Details for Patent: 7,776,838
Which drugs does patent 7,776,838 protect, and when does it expire?
Patent 7,776,838 protects VISTOGARD and is included in one NDA.
This patent has one hundred and seventy-five patent family members in twenty-one countries.
Summary for Patent: 7,776,838
| Title: | Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides | ||||||||||||||||||||||||||||||||||||||||||||||||
| Abstract: | The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents. Disclosed are acylated derivatives of non-methylated pyrimidine nucleosides. These compounds are capable of attenuating damage to the hematopoietic system in animals receiving antiviral or antineoplastic chemotherapy. | ||||||||||||||||||||||||||||||||||||||||||||||||
| Inventor(s): | Reid W. von Borstel, Michael K. Bamat | ||||||||||||||||||||||||||||||||||||||||||||||||
| Assignee: | BTG International Inc | ||||||||||||||||||||||||||||||||||||||||||||||||
| Application Number: | US08/460,186 | ||||||||||||||||||||||||||||||||||||||||||||||||
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Patent Claim Types: see list of patent claims | Use; | ||||||||||||||||||||||||||||||||||||||||||||||||
| Patent landscape, scope, and claims: | US Patent 7,776,838: Claim Scope, Uridine Triacetate Protection and Patent LandscapeUS Patent 7,776,838 covers methods of reducing toxicity caused by pyrimidine nucleoside analogs through administration of an acylated uridine or cytidine derivative. Its commercial significance centers on triacetyluridine, also known as uridine triacetate, the active ingredient in Vistogard. The patent is a method-of-treatment patent. It does not broadly claim uridine triacetate as a chemical compound, a finished pharmaceutical composition, or every use of the compound. Its core requirement is the administration of a listed acylated nucleoside to treat toxicity caused by a listed pyrimidine analog, particularly 5-fluorouracil and AZT. The claim set also covers combinations with metabolic inhibitors, nucleoside-transport inhibitors, hematopoietic agents and uptake-enhancing agents. What does US Patent 7,776,838 protect?The patent protects a treatment protocol with four principal elements:
Claim 1 is the independent claim. Claims 2 through 11 narrow the treatment by specifying the affected tissue, rescue agents, active ingredients and toxic agents.
How broad is claim 1?Claim 1 is broad in the number of covered toxic agents but narrower than a general claim to treating toxicity with uridine triacetate. The listed toxic agents include:
The claim is a closed Markush claim. A product or treatment involving a compound outside the listed pyrimidine analogs would not automatically fall within claim 1. The same limitation applies to the antidote: the claim identifies triacetyluridine, ethoxycarbonyluridine and triacetylcytidine rather than every acylated nucleoside. The claim also requires treatment of toxicity involving hematopoietic or mucosal tissue. Toxicity affecting another organ system, standing alone, presents a weaker literal infringement case unless the treatment also addresses one of those claimed tissue injuries. What does claim 9 protect?Claim 9 narrows claim 1 to triacetyluridine. It is commercially important because triacetyluridine is the active ingredient in Vistogard. The claim still incorporates the other limitations of claim 1. It therefore requires:
Claim 9 does not cover every administration of uridine triacetate. Administration for an unrelated metabolic condition, for example, would not satisfy the claim unless the required toxicity and causative analog limitations are present. What does claim 10 protect for 5-FU?Claim 10 is the most commercially relevant narrow claim for fluoropyrimidine rescue. It covers triacetyluridine administered to treat toxicity caused by 5-FU. The claim does not expressly require:
Those limitations may appear in the FDA-approved labeling, clinical protocols or later patents, but they are not stated in claim 10 as provided. Claim 10 can therefore reach a broad range of triacetyluridine rescue protocols for 5-FU toxicity, provided the treatment is directed to hematopoietic or mucosal injury. What does claim 11 protect for AZT?Claim 11 covers triacetyluridine for AZT-induced hematopoietic toxicity. AZT, or zidovudine, was historically associated with bone-marrow suppression, including anemia and neutropenia. The claim is narrow because it requires all of the following:
The claim does not cover AZT toxicity generally if the injury is limited to a non-hematopoietic tissue. How do claims 4 through 8 affect infringement risk?Claims 4 through 8 add optional co-therapies. They are dependent claims and require the limitations of claim 1 plus the specified additional agent. Claim 4: uridine phosphorylase inhibitionClaim 4 covers co-administration of triacetyluridine, ethoxycarbonyluridine or triacetylcytidine with one of several uridine phosphorylase inhibitors. The technical objective is to slow degradation of uridine or increase systemic exposure. A product does not need to include one of these inhibitors to infringe claim 1, 9 or 10. The inhibitors matter only for claim 4. Claim 5: cytidine deaminase inhibitionClaim 5 requires triacetylcytidine and a cytidine deaminase inhibitor, including tetrahydrouridine or tetrahydro-2'-deoxyuridine. It does not cover triacetyluridine under the literal wording. Claim 6: nucleoside transport inhibitionClaim 6 covers combination treatment with dipyridamole, probenecid, lidoflazine or nitrobenzylthioinosine. The claim targets cellular transport and tissue distribution rather than the antidote alone. Claim 7: hematopoietic supportClaim 7 covers co-administration of hematopoietic agents, including interleukins, granulocyte colony-stimulating factor, granulocyte-macrophage colony-stimulating factor, stem-cell factor, erythropoietin, glucan and polyinosine-polycytidine. Claim 8: cellular uptake enhancementClaim 8 covers insulin or an insulinogenic carbohydrate administered with the claimed antidote. The intended mechanism is increased nucleoside uptake or phosphorylation. These dependent claims add technical breadth to the patent family but are less likely than claim 10 to define the primary commercial boundary around Vistogard. Is US 7,776,838 a formulation patent?No. Based on the provided claims, US 7,776,838 is principally a therapeutic-use patent. It does not claim:
A competing product could avoid the patent's formulation-related exposure by using a different composition, but a different formulation would not avoid infringement if the product is administered for the claimed 5-FU toxicity treatment. This distinction is central to generic and 505(b)(2) analysis. A formulation patent may be avoided through design-around chemistry or excipient selection. A method patent requires a different strategy, such as a non-infringing label, an ANDA section viii carve-out where available, or an invalidity and non-infringement position. What is the FDA status of uridine triacetate?The FDA approved Vistogard, containing uridine triacetate, for emergency treatment of adults and children who:
The approved product is orally administered. The FDA indication aligns closely with claims 9 and 10, although the label contains clinical timing and eligibility restrictions not expressly recited in those claims.[1] Capecitabine is converted to 5-FU in vivo. The patent claims expressly list 5-FU but, based on the claim text supplied, do not expressly list capecitabine. This creates an important claim-scope distinction. Treatment of capecitabine toxicity may be supported by the FDA label and by later patent claims or infringement theories involving conversion to 5-FU, but literal coverage under claim 10 depends on how the causative pyrimidine analog limitation is construed. What is the Orange Book status?The FDA Orange Book is the controlling source for patents submitted by an NDA holder and listed against an approved drug product. Orange Book listing does not establish validity or infringement. It creates procedural consequences for ANDA applicants, including notice and potential Hatch-Waxman litigation.[2] For Vistogard, the relevant analysis should separate:
US 7,776,838 should not be treated as the entire Vistogard estate. Later patents may cover specific uses, dosing windows, formulations or manufacturing aspects. A freedom-to-operate review must reconcile the patent's continuity data, terminal disclaimers, patent-term adjustment, Orange Book listing and any later-issued family members. When does US 7,776,838 lose exclusivity?Patent expiration cannot be determined from the issue date alone. The relevant calculation uses the earliest effective nonprovisional filing date in the priority chain, adjusted for patent-term adjustment, terminal disclaimers and any applicable patent-term extension. The controlling records are:
The patent issued on August 17, 2010, but its term does not ordinarily run 20 years from issuance.[3] A business launch analysis should therefore use the USPTO term record rather than an issue-date calculation. Any Orange Book patent-term extension applies only to the qualifying regulatory patent and only to the approved product and statutory scope. Which companies are challenging Vistogard exclusivity?The central competitive threat is a generic or 505(b)(2) applicant seeking approval of oral uridine triacetate. The relevant pathway depends on whether the applicant seeks:
