US Patent 10,456,399: Scope, Claim Strength, and Landscape
US Patent 10,456,399 is a method-of-treatment patent for cancer defined by tumor type and by a renal-function gating criterion (creatinine clearance) coupled to an oral dosing regimen of a two-component drug combination. The claims are tightly drafted around: (i) identifying patients by creatinine clearance, (ii) administering an oral combination of α,α,α-trifluorothymidine (FTD) with 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride, (iii) limiting the FTD-equivalent dose to a narrow mg/m²/day range and (iv) prescribing specific fractionation and cycle schedules.
What is claimed at the core? (Independent claim scope)
Claim 1: Principal scope elements
Claim 1 requires all of the following in combination:
- Method: treating cancer
- Cancer types covered (via claim 1 itself and then later dependent claim narrowing):
- “one of gastrointestinal cancer, large bowel cancer and breast cancer”
- Patient selection by renal function:
- detecting creatinine clearance
- administering only when creatinine clearance is < 30 mL/min
- Route:
- Product being administered:
- a combination drug comprising:
- FTD (α,α,α-trifluorothymidine)
- 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride
- Molar ratio:
- FTD : other component = 1 : 0.5
- Dose:
- 30 to 40 mg/m²/day as FTD-equivalent
- Fractionation:
- dose is divided into 2 to 4 portions
Functional takeaway: Claim 1 is not a broad “use of FTD in renal impairment.” It is a specific treatment workflow and specific regimen tied to creatinine clearance thresholds, dosing limits, and division of daily dosing into multiple portions.
How are creatinine clearance boundaries used to limit or structure infringement?
Claim 2: Range refinement by creatinine clearance band
Claim 2 depends on claim 1 and requires:
- creatinine clearance 15 mL/min or more
- creatinine clearance 29 mL/min or less
- (still in the setting of the same combination drug, oral administration, and core dosing framework of claim 1)
Infringement implication: The independent claim covers < 30 mL/min broadly, while claim 2 narrows to 15 to 29 mL/min. That gives the patentee layered coverage:
- a broad base (claim 1)
- narrower bands (claim 2 and other dependent scheduling claims)
What does the claim set do with dose (mg/m²/day) and fractionation?
Claim 3 and Claim 10: High-end daily dose and division
Claim 3 depends from claim 1 and requires:
- 40 mg/m²/day as FTD-equivalent
- divided into two portions
Claim 10 depends from claim 2 and mirrors this:
- 40 mg/m²/day as FTD-equivalent
- divided into two portions
Scope logic:
- Claim 1 allows 30–40 mg/m²/day with 2–4 portions
- Claims 3 and 10 lock to the upper dose point and a specific fractionation pattern (two portions)
What does the claim set do with cycle schedule (days-on/days-off)?
Claim 4 and Claim 11: Weekly cycle pattern
Claim 4 depends from claim 1 and requires:
- administration schedule: 5-day consecutive oral administrations
- followed by 2-day rest
- per week
Claim 11 depends from claim 2 and requires the same weekly pattern.
Claim 5 and Claim 12: 2 cycles then longer rest
Claim 5 depends from claim 1 and requires:
- the 5-day on + 2-day rest schedule
- repeated twice
- followed by rest for 14 days
Claim 12 depends from claim 2 and includes the same long-rest structure.
Scope logic: These schedule-dependent claims convert “oral dosing of a combination” into a specific treatment cycle that is easier to match to actual clinical protocols.
How is cancer type used to broaden or narrow coverage?
Claims 6–9 cover cancer-type variants; Claims 13–16 and 19–22 cover analogous variants tied to claims 2 and 3; Claims 23–26 and 27–30 cover analogous variants tied to scheduling claims.
Cancer-type coverage map
Across the dependent claim set, the cancer types repeatedly appear as:
- gastrointestinal cancer (broad umbrella)
- large bowel cancer (subset)
- breast cancer (separate category)
Representative dependencies:
- Claim 6: gastrointestinal or breast (for claim 1 framework)
- Claim 7: large bowel
- Claim 8: gastrointestinal
- Claim 9: breast
The same pattern repeats under the creatinine-clearance band (claim 2), under the high-dose two-portion variant (claim 3), and under the weekly/long-rest schedules (claims 4 and 5).
Infringement implication: If a regimen uses the same drug combination and renal gating but treats a tumor outside these listed categories, these claims do not directly reach it.
Claim strategy: what the claim architecture suggests about novelty and enforcement posture
This is a tightly bounded method claim
Claim 1 is not framed as:
- a composition claim,
- a per-patient label statement only,
- or a general “FTD-containing therapy in renal impairment.”
Instead, it is framed as a method combining:
- patient selection by creatinine clearance,
- dosing amount and fractionation,
- and oral administration,
- plus a specific combination composition and molar ratio,
- plus cancer type constraints.
This architecture is consistent with patents that aim to control:
- how clinicians stratify renal impairment, and
- exactly how they dose combination therapy in that setting.
Dependent claims reinforce enforceability by creating multiple “hooks”
The claim set repeats the same tumor-type structure across multiple dependent branches:
- creatinine clearance banding (claim 2)
- dose and fractionation (claims 3 and 10)
- weekly cycle (claims 4 and 11)
- multi-cycle + long rest (claims 5 and 12)
This reduces the chance that a single design-around fully avoids infringement.
