United States Patent 11,819,533: Scope, Claim Strength, and US Landscape
United States Drug Patent US 11,819,533 claims an intravenous formulation of CD101 acetate with a defined saccharide level plus an intravenous solubility promoter at a specific promoter-to-CD101 w/w ratio (>=2, and 2-8 in dependent claims), with downstream method-of-use claims for systemic fungal infections via IV infusion schedules and dose reconstitution from a lyophilized form.
What does US 11,819,533 claim, in plain claim scope?
Core product claim (Claim 1)
Claim 1 defines an IV injectable aqueous solution with these hard parameters:
- Solvent: aqueous solution comprising at least 85% (w/w) water
- Active: CD101 acetate at 0.8 mg/mL to 1.6 mg/mL
- Saccharide: 0.12% to 0.6% (w/w)
- Solubilizer system: includes an intravenous solubility promoter
- Critical ratio: w/w ratio of solubilizer promoter to CD101 acetate is at least 2
- (This ratio control drives much of the infringement math and invalidity exposure.)
Narrowing product coverage (Claim 2)
Claim 2 narrows the ratio window:
- promoter:CD101 acetate between 2 and 8 (w/w)
Solubilizer identity (Claims 3 and 4)
Claim 3 lists an explicit set of IV solubility promoters. The claim is “selected from the group,” so it is closed to the listed excipients unless the doctrine of equivalents is pursued:
- polysorbate 20
- polysorbate 40
- polysorbate 60
- polysorbate 80
- 13-cyclodextrin
- polyoxyl 35 castor oil
- polyoxyl 40 hydrogenated castor oil
- polyoxyl 60 hydrogenated castor oil
- D-a-tocopheryl polyethylene glycol 1000 succinate
- sorbitan monooleate
- polyoxyl 8 stearate
- polyoxyl 40 stearate
- PEG 400 caprylic/capric glycerides
- PEG 300 oleic glycerides
- phosphatidylcholine
- alkylglucoside
- sucrose monolaurate
- sucrose monooleate
- polyoxyethylene-polyoxypropylene block copolymer
Claim 4 further locks:
- intravenous solubility promoter is polysorbate 80
Buffer variant (Claim 5)
- Claim 1 composition further comprises a buffer (expands formulation embodiments; does not change the ratio window)
Lyophilized product + reconstitution (Claim 6)
Claim 6 adds a second formulation modality:
- Composition comprises effective amount of CD101 acetate
- Saccharide: 2% to 10% (w/w) in the lyophilized composition
- Solubilizer in lyophilized composition
- Promoter:CD101 acetate ratio between 2 and 8 (w/w)
This claim is important because it separates lyophilized excipient loading (higher saccharide) from reconstituted aqueous concentration (Claim 1’s 0.8 to 1.6 mg/mL CD101 acetate window).
What do the method claims cover?
Indication: fungal infections (Claims 7 and 13)
Claim 7 claims a method:
- Treating or preventing fungal infection by IV administration of the Claim 1 composition.
Claim 13 supplies an enumerated infection list, spanning yeast (Candida), molds (Aspergillus), and endemic mycoses, including:
- candidemia, invasive candidiasis
- multiple forms of candidiasis (oral, vaginal, systemic, mucocutaneous, respiratory, biliary, eosophageal, urinary)
- aspergillosis, mucormycosis
- paracoccidioidomycosis, blastomycosis, histoplasmosis, coccidioidomycosis
- sporotrichosis
- fungal sinusitis / chronic sinusitis
- and multiple dermatophyte/tinea conditions (tinea capitis/corporis/pedis), plus onychomycosis and perionychomycosis
Administration mechanics and dosing (Claims 8 to 12)
Claim 8 ties reconstitution and concentration:
- (i) reconstitute Claim 6 lyophilized composition to aqueous solution
- (ii) IV administer
- CD101 acetate concentration in aqueous solution: 0.8 mg/mL to 1.6 mg/mL
Claims 9 to 12 add delivery constraints:
- Claim 9: IV by infusion
- Claim 10: infusion at constant rate 2 mL/minute to 9 mL/minute
- Claim 11: infusion duration 30 to 120 minutes
- Claim 12: one dose every 5 to 15 days
These constraints can be infringement-relevant if a competitor uses different infusion rates or schedules.
Where is the patent strong, and where is it vulnerable?
Strength drivers
- Ratio limitation is a numerical handle
The promoter:CD101 w/w ratio >=2 (and 2-8 in dependent claims) is a direct formulation parameter that is measurable analytically (weight fractions, assay plus excipient quant).
- Tight concentration window
CD101 acetate in IV solution: 0.8 to 1.6 mg/mL.
- Specific solubilizer group (and polysorbate 80 as a sub-scope)
Claim 3 is limited to a defined list; Claim 4 narrows to polysorbate 80.
- Lyophilized embodiment with reconstitution concentrations
Claim 6 plus Claim 8 creates a path from solid dosage manufacturing to the exact IV solution parameters.
Potential vulnerability points
- Formulation obviousness risk: common excipients + standard solubilizer approach
Several listed solubilizers (e.g., polysorbates, cyclodextrins, PEG-based surfactants) are conventional for IV insoluble drugs. The key differentiator is the ratio and CD101/saccharide windows.
- Saccharide range may map to typical lyophilization protectants
Claim 1: 0.12% to 0.6% (w/w) saccharide in solution; Claim 6: 2% to 10% (w/w) in lyophilized form. If prior art teaches similar stabilizing sugars for reconstitution, the decisive factor becomes whether the specific combination with CD101 acetate and the promoter ratio is taught.
