> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/orlistat-efe96c73-de97-4970-9f8d-0c5633a8b660 > Record changed: 2026-10-13 # Orlistat Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) First approval year 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) ## Development status **First approval year** 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **Drug name** Orlistat Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **Molecular weight** 495.75 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **Structure (SMILES)** CCCCCCCCCCC\[C@@H\](C\[C@@H\]1OC(=O)\[C@H\]1CCCCCC)OC(=O)\[C@H\](CC(C)C)NC=O Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) ### Brand names (8) - alli - Alli - Alli (previously orlistat gsk) - alli previously orlistat gsk - beacita - Beacita - xenical - Xenical ### Other names (56) - 120 mg orlistat - 60 mg orlistat - Alli® 60 mg - l leucine n formyl 1 3 hexyl 4 oxo 2 oxetanyl methyl dodecyl ester 2s 2 alpha r 3 beta - L-LEUCINE, N-FORMYL-, 1-((3-HEXYL-4-OXO-2-OXETANYL)METHYL)DODECYL ESTER, (2S-(2.ALPHA.(R\*),3.BETA.))- - lipstatin - Lipstatin - n formyl l leucine ester with 3s 4s 3 hexyl 4 2s 2 hydroxytridecyl 2 oxetanone - N-FORMYL-L-LEUCINE, ESTER WITH (3S,4S)-3-HEXYL-4-((2S)-2-HYDROXYTRIDECYL)-2-OXETANONE - nsc 758881 - NSC-758881 - orlipastat - Orlipastat - orlistat - Orlistat - Orlistat (Xenical) - ORLISTAT \[EMA EPAR\] - ORLISTAT \[HSDB\] - orlistat \[INN\] - ORLISTAT \[JAN\] - ORLISTAT \[MART.\] - ORLISTAT \[MI\] - ORLISTAT \[ORANGE BOOK\] - ORLISTAT \[USAN\] - ORLISTAT \[USP MONOGRAPH\] And 31 more, listed on the interactive page. ## Identifiers **ATC classification codes** - A08AB01 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **CAS registry numbers** - 96829-58-2 **ChEMBL ID** CHEMBL175247 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **InChIKey** AHLBNYSZXLDEJQ-FWEHEUNISA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL175247) **PubChem compound IDs** - 3034010 **RxNorm IDs (RxCUI)** - 37925 **FDA ingredient codes (UNII)** - 95M8R751W8 ## Regulatory information ### United States **Applicant** CHEPLAPHARM **Approval date** 23 Apr 1999 **Application number** NDA020766 ### European Union **Status** Authorised **Status date** 29 Jul 1998 **Authorisation date** 29 Jul 1998 **Approved indications** Xenical is indicated in conjunction with a mildly hypocaloric diet for the treatment of obese patients with a body mass index (BMI) greater or equal to 30 kg/m2, or overweight patients (BMI > 28 kg/m2) with associated risk factors. Treatment with orlistat should be discontinued after 12 weeks if patients have been unable to lose at least 5% of the body weight as measured at the start of therapy. **Product number** EMEA/H/C/000154 **Authorisation holder** CHEPLAPHARM Arzneimittel GmbH **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **Biosimilar medicines** 0 **Advanced therapy** No **Conditional approval** No **Additional monitoring** No **Accelerated assessment** No **Exceptional circumstances** No #### Therapeutic areas - Obesity European medicines record Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/xenical) ### Other regulatory facts **Patents** 0 **Designations** 1 **First in class** No **Fast track** No **Breakthrough designation** No **Orphan designation** No **Priority review** Yes **Orphan exclusivity** No **Accelerated approval** No **Availability** Over the counter ## Pharmacology ### Drug classification **Pharmacology name** orlistat **Type** Synthetic organic **Drug name stem** \-stat **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (7) - **Action** Inhibition **Action type** Inhibitor **Target** pancreatic lipase **Gene symbol** PNLIP **Protein identifier** P16233 **Median affinity** 8.9 **Affinity units** pIC50 **Primary target** Yes - **Action** Inhibition **Action type** Inhibitor **Target** fatty acid synthase **Gene symbol** FASN **Protein identifier** P49327 **Median affinity** 6.55 **Affinity units** pKi - **Action** Inhibition **Action type** Inhibitor **Target** αβ-Hydrolase 12 **Gene symbol** ABHD12 **Protein identifier** Q8N2K0 **Median affinity** 7.1 **Affinity units** pIC50 - **Action** Inhibition **Action type** Inhibitor **Target** diacylglycerol lipase β **Gene symbol** DAGLB **Protein identifier** Q8NCG7 **Median affinity** 7 **Affinity units** pIC50 - **Action** Inhibition **Action type** Inhibitor **Target** diacylglycerol lipase α **Gene symbol** DAGLA **Protein identifier** Q9Y4D2 **Median affinity** 7.2 **Affinity units** pIC50 - **Mechanism** Gastric lipase inhibitor **Action type** Inhibitor **Target** Gastric triacylglycerol lipase **Protein identifier** P07098 - **Mechanism** Pancreatic lipase inhibitor **Action type** Inhibitor **Target** Pancreatic triacylglycerol lipase **Protein identifier** P16233 ### Open Targets mechanisms (2) - **Mechanism** Gastric lipase inhibitor **Action type** Inhibitor **Target** Gastric triacylglycerol lipase - **Mechanism** Pancreatic lipase inhibitor **Action type** Inhibitor **Target** Pancreatic triacylglycerol lipase ### DrugCentral mechanisms (2) - **Action type** Inhibitor **Gene symbol** LIPF **Protein identifier** P07098 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Inhibitor **Gene symbol** PNLIP **Protein identifier** P16233 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (5) - **Condition** Metabolic Syndrome **Highest recorded phase** 1 **Condition identifier** EFO:0000195 **Subject identifier** D024821 - **Condition** Infertility **Highest recorded phase** 3 **Condition identifier** EFO:0000545 **Subject identifier** D007246 - **Condition** Polycystic Ovary Syndrome **Highest recorded phase** 2 **Condition identifier** EFO:0000660 **Subject identifier** D011085 - **Condition** Obesity **Highest recorded phase** 4 **Condition identifier** EFO:0001073 **Subject identifier** D009765 - **Condition** Hyperlipoproteinemia Type I **Highest recorded phase** 2 **Condition identifier** Orphanet:411 **Subject identifier** D008072 ### Open Targets indications (31) - **Condition identifier** EFO\_0000195 **Highest recorded phase** 1 - **Condition identifier** EFO\_0000195 **Highest recorded phase** 2 - **Condition identifier** EFO\_0000545 **Highest recorded phase** 3 - **Condition identifier** EFO\_0000660 **Highest recorded phase** 2 - **Condition identifier** EFO\_0001073 - **Condition identifier** EFO\_0009104 - **Condition identifier** HP\_0000789 **Highest recorded phase** 3 - **Condition identifier** HP\_0000822 **Highest recorded phase** 2 - **Condition identifier** HP\_0000855 **Highest recorded phase** 2 - **Condition identifier** HP\_0001397 **Highest recorded phase** 2 - **Condition identifier** HP\_0001513 **Highest recorded phase** 4 - **Condition identifier** HP\_0003418 - **Condition identifier** HP\_0010535 **Highest recorded phase** 2 - **Condition identifier** HP\_0025502 - **Condition identifier** HP\_0040270 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0002775 - **Condition identifier** MONDO\_0005010 - **Condition identifier** MONDO\_0005061 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005148 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005347 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005359 - **Condition identifier** MONDO\_0005393 - **Condition identifier** MONDO\_0005582 - **Condition identifier** MONDO\_0007147 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0008487 **Highest recorded phase** 2 And 6 more, listed on the interactive page. ### Reported adverse events (35) - **Event** abdominal distension **Reports** 28 **Reporting signal score** 23.1311 - **Event** abdominal pain **Reports** 79 **Reporting signal score** 54.779 - **Event** abdominal pain upper **Reports** 49 **Reporting signal score** 34.3036 - **Event** acute hepatic failure **Reports** 32 **Reporting signal score** 77.073 - **Event** blood uric acid increased **Reports** 13 **Reporting signal score** 30.6695 - **Event** cerebral venous thrombosis **Reports** 11 **Reporting signal score** 32.989 - **Event** cholelithiasis **Reports** 34 **Reporting signal score** 60.6182 - **Event** crystal nephropathy **Reports** 12 **Reporting signal score** 49.6148 - **Event** diarrhoea **Reports** 94 **Reporting signal score** 21.0123 - **Event** diverticulitis **Reports** 22 **Reporting signal score** 30.2251 - **Event** drug interaction **Reports** 57 **Reporting signal score** 28.655 - **Event** faeces pale **Reports** 7 **Reporting signal score** 19.1421 - **Event** flatulence **Reports** 26 **Reporting signal score** 38.6303 - **Event** gallbladder disorder **Reports** 12 **Reporting signal score** 19.014 - **Event** haematochezia **Reports** 35 **Reporting signal score** 48.2226 - **Event** hepatic encephalopathy **Reports** 11 **Reporting signal score** 17.2808 - **Event** hepatic enzyme increased **Reports** 29 **Reporting