APTIVUS Drug Patent Profile

Which patents cover Aptivus, and when can generic versions of Aptivus launch?

Aptivus is a drug marketed by Boehringer Ingelheim and is included in two NDAs.

The generic ingredient in APTIVUS is tipranavir. There are two drug master file entries for this compound. One supplier is listed for this compound. Additional details are available on the tipranavir profile page.

Summary for APTIVUS

US Patents:	0
Applicants:	1
NDAs:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	1
Clinical Trials:	7
Patent Applications:	6,155
Drug Prices:	Drug price information for APTIVUS
What excipients (inactive ingredients) are in APTIVUS?	APTIVUS excipients list
DailyMed Link:	APTIVUS at DailyMed

See drug prices for APTIVUS

Recent Clinical Trials for APTIVUS

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

Sponsor	Phase
Boehringer Ingelheim	Phase 3
National Institutes of Health (NIH)	Phase 2/Phase 3
National Institute of Mental Health (NIMH)	Phase 2/Phase 3

See all APTIVUS clinical trials

Pharmacology for APTIVUS

Drug Class	Protease Inhibitor
Mechanism of Action	HIV Protease Inhibitors

US Patents and Regulatory Information for APTIVUS

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Boehringer Ingelheim	APTIVUS	tipranavir	CAPSULE;ORAL	021814-001	Jun 22, 2005		RX	Yes	Yes
Boehringer Ingelheim	APTIVUS	tipranavir	SOLUTION;ORAL	022292-001	Jun 23, 2008		DISCN	Yes	No

Expired US Patents for APTIVUS

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Boehringer Ingelheim	APTIVUS	tipranavir	SOLUTION;ORAL	022292-001	Jun 23, 2008
Boehringer Ingelheim	APTIVUS	tipranavir	CAPSULE;ORAL	021814-001	Jun 22, 2005
Boehringer Ingelheim	APTIVUS	tipranavir	SOLUTION;ORAL	022292-001	Jun 23, 2008

EU/EMA Drug Approvals for APTIVUS

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Boehringer Ingelheim International GmbH	Aptivus	tipranavir	EMEA/H/C/000631Aptivus, co-administered with low-dose ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infection in highly pretreated adults and adolescents 12 years of age or older with virus resistant to multiple protease inhibitors.Aptivus should only be used as part of an active combination antiretroviral regimen in patients with no other therapeutic options.This indication is based on the results of two phase-III studies, performed in highly pretreated adult patients (median number of 12 prior antiretroviral agents) with virus resistant to protease inhibitors and of one phase-II study investigating pharmacokinetics, safety and efficacy of Aptivus in mostly treatment-experienced adolescent patients aged 12 to 18 years.In deciding to initiate treatment with Aptivus, co-administered with low dose ritonavir, careful consideration should be given to the treatment history of the individual patient and the patterns of mutations associated with different agents. Genotypic or phenotypic testing (when available) and treatment history should guide the use of Aptivus. Initiation of treatment should take into account the combinations of mutations which may negatively impact the virological response to Aptivus, co-administered with low-dose ritonavir.	Authorised	no	no	no	2005-10-25

International Patents for APTIVUS

See the table below for patents covering APTIVUS around the world.

Country	Patent Number	Title	Estimated Expiration
Spain	2219895
China	1154642
Slovenia	0999826

Supplementary Protection Certificates for APTIVUS

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
0758327	300216	Netherlands		300216, 20150504, EXPIRES: 20200503
0758327	SPC034/2005	Ireland		SPC034/2005: 20061023, EXPIRES: 20200503
0758327	CA 2005 00052	Denmark

Market Dynamics and Financial Trajectory for the Pharmaceutical Drug: APTIVUS (Amprenavir)

Last updated: July 27, 2025

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Introduction

APTIVUS, the brand name for amprenavir, is an antiretroviral medication developed by GlaxoSmithKline (GSK) for the treatment of HIV/AIDS. Since its approval in 1999, APTIVUS has played a significant role in antiretroviral therapy (ART), especially for patients with resistant HIV strains. This analysis explores the evolving market dynamics, competitive landscape, and financial trajectory of APTIVUS, providing key insights for pharmaceutical stakeholders, investors, and healthcare providers.

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Market Overview and Therapeutic Significance

The HIV/AIDS therapeutics market remains vital despite the advent of newer agents. APTIVUS functions as a protease inhibitor (PI), targeting the HIV-1 protease enzyme necessary for viral replication. Its mechanism synergizes well with various ART combination regimens to suppress viral loads.

However, the market landscape has shifted markedly since APTIVUS's initial launch. The rise of integrase strand transfer inhibitors (INSTIs), such as dolutegravir and bictegravir, propelled by their superior tolerability profiles and simplified dosing, has gradually displaced PIs like amprenavir from first-line therapy. Nonetheless, APTIVUS maintains a niche role, chiefly in salvage therapy and resistant HIV cases.

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Market Dynamics

1. Competitive Landscape

The antiretroviral market is highly competitive, with multiple drugs vying for dominance. The primary competitors include:

• Integrase Inhibitors: Dolutegravir (Tivicay), bictegravir (Biktarvy) — preferred for their efficacy and safety.
• Other Protease Inhibitors: Darunavir (Prezista), atazanavir (Reyataz) — offer alternative PI options with improved tolerability.
• Fixed-Dose Combinations: Simplify regimens, boosting adherence.

Aptivus's role has diminished as first-line regimens favor INSTIs due to fewer side effects and once-daily dosing. Nevertheless, APTIVUS remains relevant within CD4-positive, heavily treatment-experienced populations, particularly where resistance mutations limit options.

