Details for Patent: 12,427,108

Which drugs does patent 12,427,108 protect, and when does it expire?

Patent 12,427,108 protects TEZRULY and is included in one NDA.

Summary for Patent: 12,427,108

Title:	Stable oral liquid composition of terazosin
Abstract:	The present invention relates to novel stable oral liquid composition of Terazosin and its pharmaceutically acceptable salt which is useful for treating symptomatic benign prostatic hyperplasia (BPH) and hypertension.
Inventor(s):	Muthusamy Shanmugam, Palanisamy Sivakumar
Assignee:	Novitium Pharma LLC
Application Number:	US17/458,674
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 12,427,108 (Terazosin Oral Liquid): Claim Scope, Legal Boundaries, and US Patent Landscape

Executive summary: US Patent 12,427,108 claims a tightly specified terazosin-containing oral liquid defined by (i) terazosin concentration 0.5–5 mg/mL, (ii) pH 5.0–6.5 (with dependent narrower range 5.0–6.0), (iii) a defined cosolvent/humectant excipient band of 15–25% w/v glycerine and/or propylene glycol, (iv) an allowed pH-modifier list and defined pH-modifier concentration bands, and (v) an exclusion: no other antihypertensive active agent. The estate also includes use claims for symptomatic BPH and hypertension. The combination of concentration windows, excipient percentage limits, pH targets, and formulation exclusions creates both (a) a clear infringement hook for near-copy formulations and (b) a predictable design-around route for competitors who can shift pH, terazosin concentration, excipient composition/level, or alter the “no other antihypertensive active agent” boundary.

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What does US Patent 12,427,108 claim for terazosin oral liquid compositions?

Core claimed subject matter (independent claim 1): A specific oral liquid pharmaceutical composition comprising:

• Active: terazosin or salt, 0.5–5 mg/mL (terazosin content basis).
• pH: composition has pH 5.0–6.5.
• pH modifier: at least one pH modifier (from a defined list in dependent claim 5).
• Vehicle: liquid vehicle comprising water.
• Excipients: includes at least one pharmaceutically acceptable excipient where excipient comprises 15–25% w/v glycerine, propylene glycol, or combination.
• Exclusion: the oral liquid does not contain any other antihypertensive active agent.
• Optional add-ins (dependent claims): preservatives, sweeteners, each with defined exemplified lists and concentration bands.

Claim architecture: Claim 1 is a formulation “box.” Dependent claims progressively narrow:

• Salt form: claim 2 (terazosin HCl).
• Dose band: claims 3 and 4 (terazosin 1–4 mg/mL; and specifically ~1 mg/mL).
• pH modifier identity: claim 5 (fixed list of inorganic/organic acids, bases, salts).
• pH modifier quantity bands: claims 6 and 7 (0.05–2 mg/mL; and 0.15–2 mg/mL).
• Excipient concentration refinement: claim 9 (18–22% w/v glycerine/propylene glycol/combination).
• Preservatives list and concentration: claims 10 and 12.
• Sweeteners list and concentration: claims 11 and 13.
• pH subrange: claim 14 (5.0–6.0).
• Stability/assay window: claim 15 (content retention after storage conditions).
• Indications/methods: claims 16–17.

What is the likely literal scope of “15% w/v to 25% w/v glycerine, propylene glycol, or combination thereof”?

Literal infringement depends on whether the accused product has:

• Total glycerine and propylene glycol (if “combination thereof” is interpreted as the total of those two) within 15–25% w/v; and
• The composition is an oral liquid with water and pH 5.0–6.5.

Practical enforcement: Competitors can narrow risk by altering the humectant/cosolvent band (below 15% or above 25%, or swapping to different excipients such as PEGs, sorbitol-only, or ethanol-free but different solubilizers), unless other claims create overlap.

How does the “no other antihypertensive active agent” limitation affect infringement risk?

Claim 1 expressly excludes combinations with other antihypertensive active agents. This does two things:

• It blocks infringement for combination therapy products.
• It may create factual/legal complexity over what counts as an “antihypertensive active agent,” especially where other actives are present for co-morbidities (for example, diuretics, beta blockers, calcium-channel blockers, ACE inhibitors, ARBs, direct renin inhibitors) versus non-antihypertensive actives.

Design-around lever: a generic/sponsor could argue it does not “contain any other antihypertensive active agent” by formulating with only terazosin plus non-antihypertensive actives. If other antihypertensives are not present, this limitation becomes less of a differentiator.

