Drug intelligence / Profile preview

atorvastatin + lisinopril + orlistat + pioglitazone + vitamin E

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination of five agents, each with distinct mechanisms and indications: - **Atorvastatin** is an HMG-CoA reductase inhibitor (statin) used to lower cholesterol by inhibiting the rate-limiting step in cholesterol biosynthesis. - **Lisinopril** is an angiotensin-converting enzyme (ACE) inhibitor used primarily for hypertension and heart failure by blocking the conversion of angiotensin I to angiotensin II, leading to vasodilation. - **Orlistat** is a gastrointestinal lipase inhibitor that reduces dietary fat absorption, indicated for obesity management. It acts locally in the gut without systemic absorption[7]. - **Pioglitazone** is a thiazolidinedione antidiabetic agent that acts as a peroxisome proliferator–activated receptor gamma (PPARγ) agonist, improving insulin sensitivity and glucose metabolism[2][8][9][10]. - **Vitamin E** is a fat-soluble antioxidant supplement; it protects cell membranes from oxidative damage. In some contexts, it has been studied in combination with pioglitazone for nonalcoholic steatohepatitis (NASH)[2]. There are no known approved pharmaceutical products combining all five ingredients into one formulation. The combination would be highly unusual due to potential drug-drug interactions—especially between orlistat and both pioglitazone and vitamin E—and differing indications[1][3][5]. Each component has established uses but also specific contraindications when combined.

02

Targets

ACE (Angiotensin Converting Enzyme)PNLIP (Pancreatic triacylglycerol lipase)PPARG (Peroxisome proliferator-activated receptor gamma)PDE6D (Phosphodiesterase 6-delta)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)LIPF (Gastric lipase)TTPA (Alpha-tocopherol transfer protein)

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