Pancrelipase (DB00085) - A Definitive Monograph

1.1. Executive Summary

Pancrelipase (DrugBank ID: DB00085) is a cornerstone therapy for the management of exocrine pancreatic insufficiency (EPI). It is a complex biological drug product, not a single chemical entity, derived from porcine pancreatic glands and standardized for its enzymatic activity.[1] Its primary function is to replace the endogenous digestive enzymes—lipase, protease, and amylase—that are deficient in patients with EPI, a condition arising from various underlying pathologies such as cystic fibrosis, chronic pancreatitis, and pancreatectomy.[3]

The therapeutic action of pancrelipase is executed locally within the lumen of the gastrointestinal (GI) tract, specifically the duodenum and small intestine. The enzymes facilitate the breakdown of dietary fats, proteins, and starches into absorbable components, thereby mitigating malabsorption, steatorrhea, and malnutrition.[3] A critical aspect of its pharmacology is its formulation; modern pancrelipase products are delivered in delayed-release capsules containing enteric-coated microspheres or minitablets. This technology is essential to protect the acid-labile enzymes from the gastric environment and ensure their release in the alkaline milieu of the small intestine where they are active.[5] Consequently, pancrelipase exhibits minimal to no systemic absorption, and traditional pharmacokinetic parameters such as distribution, metabolism, and half-life are not clinically relevant.[1]