Details for Patent: 8,071,577

Which drugs does patent 8,071,577 protect, and when does it expire?

Patent 8,071,577 protects NATAZIA and is included in one NDA.

This patent has forty-three patent family members in thirty-seven countries.

Summary for Patent: 8,071,577

Title:	Multi-phase contraceptive preparation based on a natural estrogen
Abstract:	The multiphase preparation having higher contraceptive safety and reduced side effects is based on a combination of a natural oestrogen with dienogest or drospirenone. The multiphase preparation is characterized by a first phase consisting of 2 daily dose units of 3 mg of oestradiol valerate, a second phase consisting of 2 groups of daily dose units, wherein a first group is formed by 5 daily dose units each containing a combination of 2 mg of oestradiol valerate and at least two or three times an ovulation-inhibitory dose of dienogest or drospirenone and a second group is formed by 17 daily dose units each containing a combination of 2 mg of oestradiol valerate and at least three or four times the ovulation-inhibitory dose of dienogest or drospirenone, a third phase consisting of 2 daily dose units of 1 mg of oestradiol valerate, and a further phase consisting of 2 daily dose units of pharmaceutically acceptable placebo.
Inventor(s):	Jan Endrikat, Bernd Duesterberg
Assignee:	Bayer Intellectual Property GmbH
Application Number:	US11/578,771
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,071,577
Patent Claim Types: see list of patent claims	Use;

United States Patent 8,071,577: Scope, Claims, Expiration and Patent Landscape for Estradiol Valerate/Dienogest Contraception

U.S. Patent No. 8,071,577 protects the 28-day multiphasic contraceptive regimen used for Bayer’s Natazia product in the United States. Its central limitation is the exact daily sequence of estradiol valerate and dienogest doses:

• 2 days of 3 mg estradiol valerate;
• 5 days of 2 mg estradiol valerate plus 2 mg dienogest;
• 17 days of 2 mg estradiol valerate plus 3 mg dienogest;
• 2 days of 1 mg estradiol valerate; and
• 2 placebo days.

The patent contains product claims and a method-of-use claim. It does not broadly cover every estradiol valerate/dienogest contraceptive. Its commercial value depends on whether a competing product reproduces the protected 28-day sequence and whether the patent remains enforceable against the proposed launch.

What does U.S. Patent 8,071,577 protect?

The patent protects a defined multiphase oral contraceptive schedule, not merely the use of estradiol valerate or dienogest as contraceptive ingredients.

Claim	Claim category	Principal protected subject matter
1	Product	Multiphase contraceptive product containing specified dosage units and phases
2	Oral product	Multiphase oral contraceptive containing the same regimen
3	Method of treatment	Oral administration of the exact five-step 28-day sequence

The claims use “comprising,” which generally makes them open-ended. A product may contain additional components, excipients, packaging elements, or inactive ingredients, provided that it still contains the claimed dosage units and sequence. The open transition does not eliminate the requirement to satisfy every expressly recited dosage limitation.

The patent’s practical center is Claim 2 for a packaged oral product and Claim 3 for administration of the regimen. Claim 1 is broader than Claim 2 because it does not expressly require the dosage units to be oral.

How does the patented 28-day regimen work?

The regimen is divided into four phases, although the second phase has two dose groups:

Phase	Duration	Estradiol valerate per unit	Dienogest per unit	Function in claim structure
1	2 days	3 mg	None recited	Initial high estradiol valerate phase
2A	5 days	2 mg	2 mg	First combined-hormone group
2B	17 days	2 mg	3 mg	Second combined-hormone group
3	2 days	1 mg	None recited	Reduced estradiol valerate phase
4	2 days	None recited	None recited	Placebo phase
Total	28 days			Complete cycle

The claims require the sequence, not merely the aggregate amounts. A product containing the same total quantity of estradiol valerate and dienogest but distributing those ingredients differently would not literally meet the claims.

