Larotrectinib sulfate - Generic Drug Details

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

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-one patent family members in fifty countries.

Two suppliers are listed for this compound.

Summary for larotrectinib sulfate

International Patents:	281
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:	126
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

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 Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-001	Nov 26, 2018		RX	Yes	No	10,774,085
Bayer Healthcare	VITRAKVI	larotrectinib sulfate	SOLUTION;ORAL	211710-001	Nov 26, 2018		RX	Yes	Yes	8,865,698
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	8,513,263		Y	Y
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	11,974,998
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	10,799,505		Y	Y
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	9,676,783
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	11,337,967

International Patents for larotrectinib sulfate

Country	Patent Number	Title	Estimated Expiration
Singapore	196855	SUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS
Australia	2022228153	METHODS OF TREATMENT
Japan	2019510827	小児癌の処置方法
Brazil	PI0919873	composto de pirazol[1,5-a]pirimidina substituídos como inibidores da quinase trk
Ukraine	106054	ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ КАК ИНГИБИТОРЫ ТРК-КИНАЗЫ;ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]ПІРИМІДИНОВІ СПОЛУКИ ЯК ІНГІБІТОРИ TРK-КІНАЗИ (Normal;heading 1;heading 2;heading 3;SUBSTITUTED IMIDAZO[1,5-a]PYRIDAZINE COMPOUNDS AS TRK KINASE INHIBITORS)
Lithuania	3699181
Hungary	S2000006

Supplementary Protection Certificates for larotrectinib sulfate

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
3106463	C202030011	Spain		PRODUCT NAME: LAROTRECTINIB Y/O UNA SAL FARMACEUTICAMENTE ACEPTABLE DEL MISMO, PARTICULARMENTE SULFATO DE LAROTRECTINIB QUE INCLUYE HIDROGENOSULFATO DE LAROTRECTINIB; NATIONAL AUTHORISATION NUMBER: EU/1/19/1385; DATE OF AUTHORISATION: 20190919; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/19/1385; DATE OF FIRST AUTHORISATION IN EEA: 20190919
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	C20200005 00308	Estonia		PRODUCT NAME: LAROTREKTINIIB;REG NO/DATE: EU/1/19/1385; 23.09.2019
3106463	301033	Netherlands		PRODUCT NAME: LAROTRECTINIB, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVAARDBAAR ZOUT, IN HET BIJZONDER LAROTRECTINIBSULFAAT, MET INBEGRIP VAN LAROTRECTINIBSULFAAT MONOHYDRAAT; REGISTRATION NO/DATE: EU/1/19/1385 20190923
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	CA 2020 00013	Denmark		PRODUCT NAME: LAROTRECTINIB OG/ELLER ET FARMACEUTISK ACCEPTABELT SALT DERAF, SAERLIGT LAROTRECTINIBSULFAT, INKLUSIV LAROTRECTINIBHYDROGENSULFAT; REG. NO/DATE: EU/1/19/1385 20190923
3106463	2090009-8	Sweden		PRODUCT NAME: LAROTRECTINIB,OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, PARTICULARLY LAROTRECTINIB SULFATE INCLUDING LAROTRECTINIB HYDROGEN SULFATE; REG. NO/DATE: EU/1/19/1385 20190923

Market Dynamics and Financial Trajectory for Larotrectinib Sulfate

Introduction to Larotrectinib Sulfate

Larotrectinib sulfate, marketed under the brand name Vitrakvi, is a tyrosine kinase inhibitor specifically designed to target solid tumors with neurotrophic receptor tyrosine kinase (NTRK) gene fusions. This drug has been a significant advancement in the treatment of certain types of cancer, particularly those that are metastatic or cannot be treated with surgery.

Approval and Regulatory Status

Larotrectinib sulfate was granted accelerated approval by the US FDA in November 2018 for the treatment of adult and pediatric patients with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation[1][2][4].

Market Size and Growth

The global TRK inhibitor market, which includes larotrectinib sulfate, is projected to surpass $2 billion by 2026. This growth is driven by several factors:

• Increasing Prevalence of Cancer: The rising incidence of cancer globally is a significant driver for the demand of targeted therapies like TRK inhibitors.
• Growing Research and Development: Continuous research and development activities are leading to the discovery of new TRK inhibitors and improving existing ones.
• Awareness and Government Initiatives: Increased awareness about the availability of these drugs and government initiatives to support cancer research are also boosting market growth[3].

