US Patent 12,465,606: Scope, Claims, and US Patent Landscape for Dasatinib pH-Responsive Amorphous Solid Dispersions
What does US Patent 12,465,606 claim in the US?
US Drug Patent 12,465,606 claims a dasatinib amorphous solid dispersion (ASD) that uses a specific pH-dependent polymer system to control solubility across gastric to intestinal pH ranges. The invention scope is centered on (i) the polymer chemistry (methacrylic acid and ethyl acrylate copolymer), (ii) functional solubility behavior (insoluble at pH ≤5 and soluble at pH ≥5.5), and (iii) a specific drug-to-polymer weight ratio window. It extends beyond the composition into dosage form and kit claims, including a package insert co-administration narrative about gastric pH modifiers.
Core independent claim (Claim 1)
Claim 1 is a composition claim that requires all of the following:
- A pharmaceutical composition comprising an amorphous solid dispersion
- The ASD comprises:
- Dasatinib
- A methacrylic acid and ethyl acrylate copolymer that exhibits pH-dependent solubility
- Drug:polymer weight ratio in the ASD:
- 30:70 to 95:5 (dasatinib:copolymer), w/w
Dependent pH-behavior claims (Claims 2, 4, 18, 20)
Several claims narrow the polymer behavior to a concrete pH solubility boundary:
- The copolymer is insoluble at aqueous pH ≤ 5
- The copolymer is soluble at aqueous pH ≥ 5.5
These appear as:
- Claim 2 (composition)
- Claim 4 (composition plus narrowed ratio via Claim 3)
- Claim 18 (kit)
- Claim 20 (kit plus narrowed ratio via Claim 19)
Drug:polymer ratio narrowing (Claims 3, 4, 19, 20)
Claim 3 narrows Claim 1’s ratio window:
- 40:60 to 70:30 (dasatinib:copolymer), w/w
Claim 4 adds the same pH solubility behavior (insoluble ≤5, soluble ≥5.5).
Claim 19 and Claim 20 mirror these ratio and pH conditions inside the kit context.
Functional excipient coverage via antioxidants (Claims 5-7)
The patent also sweeps in multifunctional formulations:
-
Claim 5: ASD includes one or more functional components selected from:
- Antioxidants
- Wetting agents
- Solubilizers
-
Claim 6: if antioxidants are present, they are in 0.001% to 2% by weight of the ASD.
-
Claim 7: lists exemplary antioxidants, including (non-exhaustive from the claim):
- Acetylcysteine
- Ascorbyl palmitate
- BHA, BHT
- Monothioglycerol
- Potassium nitrate, sodium ascorbate
- Sulfite/sulfate systems: sodium formaldehyde sulfoxylate, sodium metabisulfite, sodium bisulfate
- Vitamin E or derivatives
- Propyl gallate
- Chelators: EDTA (or salt), DTPA (or salt)
- Bismuth sodium triglycollamate
- Plus “combination thereof”
This is important for landscape and design-arounds because it limits the antioxidant inclusion to explicit families and concentrations (when using antioxidants).
Dosage form and “gastric acid-insensitive” positioning (Claims 8-10)
Claim 8 broadens to compositions including “one or more pharmaceutically acceptable additives.”
Claim 9 limits the composition to a solid dosage form suitable for oral administration.
Claim 10 adds a functional designation:
- The pharmaceutical composition is a gastric acid-insensitive composition
This term matters for enforcement because it can pull in products marketed as tolerant of elevated gastric pH or impaired acid secretion, even if the product is not described purely as “insensitive” in the ASD itself.
Kit claims and package insert statements (Claims 11-17)
The patent includes a method-ofmarketing-style kit:
- Claim 11: a kit with:
- The claimed pharmaceutical composition
- A package insert
Then Claims 12-17 define specific informational content in the insert, including co-administration statements and patient conditions.
Key kit limitations:
- Claim 12: insert informs user the composition can be co-administered with a gastric acid-reducing agent
- Claim 13: insert informs user it can be co-administered with H2 antagonists or proton pump inhibitors (PPIs)
- Claim 14: insert does not comprise a warning that it should not be co-administered with H2 antagonists or PPIs
- Claim 15: insert informs suitable administration if the user has chronically elevated gastric pH
- Claim 16: insert informs suitable administration if diagnosed with or afflicted by:
- achlorhydria
- hypochlorhydria
- Claim 17: insert informs suitable administration if diagnosed with or afflicted by:
- Helicobacter pylori infection
These claims are structurally distinct from the composition claims: the “infringement hook” is as much about label/insert content as about formulation.
How broad is the claim scope in practice?
The scope breaks into three concentric layers: polymer selection, solubility behavior, and ratio window, plus secondary layers covering dosage form, antioxidants/excipients, and kit labeling.
Polymer and pH solubility are the core scope drivers
- The polymer is constrained to methacrylic acid and ethyl acrylate copolymer with pH-dependent solubility.
- Some dependent claims lock the solubility boundary tightly (≤5 insoluble; ≥5.5 soluble). Claim 1 does not require that exact boundary, only that it exhibits pH-dependent solubility.
Practical breadth implication:
A competitor product using the same ASD concept but with a different polymer or different pH cutoff may avoid dependent claim structures, but Claim 1’s “pH-dependent solubility” language still captures many systems if the polymer is within the same chemical class and demonstrates a pH response.
Drug:polymer ratio is bounded but still wide in Claim 1
- Claim 1: 30:70 to 95:5
- Claim 3: 40:60 to 70:30
Practical breadth implication:
The Claim 1 ratio window is expansive. Many dasatinib ASD formulations (if dasatinib loading is in that range) remain within scope even if optimization targets differ. The narrower dependent ratio claims can be used for additional infringement leverage.
Antioxidant and additive coverage is real, but excipient substitution can still matter
Claims 5-7 let competitors potentially argue that they omit antioxidants entirely (or use antioxidants outside the enumerated list) while still meeting the ASD core. However:
- Claim 5 includes antioxidants plus other functional components (wetting agents, solubilizers). So omitting antioxidants does not remove the claim unless the formulation also lacks the specified functional components or the polymer system already satisfies Claim 1 without them.
- Claim 6 and 7 constrain antioxidant inclusion only when antioxidants are present in the specified amounts.
“Gastric acid-insensitive” is a functional statement that can be used in enforcement
Claim 10’s phrase anchors a performance narrative: products that can tolerate elevated pH are aligned. This matters because the polymer’s solubility shift (≤5 to ≥5.5) is structurally consistent with gastric-to-upper intestinal transitions and with co-administration of acid suppressants.
Kit claims create a labeling-based infringement pathway
The kit claims (Claims 11-17) can be powerful because the “infringement fact pattern” can occur in commercial distribution:
- If a label or insert includes the specific statements and omits the specific warning (Claim 14), then marketing compliance itself can collide with the patent.
What is the likely patent landscape in the US around this concept?
A full landscape normally requires bibliographic data, family members, assignees, priority dates, prosecution history, and claim charts across the same polymer concept and dasatinib ASD systems. The record provided here includes only the claim set for US 12,465,606 and not the patent’s title/assignee, priority, filing dates, prosecution outcomes, cited references, or related family identifiers. Without those elements, a complete and accurate US landscape cannot be produced under a strict patent-analytics standard.
Claim-by-claim scope map (enforcement relevance)
The table below ranks which claim elements are most likely to be dispositive for infringement analysis.