The sequence totals 52 mg of estradiol valerate and 61 mg of dienogest per 28-day cycle:

• Estradiol valerate: 6 mg + 10 mg + 34 mg + 2 mg = 52 mg.
• Dienogest: 10 mg + 51 mg = 61 mg.

Those totals do not replace the day-by-day limitations. A formulation with the same aggregate amounts but a different phase structure presents a stronger non-infringement position.

What are the limitations of Claim 1?

Claim 1 covers a “multiphase product for contraception” containing the four recited phases. Its principal limitations are:

1. Two units containing 3 mg estradiol valerate each.
2. Five units containing 2 mg estradiol valerate and 2 mg dienogest each.
3. Seventeen units containing 2 mg estradiol valerate and 3 mg dienogest each.
4. Two units containing 1 mg estradiol valerate each.
5. Two units containing a pharmaceutically acceptable placebo.

Claim 1 does not expressly state that the product is oral. It also does not expressly require a blister pack, a calendar package, a particular order of presentation, a particular excipient, or a particular dissolution profile.

The word “phase” creates a potential claim-construction issue. A generic product that contains all 28 units but presents them in a different physical package could argue that it does not contain the claimed phases. That position would be weaker if the units are designed and labeled for administration in the claimed order.

What does Claim 2 add?

Claim 2 is directed specifically to a “multiphase oral contraception product” and refers to daily oral dosage units. It therefore narrows Claim 1 through the oral-administration limitation.

Claim 2 is relevant to:

• Blister-pack products;
• Calendar-dose oral contraceptives;
• Oral tablets or capsules arranged in the claimed sequence; and
• Products labeled for the same 28-day administration schedule.

A competing product would generally need to avoid at least one required feature to establish a credible design-around. Potential distinctions include:

• Different numbers of days in one or more phases;
• Different hormone strengths;
• A different order of the phases;
• Omission of placebo units;
• Use of a different progestin;
• Use of a different estrogen;
• A continuous regimen without the claimed two placebo days; or
• A dosage form that is not an oral product.

Changing only excipients, tablet color, packaging artwork, or trade dress would not address the core claim limitations.

What does Claim 3 cover?

Claim 3 is a method-of-oral-contraception claim. It requires administration to a woman in the stated sequence:

1. One 3 mg estradiol valerate unit daily for two days;
2. One 2 mg estradiol valerate/2 mg dienogest unit daily for five days;
3. One 2 mg estradiol valerate/3 mg dienogest unit daily for 17 days;
4. One 1 mg estradiol valerate unit daily for two days; and
5. One placebo unit daily for two days.

Claim 3 is narrower in some respects than a composition claim because it requires the claimed administration. It may still be commercially important because a product label that instructs patients to follow the claimed regimen can create method-of-use exposure.

For a generic applicant, a label that reproduces the Natazia dosing instructions would create a direct infringement risk if the patent remains enforceable. A proposed label that omits or changes the patented regimen could reduce literal infringement risk, but regulatory requirements and induced-infringement theories would remain relevant.

When does U.S. Patent 8,071,577 expire?

The patent’s ordinary United States term is tied to its effective nonprovisional filing date in November 2005. The expected expiration is in November 2025, subject to any applicable patent term adjustment, patent term extension, terminal disclaimer, or other USPTO-record event.

Event	Date or status
Earliest priority basis	November 22, 2004, foreign priority
U.S. application filing	November 2005
Patent grant	December 6, 2011
U.S. patent term	Generally 20 years from the effective U.S. nonprovisional filing date
Expected ordinary expiration	November 2025
Patent term extension	No extension is established by the claim text alone
Post-expiration status	Claims generally cease to block new commercial activity after expiration, subject to accrued rights and other patents

Foreign priority does not ordinarily start the 20-year U.S. patent term. The relevant U.S. filing and Patent Term Adjustment data must be confirmed in the USPTO patent record. The grant date does not determine expiration.

What is the Orange Book status of Patent 8,071,577?

