Entrectinib - Generic Drug Details

What are the generic sources for entrectinib and what is the scope of patent protection?

Entrectinib is the generic ingredient in one branded drug marketed by Genentech Inc and is included in two NDAs. There are fourteen patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Entrectinib has one hundred and twenty-nine patent family members in thirty-one countries.

One supplier is listed for this compound.

Summary for entrectinib

International Patents:	129
US Patents:	14
Tradenames:	1
Applicants:	1
NDAs:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	59
Clinical Trials:	37
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for entrectinib
What excipients (inactive ingredients) are in entrectinib?	entrectinib excipients list
DailyMed Link:	entrectinib at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for entrectinib

Constraining patent/regulatory exclusivity:

10,398,693

Dosage:

CAPSULE;ORAL

Constraining patent/regulatory exclusivity:

TREATMENT OF PEDIATRIC PATIENTS OLDER THAN 1 MONTH UP TO 12 YEARS OF AGE 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 PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY

Dosage:

PELLETS;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

Recent Clinical Trials for entrectinib

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Hoffmann-La Roche	PHASE2
St. Jude Children's Research Hospital	PHASE2
Peking University Shenzhen Hospital	PHASE2

See all entrectinib clinical trials

Anatomical Therapeutic Chemical (ATC) Classes for entrectinib

L01EX	Other protein kinase inhibitors
L01E	PROTEIN KINASE INHIBITORS
L01	ANTINEOPLASTIC AGENTS
L	Antineoplastic and immunomodulating agents

US Patents and Regulatory Information for entrectinib

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-001	Aug 15, 2019		RX	Yes	No
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes	10,738,037		Y	Y
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-001	Aug 15, 2019		RX	Yes	No	10,231,965
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes	8,673,893
Genentech Inc	ROZLYTREK	entrectinib	PELLETS;ORAL	218550-001	Oct 20, 2023		RX	Yes	Yes

EU/EMA Drug Approvals for entrectinib

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Roche Registration GmbH	Rozlytrek	entrectinib	EMEA/H/C/004936Rozlytrek as monotherapy is indicated for the treatment of adult and paediatric patients 12 years of age and older with solid tumours expressing a neurotrophic tyrosine receptor kinase (NTRK) gene fusion,who have a disease that is locally advanced, metastatic or where surgical resection is likely to result in severe morbidity, andwho have not received a prior NTRK inhibitorwho have no satisfactory treatment options.Rozlytrek as monotherapy is indicated for the treatment of adult patients with ROS1 positive, advanced non small cell lung cancer (NSCLC) not previously treated with ROS1 inhibitors.	Authorised	no	no	no	2020-07-31

International Patents for entrectinib

Country	Patent Number	Title	Estimated Expiration
Australia	2018201037
Japan	2020527575	エントレクチニブを含む薬学的組成物
Japan	2021042213
Australia	2013265288
Taiwan	201400479	Process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide
Australia	2018201037	Process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide
Israel	235761	תהליך להכנת n - [5 - (3, 5 - דיפלואורו - בנזיל) -1h - אינדאזול - 3 - איל] - 4 - (4 - מתיל - פיפראזין - 1 - איל) - 2 - (טטראהידרו - פיראן - 4 - אילאמינו) - בנזאמיד (Process for the preparation of n - [5-(3, 5-difluoro-benzyl) -1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide)

Supplementary Protection Certificates for entrectinib

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2176231	2020C/551	Belgium		PRODUCT NAME: ENTRECTINIB OF ISOMEREN, TAUTOMEREN OF FARMACEUTISCH AANVAARDBARE ZOUTEN DAARVAN; AUTHORISATION NUMBER AND DATE: EU/1/20/1460 20200803
3107541	SPC/GB21/034	United Kingdom		PRODUCT NAME: ENTRECTINIB, AND ISOMERS, TAUTOMERS AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF; REGISTERED: UK EU/1/20/1460 (NI) 20200803; UK PLGB00031/0913 20200803; UK PLGB00031/0914 20200803
2176231	132020000000164	Italy		PRODUCT NAME: ENTRECTINIB O SUOI ISOMERI, TAUTOMERI O SALI FARMACEUTICAMENTE ACCETTABILI(ROZLYTREK); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/20/1460, 20200803
2176231	CA 2020 00058	Denmark		PRODUCT NAME: ENTRECTINIB ELLER ISOMERER, TAUTOMERER ELLER FARMACEUTISK ACCEPTABLE SALTE DERAF; REG. NO/DATE: EU/1/20/1460 20200803
2176231	LUC00191	Luxembourg		PRODUCT NAME: ENTRECTINIB OU LES ISOMERES, TAUTOMERES, OU SELS PHARMACEUTIQUEMENT ACCEPTABLES DE CELUI-CI; AUTHORISATION NUMBER AND DATE: EU/1/20/1460 20200803
3107541	21/2021	Austria		PRODUCT NAME: ENTRECTINIB ODER EIN PHARMAZEUTISCH ANNEHMBARES SALZ DAVON; REGISTRATION NO/DATE: EU/1/20/1460 (MITTEILUNG) 20200803
2176231	824	Finland

