Patent 5,753,618 Landscape: Scope, Claim Parsing, and US Exclusivity Risk for Octreotide Acetate + Lactic Acid Parenteral Formulations

United States Patent 5,753,618 centers on a specific parenteral formulation of octreotide acetate with lactic acid at defined ratios and pH control using sodium hydrogen carbonate, with mannitol in isotonic sterile water. The patent also includes method-of-treatment claims for breast cancer and adds a dependent co-administration claim with a dopamine agonist. The scope is formulation- and parameter-bound (ratio, pH range, mg/mL ranges), which narrows both design-around space and infringement analysis. Risk to competitors is tied to whether an accused product matches the claim parameters and whether the method claims are pursued in the US with the claimed administration regimen.

What does US Patent 5,753,618 claim for octreotide acetate + lactic acid parenteral compositions?

Core claim theme. Claim 1 is a composition claim with multiple conjunctive limitations:

active = octreotide acetate
excipient system = 88% lactic acid
ratio constraint between octreotide acetate and lactic acid
pH control window using sodium hydrogen carbonate (hydrogen carbonate) to pH 4 to 4.5
mannitol in isotonic sterile water
intended parenteral administration

Because infringement of a composition claim generally requires all limitations, the claim’s “design-around” relevance is driven by how strictly a product matches the ratio, lactic acid concentration identity (88% lactic acid), pH target window, and the inclusion of mannitol plus isotonic sterile water.

Claim 1 limitations decoded (practical infringement elements)

Claim 1: “A pharmaceutical composition consisting of …”

“Consisting of” is a limiting term. It generally excludes additional ingredients beyond those recited, unless they are impurities or do not meaningfully add to the composition. For litigation strategy and infringement mapping, this pushes the analysis toward “literal fit” of ingredient list and whether any additional stabilizers, buffers, tonicity agents, or preservatives are used.

Octreotide acetate + 88% lactic acid

“88% lactic acid” is a specificity lever. Products using different lactic acid concentrations or salts (for example, sodium lactate rather than lactic acid at a defined strength) can fall outside literal scope depending on formulation details.

Ratio requirement

Octreotide acetate to lactic acid ratio is stated as:
- “1 part octreotide to 5 parts lactic acid”
- “up to 1 part octreotide to 60 parts lactic acid”

Interpreting that in a claim-construction manner: the ratio range is effectively between 1:5 and 1:60 (octreotide acetate : lactic acid), inclusive on endpoints as written.

pH control with sodium hydrogen carbonate

Sodium hydrogen-carbonate is used “to pH 4 to 4.5.”
This ties infringement to the final formulation pH at administration, not just buffering capability.

Mannitol in isotonic sterile water

This adds a second tonicity agent/tenderization requirement: mannitol must be present, and the vehicle must be isotonic sterile water.

Claims 2-4 narrow the ratio and strength further

Claim 2 (ratio subrange)

Octreotide acetate : lactic acid ratio is “1 to 5 up to 1 to 40.”
This is a tighter band than Claim 1. It matters because a competitor could be within Claim 1 but outside Claim 2 (for example, using ratios between 40 and 60).

Claim 3 (concentration window)

Octreotide acetate: 0.05 to 1 mg/mL
Lactic acid: 3 mg/mL
This is both a concentration and fixed-concentration constraint for lactic acid. It can be an infringement “gate” because Claim 3 sets lactic acid at 3 mg/mL, even though Claim 1 allows broader ratios.

Claim 4 (pH fixed point)

pH is 4.2.
This is an even tighter parameter for the pH. A product buffered to 4.1 or 4.3 can avoid literal scope for Claim 4 while potentially remaining within Claim 1 (pH 4 to 4.5).

What method-of-use claims does US 5,753,618 cover for breast cancer and dopamine agonist co-administration?

The patent adds treatment claims that depend on administering the composition of Claim 1 (or Claim-set composition).

Claim 5: breast cancer treatment

“A method of treating breast cancer … administering a therapeutically effective amount of the composition of claim 1.”

This is a classic method-of-use claim tied to a specific formulation. For method-of-use infringement, the accused activity must include:

a subject with breast cancer
administration of a therapeutically effective amount
using the exact composition of Claim 1 (including formulation parameters)

Claim 6: co-administration with a dopamine agonist

“The composition … co-administered with a dopamine agonist.”

