United States Patent 12,329,742 (Darolutamide Tablet Composition) Scope, Claim Coverage, and US Patent Landscape
Executive summary: US 12,329,742 claims a darolutamide (or salt) direct-compression tablet composition defined by tight excipient ranges (notably calcium hydrogen phosphate 7–20 wt%, lactose 25–35 wt%, plus disintegrant/binder/lubricant ranges) and, in dependent claims, specific excipient identities (croscarmellose sodium, PVP, magnesium stearate) and specific 300 mg/600 mg dosage embodiments with a tableted core + film coating formulation. Claim scope is strongest against ANDA tablets that replicate (i) the same excipient species and ratios, (ii) the same 300 mg/600 mg strengths, and (iii) the same crystalline/solid form for darolutamide.
What the claims protect (high level):
- Tablet composition defined by ingredient type + quantitative wt% ranges
- Specific excipients and specific core composition for 300 mg/600 mg embodiments
- Crystalline form limitation of darolutamide (in claim 6)
- A tablet core + film coat embodiment (claim 5), with specified core composition
What does US 12,329,742 claim for darolutamide tablet formulations?
Direct answer: The patent covers pharmaceutical compositions in tablet form comprising darolutamide (or pharmaceutically acceptable salt) at 45–80 wt%, plus specific excipient classes with defined wt% ranges, optionally with specific excipient identities and crystalline solid form.
Independent claim 1: core composition boundaries
Claim 1 requires a tablet containing, by weight of the composition:
- Darolutamide (or salt): 45–80%
- Calcium hydrogen phosphate: 7–20%
- Lactose: 25–35%
- Disintegrant: 0.5–10%
- Binder: 0.5–10%
- Lubricant: 0.2–5%
Implication for infringement: A tablet “runs into” claim 1 if the final tablet blend (or composition as claimed) meets these numerical wt% ranges. Because the claim is composition-wide and not limited to process parameters, manufacturing route is secondary for claim 1; composition composition is primary.
Dependent claim 2: excipient species narrowing
Claim 2 narrows claim 1 by specifying:
- Disintegrant = croscarmellose sodium
- Binder = polyvinylpyrrolidone (PVP)
- Lubricant = magnesium stearate
Implication: Even if a generic uses the correct ranges for excipient categories, using different excipient species (eg, different disintegrant types) can avoid claim 2 while still possibly reading on claim 1, depending on whether claim 1 is still met with the alternative disintegrant/binder/lubricant.
Dependent claims 3 and 4: strength limitation (300 mg or 600 mg)
Claim 3 requires darolutamide (or salt) amount at:
Claim 4 mirrors claim 3 but under claim 2’s excipient species constraints.
Implication: The “strength” language is not about dosing instructions; it is a composition embodiment. For an accused tablet to infringe these claims, the tablet strength must match.
Dependent claim 5: exact core composition + film coating
Claim 5 specifies a tablet core with approximately:
- ~300 mg darolutamide (or salt)
- ~60 mg calcium hydrogen phosphate
- ~180 mg lactose monohydrate
- ~30 mg croscarmellose sodium
- ~24 mg polyvinylpyrrolidone
- ~5.4 mg magnesium stearate
…and the tablet has a film coating.
Implication: This is the tightest “engineering” target. An ANDA would need to match (or be shown to meet the claim’s approximations) the exact mg amounts in the core for the 300 mg embodiment plus the claimed coating structure (core + film coat).
Dependent claim 6: crystalline form requirement
Claim 6 requires that darolutamide (or salt) is present in a crystalline form.
Implication: This is a solid-state carve-in. A generic using an amorphous form or a different crystalline form would aim to avoid this dependent limitation. If the generic’s API is characterized as crystalline but not the specific form contemplated by the patent, litigation hinges on claim construction and evidence (XRD patterns, DSC, polymorph identification).
How broad is claim 1’s “45–80 wt% darolutamide” and what does it mean for generics?
Direct answer: The API loading is unusually high for a branded tablet composition claim. Claim 1’s 45–80% w/w darolutamide plus lactose at 25–35% creates a narrow formulation space in which many generic blends may or may not fall.
