ENTRECTINIB - Generic Drug Details

What are the generic drug sources for entrectinib and what is the scope of freedom to operate?

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 thirty patent family members in thirty-one countries.

One supplier is listed for this compound.

Summary for ENTRECTINIB

International Patents:	130
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
St. Jude Children's Research Hospital	PHASE2
Hoffmann-La Roche	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	PELLETS;ORAL	218550-001	Oct 20, 2023		RX	Yes	Yes
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-001	Aug 15, 2019		RX	Yes	No	9,085,565		Y	Y
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes	9,085,565		Y	Y
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes	10,561,651

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
New Zealand	703124	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
South Korea	102718538
Israel	260297	תהליך להכנת n-[5-(5,3-דיפלואורו-בנזיל)-h1-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)
Brazil	PI0814628	derivados ativos de indazol substituídos como inibidores da quinase
Mexico	2016010519	MOLECULAS PARA ADMINISTRACION A CELULAS CANCEROSAS MUTANTES ROS1. (COMPOUNDS FOR TREATING PATIENTS WITH ROS1 MUTANT CANCER CELLS.)

Supplementary Protection Certificates for ENTRECTINIB

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2176231	C 2020 048	Romania		PRODUCT NAME: ENTRECTINIB SAU IZOMERI, TAUTOMERI SAU SARURILE ACCEPTABILE FARMACEUTIC ALE ACESTORA; NATIONAL AUTHORISATION NUMBER: EU/1/20/1460; DATE OF NATIONAL AUTHORISATION: 20200731; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/20/1460; DATE OF FIRST AUTHORISATION IN EEA: 20200731
2176231	20C1064	France		PRODUCT NAME: ENTRECTINIB OU SES TAUTOMERES OU SELS PHARMACEUTIQUEMENT ACCEPTABLES; REGISTRATION NO/DATE: EU/1/20/1460 20200803
2176231	C02176231/01	Switzerland		PRODUCT NAME: ENTRECTINIB; REGISTRATION NO/DATE: SWISSMEDIC-ZULASSUNG 67280 05.11.2020
3107541	301111	Netherlands		PRODUCT NAME: ENTRECTINIB OF EEN FARMACEUTISCH AANVAARDBAAR ZOUT DAARVAN; REGISTRATION NO/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

Market Dynamics and Financial Trajectory for Entrectinib

Last updated: February 20, 2026

What is the Current Market Position of Entrectinib?

Entrectinib (marketed as Rozlytrek by Genentech/Roche) is a targeted therapy approved for specific cancers exhibiting NTRK gene fusions and ROS1-positive non-small cell lung cancer (NSCLC). It has received approval in multiple regions, including the US, EU, and Japan. As of 2023, global sales for Rozlytrek have surpassed $250 million, with rapid growth observed since initial launch in 2019.

How Does the Market Size and Growth Potential Look?

The global market for NTRK fusion-positive cancers is projected to grow at a compound annual growth rate (CAGR) of 20-25% through 2030. In 2022, diagnosed cases worldwide approached 4,000, with an estimated 60-70% being eligible for targeted therapy like entrectinib.

For ROS1-positive NSCLC, the market is more established. The ROS1 fusion occurs in approximately 1-2% of NSCLC cases, with an estimated 250,000 new NSCLC diagnoses annually worldwide. Entrectinib’s market share in this segment has been around 15-20%.

What is the Competitive Landscape?

• Larotrectinib (Vitrakvi, Bayer/Loxo Oncology): Approved for NTRK fusion-positive cancers, with global sales reaching $270 million in 2022.
• Entrectinib: Offers broader tissue penetration due to its CNS activity, giving it an edge in metastasis cases.
• Other emerging therapies: Several pipeline candidates are targeting NTRK and ROS1 fusions but lack global approval.

What Factors Drive Market Dynamics?

1. Regulatory Approvals and Indications

Initial approvals for adult and pediatric NTRK fusion cancers expanded to include first-line settings in some regions. Recent approvals of entrectinib in Japan and the US expand its market reach.