This creates additional specificity: a regimen that pairs the octreotide acetate formulation with a dopamine agonist in the breast cancer treatment setting.

Litigation implication. Claim 6 is not just “octreotide formulation used for breast cancer.” It is “octreotide formulation used for breast cancer with a dopamine agonist co-administered.” If a competitor treats breast cancer with octreotide but without dopamine agonist co-therapy, Claim 6 is harder to match.

How broad is US 5,753,618 compared with typical octreotide parenteral formulation patents?

Featured-scope conclusion: The claims are narrower than broad peptide formulation patents because they require:

octreotide acetate formulated specifically with 88% lactic acid
a defined octreotide:lactic acid ratio range
sodium hydrogen carbonate used to achieve a strict pH window
mannitol in isotonic sterile water
“consisting of” language that constrains ingredient add-ons

These limits reduce the effective claim coverage across the full octreotide parenteral product universe, where formulations often use different buffers, different acidity systems, or different tonicity agents.

Where scope is strongest

Products designed to replicate a lactic-acid based solubilization and pH stabilization strategy with mannitol as tonicifier
Formulations that land inside pH 4 to 4.5 and use sodium hydrogen carbonate for that pH setpoint
Products dosing octreotide acetate in the stated mg/mL band and containing lactic acid at 3 mg/mL (Claim 3)

Where scope is weakest (design-around levers)

Using lactic acid but not at “88% lactic acid” (composition identity mismatch)
Choosing a different buffering agent strategy so that sodium hydrogen carbonate is not used to reach pH 4 to 4.5
Targeting final pH outside the window (below 4 or above 4.5)
Omitting mannitol or using an alternative tonicity agent that changes isotonic system composition
Adding formulation ingredients that conflict with “consisting of” unless they are truly not additional components under claim construction

What patents likely intersect with the same octreotide formulation space?

Without reproducing an external patent map, the only defensible statement from the claim text alone is that this patent’s overlap zone is defined by:

octreotide acetate parenteral liquid formulations
lactic acid as an acid component (in a specific strength)
pH-adjustment using hydrogen carbonate/bicarbonate chemistry
mannitol isotonicity approach
anticancer method-of-use contexts (breast cancer specifically) and dopamine agonist co-therapy

In practice, competitive filings often fall into one of three buckets that can overlap:

formulation stability/solubility patents for peptide injectables
buffer and pH profile patents for injectable delivery
method-of-use patents for octreotide in oncology or combination regimens

US 5,753,618 spans both composition and method-of-use, increasing the chance that other patents cover adjacent features (stability, process, or alternative disease indications), but the claim’s strict parameter constraints reduce how often those other patents fully duplicate its scope.

When does US 5,753,618 lose enforceability for generic or biosimilar entry risk?

No expiration dates or statutory term data are provided in the prompt, and no claims/filing details beyond the claim text are present. A defensible timeline cannot be produced from the supplied information.

What is the Orange Book status of US 5,753,618?

No Orange Book listing information is provided, and the prompt does not include the drug product name, NDA/BLA number, listed formulation, or the Orange Book patent codes. A status determination cannot be produced.

Which competitors would face the highest formulation infringement risk?

Risk is highest for companies selling an octreotide acetate parenteral liquid that matches all of the following simultaneously:

includes 88% lactic acid
octreotide acetate:lactic acid ratio within 1:5 to 1:60 (and preferably 1:5 to 1:40 for Claim 2)
pH of 4.0 to 4.5 set using sodium hydrogen carbonate
includes mannitol and isotonic sterile water vehicle
uses “consisting of” compatible ingredient set (no material extra components, depending on claim construction)

Risk is specifically reduced if:

pH is outside 4 to 4.5
sodium hydrogen carbonate is replaced by another buffering system that does not use hydrogen carbonate to set pH
lactic acid strength differs from 88%
tonicity is achieved without mannitol
the composition differs meaningfully such that “consisting of” is not met

What generic entry risks exist under this patent’s claim structure?

Composition gatekeeping. Because Claim 1 is parameter-bound, a generic that uses a different acid or buffering strategy can reduce literal infringement exposure even if it shares octreotide acetate as the active.

