Relevance of Gut Wall First-Pass Metabolism

from a pharmaceutical industry perspective, drug candidate attrition rates owing to an unexpectedly high gastrointestinal first-pass effect are low, because the majority of intestinal metabolic liabilities will have been readily detected in systems geared toward hepatic metabolism. 

The role of the gut mucosa in metabolically based drug-drug interactions. Drugs and the Pharmaceutical Sciences, 116, 359—385. 

3 Agoram, B., Woltosz, W.S. and Bolger, M.B. (2001) Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Advanced Drug Delivery Reviews, 50 (Suppl. 1), S41-S67. 

4 Yang, J., Jamei, M., Rowland Yeo, K., Tucker, G.T. and Rostami-Hodjegan, A. (2007) Prediction of intestinal first-pass metabolism. Current Drug Metabolism, 8, 676-684. 

5 Fagerholm, U. (2007) Prediction of human pharmacokinetics - gut-wall metabolism. The Journal of Pharmacy and Pharmacology, 59, 1335-1343. 

---