Details for Patent: 10,357,570

Summary for Patent: 10,357,570

Title:	Methods of treating nausea utilizing semi-solid delivery vehicle compositions comprising granisetron
Abstract:	A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
Inventor(s):	Steven Y. Ng, Hui-Rong Shen, Jorge Heller
Assignee:	Heron Therapeutics LLC
Application Number:	US15/897,093
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 10,357,570: Scope, Claims, and US Landscape

What is US Patent 10,357,570 trying to protect?

US Drug Patent 10,357,570 claims a method of treating nausea and vomiting by administering a specific semi-solid antiemetic composition. The composition is defined by three hard components and multiple internal constraints:

• A polyorthoester polymer with defined subunit composition and molecular weight
• Polyethylene glycol monomethyl ether (PEG monomethyl ether) with a defined molecular-weight window and 10-50 wt%
• Granisetron at 1-5 wt% (optionally at specific wt% values)

The claimed method scope is anchored to:

• the route and delivery form (semi-solid, injection, subcutaneous, syringe/needle gauge)
• clinical timing (acute or delayed; includes chemotherapy-associated nausea and vomiting)
• function/performance (irradiation stability, sterilization stability, sustained and controlled release, dispensability)

This is not a formulation for granisetron alone. It is a formulation-plus-method bundle: the polymer system plus delivery-ready semi-solid properties paired to a granisetron dosing concept for emesis indications.

---

What is the independent claim (Claim 1) in enforceable terms?

Claim 1 is a method claim with these composition limitations and treatment context:

Core treatment element

• “A method for the treatment of nausea and vomiting in a patient in need thereof”
• includes administering a semi-solid pharmaceutical composition

Composition element: required quantitative ranges

The semi-solid pharmaceutical composition must comprise:

1. Polyorthoester (balance component; implied by 10-50% PEG monomethyl ether and 1-5% granisetron)
2. 10-50 wt% polyethylene glycol monomethyl ether
   • PEG monomethyl ether MW 200 to 4,000
3. 1-5 wt% granisetron

Composition element: polyorthoester identity constraints

The polyorthoester must have:

• Subunits selected from a defined set (polyorthoester subunit structures are specified in the claim text with variables):
  • x is an integer 1-4
  • total amount of p is an integer 1-20
  • s is an integer 1-4
• α-hydroxyacid containing subunits: 0.1 to 25 mole %
• Polyorthoester molecular weight: 1000 to 10,000

Method-administering element

• “administering” is not limited in Claim 1 beyond later dependent claims (route is introduced in Claims 15-17)

Resulting claim meaning (how infringement is typically assessed)

To infringe Claim 1, an accused product/process must meet all of these:

• patient with nausea/vomiting
• semi-solid composition
• polyorthoester with the specified structural constraints and MW window
• PEG monomethyl ether at 10-50 wt% with MW 200-4,000
• granisetron at 1-5 wt% If any element fails, Claim 1 does not read.

---

What do the dependent claims narrow, and where are the “hard edges”?

Dependent claims set additional constraints that create multiple narrower enforcement footholds.

PEG molecular weight and granisetron dosing specifics

• Claim 2: PEG monomethyl ether MW about 550
• Claim 3: granisetron 2-3 wt%
• Claim 4: a specific example formulation:
  • 78.4 wt% polyorthoester
  • 19.6 wt% PEG monomethyl ether
  • about 2 wt% granisetron

These create an obvious “numerical moat” around preferred compositions: targets that use PEG monomethyl ether around 550 MW and granisetron around 2 wt% are squarely within Claim 2-4.

Polyorthoester molecular weight specifics

• Claim 5: polyorthoester MW about 6,500

This is another narrow “hit box” that often matches a disclosed exemplar.

Performance/quality attributes

• Claim 6: stable upon irradiation
• Claim 7: stable upon sterilization
• Claim 10: capable of sustained and controlled release after administration

These add functional limitations that can still be satisfied even if exact formulation varies within earlier numeric ranges, but they also provide grounds to invalidate or distinguish products based on stability/release testing.

