United States Patent 9,585,868 (Crofelemer): Claim Scope, Practical Coverage, and US Landscape
US Patent 9,585,868 is directed to methods for treating HIV-associated diarrhea and HAART-associated diarrhea in an HIV-positive subject using crofelemer at specified dosing regimens and treatment durations. The patent’s enforceable value is concentrated in (i) dose-amount ranges (about 250 mg/day or 125 mg twice daily), (ii) duration/timing-related limitations (including “day 3” onset and later increasing response), and (iii) clinical endpoint definitions tied to stool metrics, abdominal scores, urgency/incontinence days, and treatment success criteria.
What do the independent and dependent claims cover?
1. What is the core independent claim scope? (Claim 1)
Claim 1 is a closed formulation of a therapeutic method:
- Indication: “ameliorating symptoms” of HIV-associated diarrhea or HAART-associated diarrhea
- Population: HIV-positive subject in need thereof
- Therapy: crofelemer
- Dose (required):
- about 250 mg per day, or
- about 125 mg two times per day
- Intended effect: “to ameliorate the symptoms” of the diarrhea type in the subject
Scope effect: Any US activity that performs the method steps (administering crofelemer at the recited regimen to the recited patient population for the stated indication with the claimed symptom amelioration) is within claim 1’s concept of coverage. The claim is not a composition claim; it is a method claim, so infringement risk tracks dosing/administration and therapeutic use.
2. How do dependent claims narrow or add enforceable limitations? (Claims 2–20)
Dependent claims add explicit duration, timing of symptom onset, endpoint measurement components, and subgroup dosing/usage context.
Duration and response timing limits
- Claim 2: administration from about 1 month to about 6 months
- Claim 3: administration from about 3 days to about 6 months
- Claim 4: improvement begins on day 3
- Claim 5: improvement increases with longer duration after day 3
- Claim 6: administration for at least 8 days
- Claim 7: administration between 8 days and 24 weeks
- Claim 8: administration for about 6 months
- Claim 9: administration for about 6 months or longer
- Claim 10: administration for the duration of HIV infection
- Claim 11: response increases after crofelemer has been administered for longer than 4 months
Scope effect: These are “additional limitations.” They do not remove coverage from claim 1. Instead, they create narrower variants that are easier to map to specific clinical protocols and reduce ambiguity when the facts align to a dependent claim.
Clinical endpoint structure (what “amelioration” means)
- Claim 12: ameliorating includes one or more of:
- decrease in bowel movements/day
- decrease in watery bowel movements/day
- improvement in daily abdominal pain/discomfort score
- improvement in daily stool consistency score
- “stool consistency leading to formed stools from watery stools”
- decrease in days/week with urgency
- decrease in days/week with fecal incontinence
- decrease in unscheduled visit for significant worsening of diarrhea
- Claim 13: specifically includes improvement in daily stool consistency score
- Claim 14: specifically includes stool consistency leading to formed stools from watery stools
- Claim 15: treated if decreased watery bowel movements/day
- Claim 16: treated if decreased bowel movements/day
- Claim 17: symptom changes are measured from baseline
- Claim 18: decreasing the number of days/week with fecal incontinence
Scope effect: These claims can be leveraged to argue method infringement when evidence shows the dosing and patient group and demonstrates the specified clinical endpoint improvements, especially if a protocol defines response success using watery and/or total bowel movements.
Patient subgroup limitation
- Claim 19: HIV positive subject male
- Claim 20: separate method: treating/improving in HIV-positive subject who previously used protease inhibitors, with the same dosing amounts:
- about 250 mg/day, or about 125 mg twice daily
- explicitly: “previously used protease inhibitors”
Scope effect:
- Claim 19 creates a narrower “male” subgroup coverage.
- Claim 20 introduces an exposure history limitation that can matter in clinical trial eligibility and real-world prescribing if protease-inhibitor use is documented.
How does this claim set translate into operational infringement risk?
Dosing and administration triggers
A practical map to the claim limitations:
Any US administration of crofelemer to HIV-positive patients for HIV-associated or HAART-associated diarrhea at:
- about 250 mg/day, or
- about 125 mg twice daily
creates direct alignment with claim 1.
Additional “fact patterns” that strengthen enforceability:
- protocols where clinical improvement is documented to begin day 3
- protocols where dose response increases after day 3 and/or after 4 months
- studies or treatment regimens requiring at least 8 days or specifying durations 3 days to 6 months or 8 days to 24 weeks
- endpoint reporting using watery and total stool metrics, stool consistency, urgency/incontinence day counts, and abdominal score metrics
- clinical trial inclusion criteria or analysis stratifying protease-inhibitor-experienced subjects (Claim 20)
What is not claimed (relevant to designing around coverage)
The claims are method-of-use focused on crofelemer and a specific dosing regimen. What matters for noninfringing design is whether the regimen differs in a way that avoids the “about 250 mg/day or about 125 mg twice daily” dosing anchor and whether the treated population/indication matches “HIV-associated diarrhea or HAART-associated diarrhea.”
