Question

Which of the following is peroxisome proliferator-activated receptor-alpha (PPAR-α) agonist:

• A. Ezetimibe
• B. Niacin
• C. Colesevelam
• D. Gemfibrozil

Answer 1

The Correct Option is D

The correct option is (D): Gemfibrozil.

Answer 2

Peroxisome proliferator-activated receptor-alpha (PPAR-α) is the nuclear receptor targeted specifically by the fibrate class of lipid-lowering drugs, and each option can be checked against its actual pharmacological class and mechanism:

1. Ezetimibe: Ezetimibe lowers LDL cholesterol by selectively inhibiting the intestinal absorption of dietary and biliary cholesterol at the brush border (via the NPC1L1 transporter); it does not act on PPAR-α at all.
2. Niacin: Niacin (nicotinic acid) lowers triglycerides and raises HDL mainly by inhibiting lipolysis in adipose tissue through a separate G-protein-coupled receptor (GPR109A), not through PPAR-α activation.
3. Colesevelam: This is a bile acid sequestrant that binds bile acids in the intestine, promoting their faecal excretion and forcing the liver to convert more cholesterol into new bile acids; its action has nothing to do with PPAR-α.
4. Gemfibrozil: Gemfibrozil belongs to the fibrate class, and fibrates work precisely by activating PPAR-α in the liver, which upregulates lipoprotein lipase activity and fatty-acid oxidation, lowering triglyceride levels. This mechanism directly matches what the question asks for.

Only gemfibrozil, among the four, works through activation of the PPAR-α receptor.

Therefore, the correct answer is Gemfibrozil.