List of Excipients in Branded Drug DARUNAVIR

Generic Drugs Containing DARUNAVIR

Company	Ingredient	NDC	Excipient
Teva Pharmaceuticals Inc	darunavir	0480-7736	CELLULOSE, MICROCRYSTALLINE
Teva Pharmaceuticals Inc	darunavir	0480-7736	CROSPOVIDONE
Teva Pharmaceuticals Inc	darunavir	0480-7736	FD&C RED NO. 40
Teva Pharmaceuticals Inc	darunavir	0480-7736	FD&C YELLOW NO. 6
Teva Pharmaceuticals Inc	darunavir	0480-7736	MAGNESIUM STEARATE
Teva Pharmaceuticals Inc	darunavir	0480-7736	POLYETHYLENE GLYCOL 3350
Teva Pharmaceuticals Inc	darunavir	0480-7736	POLYVINYL ALCOHOL

What are the Most Frequently-Used Excipients in DARUNAVIR?

# Of NDCs	Excipient
11	CELLULOSE, MICROCRYSTALLINE
1	CROSCARMELLOSE SODIUM
12	CROSPOVIDONE
1	FD&C RED NO. 40
7	FD&C YELLOW NO. 6
5	FERRIC OXIDE RED
5	FERRIC OXIDE YELLOW

Darunavir Excipient Strategy and Commercial Opportunities

Last updated: September 3, 2026

Darunavir is a mature HIV-1 protease inhibitor with limited exclusivity on the active pharmaceutical ingredient and continuing commercial value in fixed-dose combinations, pediatric delivery, long-acting concepts, and differentiated generic formulations. The strongest excipient opportunities address darunavir’s poor aqueous solubility, food-dependent absorption, high tablet burden, taste, and compatibility with pharmacokinetic boosters such as cobicistat and ritonavir.

What is the commercial status of darunavir?

Darunavir is marketed primarily as Prezista, a Janssen product, and in fixed-dose combinations including Prezcobix and Symtuza. The drug is administered with ritonavir or cobicistat because its oral exposure is materially increased by CYP3A inhibition.[1-3]

Product	Active ingredients	Manufacturer or sponsor	Dosage form	Principal commercial role
Prezista	Darunavir	Janssen	Film-coated tablets; oral suspension in some markets	Boosted protease inhibitor
Prezcobix	Darunavir/cobicistat	Janssen	Film-coated tablet	Two-drug boosted regimen
Symtuza	Darunavir/cobicistat/emtricitabine/tenofovir alafenamide	Janssen	Film-coated tablet	Complete single-tablet regimen
Generic darunavir	Darunavir	Multiple generic manufacturers	Film-coated tablets	Price competition and formulary substitution

Darunavir was approved by the U.S. Food and Drug Administration in 2006. Its original five-year new chemical entity exclusivity expired in 2011. The main composition patent estate has also matured, leaving formulation, combination, process, pediatric, and jurisdiction-specific rights as the more relevant areas for current diligence.[1,4]

Darunavir remains commercially relevant because HIV treatment is chronic, adherence-sensitive, and heavily influenced by treatment guidelines, resistance profiles, procurement contracts, and fixed-dose convenience. The product’s value is concentrated in differentiated delivery rather than basic active-ingredient exclusivity.

What excipients are used in darunavir products?

Approved darunavir products use conventional solid-dose excipients selected to support tablet compression, film coating, stability, and drug release. The exact composition varies by product and market.

Prezista tablet excipients

The U.S. prescribing information identifies excipients including:

• Microcrystalline cellulose
• Crospovidone
• Hypromellose
• Colloidal silicon dioxide
• Magnesium stearate
• Polyethylene glycol
• Polyvinyl alcohol
• Talc
• Titanium dioxide

These materials support tablet structure, disintegration, lubrication, coating, and appearance.[1]

Symtuza excipient requirements

Symtuza combines four active ingredients in a single tablet. Its excipient strategy must accommodate:

• Darunavir’s low aqueous solubility
• Cobicistat’s formulation and stability requirements
• Tenofovir alafenamide’s low-dose potency
• Emtricitabine’s higher dose contribution
• Chemical and physical compatibility among four active ingredients
• A tablet size acceptable for daily long-term use

The combination creates a more difficult formulation problem than darunavir monotherapy. Excipients that improve darunavir wetting or dissolution can affect the stability, compression, or release characteristics of the other active ingredients. The label and regulatory dossier for the specific product should control any commercial development program.[2]

What formulation problems should an excipient strategy solve?

