Cetilistat is a novel, peripherally acting lipase inhibitor used for the management of obesity in conjunction with a mildly hypocaloric diet. It acts locally in the gastrointestinal tract to inhibit dietary fat absorption. Approved in India in 2015, it offers an alternative to orlistat with a potentially different side effect profile, particularly regarding gastrointestinal adverse events.
Adult: One 60mg capsule, taken three times daily (TDS) immediately before, during, or up to one hour after each main meal containing fat.
Note: Must be taken with meals. If a meal is missed or contains no fat, the dose should be omitted. The capsule should be swallowed whole with a glass of water. A daily multivitamin supplement (containing fat-soluble vitamins A, D, E, K) is recommended, to be taken at least 2 hours before or after cetilistat (e.g., at bedtime).
Cetilistat is a potent and reversible inhibitor of gastrointestinal lipases, primarily pancreatic lipase. It forms a covalent bond with the active serine site of the lipase enzyme within the lumen of the stomach and small intestine. This inhibition prevents the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides. As a result, undigested triglycerides are excreted in the feces, creating a caloric deficit.
Pregnancy: Category X. Contraindicated. Weight loss offers no potential benefit during pregnancy and may cause fetal harm.
Driving: No effect. Cetilistat does not cause sedation or affect cognitive function.
| Cyclosporine | Reduced absorption of cyclosporine leading to subtherapeutic levels. Monitor levels closely. | Major |
| Amiodarone | Theoretical risk of reduced absorption. Monitor efficacy. | Moderate |
| Acarbose | Increased gastrointestinal side effects. Use with caution. | Moderate |
| Orlistat | Concomitant use not studied; likely additive GI effects and no added benefit. Contraindicated. | Major |
| Warfarin & other Anticoagulants | Potential reduced absorption of Vitamin K, potentially enhancing anticoagulant effect. Monitor INR closely. | Major |
| Antiepileptics (e.g., Phenytoin, Valproate) | Theoretical risk of reduced absorption. Monitor drug levels and clinical effect. | Moderate |
| Levothyroxine | Potential reduced absorption. Administer levothyroxine at least 4 hours apart from cetilistat. | Moderate |
| Fat-soluble Vitamin Supplements (A, D, E, K) | Reduced absorption of vitamins. Administer supplements at least 2 hours before or after cetilistat. | Moderate |
Same composition (Cetilistat (60mg)), different brands: