US Patent 10,010,507 (Ibrutinib Micronized Tablet): Claim Scope, Practical Coverage, and US Patent Landscape
US Patent 10,010,507 claims a specific US solid tablet formulation of ibrutinib: micronized ibrutinib (Compound 1) at defined strength amounts (140/280/420/560 mg) combined with conventional excipient classes, with claim-dependent particle-size ceilings and excipient sub-compositions (including intragranular vs extragranular partitioning and specific excipient examples). The claims are formulation-scoped (not a method-of-treatment claim in the text provided) and are strongest where competitors keep the same ibrutinib form (micronized), the same strength targets, and the same excipient architecture (including certain lactose/MCC/HPc/croscarmellose/magnesium stearate combinations and intragranular vs extragranular assignments).
What is US Patent 10,010,507 claiming for micronized ibrutinib tablet formulations?
Core claim (Claim 1)
Claim 1 is the anchor. It requires all elements below:
- Dosage form: solid tablet formulation.
- Active: ibrutinib defined as “a compound with the structure of Compound 1.”
- Solid-state attribute: ibrutinib is in micronized form.
- Strength targets: the tablet contains about 140 mg, 280 mg, 420 mg, or 560 mg ibrutinib.
- Excipients: one or more pharmaceutically acceptable excipients.
That combination creates a tight boundary: any accused tablet must (i) be a tablet, (ii) contain the claimed amount range tied to those strengths, and (iii) use micronized ibrutinib (as opposed to non-micronized or a different controlled particle-size specification), even if the excipient set is otherwise conventional.
Key practical levers inside Claim 1
- Micronized ibrutinib is the highest-risk technical element for a generic or an alternative manufacturer. Particle-size evidence typically becomes a fight point: laser diffraction, sieve analysis, D50/D90, and the method used matter.
- Strength lock-in (140/280/420/560 mg) matters for label strengths and for fixed-dose combinations. If a competitor’s product is only offered at different strengths, it may avoid element-by-element claim coverage.
How broad are the micronization and particle-size claim limits in US 10,010,507?
Claims 2–4 narrow Claim 1 by adding explicit particle-size ceilings:
- Claim 2: micronized ibrutinib particle size ≤ 30 microns.
- Claim 3: particle size ≤ 10 microns.
- Claim 4: particle size < 1 micron.
Scope read-through
- Claim 1 already requires “micronized” but does not define a number.
- Claims 2–4 supply numeric thresholds that can be used two ways:
- Assert dependent coverage when a competitor’s particle-size is known or measured to fall under one of these cutoffs.
- Create non-infringement positions if a competitor can show their material is micronized under a different definition or has a particle distribution that sits above a threshold used in the asserted dependent claim.
Litigation leverage
- If a dispute targets Claim 2, the evidentiary hinge is whether accused ibrutinib in the finished product meets “about or less than 30 microns.”
- If Claim 3 is asserted, “about or less than 10 microns” becomes narrower.
- Claim 4 (“less than about 1 micron”) is the tightest; it is easiest for a defendant to argue non-meeting if they do not use submicron milling or if their distribution includes a tail.
What excipient categories are protected, and how do the claim examples constrain or expand coverage?
Claims 5–14 provide broad excipient class coverage and then enumerate specific exemplar materials.
Broad structure (Claims 5–6)
- Claim 5: formulation further comprises one or more diluents.
- Claim 6: diluents are selected from a large group that includes lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate/sulfate, starches/modified starches, cellulose/MCC, and talc.
This group is broad enough that most standard tablet diluents would fall under it.
Lubricants (Claims 8–9)
- Claim 8: one or more lubricants.
- Claim 9: selected from stearate, PEG, or wax.
Most conventional tablet magnesium stearate formulations will land here.
Disintegrants (Claims 10–12)
- Claim 10: one or more disintegrating agents.
- Claim 11 and Claim 12: disintegrants are selected from a long list including starches, methylcellulose/methylcrystalline cellulose, croscarmellose/croscarmellose sodium, cross-linked CMC, cross-linked starch, cross-linked PVP, sodium alginate, clays, gums, plus crospovidone.
This again is broadly protective, and it creates multiple entry points for infringement via different disintegrant choices.
Binders (Claims 13–14)
- Claim 13: one or more binders.
- Claim 14: binders are PVP or hydroxypropyl cellulose.
So, if a competitor avoids both PVP and HPMC/HPc binder choices, it may try to avoid dependent claim coverage that includes binders, though Claim 1 may still be asserted without binders being required.
How do the composition percentage claims affect generic design-around strategies?
The claims include both qualitative and quantitative ranges.
Claim 15
- ≥ 50% w/w ibrutinib
- plus one or more diluents
- plus one or more lubricants
This makes “high drug load” a coverage trigger.