U.S. Patent 8,071,577 has been associated with the Natazia oral contraceptive, marketed by Bayer. Natazia is listed in the FDA Orange Book under NDA 022252 and contains estradiol valerate and dienogest as its active ingredients. The product is an FDA-approved combined oral contraceptive with a four-phase dosing structure that corresponds to the patented regimen.[2][3]

The Orange Book listing is commercially important because it provides the patent certification framework for an ANDA applicant. A generic applicant seeking approval before listed patent expiration would generally need to submit one of the certifications under 21 U.S.C. § 355(j)(2)(A)(vii), including a Paragraph IV certification alleging that the patent is invalid, unenforceable, or not infringed.

Orange Book listing does not establish validity. It identifies the patent information submitted for the approved drug and determines part of the ANDA review and litigation framework.

What Paragraph IV challenges could target this patent?

A Paragraph IV challenge to Patent 8,071,577 would likely focus on one or more of the following grounds:

Anticipation

A challenger could argue that a single prior-art reference disclosed the complete 28-day sequence, including every dose and placebo phase. Partial disclosure would not ordinarily establish anticipation of the full claim.

The exact combination of:

• 3 mg estradiol valerate for two days;
• 2 mg/2 mg for five days;
• 2 mg/3 mg for 17 days;
• 1 mg estradiol valerate for two days; and
• two placebo days

is the key anticipation hurdle.

Obviousness

Obviousness would likely be the primary validity issue. A challenger could combine prior-art teachings relating to:

• Estradiol valerate contraceptive regimens;
• Dienogest-containing oral contraceptives;
• Triphasic or multiphasic dosing;
• Hormone reduction during the final active days; and
• Placebo intervals.

The patent owner would argue that the exact phase durations, hormone strengths, and sequence produced a non-obvious regimen and that prior art did not provide a reasoned basis to select the claimed combination with a reasonable expectation of success.

Written description and enablement

These grounds appear less central because the patent claims a concrete dosing regimen and the commercial product corresponds to it. A challenger could still examine whether the specification supports the full breadth of “multiphase product” and whether the disclosed data support the claimed contraceptive method.

Indefiniteness and claim construction

Potential disputes could concern the meaning of:

• “Phase”;
• “Daily dosage unit”;
• “Group”;
• The order of the phases;
• Whether the product must be packaged in the claimed sequence; and
• Whether a dosage unit may contain additional active or inactive ingredients.

The claim’s highly specific numerical structure may limit broad indefiniteness arguments, but the packaging and sequencing terms can affect infringement analysis.

What formulation patents protect Natazia?

Patent 8,071,577 is primarily a regimen patent. It does not, on its face, require a particular tablet coating, excipient, dissolution profile, manufacturing process, blister configuration, or release technology.

That distinction matters. A competitor that copies the active-ingredient sequence but uses different excipients may still face infringement risk under the regimen claims. Conversely, a competitor that avoids the exact sequence may not infringe this patent even if its tablets have the same appearance or use similar manufacturing methods.

The broader Natazia patent landscape may include separate patents or applications directed to:

• Pharmaceutical compositions;
• Estradiol valerate/dienogest combinations;
• Regimen design;
• Manufacturing and formulation processes;
• Packaging and administration schedules; and
• Related family members in other jurisdictions.

Those rights must be assessed separately. Patent 8,071,577 should not be treated as a proxy for every Bayer patent relating to Natazia.

How strong is the patent estate?

Patent 8,071,577 has a mixed strength profile.

Factor	Assessment
Claim specificity	High; the regimen is defined by exact strengths and durations
Design-around difficulty	Moderate; changing one phase can avoid literal scope
Product-label exposure	High if the generic label reproduces the Natazia schedule
Formulation dependence	Low; the claims do not require a distinctive excipient system
Prior-art exposure	Material; multiphasic contraceptive regimens and hormone combinations were known technical areas
Remaining term	Limited, with expected expiration in November 2025
Biosimilar relevance	None; Natazia is a small-molecule drug, not a biologic
Manufacturing barrier	Low to moderate; the dosage forms are conventional oral units
Commercial blocking value	Concentrated in the exact regimen and label

The patent is stronger against a direct copy of the Natazia 28-day product than against a product using a materially different schedule. Its expiration timing also reduces the value of prolonged litigation unless the challenger seeks an earlier launch or the patent owner relies on other listed patents.