The central development problem is not simply tablet manufacture. It is achieving reproducible exposure while reducing the clinical and commercial penalties of darunavir’s physicochemical and pharmacokinetic profile.

Poor aqueous solubility

Darunavir is a poorly water-soluble compound. Conventional immediate-release tablets depend on particle wetting, deaggregation, dissolution, and absorption under fed conditions. Excipients that can improve performance include:

• Surfactants and wetting agents
• Polymer-based precipitation inhibitors
• Amorphous solid-dispersion carriers
• Cocrystal or salt-forming systems, where chemically and regulatorily feasible
• Lipid-based excipient systems
• Nanocrystal stabilizers
• Porosity enhancers and superdisintegrants

A development program should measure not only dissolution in standard media but also precipitation after dilution, supersaturation duration, and exposure under fed and fasted conditions.

Food dependence

Darunavir is administered with food under approved labeling. A formulation that reduces food effect could improve adherence and reduce regimen complexity. Excipients with potential value include lipidic vehicles, surfactant systems, precipitation inhibitors, and particle-engineering approaches.

A reduced-food-effect claim would require clinical bridging. In vitro dissolution improvement alone would not create a commercially defensible product advantage.

High tablet burden

Darunavir is used at doses of 600 mg twice daily with ritonavir in some treatment settings, or 800 mg once daily with a booster in others. High drug loading limits the amount of excipient available for solubility enhancement and can produce large tablets.

Commercially attractive approaches include:

• Higher drug-loading granulation
• Direct compression with engineered excipients
• Coated drug particles
• Bilayer or multilayer tablets
• Multiparticulate dosage forms
• Mini-tablets for pediatric use
• Fixed-dose combination manufacturing with controlled segregation

Taste and pediatric acceptability

Darunavir oral suspension and pediatric formulations create an excipient opportunity around taste masking, redispersibility, dose uniformity, and preservative systems. Taste-masking options include polymer coatings, ion-exchange resins, lipid barriers, complexation, and flavor systems.

A pediatric product must also address:

• Alcohol and propylene glycol exposure
• Sugar content
• Preservative tolerability
• Dosing-device accuracy
• Storage after opening
• Palatability across age groups
• Excipient safety in infants and young children

The commercial opportunity is strongest where an improved formulation can replace a suspension or reduce dosing complexity without compromising exposure.

Which excipient technologies have the greatest commercial potential?

Amorphous solid dispersions

Amorphous solid dispersions can increase apparent solubility and dissolution by dispersing darunavir in a polymeric carrier. Relevant polymers include hypromellose-based systems, hypromellose acetate succinate, polyvinylpyrrolidone derivatives, and copovidone.

The key risks are recrystallization, moisture sensitivity, processing temperature, residual solvent, and scale-up. A defensible patent position would normally require more than naming a polymer. It would need a specific drug-to-polymer ratio, solid-state profile, manufacturing process, dissolution result, or stability performance.

Nanocrystal formulations

Nanocrystals can increase surface area and improve dissolution without requiring a large quantity of solubilizing excipient. Stabilizers may include polymeric or surfactant systems.

Nanocrystals are attractive for high-dose drugs because they can preserve drug loading. Their challenges include aggregation, milling or precipitation scale-up, content uniformity, and physical stability during compression and coating.

Lipid-based delivery

Lipid-based systems may reduce food dependence and improve dissolution after gastrointestinal dilution. They are more likely to fit softgel, capsule, or liquid formats than conventional high-dose tablets.

The main barriers are capsule fill volume, lipid oxidation, compatibility with capsule shells, leakage, and patient acceptance. A lipid formulation is commercially more compelling if it enables lower booster exposure, food-independent dosing, or a pediatric dosage form.

Multiparticulates and coated particles

Multiparticulates can separate darunavir from incompatible actives, support taste masking, and enable flexible pediatric dosing. They may also support modified release, although prolonged release must be assessed against the pharmacokinetic need for reliable boosted exposure.