Claim 16 (quantitative high-load range)
- 50% to 90% w/w ibrutinib
- 5% to 20% w/w diluents
- 0.1% to 1.5% w/w lubricants
This is a meaningful restriction because many tablet formulations for poorly compressible actives have different drug load targets. If a competitor reformulates to reduce ibrutinib fraction, they may avoid Claim 16.
Claims 28 and 27
- Claim 28: 60% to 80% w/w ibrutinib.
- Claim 27: “high-load solid tablet formulation” used for one tablet once a day dosing.
Those dependent claims can be asserted when the accused product matches both the drug load window and the once-daily dosing claim framing.
What does intragranular vs extragranular excipient architecture protect?
Claims 17–18 introduce a manufacturing-process architecture in the form of granulation compartmentalization (not a full process claim, but a formulation architecture claim).
- Claim 17: excipients comprise intragranular and extragranular excipients; intragranular include diluents; extragranular include lubricants.
- Claim 18: specifically intragranular are lactose and MCC; extragranular is magnesium stearate.
This can be important for design-around:
- If a competitor uses a single blend without a meaningful intragranular/extragranular distinction, or assigns lubricant differently, it may avoid dependent coverage.
- But if the competitor follows a conventional granulation route with separate lubricant addition at the extragranular step, it will tend to match the architecture.
More specific mixed excipient architecture (Claim 22)
- Intragranular: lactose, microcrystalline cellulose, croscarmellose sodium, hydroxypropyl cellulose
- Extragranular: croscarmellose sodium and magnesium stearate
That exact partitioning is narrower and creates a clear infringement target if the accused product uses this architecture.
Which specific excipient component amounts are claimed as ranges?
Claims 19–24 and 26 enumerate numeric windows for select excipients.
Lactose (Claim 19)
Lactose in about:
- 5% to 20% w/w (plus multiple subranges like 10–20%, 8–15%, 8.5–14%, 12–15%)
Microcrystalline cellulose (Claim 20)
- 5–20% w/w (with additional subranges 8–20%, 8–15%, 1–10%, 2–5%)
Magnesium stearate (Claim 21)
- 0.1–1.5% w/w (also 0.4–0.8%, 0.5–0.6%)
Croscarmellose sodium (Claim 23)
Multiple windows including:
- 0–10%
- 0–5%
- 1–10%
- 2–5%
- 2–4%
- 3–7%
- 1–3%
Hydroxypropyl cellulose (Claim 24)
Multiple windows including:
PVP (Claim 26)
Interpretation
These ranges are the main “numbers” the market cares about. A generic-development team can often match excipient types but may struggle to land inside every dependent range simultaneously. In litigation, the asserted dependent claims typically drive the infringement analysis.
How many tablet-strength variants are covered, and what is the risk by strength?
Claim 1 ties coverage to tablets containing:
- about 140 mg
- about 280 mg
- about 420 mg
- about 560 mg ibrutinib
A company making a different labeled strength (or a different dose regimen not matching those amounts) may aim to avoid the strength-limitation element.
A company manufacturing those strengths remains exposed if it also uses micronized ibrutinib and conventional excipients included by the dependent claims.
What is the likely technical “center of mass” of the claim set?
Across the claim family you provided, the densest overlap is:
- micronized ibrutinib (with potential particle-size subranges),
- high drug load (≥50% and often 60–80% w/w in dependent claims),
- lactose + microcrystalline cellulose as key excipients,
- croscarmellose sodium and hydroxypropyl cellulose as disintegrant/binder,
- magnesium stearate as extragranular lubricant,
- intragranular/extragranular compartmentalization typical of granulation.
That combination reads like a conventional direct compression or granulation-friendly formulation with controlled particle size on the active.
What does the claim language imply about infringement proof and defendant defenses?
Plaintiff proof pressure points
- Particle size of ibrutinib in the accused tablet (micronized; ≤30 microns; ≤10 microns; <1 micron depending on asserted claims).
- Tablet strength: 140/280/420/560 mg.
- Excipient mapping: whether specific excipient classes and compositions fall within the dependent ranges.
- Intragranular/extragranular architecture: whether the accused formulation has the claimed compartmentalization.
Common defense levers
- Particle-size avoidance: demonstrate a different particle-size distribution inconsistent with “micronized” as defined in the asserted dependent claim.
- Strength avoidance: do not market or manufacture within those exact strength targets.
- Excipient range avoidance: shift lactose/MCC/croscarmellose/magnesium stearate/PVP/HPc amounts outside claimed windows.
- Architecture avoidance: change granulation and mixing strategy so lubricant and diluents do not fall into the claimed intragranular/extragranular categories.
US patent landscape context: how 10,010,507 fits vs typical ibrutinib protection themes
Ibrutinib’s broader US patent landscape typically clusters around three themes that matter for strategy around tablets:
-
API solid state and particle size
Particle size and micronization are often covered via formulation-adjacent patents or composition-of-matter improvements.