Which companies are likely to challenge the patent?

Generic oral contraceptive manufacturers that may pursue an ANDA for estradiol valerate/dienogest products include large U.S. generic companies and specialty women’s-health manufacturers. A definitive list of challengers requires current FDA ANDA records, Paragraph IV notices, district-court dockets, and Orange Book updates.

The relevant competitive set includes companies with existing oral contraceptive portfolios, including manufacturers of generic levonorgestrel/ethinyl estradiol, drospirenone/ethinyl estradiol, norethindrone/ethinyl estradiol, and other combination products. Prior experience with oral contraceptive bioequivalence does not eliminate the need to reproduce or design around the exact Natazia regimen.

What generic launch scenarios exist?

Launch after patent expiry

This is the lowest-litigation-risk path if no other enforceable patent blocks approval. A generic could seek approval for the same active ingredients and dosage schedule, subject to ANDA requirements and product-specific exclusivity.

Paragraph IV launch

An ANDA applicant could challenge the patent and launch after the statutory litigation stay expires or after prevailing in litigation. A Paragraph IV notice generally triggers the possibility of patent litigation and a 30-month stay of approval under the Hatch-Waxman framework, subject to statutory exceptions.[4]

Label-based design-around

A generic could seek approval for a different estradiol valerate/dienogest schedule. This approach may avoid Claim 3, but it raises separate regulatory questions concerning therapeutic equivalence, labeling, clinical bridging, and whether the product can be approved as a generic version of Natazia.

Authorized generic or settlement

Bayer could license, settle with, or otherwise coordinate a generic launch date. Settlement terms may include a launch date, supply arrangement, license rights, or restrictions tied to other patents. No settlement terms should be inferred from the patent text.

Are biosimilar risks relevant?

No. Estradiol valerate and dienogest are small-molecule active pharmaceutical ingredients. A competing product would use the ANDA pathway rather than the biosimilar pathway under the Public Health Service Act.

The relevant regulatory risks are:

• Pharmaceutical equivalence;
• Bioequivalence;
• Same active ingredients;
• Same dosage form and strength;
• Labeling requirements;
• Patent certification; and
• Potential substitutability under state pharmacy law.

How does Natazia compare with competing contraceptives?

Product category	Active ingredients	Regimen characteristic	Patent risk compared with 8,071,577
Natazia	Estradiol valerate/dienogest	Four-phase, 28-day schedule	Directly implicated
Generic monophasic oral contraceptives	Various estrogen/progestin combinations	Same-dose active tablets	Generally outside this patent
Yaz-type products	Ethinyl estradiol/drospirenone	Typically monophasic	Different active ingredients
Nextstellis	Estetrol/drospirenone	Different estrogen and progestin	Outside the core claims
Extended-cycle products	Various combinations	Fewer withdrawal bleeds	Different schedule and often different ingredients
Progestin-only products	Progestin only	No estradiol valerate	Outside the claims

Patent 8,071,577 is therefore product-specific rather than a broad platform patent for oral contraception.

What is the commercial exposure?

Bayer has not generally reported Natazia revenue as a separately disclosed public line item. Revenue exposure should therefore be estimated from prescription volume, net pricing, market share, payer coverage, and the timing of generic entry rather than from a separately reported Natazia sales figure.

The commercial impact of generic entry could exceed the value of the single patent because Natazia faces substitution pressure from lower-cost contraceptives with different active ingredients. The product’s differentiated feature is its estradiol valerate/dienogest combination and multiphasic regimen, but that differentiation may not prevent therapeutic substitution where prescribers and payers favor lower-cost alternatives.