Particle size and syringeability

• Claim 8: granisetron as a solid with particle size <100 microns
• Claim 9: capable of being dispensed from a 16-25 gauge needle
• Claim 16-17: administering by subcutaneous injection (Claim 16) via syringe with 16-25 gauge needle (Claim 17)
• Claim 15: administering by injection

These claims are particularly relevant for a product’s physical form (granisetron particle size) and device compatibility (needle gauge).

Indication timing and patient context

• Claim 11: nausea/vomiting associated with chemotherapy
• Claim 12: nausea/vomiting is acute or delayed
• Claim 13-14: administered in combination with another antiemetic (Claim 13 refers to Claim 12 dependent structure; Claim 14 repeats combination with another antiemetic for claim 12)

These create clinical scope for oncology supportive care use, including acute and delayed emesis paradigms.

---

How broad is the Claim 1 formulation space?

Claim 1 is broad on some axes and narrow on others.

Broad ranges (high likelihood of overlap across generics or follow-on formulations)

• PEG monomethyl ether: 10-50 wt%
• PEG monomethyl ether MW: 200-4,000
• granisetron: 1-5 wt%
• polyorthoester MW: 1,000-10,000
• α-hydroxyacid containing subunits: 0.1-25 mole%

Narrow identity constraints (hard to “design around”)

• polyorthoester subunits must match the claimed structural selection (variables x, p, s)
• PEG monomethyl ether must be the specific chemical class (not a different PEG-ether variant)
• functional stability and release are not in Claim 1 but are in dependent claims

Net: Claim 1 is not a one-formula monopoly; it is a “polymer-composition window” monopoly tied to specific structural polymer identity plus a specific small-molecule granisetron plus a PEG monomethyl ether excipient.

---

What is the enforceable treatment scope?

The claim is a method claim, so it targets conduct: giving the semi-solid composition to treat nausea/vomiting. The dependent claims specify:

• chemotherapy-associated emesis (Claim 11)
• acute or delayed nausea/vomiting (Claim 12)
• combination with another antiemetic (Claims 13-14)
• injection route and subcutaneous administration with standard needle ranges (Claims 15-17)

A product can still infringe Claim 1 even if it is not marketed solely as chemotherapy supportive care, provided it is used in a patient “in need thereof” for nausea/vomiting and the administered formulation meets the composition requirements.

---

What parts are most “design-around” sensitive?

A competitor seeking to avoid literal infringement typically focuses on at least one of these “anchor” constraints:

1. Granisetron wt%
   • must avoid 1-5 wt% for Claim 1 or 2-3 wt% for Claim 3
2. PEG monomethyl ether presence/amount/MW
   • Claim 1 requires 10-50 wt% PEG monomethyl ether and MW 200-4,000
   • specific PEG MW about 550 is targeted by Claim 2
3. Polyorthoester subunit identity and α-hydroxyacid mole %
   • Claim 1 constrains α-hydroxyacid-containing subunits to 0.1-25 mole% plus defined subunit selections with integer parameters
4. Polyorthoester molecular weight
   • Claim 1 constrains 1,000-10,000 MW; Claim 5 targets ~6,500
5. Device/physical form limitations (dependent claims)
   • particle size <100 microns (Claim 8)
   • ability to dispense from 16-25 gauge needle (Claim 9) and subcutaneous injection (Claim 16-17)

If a generic or follow-on changes the polymer system to a non-matching polyorthoester structure, it may avoid the subunit-based limitations. If it switches to a different antiemetic or changes granisetron dosing outside the claimed wt%, it may avoid.

---

Where does this sit in the broader patent landscape for antiemetic controlled release?

Practical landscape segmentation for investment and R&D

For granisetron antiemetic programs, US IP usually clusters into:

• Granisetron formulations (solutions, tablets, orally disintegrating forms)
• Depot or sustained-release delivery (injectables intended for longer dosing intervals)
• Polymeric controlled release systems (biodegradable polymers, in-situ forming depots)
• Combination antiemetic regimens (5-HT3 antagonists with NK1 antagonists, corticosteroids, etc.)

US 10,357,570 is specifically a semi-solid depot-like injection formulation built on a polyorthoester plus a PEG monomethyl ether component and uses granisetron.