- Method claim dependence on product parameters
Method claims rely on using the Claim 1 (and/or Claim 6 then reconstitution) formulation. Invalidating the product claims can sink the method claims, unless there is independent inventive basis.
- Infection list breadth versus enabled overlap
Claim 13 lists many fungal diseases. Enforcement often focuses on clinical use tied to likely patient populations. If some indications are not supported by the specification’s data, there can be claim-quality leverage, but this depends on the patent’s disclosure record.
Claim chart style breakdown (what each independent element requires)
Claim 1 elements checklist
- IV injectable aqueous solution
- Water: >=85% w/w
- CD101 acetate: 0.8-1.6 mg/mL
- Saccharide: 0.12%-0.6% w/w
- Intravenous solubility promoter present
- Promoter:CD101 acetate w/w ratio >=2
Claim 2
- Promoter:CD101 acetate 2-8 w/w
Claim 3 / Claim 4
- Promoter is within listed group
- or specifically polysorbate 80
Claim 6
- Lyophilized composition
- Saccharide: 2%-10% w/w
- Promoter present
- Promoter:CD101 2-8 w/w
Claim 8
- Reconstitute Claim 6 into aqueous solution
- IV administer
- Reconstituted CD101 acetate: 0.8-1.6 mg/mL
Claim 10-12 (administration constraints)
- infusion rate: 2-9 mL/min
- infusion time: 30-120 min
- dosing interval: every 5-15 days
How would competitors design around, based on claim math?
Best target for design-around
The most “mathematically direct” design-around lever is the promoter:CD101 acetate w/w ratio.
- If a competitor moves to a ratio below 2, it avoids Claim 1 and Claim 2 ranges, but this can conflict with solubility and stability requirements.
- If a competitor uses a promoter outside the Claim 3 closed list, they can avoid literal coverage of Claim 3 and Claim 4, though Claim 1 still requires “an intravenous solubility promoter” (not necessarily one of the enumerated ones) unless the application’s claim construction ties it to the later dependent list.
Secondary design-around
- Move CD101 acetate concentration outside 0.8-1.6 mg/mL in the IV solution
- Shift saccharide concentration outside 0.12%-0.6% w/w (solution) or 2%-10% w/w (lyo)
- Change infusion rate/time or dosing interval to outside the specified windows (Claims 10-12)
Potential “trap”
If a product is marketed and used exactly within the reconstitution and dosing regimen, the method claims can still capture clinical administration even if a competitor changes some formulation aspect, depending on whether the method claims require the same composition as claimed (they do).
US patent landscape: what is this patent most likely anchored to?
The provided record is only the claim set. Without the patent’s application details, assignee, filing dates, priority chain, and cited references, a complete family-level and prosecution-history landscape cannot be built from the text alone.
What can be stated from the claim architecture:
- This is a formulation patent with both liquid IV and lyophilized embodiments tied to exact concentration and excipient ratios.
- The legal leverage likely comes from ratio-controlled solubilization rather than from a new active ingredient.
- Excipients are conventional; the differentiation is numeric and combinatorial, which is a familiar pattern for formulation patents that follow (or accompany) a known drug substance.
Business implications for R&D, product development, and licensing
1) Formulation package is the deal unit
Licensing or freedom-to-operate assessments should focus on:
- CD101 acetate concentration in the final IV solution (0.8-1.6 mg/mL)
- saccharide concentration in the final solution (0.12%-0.6% w/w)
- promoter identity and promoter:CD101 ratio (>=2, and 2-8 in dependent claims)
- lyophilized saccharide loading (2%-10% w/w) if the product uses solid dosage
- reconstitution to the same concentration window
2) Polysorbate 80 is a high-value sub-scope
If a product uses polysorbate 80, Claim 4 becomes a direct literal target. If the product uses other promoters, Claim 3 becomes a gate.
3) Clinical administration parameters can matter
If a competitor plans to align dosing for pharmacokinetics and safety, the specified infusion windows and dosing interval can become infringement-relevant when matched to clinical protocols.
Key Takeaways
- US 11,819,533 is a CD101 acetate IV formulation patent anchored to: CD101 concentration (0.8-1.6 mg/mL), saccharide ranges (solution 0.12%-0.6% w/w, lyophilized 2%-10% w/w), and a solubilizer promoter ratio (>=2, and 2-8 in narrower claims).
- Solubility promoter scope is controlled by a closed list (Claim 3) with polysorbate 80 singled out (Claim 4).
- Method claims cover IV treatment or prevention of fungal infections, including reconstitution from lyophilized product and specific infusion rate, duration, and dosing interval windows.
- The most actionable design-around lever is the promoter-to-CD101 w/w ratio and secondarily CD101 concentration and saccharide loading after reconstitution.
FAQs
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Does this patent cover only liquid IV formulations?
No. It covers both an aqueous IV composition (Claim 1) and a lyophilized composition with reconstitution (Claim 6, Claim 8).
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What is the most important numerical limitation for infringement?
The w/w ratio of solubility promoter to CD101 acetate: at least 2 (Claim 1) and between 2 and 8 (Claim 2 and Claim 6).
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Is polysorbate 80 explicitly protected?
Yes. Claim 4 narrows Claim 3 to polysorbate 80.
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Do the method claims require reconstitution from lyophilized material?
No. The indication method in Claim 7 uses the Claim 1 composition. Claim 8 adds a specific reconstitution pathway for the lyophilized product.
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Do infusion timing and rate matter legally?
Yes for the dependent method claims: 2-9 mL/min, 30-120 minutes, and dose every 5-15 days (Claims 10-12).
References (APA)
[No sources cited: the request contained only the claim text and did not provide patent metadata (publication, assignee, priority, prosecution history, or external references).]