| Claim |
Scope type |
Required constraints |
Main enforcement hook |
| 1 |
Independent composition |
ASD + dasatinib + methacrylic acid/ethyl acrylate copolymer that shows pH-dependent solubility; ratio 30:70 to 95:5 |
Formulation composition and composition-level polymer behavior |
| 2 |
Dependent composition |
Adds copolymer solubility boundary (insoluble ≤5; soluble ≥5.5) |
Polymer pH solubility profile |
| 3 |
Dependent composition |
Adds ratio 40:60 to 70:30 |
Drug loading within ASD |
| 4 |
Dependent composition |
Adds both boundary (≤5/≥5.5) and ratio 40:60 to 70:30 |
Combined ratio + pH cutoff |
| 5 |
Dependent composition |
Adds optional functional components (antioxidants/wetting agents/solubilizers) |
Excipient strategy and inclusion of specified functional component types |
| 6 |
Dependent composition |
Antioxidants present in 0.001% to 2% by weight |
Antioxidant selection and dosing level |
| 7 |
Dependent composition |
Antioxidants from enumerated list (or combinations) |
Specific antioxidant families |
| 8 |
Dependent composition |
“Pharmaceutically acceptable additives” |
Broadening without adding a new limitation to avoid Claim 1 |
| 9 |
Dependent composition |
Solid oral dosage form |
Dosage form format |
| 10 |
Dependent composition |
“Gastric acid-insensitive composition” |
Performance/labeling language tied to elevated gastric pH compatibility |
| 11 |
Independent kit |
Composition of Claim 1 + package insert |
Product + insert content packaging |
| 12 |
Dependent kit |
Insert allows co-administration with gastric acid-reducing agent |
Insert content |
| 13 |
Dependent kit |
Insert allows H2 antagonists/PPIs |
Insert content |
| 14 |
Dependent kit |
Insert does not contain warning against those co-administrations |
Insert content omission (negative limitation) |
| 15 |
Dependent kit |
Insert supports chronic elevated gastric pH users |
Insert content |
| 16 |
Dependent kit |
Insert supports achlorhydria/hypochlorhydria |
Insert content |
| 17 |
Dependent kit |
Insert supports H. pylori infection |
Insert content |
| 18 |
Dependent kit |
Adds copolymer boundary (≤5/≥5.5) |
Polymer profile within kit product |
| 19 |
Dependent kit |
Adds ratio 40:60 to 70:30 |
Drug loading within ASD |
| 20 |
Dependent kit |
Adds both boundary + ratio |
Combined constraints |
Design-around analysis tied to the claim language
Because the independent claim is composition-centric, design-arounds should target the claim elements that are not optional.
Likely “hard” design-arounds (high probability)
- Different polymer family: replace the methacrylic acid and ethyl acrylate copolymer with a different pH-responsive polymer not falling within the specified class. This most directly avoids Claim 1’s polymer requirement.
- Different solubility behavior: if you keep the polymer family but shift the insoluble/soluble transition such that it does not meet the dependent claim cutoffs (≤5 and ≥5.5), you may avoid dependent claims, but you may still hit Claim 1 if the polymer still “exhibits pH-dependent solubility.”
- Outside the ratio window: formulate outside 30:70 to 95:5. This avoids Claim 1 entirely. Alternatively, avoid the 40:60 to 70:30 region to reduce risk against dependent ratio claims.
Targeted “soft” design choices (risk reduction, not removal)
- Avoid antioxidant inclusion: do not include antioxidants or exclude them from the specified families or concentration range. This helps against Claims 5-7 only.
- Labeling strategy: for kit exposure, ensure the package insert does not include the specific co-administration statements or does include the warnings that are absent in Claim 14. This is a compliance-based lever, but it does not remove composition infringement risk if claims 1-10 are otherwise met.
Key takeaways
- US 12,465,606 protects a dasatinib amorphous solid dispersion using a methacrylic acid and ethyl acrylate copolymer with pH-dependent solubility, with a broad 30:70 to 95:5 drug:polymer ratio in Claim 1.
- Dependent claims add a specific solubility boundary (insoluble at pH ≤5; soluble at pH ≥5.5) and narrower ratio (40:60 to 70:30).
- The patent extends into kit claims that can be infringed through package insert content, including permissive guidance on co-administration with gastric acid-reducing agents, H2 antagonists, and PPIs, and insert statements supporting patients with chronically elevated gastric pH, achlorhydria/hypochlorhydria, or H. pylori infection.
- The most direct infringement risk sits in products that match the polymer family + pH behavior + ASD ratio and, if marketed as compatible with acid suppression, also match the insert statement set.
FAQs
1) Does Claim 1 require the specific pH cutoff at pH 5 and 5.5?
No. Claim 1 requires that the copolymer “exhibits pH-dependent solubility.” The exact cutoff appears in dependent claims.
2) What is the broadest dasatinib:copolymer ratio protected?
Claim 1 covers 30:70 to 95:5 (dasatinib:copolymer).
3) Which claim elements are most sensitive to formulation differences?
The polymer identity/class, whether it shows pH-dependent solubility, and the ASD drug:polymer ratio.
4) How can the kit claims create risk even when formulation is similar?
The kit claims tie infringement to package insert content, including statements that allow co-administration with H2 antagonists/PPIs and the absence of a warning.
5) Do antioxidants materially expand the core composition scope?
They add coverage only where the formulation includes functional components and, for Claims 6-7, specific antioxidant types and concentrations. The core scope remains the ASD polymer system and ratio.
References
[1] Provided claims text for US Drug Patent 12,465,606 (user-supplied).
