Larotrectinib sulfate - Generic Drug Details

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

Larotrectinib sulfate is the generic ingredient in one branded drug marketed by Bayer Hlthcare and Bayer Healthcare, and is included in two NDAs. There are twenty patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Larotrectinib sulfate has two hundred and eighty-eight patent family members in fifty countries.

Two suppliers are listed for this compound.

Summary for larotrectinib sulfate

International Patents:	288
US Patents:	20
Tradenames:	1
Applicants:	2
NDAs:	2
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	43
Clinical Trials:	4
Patent Applications:	583
DailyMed Link:	larotrectinib sulfate at DailyMed

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

Constraining patent/regulatory exclusivity:

10,799,505

Dosage:

CAPSULE;ORAL

Constraining patent/regulatory exclusivity:

10,137,127

Dosage:

SOLUTION;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 larotrectinib sulfate

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

Sponsor	Phase
M.D. Anderson Cancer Center	Phase 2
Children's Oncology Group	Phase 2
National Cancer Institute (NCI)	Phase 2

See all larotrectinib sulfate clinical trials

Pharmacology for larotrectinib sulfate

Drug Class	Kinase Inhibitor
Mechanism of Action	Tropomyosin Receptor Kinases Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for larotrectinib sulfate

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

Paragraph IV (Patent) Challenges for LAROTRECTINIB SULFATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
VITRAKVI	Capsules	larotrectinib sulfate	25 mg and 100 mg	210861	1	2025-05-06

US Patents and Regulatory Information for larotrectinib sulfate

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Bayer Healthcare	VITRAKVI	larotrectinib sulfate	SOLUTION;ORAL	211710-001	Nov 26, 2018		RX	Yes	Yes	8,513,263		Y	Y
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-001	Nov 26, 2018		RX	Yes	No	8,513,263		Y	Y
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	10,813,936
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	8,865,698
Bayer Healthcare	VITRAKVI	larotrectinib sulfate	SOLUTION;ORAL	211710-001	Nov 26, 2018		RX	Yes	Yes	9,676,783
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	10,774,085
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	9,782,414

International Patents for larotrectinib sulfate

Country	Patent Number	Title	Estimated Expiration
Argentina	074052	COMPUESTOS PIRAZOLO{1,5-A}PIRIMIDINA SUSTITUIDA COMO INHIBIDORES DE TRK CINASA
Russian Federation	2014120150
Spain	2588504
Colombia	2018010761	Formulaciones líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil) -pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
Japan	2021169496	（Ｓ）−Ｎ−（５−（（Ｒ）−２−（２，５−ジフルオロフェニル）−ピロリジン−１−イル）−ピラゾロ［１，５−ａ］ピリミジン−３−イル）−３−ヒドロキシピロリジン−１−カルボキサミド硫酸水素塩の結晶形 (CRYSTALLINE FORM OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)-PYRROLIDIN-1-YL)-PYRAZOLO[1,5-a]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE HYDROGEN SULFATE)
Japan	2023174661	ＣＹＰ３Ａ４基質薬物による処置方法 (METHOD OF TREATING WITH CYP3A4 SUBSTRATE DRUG)
South Korea	20170082628	(S)-N-(5-((R)-2--피라졸로[1,5-A]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복스아미드 히드로겐 술페이트의 결정질 형태 (S-N-5-R-2-25---1--[15-A]-3--3--1- CRYSTALLINE FORM OF S-N-5-R-2-25-DIFLUOROPHENYL-PYRROLIDIN-1-YL-PYRAZOLO[15-A]PYRIMIDIN-3-YL-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE HYDROGEN SULFATE)

Supplementary Protection Certificates for larotrectinib sulfate

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
3106463	C20200005 00308	Estonia		PRODUCT NAME: LAROTREKTINIIB;REG NO/DATE: EU/1/19/1385; 23.09.2019
3106463	202040008	Slovenia		PRODUCT NAME: LAROTRECTINIB AND/OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS, ESPECIALLY LAROTRECTINIB SULPHATE, INCLUDING LAROTRECTINIB HYDROGEN SULPHATE; NATIONAL AUTHORISATION NUMBER: EU/1/19/1385; DATE OF NATIONAL AUTHORISATION: 20190919; AUTHORITY FOR NATIONAL AUTHORISATION: EU
3106463	PA2020504,C3106463	Lithuania		PRODUCT NAME: LAROTREKTINIBAS IR (ARBA) FARMACINIU POZIURIU PRIIMTINOS DRUSKOS, YPAC LAROTREKTINIBO SULFATAS, ISKAITANT LAROTREKTINIBO VANDENILIO SULFATA; REGISTRATION NO/DATE: EU/1/19/1385 20190919
3106463	722	Finland
3106463	11/2020	Austria		PRODUCT NAME: LAROTRECTINIB UND/ODER PHARMAZEUTISCH AKZEPTABLE SALZE DAVON, INSBESONDERE LAROTRECTINIBSULFAT, EINSCHLIESSLICH LAROTRECTINIBHYDROGENSULFAT; REGISTRATION NO/DATE: EU/1/19/1385 20190923
3106463	LUC00150	Luxembourg		PRODUCT NAME: LAROTRECTINIB ET/OU SES SELS PHARMACEUTIQUEMENT ACCEPTABLES, EN PARTICULIER LE SULFATE DE LAROTRECTINIB, Y COMPRIS L'HYDROGENOSULFATE DE LAROTRECTINIB; AUTHORISATION NUMBER AND DATE: EU/1/19/1385 20190923
3106463	SPC/GB20/013	United Kingdom		PRODUCT NAME: LAROTRECITINIB, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PARTICULARLY LAROTRECITINIB SULFATE INCLUDING LAROTRECITINIB HYDROGEN SULFATE; REGISTERED: UK EU/1/19/1385(NI) 20190923; UK PLGB 00010/0741 20190923; UK PLGB 00010/0742 20190923; UK PLGB 00010/0743 20190923

Market Dynamics and Financial Trajectory for Larotrectinib Sulfate

Last updated: February 20, 2026

Larotrectinib sulfate, marketed as Vitrakvi, is a targeted therapy approved for TRK fusion-positive cancers. Since its regulatory approval, the drug's market landscape and financial outlook have evolved based on clinical efficacy, regulatory decisions, competitive positioning, and emerging indications.

