ASTAGRAF XL Drug Patent Profile

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When do Astagraf Xl patents expire, and when can generic versions of Astagraf Xl launch?

Astagraf Xl is a drug marketed by Astellas and is included in one NDA.

The generic ingredient in ASTAGRAF XL is tacrolimus. There is one drug master file entry for this compound. Thirty-six suppliers are listed for this compound. Additional details are available on the tacrolimus profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Astagraf Xl

A generic version of ASTAGRAF XL was approved as tacrolimus by SANDOZ on August 10^th, 2009.

Summary for ASTAGRAF XL

US Patents:	0
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	80
Clinical Trials:	10
Drug Prices:	Drug price information for ASTAGRAF XL
What excipients (inactive ingredients) are in ASTAGRAF XL?	ASTAGRAF XL excipients list
DailyMed Link:	ASTAGRAF XL at DailyMed

See drug prices for ASTAGRAF XL

Recent Clinical Trials for ASTAGRAF XL

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

Sponsor	Phase
Shahid Beheshti University of Medical Sciences	NA
University of Colorado, Denver	Early Phase 1
Cedars-Sinai Medical Center	Phase 4

See all ASTAGRAF XL clinical trials

Pharmacology for ASTAGRAF XL

Drug Class	Calcineurin Inhibitor Immunosuppressant
Mechanism of Action	Calcineurin Inhibitors

Paragraph IV (Patent) Challenges for ASTAGRAF XL

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
ASTAGRAF XL	Extended-release Capsules	tacrolimus	0.5 mg, 1 mg, and 5 mg	204096	1	2013-09-24

US Patents and Regulatory Information for ASTAGRAF XL

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-001	Jul 19, 2013	AB	RX	Yes	No
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-002	Jul 19, 2013	AB	RX	Yes	No
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-003	Jul 19, 2013	AB	RX	Yes	Yes

Expired US Patents for ASTAGRAF XL

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-003	Jul 19, 2013	6,576,259
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-001	Jul 19, 2013	8,551,522
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-002	Jul 19, 2013	8,551,522
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-003	Jul 19, 2013	6,884,433
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-001	Jul 19, 2013	6,440,458
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-003	Jul 19, 2013	6,440,458
Astellas	ASTAGRAF XL	tacrolimus	CAPSULE, EXTENDED RELEASE;ORAL	204096-002	Jul 19, 2013	6,440,458

EU/EMA Drug Approvals for ASTAGRAF XL

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Astellas Pharma Europe B.V.	Modigraf	tacrolimus	EMEA/H/C/000954Prophylaxis of transplant rejection in adult and paediatric, kidney, liver or heart allograft recipients.Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult and paediatric patients.	Authorised	no	no	no	2009-05-15
Astellas Pharma Europe BV	Advagraf	tacrolimus	EMEA/H/C/000712Prophylaxis of transplant rejection in adult kidney or liver allograft recipients.Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.	Authorised	no	no	no	2007-04-23
Chiesi Farmaceutici S.p.A.	Envarsus	tacrolimus	EMEA/H/C/002655Prophylaxis of transplant rejection in adult kidney or liver allograft recipients. Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.	Authorised	no	no	no	2014-07-18
LEO Pharma A/S	Protopic	tacrolimus	EMEA/H/C/000374Flare treatmentAdults and adolescents (16 years of age and above)Treatment of moderate to severe atopic dermatitis in adults who are not adequately responsive to or are intolerant of conventional therapies such as topical corticosteroids.Children (two years of age and above)Treatment of moderate to severe atopic dermatitis in children (two years of age and above) who failed to respond adequately to conventional therapies such as topical corticosteroids.Maintenance treatmentMaintenance treatment of moderate to severe atopic dermatitis for the prevention of flares and the prolongation of flare-free intervals in patients experiencing a high frequency of disease exacerbations (i.e. occurring four or more times per year) who have had an initial response to a maximum of six weeks treatment of twice daily tacrolimus ointment (lesions cleared, almost cleared or mildly affected).	Authorised	no	no	no	2002-02-27
Teva B.V.	Tacforius	tacrolimus	EMEA/H/C/004435Prophylaxis of transplant rejection in adult kidney or liver allograft recipients.Treatment of allograft rejection resistant to treatment with other immunosuppressive medicinal products in adult patients.	Authorised	yes	no	no	2017-12-08
Astellas Pharma GmbH	Protopy	tacrolimus	EMEA/H/C/000375Treatment of moderate to severe atopic dermatitis in adults who are not adequately responsive to or are intolerant of conventional therapies such as topical corticosteroids. Treatment of moderate to severe atopic dermatitis in children (2 years of age and above) who failed to respond adequately to conventional therapies such as topical corticosteroids.Maintenance treatment of moderate to severe atopic dermatitis for the prevention of flares and the prolongation of flare-free intervals in patients experiencing a high frequency of disease exacerbations (i.e. occurring 4 or more times per year) who have had an initial response to a maximum of 6 weeks treatment of twice daily tacrolimus ointment (lesions cleared, almost cleared or mildly affected).	Withdrawn	no	no	no	2002-02-28

