Rolapitant hydrochloride - Generic Drug Details

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

Rolapitant hydrochloride is the generic ingredient in one branded drug marketed by Tersera and is included in two NDAs. There are eight patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Rolapitant hydrochloride has one hundred and fifty-eight patent family members in thirty-five countries.

One supplier is listed for this compound.

Summary for rolapitant hydrochloride

International Patents:	158
US Patents:	8
Tradenames:	1
Applicants:	1
NDAs:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	98
Clinical Trials:	15
DailyMed Link:	rolapitant hydrochloride at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for rolapitant hydrochloride

Constraining patent/regulatory exclusivity:

7,049,320

Dosage:

EMULSION;INTRAVENOUS

Constraining patent/regulatory exclusivity:

8,361,500

Dosage:

TABLET;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 rolapitant hydrochloride

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

Sponsor	Phase
Guangxi Medical University	Phase 3
ECONiX Araştırma Analiz ve Danışmanlık A.Ş.	Phase 2
PlusVitech S.L.	Phase 2

See all rolapitant hydrochloride clinical trials

Pharmacology for rolapitant hydrochloride

Drug Class	Substance P/Neurokinin-1 Receptor Antagonist
Mechanism of Action	Breast Cancer Resistance Protein Inhibitors Cytochrome P450 2D6 Inhibitors Neurokinin 1 Antagonists P-Glycoprotein Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for rolapitant hydrochloride

A04AD	Other antiemetics
A04A	ANTIEMETICS AND ANTINAUSEANTS
A04	ANTIEMETICS AND ANTINAUSEANTS
A	Alimentary tract and metabolism

US Patents and Regulatory Information for rolapitant hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes	8,178,550		Y	Y
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes	7,563,801		Y
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes	8,404,702
Tersera	VARUBI	rolapitant hydrochloride	EMULSION;INTRAVENOUS	208399-001	Oct 25, 2017		DISCN	Yes	No	8,470,842
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes	7,049,320		Y	Y
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015		RX	Yes	Yes	8,470,842

Expired US Patents for rolapitant hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Tersera	VARUBI	rolapitant hydrochloride	EMULSION;INTRAVENOUS	208399-001	Oct 25, 2017	8,796,299
Tersera	VARUBI	rolapitant hydrochloride	TABLET;ORAL	206500-001	Sep 1, 2015	8,796,299

International Patents for rolapitant hydrochloride

Country	Patent Number	Title	Estimated Expiration
European Patent Office	2464230	FORMULATIONS INTRAVEINEUSES D'ANTAGONISTES DE NEUROKININE-1 (INTRAVENOUS FORMULATIONS OF NEUROKININ-1 ANTAGONISTS)
Portugal	1463716
European Patent Office	2662373
Colombia	5590915	DERIVADOS DE PIPERIDINA COMO ANTAGONISTAS NK1 ( RECEPTOR DEL NEUROPEPTIDO NEUROQUININA-1) CON ACTIVIDAD ANTAGONISTA SUPERIOR EN TRATAMIENTOS DE TRASTORNOS FISIOLOGICOS Y DISMINUCION DE EFECTOS COLATERALES
Peru	20030762	COMPUESTOS HETEROCICLICOS COMO ANTAGONISTAS NK1
Japan	2015108023

Supplementary Protection Certificates for rolapitant hydrochloride

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1463716	C201730043	Spain		PRODUCT NAME: ROLAPITANT, OPCIONALMENTE EN FORMA DE UNA SAL FARMACEUTICAMENTE ACEPTABLE, INCLUYENDO ROLAPITANT CLORHIDRATO MONOHIDRATO; NATIONAL AUTHORISATION NUMBER: EU/1/17/1180; DATE OF AUTHORISATION: 20170420; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/17/1180; DATE OF FIRST AUTHORISATION IN EEA: 20170420
1463716	2017/042	Ireland		PRODUCT NAME: ROLAPITANT, OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, INCLUDING ROLAPITANT HYDROCHLORIDE MONOHYDRATE; REGISTRATION NO/DATE: EU/1/17/1180 20170420
1463716	609	Finland
1463716	C20170033 00237	Estonia		PRODUCT NAME: ROLAPITANT;REG NO/DATE: EU/1/17/1180 24.04.2017
1463716	LUC00043	Luxembourg		PRODUCT NAME: ROLAPITANT, OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, INCLUDING ROLAPITANT HYDROCHLORIDE MONOHYDRATE; AUTHORISATION NUMBER AND DATE: EU/1/17/1180/001 20170424
2004646	300898	Netherlands		PRODUCT NAME: ROLAPITANT HYDROCHLORIDE-MONOHYDRAAT; REGISTRATION NO/DATE: EU/1/17/1180 20170424