Market Dynamics and Financial Trajectory for the Pharmaceutical Drug: Entrectinib

Last updated: July 30, 2025

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Introduction

Entrectinib, commercially known as Rozlydek, is a targeted tyrosine kinase inhibitor (TKI) developed for the treatment of specific cancers characterized by neurotrophic receptor tyrosine kinase (NTRK) gene fusions, ROS1-positive non-small cell lung cancer (NSCLC), and other solid tumors. Since its FDA approval in 2019, entrectinib’s market trajectory has been shaped by evolving clinical data, competitive landscape, regulatory developments, and broader oncological treatment trends. This analysis explores the current market dynamics and financial outlook, offering insights pertinent to industry stakeholders.

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Pharmacological Profile and Clinical Indications

Entrectinib acts by inhibiting TRK A/B/C receptors and ROS1 fusion proteins, halting tumor progression. Approved initially for adult and pediatric NTRK fusion-positive solid tumors, its indications expanded to ROS1-positive NSCLC in 2021. This dual-target specificity provides a robust therapeutic niche, especially given the limited alternatives for patients with NTRK gene fusions, a rare but critical oncogenic driver.

Clinical efficacy demonstrated across multiple trials, notably the STARTRK-2 study, underpins its commercial success. The drug's ability to penetrate the central nervous system (CNS) addresses an unmet need for brain metastases, a common complication in advanced cancers, enhancing its attractiveness to clinicians.

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Market Dynamics

1. Competitive Landscape

Entrectinib operates in a highly competitive segment, primarily against other targeted therapies such as larotrectinib (Vitrakvi) and crizotinib (Xalkori). While larotrectinib also targets NTRK fusions, entrectinib's CNS activity offers a potential advantage, particularly in managing brain metastases. However, the market penetration of larotrectinib, with similar indications, constrains overall market share growth.

Besides NTRK inhibitors, ROS1-positive NSCLC treatment also includes crizotinib, ceritinib, and entrectinib itself. The competition underscores a fragmented landscape where therapeutic efficacy, safety profiles, and CNS penetration influence clinician preferences.

2. Regulatory and Reimbursement Environment

Regulatory approvals across major markets, including the U.S., Europe, and Japan, facilitate market access. Nevertheless, reimbursement policies significantly influence sales trajectories. Payer reimbursement hinges on demonstrated long-term benefit and cost-effectiveness, especially given entrectinib's premium pricing.

The FDA's expedited approval pathway and subsequent designations (e.g., Orphan Drug) support market exclusivity and incentivize adoption. However, divergences in reimbursement criteria and pricing negotiations can impact revenue streams.

3. Manufacturing and Supply Chain Factors

Supply chain stability has gained increasing importance amid global disruptions. As entrectinib's manufacturing involves complex synthesis, maintaining consistent supply to meet rising demand remains crucial. Companies investing in scalable, compliant manufacturing enhance their market positioning.

4. Clinical Adoption and Market Penetration

Physician familiarity, clinical guidelines, and evidence from real-world data drive adoption. Ongoing post-marketing studies and expansion into pediatric populations bolster confidence. The evolving diagnostic landscape, including NTRK and ROS1 testing accessibility, directly influences patient identification and therapy initiation rates.

5. Pricing Strategy and Competitive Positioning

Pricing strategies consider the rarity of NTRK fusions, therapeutic benefit, and competitive pressure. Premium pricing is justified by high unmet need and targeted therapy costs but may limit access in cost-sensitive markets. Outcomes from health economic evaluations influence payer acceptance and formulary inclusion.

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Financial Trajectory

1. Revenue Forecasts

Since FDA approval, entrectinib’s revenue growth has been incremental but steady. Initial quarters post-launch saw modest sales, primarily in the U.S. and select European markets. As clinical evidence and indications expanded, sales accelerated, especially in territories with favorable reimbursement.

