Trametinib dimethyl sulfoxide - Generic Drug Details

What are the generic sources for trametinib dimethyl sulfoxide and what is the scope of freedom to operate?

Trametinib dimethyl sulfoxide is the generic ingredient in two branded drugs marketed by Novartis and Novugen, and is included in three NDAs. There are nine patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Trametinib dimethyl sulfoxide has one hundred and sixty-nine patent family members in forty-six countries.

One supplier is listed for this compound.

Summary for trametinib dimethyl sulfoxide

International Patents:	169
US Patents:	9
Tradenames:	2
Applicants:	2
NDAs:	3
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	55
Clinical Trials:	15
Patent Applications:	264
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for trametinib dimethyl sulfoxide
DailyMed Link:	trametinib dimethyl sulfoxide at DailyMed

Recent Clinical Trials for trametinib dimethyl sulfoxide

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

Sponsor	Phase
ECOG-ACRIN Cancer Research Group	Phase 2
Pediatric Brain Tumor Consortium	Phase 1/Phase 2
National Cancer Institute (NCI)	Phase 3

See all trametinib dimethyl sulfoxide clinical trials

Pharmacology for trametinib dimethyl sulfoxide

Drug Class	Kinase Inhibitor
Mechanism of Action	Protein Kinase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for trametinib dimethyl sulfoxide

G04BX	Other urologicals
G04B	UROLOGICALS
G04	UROLOGICALS
G	Genito-urinary system and sex hormones

L01EE	Mitogen-activated protein kinase (MEK) inhibitors
L01E	PROTEIN KINASE INHIBITORS
L01	ANTINEOPLASTIC AGENTS
L	Antineoplastic and immunomodulating agents

M02AX	Other topical products for joint and muscular pain
M02A	TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
M02	TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
M	Musculo-skeletal system

Paragraph IV (Patent) Challenges for TRAMETINIB DIMETHYL SULFOXIDE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
MEKINIST	Tablets	trametinib dimethyl sulfoxide	0.5 mg and 2 mg	204114	1	2023-09-28

US Patents and Regulatory Information for trametinib dimethyl sulfoxide

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-001	May 29, 2013		RX	Yes	No
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-001	May 29, 2013		RX	Yes	No
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-001	May 29, 2013		RX	Yes	No					Y
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-001	May 29, 2013		RX	Yes	No

International Patents for trametinib dimethyl sulfoxide

Country	Patent Number	Title	Estimated Expiration
Dominican Republic	P2013000138	NUEVA COMPOSICIÓN FARMACÉUTICA
Israel	226855	תכשיר רוקחי (Pharmaceutical composition)
India	449KON2015
Portugal	1761528

Supplementary Protection Certificates for trametinib dimethyl sulfoxide

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1761528	CR 2014 00055	Denmark		PRODUCT NAME: TRAMETINIB, EVENTUELT I FORM AF ET FARMACEUTISK ACCEPTABELT SALT, HYDRAT ELLER SOLVAT DERAF, HERUNDER TRAMETINIBDIMETHYLSULFOXID; REG. NO/DATE: EU/1/14/931/01-06 20140702
1761528	300701	Netherlands		PRODUCT NAME: TRAMETINIB, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVAARDBAAR ZOUT, HYDRAAT OF SOLVAAT DAARVAN; REGISTRATION NO/DATE: EU/1/14/931/01-06 20140702
1761528	C300701	Netherlands		PRODUCT NAME: TRAMETINIB, DESGEWENST IN DE VORM VAN EEN FRAMACEUTISCH AANVAARDBAAR ZOUT, HYDRAAT OF SOLVAAT DAARVAN; REGISTRATION NO/DATE: EU/1/14/931/01-06 20140702
1761528	C 2014 044	Romania		PRODUCT NAME: TRAMETINIB, OPTIONAL SUB FORMA UNEI SARI, HIDRAT SAU SOLVAT AL ACESTUIA, ACCEPTABILE FARMACEUTIC; NATIONAL AUTHORISATION NUMBER: EU/1/14/931; DATE OF NATIONAL AUTHORISATION: 20140630; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/14/931; DATE OF FIRST AUTHORISATION IN EEA: 20140630

Market Dynamics and Financial Trajectory for Trametinib Dimethyl Sulfoxide (Mekinist)

Introduction

Trametinib, marketed as Mekinist, is a potent inhibitor of mitogen-activated extracellular signal-regulated kinase 1 and 2 (MEK1 and MEK2), developed by GlaxoSmithKline (GSK). It is primarily used in the treatment of patients with unresectable or metastatic melanoma with BRAF V600 mutations. Here, we delve into the market dynamics and financial trajectory of trametinib.

