ROZLYTREK's Market Growth Reflects Transforming Treatment for NTRK and ROS1-Positive Cancers | DelveInsight

As biomarker testing and the demand for tumor-agnostic therapies rise, ROZLYTREK can potentially target a specialized yet valuable market segment. While competition from other TRK inhibitors, such as larotrectinib (VITRAKVI), may influence growth, its ability to penetrate the CNS provides a distinct advantage.

LAS VEGAS, March 12, 2025 /PRNewswire/ -- DelveInsight's "ROZLYTREK Market Size, Forecast, and Market Insight Report" highlights the details around ROZLYTREK, an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1, and ALK with IC50 values of 0.1 to 2 nM. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of ROZLYTREK. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan].

Roche's ROZLYTREK (entrectinib) Overview

ROZLYTREK is a tumor-agnostic therapy that introduces a novel approach to cancer treatment. Its active ingredient, entrectinib, inhibits tropomyosin receptor tyrosine kinases (TRKA, TRKB, and TRKC), which are encoded by the NTRK1, NTRK2, and NTRK3 genes. It also targets ROS1 and ALK, with IC50 values ranging from 0.1 to 2 nM, while showing weaker inhibition of JAK2 and TNK2 (IC50 > 5 nM). The primary active metabolite, M5, exhibits similar inhibitory activity against TRK, ROS1, and ALK.

Fusion proteins involving TRK, ROS1, or ALK kinase domains can promote tumor growth by excessively activating downstream signaling pathways, leading to uncontrolled cell proliferation. Entrectinib has demonstrated both in vitro and in vivo efficacy in inhibiting cancer cell lines across multiple tumor types carrying NTRK, ROS1, or ALK fusions. Additionally, it achieves steady-state brain-to-plasma concentration ratios between 0.4 and 2.2 in animal studies (mice, rats, and dogs) and has shown anti-tumor effects in mice with intracranial tumors driven by TRKA and ALK.

ROZLYTREK is an orally administered, once-daily treatment approved for NTRK fusion-positive solid tumors and ROS1-positive NSCLC in several countries, including Australia, Canada, the EU, Israel, Japan, New Zealand, South Korea, Taiwan, and the US, with additional regulatory reviews ongoing worldwide.

The recommended ROZLYTREK dosage for ROS1-positive NSCLC is 600 mg once daily, with or without food, until disease progression or unacceptable toxicity. For NTRK fusion-positive solid tumors, the ROZLYTREK dosage guidelines are as follows: 

• Adults and pediatric patients with a body surface area (BSA) of ≥1.51 m²: 600 mg once daily 
• Pediatric patients older than 6 months: 300 mg/m² to a maximum of 600 mg 
• Pediatric patients between 1 month and 6 months: 250 mg/m² once daily

Learn more about ROZLYTREK projected market size for ROS1 NSCLC @ ROZLYTREK Market Potential 

Receptor Tyrosine Kinase (ROS1) is an essential transmembrane receptor protein that regulates key cellular functions such as apoptosis, survival, differentiation, proliferation, migration, and transformation. It plays a pivotal role in various cancers, including glioblastoma, colorectal cancer, gastric adenocarcinoma, inflammatory myofibroblastic tumor, ovarian cancer, angiosarcoma, and NSCLC. 

A ROS1 inhibitor is a drug designed to block the activity of abnormal ROS1 fusion proteins present in certain cancer cells. By inhibiting this protein, these inhibitors help restrict cancer cell growth and metastasis. As a type of targeted therapy, ROS1 inhibitors also act on multiple kinases, including Anaplastic Lymphoma Kinase (ALK) and Mesenchymal Epithelial Transition (MET), alongside ROS1. These inhibitors specifically target the kinase domain of ROS1, with conventional kinases classified into DFG-in (active, type I) and DFG-out (inactive, type II) based on their domain structure. For patients with stage IV ROS1-positive NSCLC, treatment with a ROS1 tyrosine kinase inhibitor (TKI) is recommended. 

ROS1 inhibitors have demonstrated remarkable efficacy in treating NSCLC, encompassing both approved therapies and emerging treatments under development. They have significantly advanced NSCLC management, establishing themselves as a crucial therapeutic approach. The current market for ROS1-positive NSCLC is largely dominated by TKIs such as XALKORI. 

According to DelveInsight's analysis, the market size for ROS1 inhibitors in NSCLC across the 7MM was valued at approximately USD 290 million in 2023, with the United States contributing the largest share. The market for ROS1 inhibitors is projected to experience substantial growth in the coming years. This expansion is driven by rising biomarker testing rates, a growing number of cancer diagnoses, increased awareness of ROS1 mutations, and the introduction of next-generation ROS1 TKIs. These advanced therapies offer improved CNS penetration and a broader range of coverage against ROS1 resistance mutations compared to first-generation TKIs. 

Discover more about the ROS1 inhibitors market in detail @ ROS1 Inhibitors Market Report

Emerging Competitors of ROZLYTREK

The promising ROS1 inhibitors in the pipeline that will give tough competition to Roche's ROZLYTREK include DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Zidesamtinib (NVL-520) (Nuvalent), ANS03 (Avistone Biotechnology), Zanidatamab (Jazz Pharmaceuticals), PT-112 (Promontory Therapeutics), and others. 