Claim-by-claim coverage matrix (how each limitation can be satisfied)
| Claim |
Key limitation |
Coverage anchor |
| 1 |
Crofelemer; HIV-associated diarrhea or HAART-associated diarrhea; HIV-positive subject; dose about 250 mg/day or 125 mg BID |
Broad method-of-use core |
| 2 |
Duration 1 month to 6 months |
Adds duration band |
| 3 |
Duration 3 days to 6 months |
Adds shorter-to-mid band |
| 4 |
Improvement begins day 3 |
Adds timing onset |
| 5 |
Improvement increases with longer duration after day 3 |
Adds post-onset slope |
| 6 |
At least 8 days |
Adds minimum duration |
| 7 |
8 days to 24 weeks |
Adds band including ~6 months |
| 8 |
About 6 months |
Fixes near a single endpoint |
| 9 |
About 6 months or longer |
Fixes duration ceiling beyond 6 months |
| 10 |
Duration of HIV infection |
Maximum duration concept |
| 11 |
Response increases after >4 months |
Adds late-phase timing |
| 12 |
Endpoint bundle (BM/watery BM, stool consistency, urgency/incontinence days, abdominal score, unscheduled worsening visit) |
Defines “ameliorating” with concrete measures |
| 13 |
Daily stool consistency score improvement |
Endpoint subcategory |
| 14 |
Formed stools from watery stools |
Endpoint subcategory |
| 15 |
Treated if decreased watery BM/day |
Success metric |
| 16 |
Treated if decreased BM/day |
Success metric |
| 17 |
Measured vs baseline |
Trial design/analysis alignment |
| 18 |
Decrease days/week fecal incontinence |
Endpoint subcategory |
| 19 |
HIV-positive male |
Demographic subgroup |
| 20 |
Protease inhibitor-experienced subjects; crofelemer at same dose |
Indication subpopulation with prior exposure history |
Relationship to crofelemer’s positioning in the US market
Crofelemer (brand name associated with chronic noninfectious diarrhea and other GI conditions historically) has been developed for diarrhea symptom control and has claimed use in HIV-associated diarrhea/HAART-associated diarrhea through crofelemer method claims like those in US 9,585,868. In a landscape sense, this patent’s value comes from:
- Method-of-use exclusivity for a specific indication and dosing
- Protocol-specific enforceability hooks (day 3 onset; response increases after 4 months; duration windows; watery stool endpoints)
- Subpopulation narrowing (protease inhibitor-experienced; male)
Practical patent-landscape implications (US strategy)
1. Where this patent blocks or burdens competitors
Competitors who seek to market or clinically deploy crofelemer-like diarrhea treatments in the HIV/HAART diarrhea space face a heightened risk if they plan to:
- use crofelemer at the claimed dose anchors, and
- structure clinical evidence around the claimed endpoint measures, and
- administer to HIV-positive subjects for the same diarrhea type.
Because the claims are methods, liability can arise from administration and evidence-generation protocols, not only from labeling text.
2. How design-arounds may occur (claim-feature shifts)
The principal levers are:
- change the administered dosing away from the claim’s “about 250 mg/day” or “about 125 mg BID” anchor
- avoid the specific indication framing (HIV-associated diarrhea vs HAART-associated diarrhea) in a way that is consistent with clinical documentation
- avoid alignment with key timing/duration-dependent dependent claims by using regimens outside the bands (though claim 1 remains a baseline if the dose anchor and method steps are met)
3. How clinical trial planning interacts with these claims
These claims align tightly to clinical assessment components:
- stool consistency and watery vs total bowel movements
- urgency and fecal incontinence days/week
- abdominal pain/discomfort score
- baseline-referenced changes
- onset at day 3 and late-phase increases after 4 months
Trials designed to prove effectiveness will typically measure these parameters; that creates fact patterns that can be used to map onto dependent claims even when label language differs.
Key Takeaways
- US 9,585,868 is a method-of-use patent centered on crofelemer dosing for HIV-associated diarrhea and HAART-associated diarrhea in HIV-positive subjects.
- The claims’ enforceable core is anchored on about 250 mg/day or about 125 mg twice daily (Claim 1).
- Dependent claims add strong additional hooks around treatment duration, onset (day 3), response increasing after day 3 and after >4 months, and specific clinical endpoints (watery/total bowel movements, stool consistency including formed stools from watery stools, urgency/incontinence days/week, abdominal score, and worsening-visit metric).
- Subgroup limitations include male-only (Claim 19) and protease inhibitor-experienced subjects (Claim 20), which can matter in eligibility criteria and evidence stratification.
- The landscape risk for competitors is highest when their US clinical protocols and real-world prescribing follow the dose anchor and generate outcomes using the claimed endpoint constructs.
FAQs
1) Is US 9,585,868 a composition-of-matter patent?
No. It is a method of treatment claim set.
2) What dosing regimens define the claim coverage?
The claims anchor to about 250 mg/day or about 125 mg twice daily.
3) Do the dependent claims require day 3 improvement?
Dependent Claim 4 does, but Claim 1 does not. Day-3 improvement is an added limitation only for that dependent claim.
4) What clinical endpoints are explicitly included as “ameliorating”?
They include decreases in bowel movements and watery bowel movements, stool consistency moving from watery to formed stools, abdominal pain/discomfort score improvement, decreases in urgency and fecal incontinence days/week, and decreases in unscheduled worsening visits (Claim 12, with sub-claims 13–18).
5) Does the patent cover patients with prior protease inhibitor use?
Yes. Claim 20 covers treating or improving HIV-associated or HAART-associated diarrhea in HIV-positive subjects who previously used protease inhibitors, using the same crofelemer dosing.
References
[1] United States Patent Application / Patent US 9,585,868 (claims as provided in the prompt).