What the dependent claims add from a landscape standpoint

The dependent claims extend beyond “controlled release” as an obvious concept by specifying:

• irradiation stability (Claim 6)
• sterilization stability (Claim 7)
• needle gauge dispensability (Claim 9)
• particle size for solid granisetron (Claim 8)

These are the types of attributes that can differentiate a polymer depot system from earlier controlled release disclosures even when the broad concept of depot granisetron is known.

---

How to interpret claim strength for freedom-to-operate

For FTO, the method claims create exposure whenever:

• the composition is administered (not merely manufactured)
• a patient is treated for nausea/vomiting
• the formulation matches Claim 1 parameters

Key FTO sensitivity points are the polymer specification and semi-solid formulation identity. The most common legal and technical failure modes for designing around are:

• mismatched polyorthoester subunit identity or α-hydroxyacid mole %
• PEG monomethyl ether not within wt% or MW limits
• granisetron not within specified wt%
• granisetron not a solid with particle size <100 microns (if relying on avoiding Claim 8)
• device compatibility changes (if avoiding Claim 9 and 16-17)

---

What should be the business read-through?

US 10,357,570 is likely strongest against products that:

• use granisetron as the antiemetic API
• use a polyorthoester system with comparable subunit chemistry and MW
• include PEG monomethyl ether in the defined wt% and MW window
• are developed as injectable semi-solid depots with controlled release for acute/delayed chemotherapy emesis
• retain sterilization and irradiation stability while remaining syringe/needle dispensable

If a rival program retains the polymer class but changes the PEG or polymer details outside the claim constraints, the legal outcome can turn on claim construction and subunit-structure evidence.

---

Key Takeaways

• US 10,357,570 claims a method to treat nausea/vomiting using a semi-solid injectable composition defined by polyorthoester + PEG monomethyl ether (10-50 wt%, MW 200-4,000) + granisetron (1-5 wt%).
• The polyorthoester is not generic: it is constrained by subunit identity, α-hydroxyacid mole % (0.1-25), and polyorthoester molecular weight (1,000-10,000).
• Dependent claims create additional “narrower enforcement” targets: PEG MW about 550, granisetron 2-3 wt% (and about 2 wt% in a specific example), polyorthoester MW about 6,500, irradiation/sterilization stability, granisetron solid particle size <100 microns, and 16-25 gauge needle dispensability including subcutaneous injection.
• From an FTO angle, avoiding infringement usually requires shifting at least one of the “anchor” constraints: granisetron wt%, PEG monomethyl ether identity/amount/MW, or polyorthoester subunit chemistry and α-hydroxyacid content.

---

FAQs

1) Is this patent about granisetron itself or about a delivery system?

It is about a delivery method. The claims require administering a semi-solid composition with a constrained polyorthoester + PEG monomethyl ether + granisetron system.

2) Does Claim 1 require chemotherapy?

No. Claim 11 adds chemotherapy as a dependent limitation. Claim 1 covers nausea/vomiting more generally.

3) Can a product infringe if it is injectable but not subcutaneous?

Claim 1 covers “administering” without limiting route; dependent claims specify injection and subcutaneous delivery (Claims 15-17). Whether route matters for infringement depends on whether the asserted claim is Claim 1 or a dependent claim.

4) What is the most “numerically constrained” piece in the claims?

PEG monomethyl ether and granisetron: PEG 10-50 wt% with MW 200-4,000, and granisetron 1-5 wt% (with narrower dependent ranges).

5) Which dependent claims are most likely to be used in a dispute?

Those that tie to product testing and usability: irradiation stability (Claim 6), sterilization stability (Claim 7), controlled release (Claim 10), particle size <100 microns (Claim 8), and 16-25 gauge needle dispensability (Claim 9 and 16-17).

---

References

[1] US Patent 10,357,570 (claims as provided in the prompt).

Drugs Protected by US Patent 10,357,570

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 10,357,570

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2005289425
Canada	2579297
China	101052376
European Patent Office	1796629
European Patent Office	2902012
European Patent Office	3424492