Method-of-use exposure. The breast cancer and dopamine agonist co-administration claims create additional risk if the generic label or off-label prescribing behavior in the US corresponds to the claimed regimen using a product that practices Claim 1 composition parameters.

Practical litigation posture. For generics, the largest exposure typically comes from:

product formulation equivalence that inadvertently matches all Claim 1 parameters
proof of the “consisting of” compliance issues
evidence that the commercial use is in breast cancer settings with dopamine agonist co-therapy (for Claim 6)

How does the scope differ across claims 1-4 versus claims 5-6?

Claims 1-4 are formulation-limited

They focus on the physical composition, including excipients, pH, and quantitative ratios.
These claims can be designed around by changing pH strategy, lactic acid strength, ratio, or excipient set.

Claims 5-6 are regimen-limited

They require administration to treat breast cancer.
Claim 6 adds the additional limitation of dopamine agonist co-administration.
Even if a competitor practices the formulation, method-of-use infringement requires the use pattern consistent with the claim.

Patent claim chart (mapping the supplied claims into infringement elements)

Claim	Type	Must-have limitations (from text)	Key infringement sensitivity
1	Composition	Octreotide acetate + 88% lactic acid; ratio 1:5 up to 1:60; sodium hydrogen carbonate to pH 4-4.5; mannitol in isotonic sterile water; parenteral	pH set method and final pH; lactic acid “88%” identity; “consisting of” ingredient constraints
2	Dependent composition	Ratio 1:5 up to 1:40	ratio selection (40-60 band avoids this claim but not Claim 1)
3	Dependent composition	Octreotide 0.05-1 mg/mL; lactic acid 3 mg/mL	fixed lactic acid concentration and active concentration range
4	Dependent composition	pH exactly 4.2	fine pH control avoids literal claim
5	Method of use	Treat breast cancer by administering therapeutically effective amount of Claim 1 composition	requires matching both regimen and formulation
6	Dependent method	Claim 5 regimen plus co-administration with dopamine agonist	practice pattern: dopamine agonist pairing

Key Takeaways

US 5,753,618 protects a tightly defined octreotide acetate parenteral liquid system: 88% lactic acid, specific ratio ranges, sodium hydrogen carbonate adjusted to pH 4 to 4.5, and mannitol in isotonic sterile water, within a “consisting of” framework.
The formulation claims are narrow enough that design-around strategies using different lactic acid strength, pH/buffering system, tonicity agents, or ingredient sets can move an accused product outside literal scope.
The breast cancer and dopamine agonist co-administration claims add regimen specificity, increasing the importance of real-world prescribing and label/indication alignment.
The most credible infringement pathways are products that match all of Claim 1 parameters and use them for breast cancer treatment, with dopamine agonist co-therapy to trigger Claim 6.

FAQs

1) What pH range does US 5,753,618 require for octreotide acetate + lactic acid formulations?
Claim 1 requires pH 4.0 to 4.5; Claim 4 further fixes pH at 4.2.

2) Does the patent require 88% lactic acid specifically, or can other lactic acid strengths infringe?
Claim 1 specifies “88% lactic acid,” making lactic acid identity a key literal-scope variable.

3) What is the octreotide acetate-to-lactic acid ratio range in Claim 1?
Claim 1 covers 1 part octreotide acetate to 5 parts lactic acid up to 1 part octreotide acetate to 60 parts lactic acid.

4) What extra element does Claim 6 add beyond Claim 5?
Claim 6 requires co-administration with a dopamine agonist in the breast cancer treatment regimen.

5) How do Claims 2-4 narrow the formulation covered by Claim 1?
Claim 2 narrows ratio to 1:5 up to 1:40; Claim 3 sets octreotide 0.05-1 mg/mL and lactic acid 3 mg/mL; Claim 4 fixes pH at 4.2.

References

United States Patent 5,753,618. (Claim text provided in prompt).

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	8716324	Jul 10, 1987
United Kingdom	8716326	Jul 10, 1987

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	402896	⤷ Start Trial
Austria	A177788	⤷ Start Trial
Australia	1889388	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,753,618

Summary for Patent: 5,753,618