Rozlytrek (Entrectinib) 200mg Capsules | South Korea-Sourced NTRK/ROS1 Inhibitor | GLT

What is Rozlytrek (Entrectinib) Used For?

Rozlytrek (entrectinib) is an oral kinase inhibitor developed by Roche that selectively targets the neurotrophic tyrosine receptor kinases NTRK1, NTRK2, and NTRK3 (TRKA, TRKB, TRKC) as well as ROS1. It is approved for two indications: (1) adult patients with ROS1-positive metastatic non-small cell lung cancer (NSCLC); and (2) adult and pediatric patients (12 years and older) with NTRK gene fusion-positive solid tumors that are metastatic or where surgery would likely cause severe morbidity, and who have progressed or have no satisfactory alternative therapy. The NTRK solid-tumor indication was granted under accelerated approval based on tumor response rate and durability of response.

How Does Rozlytrek Work?

Entrectinib inhibits the kinase activity of TRKA, TRKB, and TRKC (encoded by the NTRK1, NTRK2, and NTRK3 genes) and ROS1. NTRK gene fusions and ROS1 rearrangements act as oncogenic drivers in a variety of solid tumors. By blocking these targets, entrectinib suppresses the growth of fusion-driven tumors across tumor types (tumor-agnostic). A notable advantage is its blood-brain barrier penetration, which provides meaningful intracranial activity in patients with brain metastases.

Approved Indications

• Adult patients with ROS1-positive metastatic non-small cell lung cancer (NSCLC)
• Adult and pediatric patients (12 years and older) with NTRK fusion-positive solid tumors (tumor-agnostic indication)

Clinical Efficacy (STARTRK-1/2 and ALKA-372-001)

• NTRK fusion-positive solid tumors: objective response rate (ORR) 57%, with intracranial ORR 50% in patients with CNS metastases
• ROS1-positive NSCLC: ORR 77%, median progression-free survival (mPFS) 19.0 months
• Responses observed across 10+ tumor types and across treatment lines

Dosage & Administration

The recommended adult dosage is 600 mg taken orally once daily, with or without food. Rozlytrek is available as 100 mg and 200 mg capsules. Pediatric dosing (12 years and older) is based on body surface area. Do not crush, chew, or open capsules. Select patients based on ROS1 rearrangement or NTRK gene fusion detected by an approved test (RT-PCR or NGS).

Warnings & Precautions

• Congestive heart failure — assess left ventricular ejection fraction before and during treatment
• Central nervous system effects — dizziness, cognitive impairment, mood disorders
• Skeletal fractures, hyperuricemia, QT interval prolongation
• Hepatotoxicity and embryo-fetal toxicity

Storage

Store at room temperature (20°C to 25°C / 68°F to 77°F), in the original container, away from moisture and heat.