The technology is most useful where a developer needs a sprinkle formulation, dispersible product, or dose flexibility rather than a conventional adult tablet.

Excipient-enabled fixed-dose combinations

The most valuable excipient work may occur in combination products. Darunavir must coexist with cobicistat, emtricitabine, and tenofovir alafenamide in Symtuza-like products. Excipient selection can address segregation, polymorphic conversion, moisture transfer, degradation, and dissolution differences between active ingredients.

A successful platform could support:

• Smaller single-tablet regimens
• Heat- and humidity-stable products for emerging markets
• Lower-cost generic fixed-dose combinations
• Pediatric combination products
• Combination products with alternative boosters

What patents protect darunavir formulations and excipient technologies?

The foundational darunavir compound patent is substantially less important today than formulation and combination rights. Darunavir was covered by U.S. Patent No. 6,248,775, which is associated with the compound and had a listed expiration in 2021, subject to statutory adjustments and pediatric considerations.[4]

The relevant IP categories are:

IP category	Commercial relevance	Typical claim focus
Compound patents	Historical core exclusivity	Darunavir structure and related compounds
Salt and crystalline-form patents	Moderate	Solid form, polymorph, salt, or particle properties
Formulation patents	High for differentiated products	Excipients, ratios, dissolution, stability, dosage form
Fixed-dose combination patents	High	Darunavir with cobicistat, ritonavir, emtricitabine, or tenofovir alafenamide
Method-of-use patents	Moderate	Treatment populations, dosing, resistance, or regimen use
Manufacturing patents	Moderate to high	Crystallization, purification, particle engineering, and scale-up
Device and packaging patents	Selective	Dosing systems, child resistance, moisture protection, and delivery

Excipient patents tend to be strongest when they tie the excipient system to a measurable technical outcome. Broad claims directed only to common materials such as microcrystalline cellulose, magnesium stearate, or crospovidone are vulnerable to prior art and obviousness challenges.

A generic developer should map at least four claim layers:

1. Darunavir active-ingredient rights.
2. The specific approved dosage form.
3. Fixed-dose combination patents.
4. Manufacturing, solid-form, and formulation patents in each launch market.

When does darunavir lose exclusivity?

Darunavir’s U.S. regulatory and patent timeline is substantially mature.

Milestone	Date or status
FDA approval of Prezista	2006
New chemical entity exclusivity	Expired in 2011
Foundational U.S. compound patent, US 6,248,775	Listed expiration in 2021, subject to applicable adjustments
Generic product development	Active across multiple manufacturers and jurisdictions
Biosimilar pathway	Not applicable because darunavir is a small molecule
Current commercial protection	Primarily formulation, combination, manufacturing, regulatory, and market-access factors

The relevant entry question is no longer whether darunavir itself is protected by an unexpired compound patent. It is whether a proposed product practices unexpired claims covering a specific formulation, combination, dosage regimen, or manufacturing method.

What is the Orange Book status of darunavir?

FDA Orange Book analysis should distinguish between:

• Prezista tablets
• Any listed oral suspension presentation
• Prezcobix
• Symtuza
• Separate patents listed against each reference product

Orange Book listings can change through patent expiry, delisting, corrections, pediatric exclusivity, and product-specific regulatory actions. A Paragraph IV strategy must therefore be conducted against the current product-specific listing rather than against darunavir as a molecule.

For a generic darunavir tablet, the principal regulatory route is an abbreviated new drug application. The applicant must address the reference listed drug’s labeling, strength, dosage form, route of administration, pharmaceutical equivalence, and bioequivalence. A formulation using different excipients can be acceptable if it meets the applicable requirements and does not create safety, efficacy, or performance concerns.[5]

Which companies are challenging darunavir exclusivity?

Generic competition is expected from manufacturers developing darunavir tablets and, where commercially viable, combination products. The most important competitive groups are:

• Large multinational generic companies
• Specialty HIV manufacturers
• Regional suppliers serving public procurement
• Contract development and manufacturing organizations
• Firms developing alternative fixed-dose combinations

The highest-value target is not necessarily a standalone darunavir tablet. A lower-cost complete regimen, a smaller tablet, a heat-stable combination, or a pediatric product can create greater procurement value.

