Netupitant; palonosetron hydrochloride - Generic Drug Details

What are the generic drug sources for netupitant; palonosetron hydrochloride and what is the scope of patent protection?

Netupitant; palonosetron hydrochloride is the generic ingredient in one branded drug marketed by Helsinn Hlthcare and is included in one NDA. There are twelve patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Netupitant; palonosetron hydrochloride has eighty-one patent family members in forty-one countries.

One supplier is listed for this compound.

Summary for netupitant; palonosetron hydrochloride

International Patents:	81
US Patents:	12
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Clinical Trials:	17
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for netupitant; palonosetron hydrochloride
DailyMed Link:	netupitant; palonosetron hydrochloride at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for netupitant; palonosetron hydrochloride

Dosage:

CAPSULE;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 netupitant; palonosetron hydrochloride

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

Sponsor	Phase
Sichuan Cancer Hospital and Research Institute	N/A
Helsinn Healthcare SA	Phase 4
Instituto Brasileiro de Controle do Cancer	Phase 2

See all netupitant; palonosetron hydrochloride clinical trials

Pharmacology for netupitant; palonosetron hydrochloride

Drug Class	Serotonin-3 Receptor Antagonist Substance P/Neurokinin-1 Receptor Antagonist
Mechanism of Action	Breast Cancer Resistance Protein Inhibitors Cytochrome P450 3A4 Inhibitors Neurokinin 1 Antagonists P-Glycoprotein Inhibitors Serotonin 3 Receptor Antagonists

Anatomical Therapeutic Chemical (ATC) Classes for netupitant; palonosetron hydrochloride

A04AA	Serotonin (5HT3) antagonists
A04A	ANTIEMETICS AND ANTINAUSEANTS
A04	ANTIEMETICS AND ANTINAUSEANTS
A	Alimentary tract and metabolism

US Patents and Regulatory Information for netupitant; palonosetron hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes			Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes			Y
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014		RX	Yes	Yes				Y

Expired US Patents for netupitant; palonosetron hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014
Helsinn Hlthcare	AKYNZEO	netupitant; palonosetron hydrochloride	CAPSULE;ORAL	205718-001	Oct 10, 2014

International Patents for netupitant; palonosetron hydrochloride

Country	Patent Number	Title	Estimated Expiration
European Patent Office	2794179
Ukraine	105817	КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ ТОШНОТЫ И РВОТЫ ЦЕНТРАЛЬНОГО ПРОИСХОЖДЕНИЯ;КОМПОЗИЦІЇ ДЛЯ ЛІКУВАННЯ НУДОТИ І БЛЮВАННЯ ЦЕНТРАЛЬНОГО ПОХОДЖЕННЯ (Normal;heading 1;heading 2;heading 3;COMPOSITIONS FOR TREATING CENTRALLY MEDIATED NAUSEA AND VOMITING)
Portugal	2361090
Hong Kong	1214148	用於治療中樞介導的噁心及嘔吐的組合物及方法 (COMPOSITIONS FOR TREATING CENTRALLY MEDIATED NAUSEA AND VOMITING)
Spain	2559475
Taiwan	201210593	Compositions and methods for treating centrally mediated nausea and vomiting

Supplementary Protection Certificates for netupitant; palonosetron hydrochloride

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1035115	43/2015	Austria		PRODUCT NAME: NETUPITANT; REGISTRATION NO/DATE: EU/1/15/1001 20150527
1035115	C01035115/01	Switzerland		PRODUCT NAME: NETUPITANT; REGISTRATION NO/DATE: SWISSMEDIC 65499 06.11.2015
1035115	CA 2015 00044	Denmark		PRODUCT NAME: NETUPITANT; REG. NO/DATE: EU/1/15/1001 20150527
2785706	2090015-5	Sweden		PRODUCT NAME: FOSNETUPITANT; REG. NO/DATE: EU/1/15/1001 20200317
2785706	SPC/GB20/037	United Kingdom		PRODUCT NAME: FOSNETUPITANT; REGISTERED: UK EU/1/15/1001 (NI) 20200318; UK PLGB 12333/0017-0001 20200318
1035115	CR 2015 00044	Denmark		PRODUCT NAME: NETUPITANT; REG. NO/DATE: EU/1/15/1001 20150529

Netupitant; palonosetron hydrochloride Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Netupitant-Palonosetron Hydrochloride

Market Overview

The global market for the fixed-dose combination (FDC) of netupitant and palonosetron hydrochloride, commonly known as Akynzeo, has been experiencing significant growth driven by several key factors. This combination therapy is specifically designed to prevent acute and delayed chemotherapy-induced nausea and vomiting (CINV), a common side effect of cancer chemotherapy.

Market Size and Growth

As of 2015, the global netupitant-palonosetron FDC market was valued at $257,162 million. It is projected to reach $527,187 million by 2022, growing at a Compound Annual Growth Rate (CAGR) of 10.8% during the forecast period[1].

Mechanism of Action

The efficacy of Akynzeo is rooted in its dual mechanism of action. Netupitant acts as a selective antagonist of human substance P/neurokinin 1 (NK1) receptors in the central nervous system, preventing the binding of endogenous tachykinin neuropeptide substance P, which is involved in CINV. Palonosetron, on the other hand, blocks serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors, further reducing the incidence of CINV[4].