International Patents for ASTAGRAF XL

See the table below for patents covering ASTAGRAF XL around the world.

Country	Patent Number	Title	Estimated Expiration
Argentina	023299	UNA FORMULACION DE LIBERACION PROLONGADA DE UN COMPUESTO MACRoLIDO
Austria	269075
Austria	464900
Austria	514419
Australia	2856399
Australia	749623
Brazil	9909201

Last updated: July 25, 2026

Astagraf XL market dynamics and financial trajectory (US and major ex-US markets)

Executive summary: Astagraf XL (tacrolimus extended-release capsules; Hikma Pharmaceuticals/Hikma subcontracted distribution in the US; originally developed by Astellas) is a niche, high-barrier calcineurin inhibitor (CNI) branded product tied to long-term use in solid-organ transplant. Market dynamics are shaped by (1) continued competitive pressure from tacrolimus immediate-release and delayed-release regimens, (2) insurer and transplant-center formulary switching within the tacrolimus class, and (3) generic and “authorized generic” risks that depend on Orange Book patent coverage. Financial trajectory in the US has been supported by patient retention and center protocols, but growth is constrained by an aging immunosuppressed population, limited new-to-brand starts, and competitive substitution economics.

How does Astagraf XL make money and what revenue trend does it show?

Featured snippet answer: Astagraf XL revenue is driven by ongoing maintenance dosing in stable kidney transplant recipients and by incremental switches from other tacrolimus formulations through center and payer formularies. The financial trajectory is constrained by (a) slow patient churn in transplant maintenance therapy and (b) competitive substitution within the tacrolimus category.

Revenue drivers specific to Astagraf XL

Key commercial levers typically determine branded tacrolimus extended-release performance:

• Stable maintenance persistence: Transplant maintenance is long-duration, so churn is low unless centers switch regimens due to tolerability, TDM outcomes, or payer policy.
• Therapeutic drug monitoring (TDM) fit: Tacrolimus requires trough monitoring; regimen stability and adherence advantages support continued prescribing where the extended-release profile is favored.
• Payer contracting: Net price depends on rebate intensity, managed-care preferred drug lists, and Medicare Part D formulary status for tacrolimus products.
• Distribution and copay positioning: Patient out-of-pocket costs influence initiation and switching, especially where generics compete on price.

What the demand base looks like

• The relevant treated population is kidney transplant recipients on tacrolimus-based immunosuppression, with Astagraf XL targeting those where extended-release dosing provides adherence or trough stability benefits.
• Uptake is less about “new starts” and more about protocol-driven regimen selection in transplant programs.

What market dynamics affect Astagraf XL versus tacrolimus competitors?

Featured snippet answer: Astagraf XL competes within the tacrolimus landscape. The strongest dynamics are center/payer switching between tacrolimus formulations, timing of generic/brand exclusivity erosion for comparable extended-release or equivalent tacrolimus products, and ongoing utilization management.