-
Tablet formulation excipient systems
High drug load formulations, specific disintegrants, lubricants, binders, and intragranular/extragranular partitioning are commonly claimed.
-
Dosage regimen and use
Method-of-treatment claims are common in oncology, though your provided claims are formulation-focused.
Where 10,010,507 is positioned
The claims you provided are closest to (2) and (1) at once: tablet formulation plus micronized API. That makes it a direct barrier against generic copying of the “finished tablet recipe” for the specified strengths.
How strong is the patent estate for blocking generic entry on ibrutinib tablets?
Based on the claim scope text alone, the strength drivers are:
- Specific strength mapping in Claim 1.
- Defined technical attribute: micronized ibrutinib and numeric particle-size ceilings in dependent claims.
- Multiple dependent excipient sub-combinations that increase the probability that a marketed product matches at least one dependent claim if it follows a conventional formulation.
The main weakness for a rights holder would be if a competitor can make a tablet with:
- non-micronized or differently distributed ibrutinib,
- a different strength set,
- or excipient/range changes sufficient to fall outside the dependent ranges.
Because many excipients are broadly recited by genus, the factual friction point tends to be the particle size and the quantitative windows, not the mere existence of conventional excipients.
What generic entry risks exist for products that differ only in excipient amounts?
If the competitor matches:
- tablet form,
- ibrutinib identity (Compound 1),
- strength amount,
- and micronized particle size,
then even modest excipient changes can still leave exposure because:
- Claim 1 does not require any particular excipient composition or percent, only that there are pharmaceutically acceptable excipients.
- Dependent claims add more constraints, but Claim 1 alone can support infringement for “micronized ibrutinib tablet at 140/280/420/560 mg,” even if excipients differ.
Thus, the strongest design-around is typically particle-size and/or strength, not just excipient substitutions.
What patent litigation angles are likely given the claim structure?
Infringement
- Dispute will revolve around whether the accused product uses micronized ibrutinib and whether the particle-size falls below any asserted numeric threshold.
- Secondary disputes will cover whether excipients match the claimed intragranular/extragranular architecture and quantitative windows.
Validity
- Without the full spec, you would typically expect arguments around obviousness for particle-size-controlled tablets using standard excipients and around whether the claim defines adequate disclosure for “micronized” and the specific particle-size thresholds. Those arguments are spec-dependent, and the record cannot be evaluated from claim text alone.
How to interpret claim coverage in a licensing or FTO context
For licensing, the practical question is whether a licensee intends to manufacture tablets that:
- use micronized ibrutinib, and
- target the four specific strength amounts, and
- falls into one or more excipient architecture profiles.
A “low-lift” license position is for a manufacturer whose formulation work already uses micronized ibrutinib and conventional excipients with granulation and magnesium stearate extragranular addition.
A “high-risk” position is any tablet product matching strength and micronization, because Claim 1 can be asserted without needing to prove the dependent excipient ranges.
Key Takeaways
- US 10,010,507 claims a micronized ibrutinib tablet formulation tied to 140/280/420/560 mg strengths and standard excipient use.
- The strongest technical hook is particle size: dependent claims set ceilings at ≤30 microns, ≤10 microns, and <1 micron.
- Dependent claims add formulation architecture and quantitative constraints: high drug load (≥50% and 60–80% w/w), and specific excipient compositions, including lactose, MCC, croscarmellose sodium, hydroxypropyl cellulose, PVP, and magnesium stearate, with intragranular vs extragranular placement.
- For generic risk, excipient swaps alone may not be enough because Claim 1 covers a broad excipient set; the main design-around levers are micronization/particle size and strength targeting.
FAQs
1) Does US 10,010,507 require specific excipients in the independent claim?
No. Claim 1 requires only pharmaceutically acceptable excipients. Specific excipients and percentages appear in dependent claims.
2) Can a product avoid infringement by using a different ibrutinib particle-size distribution?
Yes, if it is not “micronized” for Claim 1 or does not meet the dependent thresholds (≤30 microns, ≤10 microns, <1 micron) for the asserted dependent claims.
3) If a company makes a different labeled strength (not 140/280/420/560 mg), is it covered?
Claim 1 is written to those strength amounts. If the product does not contain those amounts “about” in the tablet, Claim 1 element coverage is weaker.
4) Do the intragranular/extragranular limitations function like manufacturing-process claims?
They are formulation-architecture limitations in your provided text, but they map to granulation practice and can be used in infringement disputes based on how the formulation is built.
5) Are the excipient range claims the main infringement path?
They are important for dependent claims, but Claim 1 can still be asserted if the accused tablet meets micronization and strength requirements even when excipient percentages differ.
References (APA)
- United States Patent 10,010,507 (claims as provided by user).