2. Clinical Data and Efficacy

Entrectinib's ability to penetrate the central nervous system (CNS) and treat brain metastases supports its preferential use in advanced cases. Its Phase II STARTRK-2 trial demonstrated an overall response rate (ORR) of 68% in NTRK fusion cancers.

3. Pricing and Reimbursement

The drug's list price ranged from $16,000 to $20,000 per month as of 2022, with reimbursement largely aligned in developed markets. Reimbursement approval processes influence sales volumes.

4. Competitive Dynamics

Larotrectinib's higher specificity for NTRK fusions and similar efficacy compete directly with entrectinib. However, entrectinib's broader targeted scope and CNS activity provide differentiation.

5. Pipeline and Next-Generation Alternatives

Pipeline candidates aim to address resistance mutations and improve CNS efficacy. The emergence of such therapies could pressure entrectinib’s market share in the future.

What Are the Revenue Projections and Financial Trajectory?

Short-term (2023-2025)

• Estimated global sales: $350–$500 million.
• Growth driven by expanding indications, increased diagnosis rates, and new regional approvals.
• Manufacturing and R&D costs remain high, with gross margins around 75%.

Medium-term (2026-2030)

• Potential to reach $1 billion in annual revenue if approved for first-line treatment in broader indications and if pricing remains stable.
• Market expansion in China and other Asia-Pacific countries could contribute 20% of total sales.
• Competition from pipeline candidates and biosimilars could suppress growth post-2030.

Key Drivers of Financial Trajectory

• Expanded indications in first-line settings.
• Price adjustments influenced by payer negotiations.
• Increased adoption due to improved CNS activity.
• Patent exclusivity until around 2030, barring generics or biosimilar entry.

How Do Regulatory and Market Trends Influence Revenue?

• Approvals in emerging markets could double access.
• Adoption in pediatric cases adds growth opportunities.
• Reimbursement policies vary widely; US and EU markets show favorable dynamics.
• Potential for combination therapies might increase overall treatment market size.

What Risks Could Affect Market and Financial Outlook?

• Resistance mutations leading to acquired resistance.
• Competitive therapies gaining approval and market share.
• Regulatory shifts around pricing and reimbursement.
• Delays in obtaining or expanding indications.

Summary of Key Financial Metrics

Metric	Value (2022)	Estimated 2025	Notes
Global sales	$250 million	$350–$500 million	Growth driven by expanded indications
Market share in NSCLC ROS1	15–20%	Stable or slightly increasing	Competition from other TKIs
Pricing per month	$16,000–$20,000	Expected stable	Payer negotiations affect discounts
Patent expiry	~2030	N/A	Patent cliff approaching; biosimilars may emerge

Key Takeaways

• Entrectinib has established a role in NTRK and ROS1-positive cancers, with sales trending upward.
• Broader indications, especially first-line use and pediatric approval, can significantly increase revenue.
• CNS efficacy provides a competitive advantage in metastatic and brain-involved cancers.
• Market growth depends heavily on regulatory approvals, pricing strategies, and competition.
• Resistance and pipeline developments pose long-term risks but also opportunities for expansion.

FAQs

1. What are the primary approved indications for entrectinib?
It is approved for NTRK fusion-positive cancers and ROS1-positive NSCLC[1].

2. How does entrectinib compare to larotrectinib?
Entrectinib has CNS activity, giving it advantages in brain metastases, while larotrectinib has higher specificity for NTRK fusions[2].

3. What is the outlook for sales growth through 2030?
Potential to reach or exceed $1 billion annually with broader indications and market penetration[3].

4. Which regions are most critical for market expansion?
The US, EU, Japan, and emerging markets like China are key for growth, given existing regulatory approvals and diagnosis rates[4].

5. What are the main factors threatening entrectinib’s market position?
Emerging pipeline drugs, resistance mutations, biosimilar competition, and regulatory or reimbursement challenges.

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References

[1] Food and Drug Administration. (2019). Rozlytrek (entrectinib) prescribing information.

[2] European Medicines Agency. (2021). Rozlytrek summary of product characteristics.

[3] Market Research Future. (2022). Global oncology targeted therapy market report.

[4] IQVIA. (2023). Global oncology market trends report.