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Which dependent claims narrow terazosin concentration, pH, and excipient ranges most?

Terazosin concentration bands (claims 3–4)

• Claim 3: terazosin 1–4 mg/mL
• Claim 4: terazosin ~1 mg/mL

Literal scope: If a product is at 0.6 mg/mL or 4.5 mg/mL, it may avoid dependent claims 3/4 while still falling under claim 1 (0.5–5 mg/mL). So claim 1 is the dominant infringement “net,” while claims 3/4 reduce safe-harbor space only if a challenger argues non-overlap with dependent features.

pH ranges (claims 14)

• Claim 1: pH 5.0–6.5
• Claim 14: pH 5.0–6.0

Design-around: Competitors can target pH 6.05–6.5 to fall outside claim 14 while staying within claim 1. Claim 1’s upper limit at 6.5 limits how far pH can be shifted without stepping outside the independent claim. Any pH strategy must preserve stability and solubility.

Excipient concentration refinement (claim 9)

• Claim 1: excipient comprises 15–25% w/v glycerine/propylene glycol/combination
• Claim 9: narrows to 18–22% w/v

Implication: A product at 15–17.9% or 22.1–25% would avoid claim 9 but likely remain within claim 1.

pH modifier identity (claim 5)

The pH modifier is limited in dependent claim 5 to a closed list including:

• acids: citric, malic, phosphoric, tartaric, fumaric, sodium dihydrogen phosphate monohydrate, etc. plus hydrochloric acid
• bases/salts: ammonium chloride, potassium bicarbonate/carbonate, sodium acetate, sodium chloride, sodium hydroxide, potassium phosphate, etc.

Claim 1 still requires “at least one pH modifier” without specifying identity; claim 5 provides a stronger, narrower infringement path for products that use one of the listed pH modifiers.

pH modifier quantity bands (claims 6–7)

• Claim 6: pH modifier 0.05–2 mg/mL
• Claim 7: pH modifier 0.15–2 mg/mL

If a competitor uses different amounts outside these bands, it can potentially avoid claims 6/7 while still satisfying claim 1.

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What stability and shelf-life requirements are in US 12,427,108?

Stability assay claim (claim 15)

Claim 15 requires the composition exhibits:

• terazosin content of 100 ± 10% labeled content for about 6 months at 25 ± 2°C and 60 ± 5% RH.

Scope impact: This is a performance-based formulation limitation. It is typically evaluated by:

• accelerated or real-time stability protocols consistent with common pharmaceutical practice,
• assay methods and acceptance criteria that match the stated content range.

Enforcement path: If an accused product is close in composition but fails the stability requirement, claim 15 may not be met even if claim 1 is met. In litigation, stability can become a decisive element for narrower dependent claim assertions.

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How do the method-of-use claims (BPH and hypertension) expand infringement?

Claim 16: treating symptomatic benign prostatic hyperplasia (BPH)

Infringement typically requires:

• administration of a therapeutically effective amount of the claimed composition to treat BPH.

Claim 17: treating hypertension

Similarly requires administration for hypertension.

Practical risk: If a product matches the formulation scope in claim 1, methods can be asserted based on:

• labeling indications and promotion (where relevant for inducement theories),
• actual prescribing/use evidence.

Design-around limits: A competitor cannot avoid a method-of-use claim simply by changing the indication if the product is marketed or used for those conditions. However, labeling-only workarounds sometimes reduce certain enforcement theories depending on jurisdiction and pleadings.

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What patent landscape issues typically surround US formulation patents like 12,427,108?

Given the claim text, the relevant landscape question for business and litigation posture is not “does the molecule have prior patents,” but whether there is:

1. a dense formulation/concentration/pH/humectant patent cluster in terazosin oral liquids, and
2. whether other patents in the estate cover manufacturing process, alternative excipient systems, additional salts, different pH modifiers, or different dosing strengths.

However, producing a complete “US patent landscape” with numbered US family members, expiration dates, and assignee mapping requires authoritative bibliographic data beyond the claim text you provided. Under the operating constraints, only the claim-scoped analysis can be produced here.

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Claim-to-design-around map: where competitors can avoid US 12,427,108

Avoid by shifting concentration

• Stay outside 0.5–5 mg/mL to avoid claim 1 entirely.
• If remaining in that window, you may still avoid dependent claims 1–4 mg/mL or ~1 mg/mL.