Competitive forces that matter

1. Within-class substitution
   • Tacrolimus immediate-release (IR) and other branded tacrolimus products can be clinically acceptable substitutes when centers prioritize cost, titration familiarity, or payer requirements.
2. Health economics
   • Rebates and preferred coverage can quickly re-rank brand vs generic economics after market entry of lower-priced alternatives.
3. Protocol inertia vs protocol change
   • Transplant centers tend to standardize on regimens for operational simplicity. When formulary policies change, conversion can be gradual, creating “stepwise” demand shifts.
4. Adherence and dosing schedule
   • Extended-release regimens can reduce dosing burden or improve trough stability. That advantage translates into stickiness only where monitoring and adherence workflows support it.

Patent and exclusivity risk as a demand factor

• In transplant immunosuppression, demand is highly sensitive to price-per-dose and formulary placement.
• Legal milestones affecting exclusivity and generic entry can create discrete revenue inflection points.

What is the Orange Book status of Astagraf XL and how does it drive generic entry risk?

Featured snippet answer: Orange Book status governs whether generic tacrolimus extended-release products can be approved for “same active ingredient, same dosage form” entry and at what timing. Astagraf XL’s generic entry risk is a function of remaining listed patents covering tacrolimus extended-release formulations, dosage forms, and related method claims.

How Orange Book listings translate into market impact

• If key formulation patents expire later than other tacrolimus products, generics can face timing barriers that preserve brand share and pricing power.
• If fewer enforceable patents remain, Paragraph IV or Section viii carve-out strategies can accelerate price erosion.
• Even when exclusivity exists, authorized generics or “non-interchangeable” positioning can still compress net prices.

Why status matters for financial trajectory

Branded immunosuppressants often experience:

• revenue stability while patents protect formulation and method-of-use aspects,
• then sharp net sales decline post entry due to payer shifts to lower-cost alternatives.

Which tacrolimus products compete most directly with Astagraf XL?

Featured snippet answer: The most direct competitive set is tacrolimus formulations used in kidney transplant immunosuppression that can be substituted by transplant centers, including immediate-release tacrolimus and any other approved tacrolimus extended-release/delayed-release alternatives.

Comparison dimensions that drive share

• Dosing schedule and adherence
• Trough variability and TDM workflow
• Interchangeability and pharmacy benefit design
• Clinical protocol preference and prescriber familiarity

Likely payer decision logic

Payers typically rank tacrolimus options based on:

• contracted net price,
• formulary tier,
• prior authorization criteria,
• step therapy policies,
• and availability of patient support programs.

When does Astagraf XL lose exclusivity and how does that timing affect sales?

Featured snippet answer: The sales impact of exclusivity loss is typically front-loaded around the first scalable generic launch and follow-on erosion via switching, with net revenue decline accelerating after formulary conversion and supply stabilization.

The typical sales curve around exclusivity events

• Pre-event: Revenue holds as prescribers and payers expect branded availability and stable monitoring.
• Launch window: Generic entry can reduce net pricing quickly, even before full switching, via competitive rebates and preferred list pressure.
• Post-switch: Maintenance persistence declines as patients are converted, usually more slowly than initiation because transplant patients are sensitive to regimen changes.

Financial trajectory implications

A staggered exclusivity landscape in the tacrolimus class can produce multiple inflection points:

• first for one competitor’s entry,
• second for later formulation or method claim erosion,
• third for additional generic entrants that intensify rebate competition.

What patent litigation and Paragraph IV risks apply to Astagraf XL?

Featured snippet answer: Paragraph IV challenges and related litigation can accelerate generic availability for tacrolimus products if courts narrow enforceable claims. In tacrolimus, even partial claim invalidation can enable launch under a tighter regulatory strategy.

Commercial significance of litigation outcomes

• Successful generic challenges can drive fast net price compression through formulary changes.
• Settlement agreements often set carve-outs on dosing forms or claim scope, shaping launch timing.
• Injunctions can delay entry and preserve branded economics.

What regulatory pathway does Astagraf XL use and how does it shape market access?

Featured snippet answer: Astagraf XL is approved as a specific tacrolimus extended-release regimen. Market access and substitution are determined by FDA labeling, interchangeability status where applicable, and payer criteria rather than by “class” alone.

Key regulatory factors

• Label indications and dosing: Impacts whether payers treat it as clinically interchangeable with other tacrolimus formulations.
• Pharmacokinetic profile: Extended-release behavior and monitoring guidance influence prescriber acceptance.
• Interchangeability and substitution rules: State and pharmacy-level rules can affect switching pace.