Market Dynamics and Financial Trajectory for Rolapitant Hydrochloride

Last updated: July 27, 2025

Introduction

Rolapitant hydrochloride is a selective neurokinin-1 (NK1) receptor antagonist used primarily to prevent chemotherapy-induced nausea and vomiting (CINV). Since its initial approval, the drug has positioned itself within the oncology supportive care sector. Understanding its market dynamics and financial trajectory involves assessing factors such as clinical efficacy, competitive landscape, regulatory developments, and broader trends in oncology supportive therapies.

Pharmacological Profile and Therapeutic Positioning

Rolapitant hydrochloride offers targeted antiemetic action by blocking NK1 receptors involved in mediating nausea and vomiting reflexes. Its distinctive pharmacokinetics, including a long half-life (~7 days), enable single-dose administration per chemotherapy cycle, improving adherence and patient quality of life. These properties distinguish it from other NK1 antagonists like aprepitant and fosaprepitant, which have shorter durations of action.

Clinically, rolapitant is indicated for prophylaxis of delayed CINV, which remains a significant unmet need despite existing antiemetics. Its efficacy, safety profile, and convenience have garnered preference among clinicians, underpinning sales within its approved indications. However, evolving clinical guidelines and alternative therapies influence its market positioning.

Market Dynamics

Demand Drivers

1. Growing Oncology Population:

   The global increase in cancer incidence, projected to reach approximately 28.4 million new cases annually by 2040, fuels the demand for supportive care drugs like rolapitant. Advances in early detection and expanding treatment protocols contribute to greater chemotherapy utilization, escalating the necessity for effective antiemetic regimens ([1]).

2. Preference for Oral Administration:

   Rolapitant's oral formulation aligns with patient-centered care trends, facilitating outpatient management and adherence. As healthcare systems and patients prioritize convenience, the drug benefits from this shift.

3. Regulatory Approvals and Label Expansions:

   Initially approved in the US in 2015 for CINV prevention in adults receiving “high emetogenic chemotherapy,” subsequent label extensions in various jurisdictions have broadened its scope. Such approvals expand the accessible patient population.

4. Reimbursement and Pricing Strategies:

   Favorable reimbursement policies and pricing strategies influence market penetration. Payers increasingly favor drugs that reduce hospitalizations and improve quality of life, benefiting agents like rolapitant.

Competitive Landscape

1. Key Competitors:

   The primary competitors include aprepitant (Emend®), fosaprepitant, and newer NK1 antagonists or combination antiemetics ([2]). Aprepitant remains the market leader, benefiting from earlier approval and established clinical practice.

2. Differentiators:

   Rolapitant’s extended half-life and favorable drug–drug interaction profile provide competitive advantages, especially for patients on complex regimens with CYP3A4 interactions, common in chemotherapy.

3. Market Share Dynamics:

   Despite its advantages, rolapitant faces challenges from entrenched competitors and clinicians' familiarity with existing protocols. Continued education and clinical evidence are crucial for expanding its market share.

Regulatory and Patent Landscape

Patent exclusivity hinders generic competition; patent lifespans typically extend until late 2020s or early 2030s, offering a period of market exclusivity that supports revenue projections. Ongoing patent litigations and patent expirations could alter the competitive landscape.

Pricing and Reimbursement Trends

Pricing varies across regions, influenced by healthcare policies and economic factors. In high-income countries, reimbursement facilitates higher pricing, whereas in emerging markets, cost considerations limit access. Strategic partnerships and differential pricing are crucial for expanding global footprint.

Financial Trajectory

Revenue Trends

Initial sales projections for rolapitant, driven by clinical adoption, indicate moderate growth owing to its niche application. The drug premium position, supported by unique pharmacokinetic features, justifies premium pricing, positively impacting gross margins.