Paragraph IV activity should be evaluated product by product. A Paragraph IV certification may challenge an Orange Book patent, but it does not establish that the generic will launch. Litigation, settlements, regulatory approval timing, manufacturing readiness, and injunction risk determine actual entry.

What patent litigation and settlement issues affect darunavir?

Darunavir litigation risk has historically centered on generic challenges to Janssen’s listed patents and on combination-product rights. Settlement agreements can create licensed entry dates, manufacturing restrictions, supply obligations, or limits on challenging later-issued patents.

A commercial diligence review should examine:

• Paragraph IV notices
• ANDA litigation under the Hatch-Waxman Act
• 30-month stays
• Preliminary injunctions
• Patent-term adjustment and pediatric extensions
• Authorized-generic arrangements
• Settlement entry dates
• Supply and co-marketing terms
• Any antitrust scrutiny of the settlement

A generic formulation that avoids a listed formulation patent may still face method-of-use or combination-product issues if its label overlaps the protected indication. Label carve-outs can reduce this exposure, but they must remain consistent with the product’s intended commercial market.

How strong is the darunavir patent estate?

The estate is strong historically but more limited for the unboosted active ingredient today.

Asset area	Relative strength	Reason
Original compound protection	Low current strength	Core term has matured
Approved fixed-dose combinations	Moderate to high, product-specific	Combination and formulation claims can extend later
Solubility-enhancing formulations	Moderate	Strength depends on claim specificity and prior art
Pediatric formulations	Moderate	Commercial value depends on approved dosage form and market
Manufacturing processes	Moderate	Can create practical barriers even after compound expiry
Excipients alone	Low	Common excipients are widely disclosed
Proprietary excipient combinations	Moderate	Stronger with demonstrated performance and narrow claim construction

The most defensible formulation estate would combine composition claims with process and performance claims. Examples include a defined amorphous dispersion, a specified particle-size distribution, a coated particle architecture, or a tablet with a distinctive dissolution profile.

What generic launch risks exist for darunavir?

Regulatory risk

A generic developer must demonstrate bioequivalence despite darunavir’s food effect and boosting requirement. The study design must reflect the reference product’s administration conditions. Fixed-dose combinations require additional attention to each active ingredient.

Formulation risk

The product must achieve consistent dissolution despite high drug loading and potential interactions with the booster. Changes in excipient grade, lubricant level, or granulation moisture can affect performance.

Manufacturing risk

Darunavir products may require tight control of:

• Solid form
• Particle size
• Residual solvents
• Moisture
• Blend uniformity
• Compression force
• Coating weight
• Dissolution across stability time points

Market risk

Standalone darunavir may face price erosion because treatment guidelines and formularies often favor complete combination regimens. A company that launches only a single-agent tablet may have less negotiating leverage than one offering a full regimen portfolio.

What commercial opportunities exist for darunavir excipients?

The most attractive opportunities are platform-based rather than commodity excipient sales.

Formulation licensing

A developer with a validated solubility-enhancement platform can license:

• Amorphous dispersion technology
• Nanocrystal processing
• Taste-masking systems
• Pediatric multiparticulates
• High-load direct-compression systems
• Moisture-barrier coatings

Licensing value increases when the technology has human bioequivalence data, scale-up data, and a clear patent position.

Generic fixed-dose combinations

A lower-cost darunavir/cobicistat or darunavir-based complete regimen could compete in markets where branded products remain expensive. The commercial proposition depends on regulatory acceptability, tablet size, stability, and access to the other active ingredients.

Public procurement and emerging markets

Heat-stable and humidity-resistant formulations have commercial value in tropical markets. Packaging and excipient selection should be designed together. A formulation that requires complex cold-chain or moisture protection can lose its procurement advantage.

Pediatric products

Pediatric darunavir offers an opportunity for oral suspension, dispersible tablets, mini-tablets, and taste-masked granules. The strongest product concept would combine dose flexibility with reduced administration volume and stable storage after opening.

Manufacturing and supply partnerships

CDMOs can capture value by offering integrated services covering particle engineering, granulation, tablet production, coating, stability, and regulatory support. The barrier is process reproducibility rather than access to standard excipients.

How does darunavir compare with other HIV protease inhibitors?