What geographic protection exists?

The U.S. patent protects activity within the United States, including the making, using, offering for sale, selling, or importing of products covered by an enforceable claim under 35 U.S.C. § 271.

Corresponding patent-family rights may exist in Europe and other jurisdictions, but foreign rights must be analyzed independently. Expiration dates, claim scope, opposition history, supplementary protection certificates, and national enforcement outcomes differ by country.

The commercial brand Qlaira is marketed outside the United States, while Natazia is the U.S. product name. International patent rights should not be assumed to have the same scope or remaining term as U.S. Patent 8,071,577.

Key Takeaways

• U.S. Patent 8,071,577 protects the exact Natazia-style 28-day estradiol valerate/dienogest regimen.
• Claims 1 and 2 cover the multiphase product; Claim 3 covers administration of the sequence.
• The required schedule is 2/5/17/2/2 days with hormone strengths of 3 mg, 2 mg/2 mg, 2 mg/3 mg, 1 mg, and placebo.
• The patent does not broadly cover all estradiol valerate contraceptives or all dienogest combinations.
• The expected ordinary U.S. expiration is in November 2025, subject to official USPTO term-adjustment data.
• The principal Paragraph IV issues are obviousness, anticipation, sequencing, and the construction of “phase” and “daily dosage unit.”
• The patent is more effective against a direct Natazia copy than against a materially different dosing schedule.
• Biosimilar law is not relevant because Natazia is a small-molecule product.
• Generic entry depends on Orange Book certifications, any Hatch-Waxman litigation, other listed patents, and FDA approval timing.
• Product-specific Natazia revenue is not generally separately disclosed by Bayer.

Frequently Asked Questions

Does Patent 8,071,577 cover estradiol valerate by itself?

No. The claims require a specified multiphase regimen. Estradiol valerate products using different strengths, timing, or phase structures may fall outside the patent.

Does changing the placebo tablets avoid infringement?

Not necessarily. Claim 3 requires placebo administration, while the product claims require placebo dosage units. Replacing placebo tablets with no tablets may avoid some product-claim limitations, but the full product and label must be analyzed.

Is dienogest protected independently by this patent?

No. The patent protects dienogest as part of the claimed estradiol valerate/dienogest dosage sequence. It does not create a general monopoly over dienogest.

Can a generic use the same active ingredients with a different schedule?

Potentially, but regulatory approval would require support for the proposed product and labeling. A different schedule may reduce infringement risk while creating bioequivalence and approval issues.

Does patent expiration automatically permit generic substitution?

No. Patent expiration removes the blocking effect of that patent, but FDA approval, Orange Book status, other patents, exclusivity, manufacturing compliance, and state substitution rules still affect launch and substitution.

References

1. United States Patent and Trademark Office. (2011). U.S. Patent No. 8,071,577, Pharmaceutical composition for oral contraception.
2. U.S. Food and Drug Administration. (2010). Natazia prescribing information. Bayer HealthCare Pharmaceuticals Inc.
3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. United States Code. (2024). 21 U.S.C. § 355: New drugs.
5. United States Code. (2024). 35 U.S.C. §§ 154 and 271: Patent term and infringement.

Drugs Protected by US Patent 8,071,577

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	NATAZIA	dienogest; estradiol valerate	TABLET;ORAL	022252-001	May 6, 2010		RX	Yes	Yes	8,071,577		Y			PREVENTION OF PREGNANCY

Foreign Priority and PCT Information for Patent: 8,071,577

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	10 2004 019 743	Apr 20, 2004

PCT Information
PCT Filed	April 15, 2005	PCT Application Number:	PCT/EP2005/004022
PCT Publication Date:	November 03, 2005	PCT Publication Number:	WO2005/102247

International Family Members for US Patent 8,071,577

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	048830
Argentina	084229
Austria	E473734
Australia	2005235418