A Paragraph IV certification would create litigation risk if an unexpired listed patent covers the proposed product or labeled use. A section viii strategy could be more viable if the applicant omits the patented emergency-rescue indication and markets for a non-patented use. That strategy is constrained if the product's practical commercial value depends on the Vistogard indication. No reliable conclusion about a current challenger, settlement or launch date follows from the claim text alone. Litigation and settlement positions must be checked against PACER, FDA ANDA records and the current Orange Book. How strong is the patent estate?The patent has meaningful historical strength because it captures the therapeutic concept that became the basis for uridine triacetate rescue of fluoropyrimidine toxicity. Its strongest commercial position is claim 10, which directly links triacetyluridine to 5-FU toxicity. Its limitations are equally clear:
The patent is stronger against a product marketed with the patented rescue indication than against a product sold without that use. Label content, physician behavior and induced-infringement evidence would be central in any generic dispute. What generic launch scenarios exist?Scenario 1: Launch after all relevant patents expireThis is the lowest-risk scenario. The applicant can market the product for the approved rescue indication without relying on a carve-out, subject to regulatory approval and non-patent exclusivities. Scenario 2: Section viii carve-outThe applicant removes a patented use from its labeling. This approach is commercially difficult where the protected use is the principal or only market for uridine triacetate. Scenario 3: Paragraph IV challengeThe applicant certifies that listed patents are invalid, unenforceable or not infringed. The NDA holder may sue within the statutory period, potentially triggering a 30-month stay. Scenario 4: 505(b)(2) launchA 505(b)(2) applicant could seek approval based on Vistogard data while pursuing a different formulation, dosing presentation or use. This route does not eliminate patent risk and may require certifications or patent statements under the FDA rules. What licensing and commercial issues matter?Vistogard's commercial value is concentrated in emergency rescue of 5-FU and capecitabine toxicity. The relevant assets include:
A licensee evaluating the estate should verify ownership and chain of title, including assignments involving the original inventors, Wellstat-related entities and any later asset purchasers. A license limited to US 7,776,838 may not provide freedom to commercialize Vistogard if later patents cover the approved use, dosage or formulation. Key Takeaways
FAQsDoes US 7,776,838 cover Vistogard?It covers a core method of using triacetyluridine to treat specified toxicity caused by 5-FU and other listed pyrimidine analogs. It does not, based on the supplied claims, claim every use or formulation of Vistogard. Does the patent cover capecitabine toxicity?Capecitabine is not expressly listed in the supplied claims. Coverage may depend on claim construction, conversion of capecitabine to 5-FU, later patent claims and the specific treatment label. Can a generic avoid this patent by changing the tablet formulation?No, not if the generic still practices the claimed treatment method. A formulation change may avoid a formulation patent but does not by itself avoid a method claim. Is uridine triacetate the same as triacetyluridine?Yes. Uridine triacetate and triacetyluridine are names used for the same active pharmaceutical ingredient in Vistogard. What evidence would be important in a Vistogard patent dispute?The decisive records would include the patent's prosecution history, priority chain, term-adjustment record, Orange Book listings, ANDA labeling, Paragraph IV notice, clinical-use evidence and any later patent-family claims. References
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Drugs Protected by US Patent 7,776,838
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Btg Intl | VISTOGARD | uridine triacetate | GRANULE;ORAL | 208159-001 | Dec 11, 2015 | RX | Yes | Yes | 7,776,838 | ⤷ Start Trial | EMERGENCY TREATMENT OF ADULT & PEDIATRIC PATIENTS FOLLOWING FLUOROURACIL OR CAPECITABINE OVERDOSE,OR WHO EXHIBIT EARLY-ONSET,SEVERE OR LIFE-THREATENING CARDIAC OR CNS TOXICITY OR UNUSUALLY SEVERE ADVERSE REACTIONS WITHIN 96 HOURS | ⤷ Start Trial | ||||
| >Applicant | >Tradename | >Generic Name | >Dosage | >NDA | >Approval Date | >TE | >Type | >RLD | >RS | >Patent No. | >Patent Expiration | >Product | >Substance | >Delist Req. | >Patented / Exclusive Use | >Submissiondate |
International Family Members for US Patent 7,776,838
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Austria | 142221 | ⤷ Start Trial | |||
| Austria | 179615 | ⤷ Start Trial | |||
| Austria | 205850 | ⤷ Start Trial | |||
| Austria | 243039 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