In the US, sales figures have shown steady growth post-approval, with estimates reflecting several hundred million USD annually. However, growth rates are tempered by competition and clinical practice inertia.

Market Penetration and Expansion

Expanded labeling in additional indications or combination therapy approvals (e.g., with dexamethasone or olanzapine) could stimulate revenue streams. International expansion, especially in Asia-Pacific and emerging markets, presents substantial growth opportunities, contingent on regulatory clearance and pricing negotiations.

Research and Development Impact

Investment in clinical trials assessing rolapitant’s efficacy for new indications—such as breakthrough CINV management, postoperative nausea, or even off-label uses—could influence long-term revenue. However, R&D expenses will temper short-term profitability.

Strategic Collaborations

Partnerships with healthcare providers, payers, and regional distributors augment market reach. Licensing agreements and joint ventures enhance financial prospects, especially in markets with complex regulatory environments.

Regulatory and Patent Trajectory Impact

Patent expirations or challenges could lead to generic entrants reducing prices and market share. Conversely, successful patent extensions or new formulation approvals reinforce revenue streams. The regulatory landscape remains dynamic, requiring ongoing compliance strategies to sustain financial performance.

Market Challenges and Opportunities

Challenges

• Competition: Established NK1 antagonists and emerging antiemetics threaten market share.
• Pricing Pressure: Cost-containment policies impact revenues.
• Clinical Adoption: Slow uptake due to clinician familiarity with existing regimens and clinical inertia.
• Regulatory Barriers: Delays or denials in new indications limit growth.

Opportunities

• Expanding Indications: Investigating rolapitant for other nausea-related conditions can unlock new markets.
• Combination Therapies: Formulation of fixed-dose combinations simplifies regimens.
• Biomarker-Guided Therapy: Personalization improves efficacy and market acceptance.
• Global Expansion: Entry into untapped markets provides substantial revenue potential.

Conclusion

The market for rolapitant hydrochloride exhibits steady growth amid a competitive and evolving landscape. Its pharmacokinetic advantages and clinical benefits underpin its position in oncology supportive care, with future growth driven by expanded indications, global penetration, and strategic collaborations. Regulatory developments and patent statuses will significantly influence its financial trajectory.

Keeping abreast of clinical evidence, payer policies, and competitive shifts remains essential for stakeholders aiming to capitalize on this therapeutic niche.

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Key Takeaways

• Growing Oncology Demographics fuel demand for targeted antiemetic agents like rolapitant.
• Pharmacokinetic Profile offers a competitive edge, supporting once-per-cycle dosing and adherence.
• Market Share depends on clinician acceptance, clinical evidence, and strategic positioning against established competitors.
• Regulatory and Patent Dynamics significantly influence revenue potential and market exclusivity.
• Global Expansion and Indication Growth are crucial channels for sustaining long-term financial stability.

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FAQs

1. What are the primary clinical advantages of rolapitant hydrochloride compared to other NK1 antagonists?
   Rolapitant's long half-life enables a single-dose regimen per chemotherapy cycle, reducing treatment complexity and improving patient compliance. It also has fewer drug–drug interactions, especially with CYP3A4 substrates, enhancing safety for patients on multiple medications.

2. How do patent expirations impact the financial outlook for rolapitant?
   Patent expirations open opportunities for generic competition, which typically causes price reductions and market share declines. Protecting market exclusivity through patent extensions or new indications is vital for sustaining revenue.

3. Which markets present the most significant growth opportunities for rolapitant?
   Emerging markets with increasing cancer incidence, such as China and India, offer substantial growth potential. Additionally, expanding indications and combination therapies in developed economies can drive revenue growth.

4. What competitive strategies can enhance rolapitant's market penetration?
   Strategies include pursuing additional indications, developing fixed-dose combination formulations, engaging in clinician education, and establishing strategic regional partnerships to increase awareness and access.

5. Are there ongoing clinical trials that could affect the use of rolapitant?
   Yes, studies investigating rolapitant for other nausea management indications or combination regimens may expand its therapeutic scope. Positive trial results could lead to regulatory approvals and new revenue streams.

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Sources:
[1] Global Cancer Statistics, World Health Organization, 2020.
[2] Market Research Future, "NK1 Receptor Antagonists Market Report," 2021.