Drug	Formulation position	Excipient opportunity	Commercial outlook
Darunavir	High-dose, boosted, established resistance profile	Solubility, pediatric delivery, fixed-dose combinations	Stronger than older protease inhibitors
Atazanavir	Lower-dose boosted product; capsule and tablet considerations	Food effect, acid-dependent absorption, formulation compatibility	Mature and more vulnerable to substitution
Lopinavir	Longstanding liquid and tablet products	Taste, liquid stability, pediatric dosing	Declining relative to newer regimens
Ritonavir	Primarily booster and combination component	Stability, taste, low-dose combination manufacturing	Strategic as a booster but limited as a standalone therapy
Cobicistat combinations	Modern boosting platform	Combination stability and tablet-size reduction	Important for darunavir fixed-dose products

Darunavir has a stronger resistance profile than several older protease inhibitors, which supports continued use in selected treatment settings. Its main commercial constraint is the complexity of boosted, high-dose oral delivery.

Key Takeaways

• Darunavir’s original compound exclusivity is mature; current value lies in formulations, combinations, manufacturing, and market access.
• The leading excipient problems are poor solubility, food-dependent absorption, high drug loading, tablet size, taste, and pediatric dosing.
• Amorphous dispersions, nanocrystals, lipid systems, coated particles, and multiparticulates are the most commercially relevant technologies.
• Fixed-dose combinations create the largest formulation and IP opportunity because excipients must support several active ingredients simultaneously.
• Darunavir has no biosimilar risk because it is a small molecule.
• Orange Book and Paragraph IV analysis must be conducted for each reference product, especially Prezista, Prezcobix, and Symtuza.
• A strong patent estate should include formulation, process, solid-state, and performance claims rather than claims directed only to common excipients.
• Generic commercial success will depend more on complete-regimen economics, tablet size, stability, pediatric utility, and procurement access than on standalone darunavir availability.

FAQs

Can a new excipient create exclusivity for darunavir?

An excipient alone rarely creates meaningful exclusivity. Patent value is stronger when the excipient is claimed as part of a defined formulation that produces improved dissolution, reduced food effect, enhanced stability, smaller tablet size, or better palatability.

Is darunavir suitable for an oral disintegrating tablet?

Potentially, but the high darunavir dose creates a tablet-size and drug-loading challenge. An orally disintegrating product would likely require particle engineering, taste masking, and a high-capacity superdisintegrant system.

Can darunavir be reformulated without ritonavir or cobicistat?

A formulation can be developed without a booster, but achieving adequate exposure may require a different delivery technology or dosing strategy. The commercial and regulatory burden would be substantially higher than for a conventional generic of an approved boosted regimen.

What is the best pediatric excipient opportunity for darunavir?

Taste-masked multiparticulates or mini-tablets offer the strongest combination of dose flexibility, portability, and palatability. A suspension remains useful but carries greater handling, preservative, redispersion, and dosing-device requirements.

Are excipient patents relevant to a darunavir Paragraph IV filing?

Yes. A listed formulation patent can create an infringement issue even after the basic darunavir compound patent expires. The applicant must assess the patent claims, proposed label, formulation composition, manufacturing process, and any applicable carve-out strategy.

References

1. U.S. Food and Drug Administration. (2024). Prezista (darunavir) prescribing information. Janssen Products, LP.

2. U.S. Food and Drug Administration. (2024). Symtuza (darunavir, cobicistat, emtricitabine, and tenofovir alafenamide) prescribing information. Janssen Products, LP.

3. U.S. Food and Drug Administration. (2024). Prezcobix (darunavir and cobicistat) prescribing information. Janssen Products, LP.

4. U.S. Patent and Trademark Office. (2001). U.S. Patent No. 6,248,775: HIV protease inhibitors. U.S. Department of Commerce.

5. U.S. Food and Drug Administration. (2023). Abbreviated new drug application submissions: ANDAs, pharmaceutical equivalence, and bioequivalence. U.S. Department of Health and Human Services.

6. World Health Organization. (2023). Consolidated guidelines on HIV prevention, testing, treatment, service delivery and monitoring. World Health Organization.

7. National Library of Medicine. (2024). DailyMed: Darunavir, Prezista, Prezcobix, and Symtuza drug labeling. U.S. National Library of Medicine.