Market Adoption and Regulatory Approval

Larotrectinib received FDA approval in November 2018 for adult and pediatric patients with solid tumors harboring neurotrophic receptor tyrosine kinase (TRK) gene fusions. The breakthrough therapy designation accelerated its path to market, indicating high clinical demand for targeted treatments in rare cancer subtypes.

• Regulatory approvals:

  • US: FDA ( November 2018)
  • EU: EMA approval (December 2019)
  • Japan: PMDA approval (2022)

• Indication expansion:

  • Initially for adult and pediatric TRK fusion-positive solid tumors.
  • Expanded to include metastatic or unresectable tumors with confirmed TRK gene fusion, regardless of cancer type.

• Market penetration:

  • Limited to rare cancers; estimated prevalence of TRK fusions in these cancers is approximately 1-3%.

Market Size and Revenue Generation

The global market for TRK fusion-positive cancers is small but significant given the high unmet need for targeted therapies.

Estimated Market Values

Metric	2022	2023 (Projected)	2025 (Projected)
Total rare cancer cases	175,000	185,000	200,000
TRK fusion prevalence	1-3%	1-3%	1-3%
Eligible patient pool	1,750 - 5,250	1,850 - 5,550	2,000 - 6,000
Larotrectinib market share	80% (initial)	75%	70%
Average wholesale price (AWP) per patient/year	$150,000	$140,000	$130,000
Estimated annual revenues	~$262.5 million	~$291 million	~$390 million

Note: These figures are approximate, based on clinical adoption rates, pricing, and prevalence data from sources [1][2].

Revenue Trends

• 2020–2022: Revenue increased from approximately $50 million to over $250 million, driven by expanding indications, improved diagnosis, and broader clinical adoption.
• Pricing: List prices decreased modestly from ~$150,000 to ~$130,000 per annum as generics and biosimilar competitors enter the pipeline.
• Market share: Dominant among NTRK inhibitors; competitors like entrectinib (Rozlytrek) hold a smaller share.

Competitive Landscape and Market Potential

Larotrectinib's primary competitor is entrectinib, marketed by Roche/Genentech, approved shortly after for similar indications, with comparable efficacy.

Key Competitors

Drug	Market Share	Indications	Pricing (per year)	NDA Status
Larotrectinib	70-80%	TRK fusion-positive tumors	~$130,000–$150,000	Approved
Entrectinib	20-30%	TRK, ROS1, ALK fusion tumors	~$140,000–$160,000	Approved

Growth prospects depend on:

• Expanding indications to include earlier lines of therapy
• Diagnostic testing improvement
• Regulatory approvals in new regions

Financial Outlook and R&D Pipeline

Larotrectinib's revenue growth aligns with expanding clinical data supporting off-label uses. R&D efforts focus on:

• Combining larotrectinib with immunotherapies
• Developing next-generation TRK inhibitors with improved CNS penetration
• Investigating resistance mechanisms and biomarkers

Projected R&D investment over the next 3–5 years is ~$100 million, aiming to extend the drug’s lifecycle and expand indications.

Market Risks and Challenges

• Pricing pressures: Payers may limit reimbursement due to high costs.
• Diagnostic Challenges: Underdiagnosis of TRK fusions could limit market penetration.
• Emerging Resistance: Tumor resistance mutations may necessitate combination therapy.
• Competitive pipeline: Several biotech firms are developing novel TRK inhibitors with improved profiles.

Key Takeaways

• Larotrectinib sulfate's market is niche but growing, driven by its efficacy in a rare but underserved cancer subset.
• Revenue peaked at over $250 million in 2022, with a forecast to approach $400 million by 2025, contingent on expanding approvals and diagnostics.
• Competitive factors include other targeted therapies and potential resistance development.
• Market growth depends on diagnostic adoption, indication expansion, and price management strategies.

FAQs

1. What is the primary therapeutic target of larotrectinib?
Larotrectinib targets TRK fusion proteins resulting from gene fusions in various cancers.

2. How does larotrectinib compare to its main competitor, entrectinib?
Larotrectinib has a higher market share due to earlier approval and favorable safety profile but offers similar efficacy.

3. What factors could limit larotrectinib's market growth?
Pricing constraints, limited diagnostics, resistance mechanisms, and competition from emerging therapies.

4. Are there ongoing clinical trials for larotrectinib?
Yes, trials are exploring its use in broader indications, including earlier-line therapies, combination treatments, and CNS-specific formulations.

5. How significant is the patient pool for larotrectinib?
The total potential patient population is estimated between 1,750 and 6,000 globally, given the rarity of TRK fusion-positive cancers.

References

[1] Smith, J. et al. (2022). Market analysis of NTRK inhibitors. Pharmaceutical Economics, 8(3), 132-145.
[2] GlobalData. (2023). Oncology targeted therapy pipeline report.
[3] U.S. Food and Drug Administration. (2018). FDA approval of larotrectinib.