United States Patent 10,272,058: Seladelpar Dose-Defined Methods for Primary Biliary Cholangitis
US Patent 10,272,058 covers methods of treating primary biliary cholangitis (PBC) with seladelpar (or a pharmaceutically acceptable salt) defined by daily dose (5 mg or 10 mg, calculated as seladelpar), with added narrowing to the seladelpar L-lysine dihydrate salt and oral once-daily administration. The claim set is tightly structured as a dose matrix with straightforward claim dependencies, making the scope easiest to map to product labels and generic design-around strategies.
What do the claims cover, claim by claim?
The independent claim set consists of two method claims on dose:
- Claim 1: Treating PBC by administering seladelpar or a salt at 5 mg/day (calculated as seladelpar).
- Claim 9: Treating PBC by administering seladelpar or a salt at 10 mg/day (calculated as seladelpar).
All other claims narrow those independent claims by selecting a specific salt form and administration characteristics.
Claim chart (scope-by-scope)
| Claim |
Patient population / disease |
Active |
Dose constraint (daily) |
Form |
Route |
Frequency |
| 1 |
PBC |
Seladelpar or salt |
5 mg/day (as seladelpar) |
Any salt |
Not limited |
Not limited |
| 2 |
PBC |
Seladelpar L-lysine dihydrate |
5 mg/day (as seladelpar) |
Specific salt |
Not limited |
Not limited |
| 3 |
PBC |
Seladelpar or salt |
5 mg/day (as seladelpar) |
Any salt |
Oral |
Not limited |
| 4 |
PBC |
Seladelpar L-lysine dihydrate |
5 mg/day (as seladelpar) |
Specific salt |
Oral |
Not limited |
| 5 |
PBC |
Seladelpar or salt |
5 mg/day (as seladelpar) |
Any salt |
Not limited |
Once/day |
| 6 |
PBC |
Seladelpar L-lysine dihydrate |
5 mg/day (as seladelpar) |
Specific salt |
Not limited |
Once/day |
| 7 |
PBC |
Seladelpar or salt |
5 mg/day (as seladelpar) |
Any salt |
Oral |
Once/day |
| 8 |
PBC |
Seladelpar L-lysine dihydrate |
5 mg/day (as seladelpar) |
Specific salt |
Oral |
Once/day |
| 9 |
PBC |
Seladelpar or salt |
10 mg/day (as seladelpar) |
Any salt |
Not limited |
Not limited |
| 10 |
PBC |
Seladelpar L-lysine dihydrate |
10 mg/day (as seladelpar) |
Specific salt |
Not limited |
Not limited |
| 11 |
PBC |
Seladelpar or salt |
10 mg/day (as seladelpar) |
Any salt |
Oral |
Not limited |
| 12 |
PBC |
Seladelpar L-lysine dihydrate |
10 mg/day (as seladelpar) |
Specific salt |
Oral |
Not limited |
| 13 |
PBC |
Seladelpar or salt |
10 mg/day (as seladelpar) |
Any salt |
Not limited |
Once/day |
| 14 |
PBC |
Seladelpar L-lysine dihydrate |
10 mg/day (as seladelpar) |
Specific salt |
Not limited |
Once/day |
| 15 |
PBC |
Seladelpar or salt |
10 mg/day (as seladelpar) |
Any salt |
Oral |
Once/day |
| 16 |
PBC |
Seladelpar L-lysine dihydrate |
10 mg/day (as seladelpar) |
Specific salt |
Oral |
Once/day |
Immediate scope implications
1) Dose-based infringement is binary.
The independent claims hinge on exact daily doses: 5 mg/day and 10 mg/day, where the label claim is calculated as seladelpar. A dosing regimen that is genuinely outside those daily totals (not a rounding artifact) falls outside these claim cores.
2) “Seladelpar or a salt thereof” expands beyond the lysine dihydrate.
Claims 1 and 9 cover any salt form, so design-around by changing salt form only helps if the dose is changed too.
3) Oral and once/day are not essential for the broadest coverage.
Even if a regimen uses multiple daily administrations or parenteral routes, claims 1 and 9 still read if the dose and PBC treatment method match.
4) The lysine dihydrate is protected at each dose level and administration setting.
Claims 2, 4, 6, 8 cover the 5 mg/day lysine dihydrate permutations; claims 10, 12, 14, 16 cover the 10 mg/day lysine dihydrate permutations.
How narrow are these claims in practice?
These are method-of-treatment claims with clear treatment parameters:
- Disease: PBC
- Drug definition: seladelpar or salt, or specifically seladelpar L-lysine dihydrate for dependent claims
- Dose: 5 mg/day or 10 mg/day calculated as seladelpar
- Route: oral in dependent claims 3,4,7,11,12,15,16
- Frequency: once/day in dependent claims 5-8 and 13-16
The “claim ladder” effect
The dependent claims do not add patient subpopulations; they add treatment mechanics. This increases enforceability against dosing that matches commercial regimens for PBC, because an accused regimen can be compared line-by-line:
-
If a competitor markets a once-daily oral seladelpar product with a 5 mg/day or 10 mg/day label for PBC, it risks hitting at least one of the dependent claims and almost certainly the corresponding independent dose claim.
-
If a competitor uses a non-lysine salt, it still faces exposure under the independent dose claims if the daily seladelpar equivalent dose remains 5 or 10 mg.
What is the likely patent landscape structure around this US patent?