Feasibility of design-arounds
A generic can try to avoid claim 1 by changing any of the required wt% boundaries, for example:
- Lowering darolutamide wt% below 45% or exceeding 80%
- Adjusting lactose wt% outside 25–35%
- Adjusting calcium hydrogen phosphate outside 7–20%
- Using excipients that fall outside the specified categories/ranges (disintegrant/binder/lubricant levels)
Key risk point: If the tablet is engineered to meet bioequivalence and manufacturability, formulation teams often land on relatively standard excipient percentages; if the ANDA target “lands inside” these numeric bands, claim 1 can become a practical infringement exposure.
Category vs identity
Claim 1 only requires excipient categories for the disintegrant/binder/lubricant. Claim 2 adds identity. That makes identity-based design-arounds more effective for claim 2 but can still leave exposure under claim 1.
What formulations are protected by US 12,329,742 for 300 mg and 600 mg tablets?
Direct answer: The patent has explicit dependent coverage for 300 mg and 600 mg strengths and provides a fully enumerated core composition for the 300 mg embodiment, including a film coating.
300 mg embodiment (claim 5 core mg targets)
- Darolutamide (or salt): ~300 mg
- Calcium hydrogen phosphate: ~60 mg
- Lactose monohydrate: ~180 mg
- Croscarmellose sodium: ~30 mg
- PVP: ~24 mg
- Magnesium stearate: ~5.4 mg
Coating structure: tablet core + film coating.
600 mg embodiment
Claim 3/4 address 300 mg or 600 mg at the API level; claim 5 is explicitly tied to “about 300 mg” core. The 600 mg embodiment therefore appears to be covered by the strength limitation plus earlier composition constraints, but not with the same explicit mg-by-mg core specification as claim 5.
Litigation posture note: Dependent claims 3 and 4 can still be asserted against a 600 mg product if the excipient categories/identities and amounts match claim 1/2 ranges.
Which specific excipients are claimed, and how do you design around croscarmellose/PVP/magnesium stearate?
Direct answer: Claim 2 locks down croscarmellose sodium as disintegrant, PVP as binder, and magnesium stearate as lubricant.
Design-around levers
- Use an alternative disintegrant (eg, sodium starch glycolate, crospovidone) at a level that still keeps the overall blend within claim 1’s disintegrant wt% range but outside claim 2’s identity.
- Use a binder other than PVP (eg, HPMC, HPC) to avoid claim 2 while keeping claim 1 risk managed through category-range compliance.
- Use a different lubricant (eg, stearic acid, glyceryl behenate) to avoid claim 2.
Residual claim 1 exposure
If the alternative excipients still fit within claim 1’s category wt% ranges, claim 1 could still read. Therefore, avoidance must be evaluated at both levels:
- Category/range compliance (claim 1)
- Species identity (claim 2)
What is the crystalline-form risk in US 12,329,742 claim 6?
Direct answer: Claim 6 requires darolutamide (or salt) to be in a crystalline form.
How “crystalline” typically plays out
In practice, crystalline status is supported by:
- X-ray diffraction (XRD) peaks
- DSC melting endotherm patterns
- solid-state form comparisons against reference API
Claim strategy impact:
- If an ANDA uses an API form that is crystalline, claim 6 becomes harder to avoid.
- If the ANDA uses a different solid-state form (eg, amorphous or a different polymorph), claim 6 may be avoidable, but claim construction on what “crystalline form” covers can be outcome-determinative.
How many claims and what scope are in US 12,329,742 based on your provided text?
Direct answer: Based on the claim set provided, the patent has at least 6 claims with one independent claim (1) and five dependent claims (2–6) that narrow by identity, strength, core mg targets, and crystalline form.
Coverage map by limitation stack
| Limitation |
Claim(s) |
Scope effect |
| Tablet form |
1–6 |
Limits to tablets (not capsules) |
| Darolutamide (or salt) 45–80 wt% |
1 |
High-level compositional gate |
| Calcium hydrogen phosphate 7–20 wt% |
1 |
Gate on one key excipient |
| Lactose 25–35 wt% |
1 |
Gate on filler choice/ratio |
| Disintegrant/binder/lubricant wt% ranges |
1 |
Broad categories; identity later |
| croscarmellose sodium + PVP + Mg stearate |
2 |
Identity lock, design-around target |
| API strength 300 mg or 600 mg |
3,4 |
Strength-limited coverage |
| Core composition mg targets + film coating |
5 |
Tight formulation embodiment, strongest factual infringement |
| crystalline form API |
6 |
Solid-state gate for dependent claim |
What does the US patent landscape look like around darolutamide tablet excipient formulations?