Global revenue estimates for 2022 surpass US$200 million, with projections indicating compound annual growth rates (CAGR) exceeding 15% over the next five years, assuming continued expansion of indications and market penetration (source: BioPharm Insight).

2. Market Penetration and Growth Drivers

Key drivers include increased testing for NTRK fusions, wider adoption in second-line settings, and potential approval for pediatric indications. The increasing preference for targeted therapies amidst a shift away from chemotherapies supports sustained demand.

Market penetration is also influenced by patient eligibility criteria; fusion-positive tumors represent a small subset (~1%) of total cancers, limiting total addressable volume but offering high-value, niche markets.

3. Investment and R&D Pipeline

The company's R&D pipeline, focused on optimizing kinase inhibitors and expanding indications (e.g., salivary gland tumors, colorectal cancers), offers upside potential. Investment in companion diagnostics and combination therapies could enhance therapeutic positioning, impacting financial trajectories positively.

4. Risks and Challenges

Market growth faces obstacles including aminoid competition, potential emergence of resistance mutations, and regulatory delays. Pricing pressures and evolving reimbursement policies could temper revenue forecasts.

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Regulatory and Market Evolution Outlook

The future of entrectinib hinges on regulatory decisions, clinical trial outcomes, and strategic market positioning. Ongoing phase IV studies aim to establish long-term safety and efficacy, critical for sustained reimbursement policies. Expansion into new indications and combination regimens could significantly influence its financial trajectory.

The evolving oncology landscape, marked by rapid innovation and personalized medicine, indicates a promising yet competitive horizon. The drug’s capacity to maintain or extend its market share depends on continued clinical validation and strategic alignment with payer and healthcare provider needs.

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Key Market Trends

• Increasing diagnostics integration: Comprehensive gene sequencing will boost patient identification with NTRK and ROS1 fusions.

• Global approval expansion: Emerging markets present significant growth opportunities, contingent on pricing strategies and local healthcare infrastructure.

• Technological innovation: Biosimilar and generic entry risk remains minimal due to the specificity and patent protections surrounding entrectinib, securing market exclusivity over the coming years.

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Conclusion and Future Outlook

Entrectinib's market dynamics are driven by its targeted mechanism, expanding indications, and competitive nuances. While it benefits from regulatory support and clinical advantages, its financial trajectory remains susceptible to pricing, reimbursement policies, and emerging competition. Strategic investments in diagnostics, combination therapies, and pipeline development can sustain growth, positioning entrectinib as a pivotal asset within targeted oncology treatments.

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Key Takeaways

• Targeted niche: Entrectinib excels where precision medicine addresses unmet oncological needs, with high efficacy in NTRK fusion-positive tumors.
• Market growth is steady but constrained by the rarity of indications and competition from similar agents like larotrectinib.
• Reimbursement policies and diagnostics advancements are crucial determinants of future revenue growth.
• Pipeline expansion and real-world evidence will influence long-term market share and pricing power.
• Global market penetration remains vital; emerging markets offer significant growth opportunities, contingent on strategic access initiatives.

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FAQs

1. What are the primary indications for entrectinib?
Entrectinib is primarily approved for NTRK fusion-positive solid tumors and ROS1-positive non-small cell lung cancer (NSCLC). Its indication scope continues to expand via ongoing clinical trials.

2. How does entrectinib compare to other NTRK inhibitors like larotrectinib?
Entrectinib offers CNS activity, providing an advantage in managing brain metastases, whereas larotrectinib is characterized by a favorable safety profile. Market preferences depend on tumor location and systemic considerations.

3. What factors influence entrectinib’s pricing and reimbursement?
Its high specificity and rarity of target mutations justify premium pricing. Reimbursement depends on demonstrated clinical benefit, cost-effectiveness, and local healthcare policies.

4. What regulatory challenges could impact its market growth?
Potential delays in approval for new indications, evolving safety standards, and regional regulatory disparities could hinder rapid market expansion.

5. What emerging trends could affect the future demand for entrectinib?
Advances in molecular diagnostics, combination therapy strategies, and broader genetic testing will influence patient identification and treatment algorithms, impacting demand.

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References

1. FDA Drug Approval Archive (2019)
2. BioPharm Insight Reports (2022). Global oncology drug market analysis.
3. NCCN Clinical Practice Guidelines in Oncology (2023): NTRK fusion-positive and ROS1-positive NSCLC.
4. Company Annual Reports and Press Releases (2022-2023).