 2 weeks during the 1st month, then monthly thereafter, and as clinically indicated; withhold and resume (at same or reduced dose) or permanently discontinue based on severity. Known long QT syndrome. Bradyarrhythmias. Uncontrolled heart failure. Electrolyte abnormalities. Assess QT interval, electrolytes, and serum uric acid levels prior to initiation then periodically; withhold and resume (at same or reduced dose) based on severity; monitor. Withhold dose if vision disorders or new changes occur until improvement or stabilization; conduct an eye exam as clinically appropriate. Embryo-fetal toxicity. Advise use of effective contraception during and for 5 weeks (females of reproductive potential) or for 3 months (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 7 days after the last dose).

Rozlytrek Pharmacokinetics

See Literature

Rozlytrek Interactions

Interactions

Potentiated by moderate or strong CYP3A inhibitors; avoid; if unavoidable, reduce dose (see Adults and Children). Avoid grapefruit products. Antagonized by moderate or strong CYP3A inducers; avoid use. Avoid concomitant other drugs known to prolong QTc interval.

Rozlytrek Adverse Reactions

Adverse Reactions

Fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, vision disorders; CHF, CNS effects, skeletal fractures, hepatotoxicity, hyperuricemia, QT prolongation.

Rozlytrek Clinical Trials

See Literature

Rozlytrek Note

Not Applicable

Rozlytrek Patient Counseling

See Literature

Rozlytrek Generic Name & Formulations

General Description

Entrectinib 100mg, 200mg; caps.

Pharmacological Class

Kinase inhibitor.

How Supplied

Caps 100mg—30; 200mg—90

Manufacturer

Generic Availability

NO

Rozlytrek Indications

Indications

Treatment of patients with solid tumors that: have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, as detected by an FDA-approved test without a known acquired resistance mutation; are metastatic or where surgical resection is likely to result in severe morbidity; and have either progressed following treatment or have no satisfactory alternative therapy.

Rozlytrek Dosage and Administration

Adult

Confirm presence of a NTRK gene fusion. Swallow whole. 600mg once daily, until disease progression or unacceptable toxicity. Avoid moderate or strong CYP3A inhibitors; if unavoidable, reduce to 200mg once daily (moderate CYP3A inhibitors); and 100mg once daily (strong CYP3A inhibitors). Dose modifications for adverse reactions: see full labeling.

Children

<12yrs: not established. Confirm presence of a NTRK gene fusion. Swallow whole. Base dose on body surface area (BSA). ≥12yrs (BSA >1.50m2): 600mg once daily; (BSA 1.11–1.50m2): 500mg once daily; (BSA 0.91–1.10m2): 400mg once daily. Give until disease progression or unacceptable toxicity. Avoid moderate or strong CYP3A inhibitors; if unavoidable and ≥12yrs (w. BSA >1.50m2), reduce to 200mg once daily (moderate CYP3A inhibitors); and 100mg once daily (strong CYP3A inhibitors). Dose modifications for adverse reactions: see full labeling.

Rozlytrek Contraindications

Not Applicable

Rozlytrek Boxed Warnings

Not Applicable

Rozlytrek Warnings/Precautions

Warnings/Precautions

Assess LVEF prior to initiation in those with risk factors for CHF. Withhold, reduce dose or permanently discontinue based on severity if CHF or CNS effects occur. Increased risk for fractures. Monitor LFTs (including AST/ALT) every 2 weeks during the 1st month, then monthly thereafter, and as clinically indicated; withhold and resume (at same or reduced dose) or permanently discontinue based on severity. Known long QT syndrome. Bradyarrhythmias. Uncontrolled heart failure. Electrolyte abnormalities. Assess QT interval, electrolytes, and serum uric acid levels prior to initiation then periodically; withhold and resume (at same or reduced dose) based on severity; monitor. Withhold dose if vision disorders or new changes occur until improvement or stabilization; conduct an eye exam as clinically appropriate. Embryo-fetal toxicity. Advise use of effective contraception during and for 5 weeks (females of reproductive potential) or for 3 months (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 7 days after the last dose).

Rozlytrek Pharmacokinetics

See Literature

Rozlytrek Interactions

Interactions

Potentiated by moderate or strong CYP3A inhibitors; avoid; if unavoidable, reduce dose (see Adults and Children). Avoid grapefruit products. Antagonized by moderate or strong CYP3A inducers; avoid use. Avoid concomitant other drugs known to prolong QTc interval.

Rozlytrek Adverse Reactions

Adverse Reactions

Fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, vision disorders; CHF, CNS effects, skeletal fractures, hepatotoxicity, hyperuricemia, QT prolongation.

Rozlytrek Clinical Trials

See Literature

Rozlytrek Note

Not Applicable

Rozlytrek Patient Counseling

See Literature