Approved Drugs in the Market

Currently, there are two FDA-approved TRK inhibitors: larotrectinib (Vitrakvi) and entrectinib (Rozlytrek). These drugs have shown significant efficacy in treating NTRK-positive solid tumors, including those with central nervous system (CNS) metastases[3].

Clinical Efficacy and Impact

Larotrectinib has demonstrated long-term efficacy in patients with NTRK-positive solid tumors. Clinical trials have shown that it increases overall survival and progression-free survival rates compared to conventional cancer therapies. This efficacy has been a key factor in its market success[3].

Patent, Price, and Sales Insight

The patent, price, and sales data for larotrectinib sulfate are closely monitored as they impact the market dynamics. The drug's sales have been robust, driven by its unique mechanism of action and the lack of alternative treatments for NTRK-positive tumors. The pricing strategy, while high due to the specialized nature of the drug, is supported by its clinical benefits and the limited competition in this niche market[3].

Market Segmentation

The TRK inhibitor market is segmented by indication, including lung, colorectal, breast, glioblastoma, and papillary thyroid cancer. Larotrectinib sulfate's versatility in treating various types of solid tumors has contributed to its market penetration across these segments[3].

Challenges and Future Outlook

Despite the initial success, there are challenges associated with the use of larotrectinib sulfate, such as acquired resistance mutations. For instance, mutations like G595R in the TRKA kinase domain and G623R, G696A, and F617L in the TRKC kinase domain have been identified as clinically relevant resistance mutations[1].

To overcome these challenges, ongoing research is focused on developing next-generation TRK inhibitors that can address these resistance mechanisms. For example, new inhibitors like JND4135 are being studied for their ability to overcome certain resistance mutations[5].

Financial Trajectory

The financial trajectory of larotrectinib sulfate is positive, driven by its strong clinical performance and market demand. Here are some key financial highlights:

• Sales Growth: The drug has seen significant sales growth since its approval, contributing to the overall revenue of its manufacturer, Loxo Oncology (now part of Eli Lilly).
• Market Share: As one of the two approved TRK inhibitors, larotrectinib sulfate holds a substantial market share in the niche market of NTRK-positive solid tumors.
• Future Projections: With the market expected to surpass $2 billion by 2026, larotrectinib sulfate is poised to continue its financial success, assuming continued clinical benefit and regulatory support[3].

Key Takeaways

• Market Growth: The global TRK inhibitor market is expected to surpass $2 billion by 2026.
• Clinical Efficacy: Larotrectinib sulfate has shown long-term efficacy in treating NTRK-positive solid tumors.
• Challenges: Acquired resistance mutations are a challenge, but ongoing research aims to address these.
• Financial Trajectory: The drug has seen significant sales growth and is expected to continue its financial success.

FAQs

What is larotrectinib sulfate used for?

Larotrectinib sulfate is used to treat adult and pediatric patients with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation. It is particularly indicated for metastatic tumors or those that cannot be removed by surgery and have no satisfactory alternative treatments[1][2].

How does larotrectinib sulfate work?

Larotrectinib sulfate works by inhibiting the tropomyosin receptor kinase (Trk) proteins, which are activated by neurotrophins. By preventing the interaction between neurotrophins and Trk proteins, it induces cellular apoptosis and inhibits tumor cell growth[1].

What are the common side effects of larotrectinib sulfate?

While specific side effects are detailed in the FDA label and patient information sheets, common side effects can include fatigue, dizziness, and gastrointestinal issues. It is important to consult the FDA label or a healthcare provider for a comprehensive list of potential side effects[2].

Is larotrectinib sulfate approved for use in children?

Yes, larotrectinib sulfate is approved for use in pediatric patients with solid tumors that have an NTRK gene fusion. The dosing regimen for pediatric patients may vary based on body surface area (BSA)[1][4].

What is the current market size of the TRK inhibitor market?

The global TRK inhibitor market is projected to surpass $2 billion by 2026, driven by increasing prevalence of cancer, growing research and development activities, and other factors[3].

Are there other TRK inhibitors available in the market?

Yes, apart from larotrectinib (Vitrakvi), another FDA-approved TRK inhibitor is entrectinib (Rozlytrek). Both drugs are used to treat NTRK-positive solid tumors[3].

Sources

1. DrugBank: Larotrectinib: Uses, Interactions, Mechanism of Action.
2. National Cancer Institute: Larotrectinib Sulfate.
3. Biospace: TRK Inhibitors Market Size, Drug Sales & Clinical Trials Insight 2026.
4. FDA: 210861Orig1s000 211710Orig1s000 - accessdata.fda.gov.
5. PMC: JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Resistance Mutations.