How does the competitive landscape differ in the US versus ex-US markets for Astagraf XL?

Featured snippet answer: Ex-US markets often have different reimbursement structures and generic launch pacing, so pricing erosion can be faster or slower depending on local patent enforcement and reimbursement formularies.

Cross-market dynamics

• US: Net sales are tightly linked to rebate levels and managed care contracting. Generic entry typically drives rapid net price compression.
• EU and other regions: Reimbursement decisions often involve national HTA bodies and negotiated pricing. Patent enforcement strength and local generics ecosystems drive timing.

What commercial levers determine Astagraf XL’s long-term growth potential?

Featured snippet answer: Growth potential is less about expanding the treated population and more about retaining share through protocol adoption, favorable formulary inclusion, and patient support mechanisms that reduce conversion resistance.

Levers that can support share

• Therapeutic differentiation messaging: Focus on trough stability, dosing convenience, and TDM workflow fit.
• Transplant center evidence: Real-world persistence and tolerability outcomes.
• Payer contracting: Preferred formulary placement and rebate structures that protect net price.
• Patient access programs: Copay assistance for eligible patients to reduce non-medical switching.

Levers that constrain growth

• generic price anchors in tacrolimus class,
• limited incremental indication expansion,
• and payer restrictions on non-preferred tacrolimus brands.

How strong is the patent estate for Astagraf XL and what does it mean for net price?

Featured snippet answer: The strength of Astagraf XL’s patent estate determines whether price compression follows generic entry timing. In tacrolimus, enforceable formulation and method claims create periods where branded net price can remain comparatively resilient.

Patent estate impacts on commercialization

• Fewer barriers to generic entry increases the probability of rapid net price compression.
• More barriers sustains higher net price and helps preserve formulary positioning and rebate leverage.

What generic entry risks exist for Astagraf XL and what launch scenarios are most damaging?

Featured snippet answer: The most damaging generic scenarios are those that combine fast FDA approval timing with broad formulary access and interchangeability-like substitution behavior at pharmacy and center levels.

High-impact launch scenarios

• Early entry of a fully substitutable tacrolimus extended-release product
• Multiple entrants, driving rebate wars and fast switching
• Settlement designs that allow near-immediate launch after a short delay

Lower-impact scenarios

• entry limited by specific claim scopes that constrain substitutability,
• narrow label carve-outs that maintain prior authorization requirements.

Astagraf XL financial sensitivity: what changes after a competitor launch?

Featured snippet answer: Branded tacrolimus revenue is sensitive to net price changes rather than unit demand because maintenance populations shift gradually. The largest near-term impact comes from rebate and tier placement changes once generics enter.

Expected post-launch pattern

• Net price declines quickly as payers renegotiate,
• unit demand declines more slowly depending on center switching rates,
• long-term revenue stabilizes only if branded differentiates strongly on outcomes or gets protected through contracting.

Key Takeaways

• Astagraf XL’s market position depends on long-duration maintenance use, payer formulary placement, and transplant center protocol inertia.
• Financial trajectory is shaped primarily by generic and settlement timing, and by within-class tacrolimus substitution economics.
• The Orange Book patent and exclusivity posture is the central determinant of net price resilience versus stepwise revenue erosion after generic entry.
• Growth is structurally constrained; the main upside is share retention through contracting and evidence-driven protocol adoption.

FAQs

1. How do payer formulary tiers change tacrolimus extended-release sales after generic entry?
2. What settlement terms in tacrolimus Paragraph IV cases most directly influence launch timing and net price compression?
3. Do transplant centers switch stable patients from tacrolimus extended-release to immediate-release quickly after competitors enter?
4. How does therapeutic drug monitoring trough variability affect prescriber preference between tacrolimus formulations?
5. Which dosing and labeling constraints most limit generic substitution for tacrolimus extended-release products?

References (APA)

1. FDA. Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. U.S. Food and Drug Administration.
2. FDA. Drugs@FDA (Astagraf XL and related tacrolimus products). U.S. Food and Drug Administration.
3. FDA. Therapeutic Equivalence Evaluations (Orange Book help content and TE methodology). U.S. Food and Drug Administration.