Clinical Efficacy

Clinical studies have demonstrated the superiority of the netupitant-palonosetron FDC over palonosetron alone in preventing both acute and delayed phases of CINV. For instance, in a pivotal trial, the combination showed a complete response (CR) rate of 87.4% to 89.6% compared to 76.5% for palonosetron alone over the 0-120 hours post-chemotherapy period[3].

Market Segmentation

The global netupitant-palonosetron FDC market is segmented based on patient pool type and geography. Geographically, the market is analyzed across North America, Europe, Asia-Pacific, and Latin America, Middle East, and Africa (LAMEA). North America and Europe are the dominant regions, driven by the increasing incidence of CINV among patients undergoing chemotherapy[1].

Key Drivers

Increasing Incidence of CINV

The rise in the number of patients undergoing chemotherapy is a significant driver for the market. As more patients receive chemotherapy, the demand for effective antiemetic treatments like Akynzeo increases[1].

Technological Advancements

Advancements in drug delivery systems, such as needle-free and painless transdermal patches, are expected to enhance patient compliance and efficacy. Novel methods like multiple dosing and variable drug delivery rates are being developed to improve treatment outcomes[1].

Approval of New Drugs

The approval of new drugs, such as rolapitant (Varubi) and Sustol (APF-530), has expanded the treatment options for CINV, further boosting the market growth. These new drugs provide cancer patients with more effective treatments for preventing delayed-phase nausea and vomiting[1].

Market Challenges

Genetic Variability

One of the challenges faced by the market is the variability in genes encoding enzymes and proteins involved in the metabolism, transport, and receptors related to antiemetic drugs. This variability can lead to suboptimal responses to current antiemetic therapies, which have an efficacy of about 70%-80% in patients treated with highly emetogenic cytotoxic drugs[1].

Safety Profile

While Akynzeo has an acceptable safety profile, common adverse events include headache, constipation, and fatigue. However, these events are generally mild to moderate in intensity. Rare but serious adverse reactions such as anaphylaxis and QT interval prolongation also need to be considered[2][4].

Competitive Landscape

The market is competitive, with major players including Helsinn Holding S.A., Heron Therapeutics, Inc., Eisai Pharmaceutical Pvt Ltd., and Acacia Pharma. These companies are adopting various strategies to sustain a competitive environment and increase their market share, including technological advancements and the development of new delivery methods[1].

Financial Trajectory

The financial trajectory of the netupitant-palonosetron FDC market is robust, driven by the increasing demand for effective antiemetic treatments. Here are some key financial highlights:

• Market Value: The market was valued at $257,162 million in 2015 and is estimated to reach $527,187 million by 2022[1].
• Revenue Growth: The market is expected to grow at a CAGR of 10.8% during the forecast period, indicating a strong financial trajectory[1].
• Regional Revenue: North America and Europe are the leading regions in terms of revenue, driven by the high incidence of CINV and the adoption of new antiemetic drugs[1].

Technological Advancements and Future Outlook

Companies are investing in technological advancements to lower production costs and discover new high-potential FDC drugs. For example, the development of rolapitant (Varubi) by Tesaro has gained significant traction in the market. These advancements are expected to continue driving the market forward by improving patient compliance and treatment efficacy[1].

Key Takeaways

• The global netupitant-palonosetron FDC market is growing rapidly, driven by the increasing incidence of CINV and technological advancements.
• The combination therapy has shown superior efficacy over single-agent treatments in clinical trials.
• Market segmentation is based on patient pool type and geography, with North America and Europe being the dominant regions.
• Challenges include genetic variability affecting drug efficacy and potential safety concerns.
• The competitive landscape is marked by major players adopting strategies to enhance market share.
• The financial trajectory is robust, with a projected market value of $527,187 million by 2022.

FAQs

What is the primary mechanism of action of the netupitant-palonosetron FDC?

The primary mechanism involves netupitant blocking substance P/neurokinin 1 (NK1) receptors and palonosetron blocking serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors to prevent CINV[4].

Which regions dominate the netupitant-palonosetron FDC market?

North America and Europe are the dominant regions in terms of revenue, driven by the high incidence of CINV and the adoption of new antiemetic drugs[1].

What are the common adverse events associated with Akynzeo?

Common adverse events include headache, constipation, and fatigue, which are generally mild to moderate in intensity[2][4].

How does genetic variability impact the efficacy of antiemetic treatments?

Genetic variability in genes encoding enzymes and proteins involved in drug metabolism and receptors can lead to suboptimal responses to antiemetic therapies, affecting about 20%-30% of patients treated with highly emetogenic cytotoxic drugs[1].

What technological advancements are expected to impact the market?

Advancements in drug delivery systems, such as transdermal patches with multiple dosing and variable drug delivery rates, are expected to enhance patient compliance and treatment efficacy[1].

Sources

1. Allied Market Research: Netupitant – Palonosetron FDC Market Size - Analysis 2022
2. Health Products and Food Branch: Summary Basis of Decision for Akynzeo
3. FDA: 205718Orig1s000 - accessdata.fda.gov
4. EMA: Akynzeo, INN-netupitant & palonosetron hydrochloride
5. FDA: Akynzeo® (netupitant-palonosetron hydrochloride) Capsules - FDA