In December 2024, Nuvation Bio announced that the US FDA had granted the application Priority Review and assigned a Prescription Drug User Fee Act (PDUFA) goal date of June 2025. The company is preparing for a launch as early as mid-2025.

To know more about the number of competing drugs in development, visit @ ROZLYTREK Market Positioning Compared to Other Drugs

Key Milestones of ROZLYTREK 

• In October 2023, the US FDA granted accelerated approval to ROZLYTREK in new oral pellet form for pediatric patients older than 1 month with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory standard therapy.
• In August 2020, the EC granted conditional marketing authorization for ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors expressing an NTRK gene fusion, who have a disease that is locally advanced, metastatic, or where surgical resection is likely to result in severe morbidity, and who have not received a prior NTRK inhibitor, who have no satisfactory treatment options. The EC also approved ROZLYTREK for the treatment of adults with ROS1-positive, advanced NSCLC not previously treated with ROS1 inhibitors.
• In February 2020, Chugai obtained approval for an additional indication of ROZLYTREK for the treatment of ROS1 fusion-positive, unresectable, advanced, or metastatic NSCLC from the MHLW.
• In September 2019, Chugai Pharmaceutical announced the launch of ROZLYTREK 100 mg and 200 mg capsules, for the treatment of NTRK fusion-positive advanced or recurrent solid tumors.
• In August 2019, the US FDA approved ROZLYTREK to treat adults with ROS1-positive, metastatic NSCLC. The FDA has also granted accelerated approval to ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy.
• In June 2019, the MHLW approved ROZLYTREK for treating adult and pediatric patients with NTRK fusion-positive, advanced recurrent solid tumors.
• In February 2019, the US FDA issued a priority review designation letter to ROZLYTREK adult patients with metastatic NSCLC whose tumors are ROS1–positive.
• In December 2018, ROZLYTREK received ODD in Japan with the intended indication of NTRK fusion-positive, locally advanced, or metastatic solid tumors.
• In September 2018, ROZLYTREK received SAKIGAKE designation for the treatment of adult and pediatric patients with NTRK gene fusion-positive, locally advanced, or metastatic solid tumors who have progressed following prior therapies or have no acceptable standard therapies. 
• In July 2018, Chugai entered into a license agreement with Roche for entrectinib. Under the terms of the agreement, Chugai obtains exclusive rights for the development and marketing of entrectinib in Japan and will make upfront and milestone payments to Roche.
• In December 2017, Roche and Ignyta entered a definitive merger agreement for Roche to fully acquire Ignyta for USD 27.00 per share in an all-cash transaction.
• In October 2017, ROZLYTREK was awarded PRIME status for treating NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or have no acceptable standard therapy by EMA.
• In May 2017, ROZLYTREK was granted BTD for the treatment of NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or who have no acceptable standard therapies by the US FDA.
• In February 2015, the US FDA granted ODD to ROZLYTREK for treating TrkA-positive, TrkB-positive, TrkC-positive, ROS1-positive or ALK-positive NSCLC.

Discover how ROZLYTREK is shaping the ROS1 NSCLC treatment landscape @ Roche ROZLYTREK 

ROZLYTREK Market Dynamics

ROZLYTREK competitive positioning in the market is driven by its tumor-agnostic approval, allowing it to cater to multiple rare cancers with a single therapy. The drug has gained regulatory approval in major markets, including the US, Europe, and Japan, benefiting from an increasing emphasis on biomarker-driven oncology treatments. Its key competitor, Bayer's VITRAKVI (larotrectinib), has a similar mechanism of action but differs in pharmacokinetics and tolerability, creating a nuanced competitive landscape.

Market adoption of ROZLYTREK is influenced by the growing use of comprehensive genomic profiling (CGP) in oncology, which facilitates the identification of eligible patients with NTRK or ROS1 fusions. However, its commercial success is partially constrained by the rarity of these genetic alterations, which limits the addressable patient population. Additionally, the high cost of precision oncology therapies and reimbursement challenges in certain healthcare systems can impact uptake. Nonetheless, increasing awareness and advancements in diagnostic infrastructure are expected to support market growth.

From a strategic perspective, Roche has leveraged partnerships and real-world evidence to expand the drug's adoption. The company is actively working on label expansions and combination strategies to maximize ROZLYTREK's commercial potential. Additionally, the growing use of next-generation sequencing (NGS) panels in routine cancer diagnostics may boost the identification rate of eligible patients, driving future market penetration.

The competitive landscape could see further evolution with the potential entry of new TRK/ROS1 inhibitors, particularly next-generation agents designed to address resistance mutations. However, ROZLYTREK's strong clinical efficacy, broad tissue-agnostic approval, and Roche's global oncology expertise position it well in the precision medicine segment. As personalized oncology continues to gain traction, the drug's long-term success will depend on physician awareness, diagnostic advancements, and favorable pricing and reimbursement strategies.

Dive deeper to get more insight into ROZLYTREK's strengths & weaknesses relative to competitors @ ROZLYTREK Market Drug Report

Table of Contents

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