Where is the practical infringement surface likely largest?
Highest-likelihood matching scenario
A regimen that mirrors all of the following would land squarely in the independent claim and likely also in one or more dependent claims:
- Oral combination therapy where the dosing component ratio is 1:0.5
- For FTD-equivalent 30–40 mg/m²/day
- In patients with creatinine clearance < 30 mL/min
- Dividing daily dose into 2–4 portions
- Using one of the listed cancer indications:
- gastrointestinal, large bowel, or breast
Secondary matching scenario
If the regimen is restricted to:
- creatinine clearance between 15 and 29 mL/min
- daily dose at 40 mg/m²/day
- divided into two portions
- and uses either:
- 5 days on + 2 days rest weekly, or
- two repeats of that schedule then 14 days rest
then dependent claims 2–5 (and their structurally aligned counterparts) are a better match.
Design-around paths implied by claim structure
Renal gating
- Switching to a dosing protocol for patients with creatinine clearance above 30 mL/min avoids claim 1’s threshold.
- Using a threshold test with a different cutoff might still infringe if the method “detects creatinine clearance” and administers when it is <30 mL/min. Claim language anchors to the cutoff value and the action that follows.
Dose and fractionation
- Staying below 30 mg/m²/day as FTD-equivalent avoids the independent claim dose range.
- Administering a schedule that does not divide the daily dose into the claimed number of portions can avoid claim 1 (which requires 2–4 portions), but may still risk dependent claim overlap if the regimen hits the exact two-portion pattern at 40 mg/m²/day.
Combination molar ratio
- The combination drug is defined by a molar ratio of 1:0.5. A different ratio is the most direct product-level design-around lever, since the drug is defined within the claim.
Scheduling
- Avoiding the claimed cycles (5-day on + 2-day rest weekly; or repeated twice then 14-day rest) can evade the dependent scheduling claims.
- But it may not avoid claim 1 unless the regimen also changes dose amount, fractionation, molar ratio, renal threshold, or tumor type.
Tumor indication
- Treating cancers other than the enumerated categories avoids claim 1’s cancer type limitations.
- Claim language is explicit about gastrointestinal, large bowel, and breast. A regimen with the same drug and dosing but different cancer categories would not satisfy the claim preamble constraints.
What is not covered by the claim set (based on the face of the claims provided)
Not claimed
From the provided claim text, these appear outside the scope of the current claim set:
- Any dosing outside 30–40 mg/m²/day as FTD-equivalent (for claim 1)
- Any creatinine clearance condition other than “< 30 mL/min” (claim 1) or 15–29 mL/min (claim 2)
- Non-oral routes
- Any molar ratios other than 1:0.5
- Any schedule other than the claimed fractionation into 2–4 portions and the specific cycle patterns for dependent claims
US patent landscape: what can be concluded from the information provided
The prompt provides the claim text but does not provide:
- prosecution history,
- priority data,
- listed assignees/owners,
- other family members,
- citation lists (patent-to-patent references),
- related continuations,
- or expiry/patent term calculations.
Under those constraints, a complete and accurate landscape (including active vs expired nearby patents; freedom-to-operate inference; or mapping to related portfolio members) cannot be produced from the information given.
The only defensible “landscape” elements derivable from the claim face are the technical coverage dimensions (renal gating, drug combination definition, oral dosing, dose range, fractionation, and schedule) and the claim architecture (a central method claim plus dependent claims that create multiple infringement entry points).
Key Takeaways
- Claim 1 is a renal-function gated, oral combination therapy method for gastrointestinal, large bowel, or breast cancer in patients with creatinine clearance < 30 mL/min, using a defined FTD : chloro-aminopyrrolidine pyrimidinedione hydrochloride molar ratio of 1:0.5 and 30–40 mg/m²/day as FTD-equivalent, split into 2–4 portions.
- Claim 2 adds a narrower renal band: 15 to 29 mL/min.
- Claims 3 and 10 lock the upper dose: 40 mg/m²/day divided into two portions.
- Claims 4–5 (and 11–12) define specific cycle schedules: 5 on + 2 rest per week, optionally repeated twice then 14 days rest.
- The claim set is structured to create multiple enforcement hooks. Design-arounds most directly target renal cutoff, dose and fractionation, combination molar ratio, tumor indication, or schedule.
FAQs
1) Is this patent about a composition or a treatment method?
It is a method for treating cancer, defined by how clinicians detect creatinine clearance and then administer an oral combination drug with specific dosing parameters.
2) What triggers dosing under claim 1?
The method requires detecting creatinine clearance and then orally administering the combination when creatinine clearance is less than 30 mL/min.
3) What exact drug combination and ratio is required?
The combination drug must comprise FTD and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5.
4) What are the key dosing constraints?
Claim 1 requires 30 to 40 mg/m²/day as FTD-equivalent, and the daily dose must be divided into 2 to 4 portions.
5) Do the claims require a specific treatment schedule?
The independent claim does not include a schedule, but the dependent claims specify:
- 5-day consecutive dosing + 2-day rest per week, and
- two repeats then 14 days rest.
Cited Sources
No external sources were provided in the prompt; the analysis above is based only on the claim text included by the user. Therefore, no citations are included.
