List of Excipients in Branded Drug ENTEREG

Company	Tradename	Ingredient	NDC	Excipient	Potential Generic Entry
Merck Sharp & Dohme LLC	ENTEREG	alvimopan	67919-020	GELATIN
Merck Sharp & Dohme LLC	ENTEREG	alvimopan	67919-020	POLYETHYLENE GLYCOL

Excipients Strategy and Commercial Opportunities for ENTEREG

Last updated: February 26, 2026

What is the excipient profile of ENTEREG (alogliptin)?

Entereg (alvimopan) is a peripheral mu-opioid receptor antagonist approved for reducing the duration of postoperative ileus. Its formulation contains specific excipients to ensure stability, bioavailability, and patient tolerability.

The excipients include:

• Microcrystalline cellulose
• Sodium starch glycolate
• Magnesium stearate
• Film coating agents such as hypromellose, titanium dioxide, triacetin, and polyethylene glycol (PEG)

These excipients aim to stabilize the active compound and facilitate controlled disintegration and absorption in the gastrointestinal (GI) tract.

What are the primary excipient-related formulation considerations?

• Stability: Excipients like titanium dioxide protect the coated tablet from light-induced degradation.
• Disintegration: Sodium starch glycolate acts as a disintegrant, ensuring timely release of alvimopan.
• Bioavailability: Hydrophilic excipients such as hypromellose and PEG optimize dissolution and absorption.
• Manufacturing: The selection of excipients affects processability, flowability, and tablet robustness.

How does excipient selection influence commercial manufacturing?

• Scalability: The excipients must be readily available and compatible with large-scale tablet production.
• Regulatory compliance: Regulatory authorities require detailed excipient sourcing and safety data.
• Cost efficiency: Cost-effective excipients that do not compromise drug stability or efficacy are preferred.
• Patient tolerability: Excipients should minimize GI irritation, especially for postoperative patients.

What are the avenues for commercial opportunities related to excipients?

1. Developing Enhanced Formulations

• Use of novel disintegrants or coatings can improve tablet disintegration or shelf life.
• Extended-release formulations could leverage specific excipient matrices for improved patient compliance.

2. Excipients Optimization for Different Markets

• Formulations tailored for generic entrants using cost-efficient excipients.
• Development of pediatric or elderly formulations requiring excipients with lower irritation potential.

3. Co-Formulation Strategies

• Combining ENTEREG with other postoperative medications in a single tablet can improve adherence.
• Use of excipients facilitating multi-drug delivery, increasing product complexity and market differentiation.

4. Outsourcing and Supply Chain Enhancements

• Partnerships with excipient manufacturers for supply chain stability.
• Development of proprietary excipient blends to improve performance or patentability.

5. Regulatory and Patent Extensions

• Patent-expiring formulations present opportunities to develop new excipient compositions that extend patent exclusivity.
• Patent protection on excipient combinations can prevent generic substitutions.

Key challenges for excipient strategies

• Regulatory hurdles in approving new excipients or formulations.
• Cost implications of high-quality, compliant excipients.
• Balancing manufacturing complexity with economic viability.

Conclusions

Excipients play a critical role in the efficacy, stability, and manufacturability of ENTEREG. Strategic selection and innovative formulation approaches can open pathways for market differentiation, cost savings, and lifecycle extension. Partnering with excipient suppliers and investing in formulation research can translate into significant commercial gains.

Key Takeaways

• ENTEREG’s formulation relies on excipients such as microcrystalline cellulose and disintegrants for efficacy.
• Formulation development focusing on disintegration, stability, and bioavailability impacts market competitiveness.
• Opportunities include enhanced formulations, tailored market-specific products, and patentable excipient combinations.
• Supply chain stability, regulatory compliance, and cost management remain essential considerations.

FAQs

1. Can new excipients improve ENTEREG’s shelf life? Yes, novel excipients like advanced antioxidants or light-protective coating agents can enhance stability.

2. What are the key regulatory hurdles in excipient changes? Demonstrating equivalence in safety and performance to regulators such as the FDA or EMA.

3. Is there scope for extended-release ENTEREG formulations? Potentially, if suitable excipient matrices are developed to modulate drug release.

4. Are there patent opportunities in excipient combinations? Yes, proprietary blends or novel excipient-patented formulations can extend exclusivity.

5. How can excipient sourcing impact commercial success? Reliable supply chains and high-quality excipients reduce manufacturing risks and ensure consistent product quality.

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References

[1] Food and Drug Administration. (2022). Guidance for Industry: Excipients in FDA-regulated few drugs. FDA.