Direct answer: Without a referenced list of US publications, Orange Book entries, assignees, filing dates, and maintenance status for US 12,329,742, the patent landscape cannot be fully reconstructed into a defensible, numbered prior-art and competitor-citation map.
What can be concluded from claim text alone:
- US 12,329,742 is targeted at formulation composition, not method-of-use.
- The invention focuses on tablet composition engineering: excipient types and ratios, and a crystalline-form dependent claim.
Actionable infringement and design-around implications:
- For generic entrants, the first screening step is to compare the proposed tablet’s excipient wt% ranges to claim 1 and the proposed excipient identities to claim 2.
- The second screening step is to match strength (300 vs 600 mg) and evaluate whether the ANDA’s core mg targets land in the claim 5 tolerance band for the 300 mg product.
- The third step is solid-state characterization of the API used for the ANDA to evaluate claim 6 exposure.
When does US 12,329,742 lose exclusivity, and what timing matters for ANDA Paragraph IV?
Direct answer: Exclusivity and expiration dates cannot be provided from the claim text alone; no filing/priority/issue/term-extension data is included in the prompt.
Practical timing variables that control Paragraph IV incentives (conceptual):
- Patent term measured from priority and any adjustments
- Potential patent term extension (PTE) if applicable
- Any statutorily excluded periods and terminal disclaimers
- Whether US 12,329,742 is listed in the FDA Orange Book for the darolutamide NDA/strength(s)
What is the Orange Book status of US 12,329,742 for darolutamide?
Direct answer: Orange Book listing status cannot be determined from the claim text provided.
How status drives litigation:
- If listed for the 300 mg and/or 600 mg strengths, it shapes Paragraph IV certifications and the litigation trigger mechanics.
What patent litigation risks exist for darolutamide tablet generics?
Direct answer: Specific litigation involving US 12,329,742 cannot be established without docket numbers, parties, or court filings.
However, the claim architecture implies the most likely litigation theories if asserted:
- Direct infringement of claim 1 by an ANDA tablet whose formulation matches excipient wt% ranges.
- Direct infringement of claim 2 where the same excipient species are used (croscarmellose sodium/PVP/magnesium stearate).
- Direct infringement of claim 3/4 by strength-matched products (300 mg and 600 mg).
- Direct infringement of claim 5 where the 300 mg core mg composition and coating structure are matched.
- Infringement of claim 6 if the API used is crystalline and falls within the claim’s construed scope.
Key Takeaways
- US 12,329,742 claim 1 is a tablet composition claim that requires darolutamide (or salt) at 45–80 wt% and lactose at 25–35 wt%, plus calcium hydrogen phosphate at 7–20 wt% and disintegrant/binder/lubricant at defined wt% ranges.
- Claim 2 materially tightens scope by requiring croscarmellose sodium, PVP, and magnesium stearate.
- Claims 3 and 4 narrow to tablet strengths containing 300 mg or 600 mg darolutamide (or salt).
- Claim 5 adds the tightest formulation lock: a tablet core + film coat with a specified 300 mg core mg composition.
- Claim 6 adds a solid-state limitation: crystalline darolutamide (or salt).
- For generic design-around, excipient identity (claim 2), excipient wt% boundaries (claim 1), strength matching (claims 3/4), core mg targets (claim 5), and API solid-state form (claim 6) are the decisive technical gates.
FAQs
- How can an ANDA avoid infringing US 12,329,742 claim 2 while still meeting claim 1 excipient categories?
- If an ANDA matches claim 1 wt% ranges, does using a different disintegrant automatically avoid infringement?
- What evidence is typically used to prove “crystalline form” for a claim like claim 6?
- How does the “tablet core and film coating” limitation in claim 5 affect formulation equivalence arguments?
- In a strength-specific dispute (300 mg vs 600 mg), how do claim 3/4 limitations change the infringement analysis?
References (APA)
- (No citable sources were provided in the prompt.)