Given only the claim text you provided, the strongest landscape conclusion is structural rather than bibliographic: this patent is a dose-and-salt method-of-treatment layer. In most real-world PBC portfolios for an oral small molecule, method-dose claims like these usually sit adjacent to at least three other families:
- Drug substance / active ingredient claims (seladelpar free base and/or core structure).
- Salt form / solid-state claims (including seladelpar L-lysine dihydrate).
- Dosing regimen claims (dose levels, frequency, route), often to secure long-lived protection in a competitor’s label corridor.
Even without those other documents in hand here, the dependence structure in 10,272,058 indicates it is meant to be asserted even when the active ingredient is not in dispute, because it focuses on how the product is used.
Scope map: what would literally infringe?
Coverage targets by regimen
| Regimen parameter |
If it matches |
Risk under 10,272,058 |
| Treating PBC |
Yes |
Required for all claims |
| Seladelpar (free base) or any salt |
Yes |
Broad coverage in claims 1 and 9 |
| Daily dose equals 5 mg (as seladelpar) |
Yes |
Directly meets claim 1 and its dependent variants |
| Daily dose equals 10 mg (as seladelpar) |
Yes |
Directly meets claim 9 and its dependent variants |
| Salt equals seladelpar L-lysine dihydrate |
Yes |
Adds coverage for claims 2,4,6,8 and 10,12,14,16 |
| Oral route |
Yes |
Adds coverage for claims 3,4,7,11,12,15,16 |
| Once/day |
Yes |
Adds coverage for claims 5-8 and 13-16 |
What would avoid literal coverage (high-level)
- Change daily dose to something other than 5 mg or 10 mg (as seladelpar).
- If the product is fixed-dose and cannot be modified, a label that uses a different dosing schedule could reduce risk if it truly changes the “daily dose” element.
Because the independent claims do not restrict route or frequency, route changes alone (e.g., non-oral) would not avoid claims 1 and 9. Similarly, frequency changes alone would not avoid claims 1 and 9.
Claim strength against common generic entry strategies
1) “Same drug, different salt” strategy
- Limited value. If the dosing stays at 5 mg/day or 10 mg/day (as seladelpar) for PBC, claims 1 and 9 still read because they cover “seladelpar or a salt thereof.”
2) “Same dose, different dosing frequency/route” strategy
- Limited value. While dependent claims include oral and once/day limitations, the independent dose claims do not.
- If a regimen is non-oral or twice-daily but still totals 5 mg/day or 10 mg/day, the independent claims remain at risk.
3) “Lower or higher daily dose” strategy
- Most direct design-around. Because the independent claims lock dose at 5 mg/day and 10 mg/day, changing the daily total can take the regimen outside the claim language.
4) “Label carve-outs” strategy (practical)
- If the product is approved for PBC at the same daily dose and method, carve-outs often fail in practice due to off-label use and marketing controls. Here, the claim language is tied to treating PBC, not contraindication conditions. If the label includes PBC at those doses, exposure increases.
Enforcement leverage: dependent claims increase the number of “hit points”
From an infringement management standpoint, the dependent claims provide multiple independent pathways to infringement when the accused regimen matches:
- A once-daily oral formulation is likely to hit claims 7/8 and 15/16 (for the relevant dose and salt form).
- Even if the salt form differs from lysine dihydrate, claims 1 and 9 still provide broad coverage on dose and disease.
This creates a higher probability that a single accused product satisfies multiple claims simultaneously, improving litigation leverage and settlement leverage.
What is the scope of “seladelpar L-lysine dihydrate” inside the patent?
The claims treat seladelpar L-lysine dihydrate salt as an alternative to “seladelpar or a salt thereof.” The effect is:
- Dependent claims 2/4/6/8 and 10/12/14/16 create separate infringement hooks for the specific salt.
- The independent claims remove the need to prove salt identity when “seladelpar or a salt” and dosing match.
So even if a competitor uses a different salt, the patent still has a broad dose target.
Key takeaways for investors and R&D decision-makers
Key Takeaways
- US 10,272,058 protects PBC treatment methods using seladelpar (or any salt) at specific daily doses: 5 mg/day and 10 mg/day (calculated as seladelpar).
- Dependent claims lock in seladelpar L-lysine dihydrate, oral administration, and once/day schedules, multiplying enforcement pathways when commercial regimens match.
- For design-around, changing route or dosing frequency alone likely does not avoid claims 1 and 9 because those do not require oral or once-daily administration.
- The most direct literal avoidance is to change the daily seladelpar-equivalent dose so it is not 5 mg/day or 10 mg/day for PBC.
FAQs
1) Does the patent require oral dosing to be infringed?
No. The broad independent claims require only PBC treatment and daily dose at 5 mg/day (claim 1) or 10 mg/day (claim 9). Oral and once/day show up in dependent claims.
2) Is the seladelpar L-lysine dihydrate salt required?
No. It is required only for the dependent claims that specify it. The independent claims cover “seladelpar or a salt thereof.”
3) What doses are explicitly covered?
The patent explicitly covers 5 mg/day and 10 mg/day of seladelpar, with daily dose calculated as seladelpar.
4) Does the patent cover dosing more than once per day?
Yes, at least for the independent dose claims. Claims that require once/day are dependent (claims 5-8 and 13-16), but claims 1 and 9 do not.
5) What is the main litigation “hit point” for an accused product?
The dosing element: whether the product’s PBC-treated daily seladelpar equivalent is exactly 5 mg/day or 10 mg/day. If so, the independent claims are directly implicated.
References
- United States Patent 10,272,058 (claims 1-16 as provided by user).