Avoid by shifting pH

• Shift to outside 5.0–6.5 to avoid claim 1.
• If staying within claim 1, shift to 6.0–6.5 to avoid claim 14.

Avoid by shifting humectant/cosolvent load

• Move outside 15–25% w/v glycerine/propylene glycol to avoid claim 1.
• If only avoiding dependent claim 9, target below 18% or above 22% while staying inside 15–25%.

Avoid by using different pH modifiers or quantities

• Use pH modifiers outside the dependent claim 5 list or outside the dependent quantity bands (claims 6–7) while maintaining the independent claim 1 requirement that the product has a pH modifier and pH target.

Avoid by combination therapy with another antihypertensive active

• If the product contains another antihypertensive active agent, it likely falls outside claim 1 due to the express exclusion. This is not always feasible clinically, but it is a clear textual boundary.

Avoid by shelf-life/stability performance

• For claim 15 specifically, a formulation that is otherwise inside claim 1 but fails the 6-month stability acceptance criteria can avoid that dependent claim.

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How strong is the patent estate likely to be for infringement risk assessments?

Based on claim 1’s structure, US 12,427,108’s strength in enforcement tends to track whether an accused product is:

• an oral liquid (not tablets/capsules),
• uses terazosin within 0.5–5 mg/mL,
• targets pH 5.0–6.5,
• has water vehicle and the humectant range of 15–25% w/v,
• excludes “other antihypertensive active agents.”

That is a relatively narrow and testable set of formulation parameters. From an infringement standpoint, this reduces the range of potential “accidental” overlap and increases the value of pre-submission formulation comparison and bench testing against pH and excipient %.

From a validity standpoint (conceptually), the tight numeric limitations can be harder to anticipate in a single prior art reference; they can also preserve novelty if the prior art discloses terazosin liquid but not in the same pH/excipient/absence-of-other-antihypertensive framework. The flip side is that if terazosin oral liquids were already taught with similar pH and excipient bands, the independent claim could be challenged for obviousness over multiple teachings. The resolution requires prior art data, which is not part of the provided input.

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Key Takeaways

1. US 12,427,108 claim 1 is a formulation “box”: terazosin 0.5–5 mg/mL, water-based oral liquid, pH 5.0–6.5, and 15–25% w/v glycerine/propylene glycol (or combination), plus an exclusion of other antihypertensive actives.
2. Dependent claims narrow terazosin strength (1–4 mg/mL; ~1 mg/mL), pH (5.0–6.0), humectant band (18–22% w/v), and specify pH modifier identity and amount.
3. Claim 15 adds a stability performance requirement: 100 ± 10% labeled content after 6 months at 25°C/60% RH.
4. Claims 16–17 are method-of-use coverage for BPH and hypertension, increasing enforcement relevance through labeling/promotion and prescribing patterns when formulation overlap exists.
5. The most direct design-arounds are to shift pH, shift terazosin concentration, or move glycerine/propylene glycol outside the defined ranges, with secondary options around pH modifier selection/quantity and stability.

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FAQs

1. What excipient changes most effectively avoid US 12,427,108 claim 1 while keeping terazosin in an oral liquid?
2. Does a terazosin oral liquid at pH 6.2 infringe claim 14 if it meets the pH 5.0–6.5 requirement of claim 1?
3. If terazosin concentration is 4.6 mg/mL, which claims are potentially avoided within the claim set?
4. How does the “no other antihypertensive active agent” limitation affect combination products that include diuretics or beta blockers?
5. What is the litigation significance of claim 15 stability testing under standard ICH storage conditions?

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References

No external sources were cited because the analysis was limited to the claim set provided in the prompt.

Drugs Protected by US Patent 12,427,108

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novitium Pharma	TEZRULY	terazosin hydrochloride	SOLUTION;ORAL	218139-001	Jul 29, 2024		DISCN	Yes	No	12,427,108		Y			TREATMENT OF HYPERTENSION IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN
Novitium Pharma	TEZRULY	terazosin hydrochloride	SOLUTION;ORAL	218139-001	Jul 29, 2024		DISCN	Yes	No	12,427,108		Y			TREATMENT OF SYMPTOMATIC BENIGN PROSTATIC HYPERPLASIA (BPH) IN PATIENTS WHO ARE IN NEED OF A LIQUID COMPOSITION OF TERAZOSIN