2. Prescribing Trends

Recent market data demonstrates a decline in APTIVUS prescriptions:

• Declining First-line Use: Shifts favor newer drugs with better safety and tolerability profiles.
• Resistant HIV Cases: APTIVUS is selectively utilized for patients with multidrug resistance, where it offers unique efficacy due to its distinct mechanism and resistance profile.
• Formulation Challenges: The original amprenavir formulation was associated with gastrointestinal side effects, leading to the development of fosamprenavir, a prodrug with improved tolerability and bioavailability.

3. Regulatory and Patent Status

APTIVUS's patent expired in the early 2010s, resulting in generic formulation availability that pressures branded sales and reduces prices. GSK's strategic focus shifted to newer pipeline agents, further limiting APTIVUS’s market exclusivity.

4. Pricing and Market Share

The generic proliferation has significantly impacted revenue streams. As of recent years, APTIVUS's market share has shrunk considerably, with the drug serving primarily in niche therapeutic settings rather than mass-market use. Price erosion due to generics and competitive pressure suppresses profit margins for branded formulations.

5. Global Market Dynamics

In low- and middle-income countries, access constraints and patent issues influence drug adoption. While generics facilitate broader access, market penetration for APTIVUS remains marginal outside specialized segments.

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Financial Trajectory

1. Revenue Trends

GSK’s reported revenues for APTIVUS have been in decline due to:

• Patent expirations.
• Replacement by newer, preferred agents.
• Shift toward combination pills containing INSTIs and other mechanisms.

Historical data indicates:

• Initial peak sales of approximately $1 billion annually post-approval.
• A steep decline to hundreds of millions in subsequent years.
• Continuing attrition as generics saturate the markets.

2. R&D and Lifecycle Management

GSK has not prioritized APTIVUS for extensive lifecycle extension beyond its original formulation. Resources have instead been reallocated towards pipeline drugs, especially next-gen ART agents with improved profiles, and adjunct therapies.

3. Future Revenue Outlook

Given current trends:

• Marginal sales are expected to persist in highly resistant cases but will not recover to former heights.
• Market consolidation with fewer branded competitors further diminishes the drug’s financial significance.

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Key Challenges and Opportunities

Challenges:

• Market Obsolescence: Dominance of injectable ART options and newer orally administered agents.
• Price Erosion: Generics reduce revenue streams and threaten profitability.
• Niche Role: Limited application outside resistant HIV contexts constrains growth.

Opportunities:

• Targeted Therapy in Resistant Cases: Continued utility in specialized populations.
• Combination Regimens: Potential integration into multi-drug formulations remains limited but could sustain small markets.
• Developing Countries: Expansion of access through licensing or partnerships might generate modest revenues.

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Regulatory and Market Outlook

The evolving HIV treatment paradigm favors drugs with improved safety profiles, simplified dosing, and minimal side effects. While APTIVUS faces obsolescence in the broader market, niche applications and resistance management could sustain minimal activity.

Regulatory pathways for newer agents suggest a declining importance for older PIs like amprenavir. However, regulators continue to recognize the importance of second-line and salvage therapies, where APTIVUS might retain relevance under specific circumstances.

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Conclusion

APTIVUS’s market and financial trajectory exemplify the typical lifecycle of a once-blockbuster HIV medication facing patent expiry, generic competition, and shifting treatment paradigms. Despite a significant decline from its peak revenues, niche applications in resistant HIV treatment sustain residual demand. The commoditization of antiretrovirals and prioritization of newer therapeutics suggest a continuing downward trend, with limited prospects for substantial recovery.

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Key Takeaways

• Market Decline: APTIVUS’s revenues have decreased substantially since patent expiration, transitioning from a flagship HIV agent to a niche drug.
• Competitive Pressure: The rise of INSTIs and improved PIs diminish APTIVUS’s role in first-line therapy.
• Niche Utility: Resistant HIV cases offer limited but meaningful markets for APTIVUS; clinicians may still prescribe it where other options are unsuitable.
• Price Erosion: Generic proliferation and patent expiries have compressed margins and sales volume.
• Future Outlook: The drug's prospects hinge on its utility in resistant HIV management but face stiff competition from newer, more tolerable agents.

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FAQs

1. What is the primary use of APTIVUS today?
   APTIVUS is primarily used in salvage therapy for HIV patients with multidrug-resistant strains where other therapies have failed or are unsuitable.

2. How has patent expiry affected APTIVUS's market?
   Patent expiry led to significant generic competition, reducing branded sales, market share, and profitability for GSK.

3. Are there ongoing developments to extend APTIVUS’s lifecycle?
   No significant development efforts are underway for APTIVUS itself; focus has shifted to newer antiretrovirals with improved profiles.

4. What competition is most impacting APTIVUS’s market share?
   Integrase strand transfer inhibitors like dolutegravir and combination therapies containing newer protease inhibitors have largely displaced APTIVUS in most treatment settings.

5. Is APTIVUS still recommended in any treatment guidelines?
   Yes, mainly in cases involving multidrug-resistant HIV or patients intolerant to other agents, but its role is limited and increasingly replaced by newer drugs.

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References

[1] GSK. (2022). HIV/AIDS treatment options. GSK Annual Report.
[2] World Health Organization. (2022). HIV/AIDS Treatment Guidelines.
[3] IQVIA. (2021). Global Market Data for HIV Antiretroviral Drugs.
[4] U.S. Food and Drug Administration. (2000). FDA Approval of Amprenavir.
[5] PharmExec. (2020). Lifecycle management in HIV therapeutics.