Mechanism of Action and Therapeutic Indication

Trametinib works by inhibiting the MEK1 and MEK2 kinases, which are part of the BRAF pathway. BRAF V600 mutations lead to the constitutive activation of this pathway, resulting in uncontrolled cellular proliferation in tumors. By inhibiting MEK, trametinib reduces this proliferation, making it an effective treatment for melanoma patients with these specific mutations[4].

Clinical Efficacy and Approval

The clinical efficacy of trametinib was established through several trials, notably the MEK114267 trial, which showed a statistically significant improvement in progression-free survival (PFS) compared to chemotherapy. Patients treated with trametinib had a median PFS of 4.8 months, significantly better than the 1.5 months observed in the chemotherapy arm[5].

Trametinib received FDA approval in 2013 for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations. This approval was based on the clinical trials that demonstrated its efficacy and safety profile[2].

Market Positioning

Trametinib is often used in combination with other drugs, such as dabrafenib, another BRAF inhibitor. This combination therapy has shown enhanced efficacy in treating melanoma patients. The combination of 150 mg dabrafenib plus 2 mg trametinib has been particularly effective, with a higher overall response rate (ORR) compared to monotherapy[5].

Safety Profile and Adverse Events

While trametinib has shown significant clinical benefits, it is associated with several adverse events. Common side effects include rash, diarrhea, fatigue, peripheral edema, nausea, and dermatitis acneiform. More serious safety concerns include cardiac issues such as cardiomyopathy and ocular adverse events like blurry vision and retinal vein occlusion[4].

Market Dynamics

The market for trametinib is influenced by several factors:

Competitive Landscape

The market for MEK inhibitors is competitive, with other drugs like cobimetinib and binimetinib also available. However, trametinib's approval and established efficacy in combination with dabrafenib have secured its position as a leading treatment option for BRAF-mutant melanoma[4].

Patient Population

The patient population for trametinib is specific, targeting those with unresectable or metastatic melanoma and BRAF V600 mutations. This specificity, while limiting the market size, ensures a dedicated patient base for the drug.

Regulatory Environment

Regulatory approvals and compliance play a crucial role in the market dynamics of trametinib. The drug has received approvals in multiple territories, including the U.S., EU, and Australia, which has expanded its market reach[5].

Financial Trajectory

Revenue Growth

Since its approval, trametinib has contributed significantly to GSK's revenue. The combination therapy with dabrafenib has been a key driver of sales, given its enhanced efficacy and broader patient base.

Market Size and Opportunity

The market opportunity for trametinib is substantial, particularly in the context of combination therapies. The estimated market size for targeted therapies in melanoma is growing, driven by the increasing incidence of melanoma and the need for effective treatments.

Cost and Pricing

The cost of trametinib is a significant factor in its market dynamics. Given its efficacy and the lack of alternative treatments for BRAF-mutant melanoma, the drug is priced accordingly. However, this can be a barrier to access in some markets, affecting its financial trajectory.

Research and Development

Continuous research and development are crucial for maintaining and expanding the market for trametinib. GSK and other pharmaceutical companies are investing in clinical trials to explore new indications and combination therapies, which can further enhance the drug's market position.

Key Takeaways

• Trametinib is a highly effective MEK inhibitor for treating BRAF-mutant melanoma.
• Its approval and established efficacy in combination with dabrafenib have secured its market position.
• The drug is associated with specific adverse events, which must be managed.
• The market is influenced by regulatory approvals, patient population, and competitive landscape.
• The financial trajectory is positive, driven by revenue growth and expanding market opportunities.

FAQs

What is the primary indication for trametinib?

Trametinib is primarily indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations[4].

How does trametinib work?

Trametinib works by inhibiting the MEK1 and MEK2 kinases, which are part of the BRAF pathway, thereby reducing uncontrolled cellular proliferation in tumors[4].

What are the common adverse events associated with trametinib?

Common adverse events include rash, diarrhea, fatigue, peripheral edema, nausea, and dermatitis acneiform. More serious concerns include cardiac and ocular adverse events[4].

Is trametinib used in combination with other drugs?

Yes, trametinib is often used in combination with dabrafenib, another BRAF inhibitor, which has shown enhanced efficacy in treating melanoma patients[5].

What is the current market status of trametinib?

Trametinib has received approvals in multiple territories and is a leading treatment option for BRAF-mutant melanoma, contributing significantly to GSK's revenue[5].

Sources

1. Australian Public Assessment Report for Trametinib - Therapeutic Goods Administration[1].
2. FDA NDA 204114: Trametinib - U.S. Food and Drug Administration[2].
3. Deciphera ESMO 2022 Investor Event - Deciphera Pharmaceuticals[3].
4. Clinical Pharmacology Review of Trametinib - U.S. Food and Drug Administration[4].
5. Product Information for Mekinist (Trametinib) - GlaxoSmithKline Australia Pty Ltd[5].