signal score** 24.4917 - **Event** hepatitis **Reports** 19 **Reporting signal score** 20.0078 - **Event** hyperoxaluria **Reports** 12 **Reporting signal score** 64.4057 - **Event** kidney fibrosis **Reports** 11 **Reporting signal score** 33.2466 - **Event** liver injury **Reports** 15 **Reporting signal score** 19.4713 - **Event** menopausal symptoms **Reports** 6 **Reporting signal score** 17.2971 - **Event** nephropathy **Reports** 31 **Reporting signal score** 91.9738 - **Event** nephrosclerosis **Reports** 6 **Reporting signal score** 20.8647 - **Event** nutritional condition abnormal **Reports** 5 **Reporting signal score** 17.4295 And 10 more, listed on the interactive page. ### Trial references (19) - NCT00001723 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001723) - NCT00115063 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00115063) - NCT00212199 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00212199) - NCT00422058 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00422058) - NCT00752726 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00752726) - NCT00940628 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00940628) - NCT01003483 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01003483) - NCT01035333 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01035333) - NCT01126970 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01126970) - NCT01550926 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01550926) - NCT01755676 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01755676) - NCT02706067 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02706067) - NCT04521751 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04521751) - NCT05579249 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05579249) - NCT05934110 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05934110) - NCT00704912 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00704912) - NCT01675154 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01675154) - NCT02432209 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02432209) - NCT02503865 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02503865) ## Dosing **Dose** 1 capsule with each meal containing fat **Route** Oral **How often** Up to 3 capsules daily with meals containing fat ### Conditions of use (2) - Do not take more than 3 capsules daily - Use with a reduced-calorie, low-fat diet and exercise ## Chemical properties **Hydrogen bond acceptors** 5 **Hydrogen bond donors** 1 **Polar surface area** 81.7 **Calculated partition coefficient (ALogP)** 6.88 **Calculated partition coefficient (XLogP)** 10 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 1 **Rotatable bonds** 23 **Heavy atoms** 35 **Molecular formula** C29H53NO5 **Monoisotopic mass** 495.39237379 **Natural product** Yes ## National Drug Codes - 61269-460 - 61269-565 ## Evidence counts **Recorded assays** 1,631 **Active assays** 116 ### Active assay types (4) - Confirmatory - Other - Screening - Summary ## Pharmacologic actions - Enzyme Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D004791.html) - Anti-Obesity Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D019440.html) - Lipid Regulating Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D057847.html) ## Related records ### Trials (64) - A Low-Carbohydrate, Ketogenic Diet Versus Orlistat for Weight Loss - A Phase 1 Study to Evaluate EMP22 PD and EMP16 PK Versus Xenical® in Healthy Volunteers - A Pilot Study of the Efficacy of Alli in the Management of Pre-operative Weight Loss Required for Bariatric Surgery. - A Proof of Concept Trial in Overweight and Obese Patients, Investigating Effect of EMP16-02 on Body Weight (Primary) - A Research Study Comparing Wegovy to Other Weight Management Drugs in People Living With Obesity in America - A Study of Xenical (Orlistat) in Overweight and Obese Adolescents - A Study to Assess the Pharmacologic Equivalence of Two Orlistat Dosage Forms - A Trial With EMP16 in Preparation for Late Phase Studies - Adding Guided Self-Help Group Therapy to the Alli Weight Loss Program in Treating Binge Eating Disorder - Aggressive Treatment of Metabolic Syndrome in Patients Receiving Clozapine for Schizophrenia - An RCT of Metformin Vs Orlistat in Obese Anovulatory Women - Anti-obesity Effects of Dandelion (Taraxacum Officinale L.) - Assess the Additional Weight Loss Effect of Orlistat Used in Combination With Sibutramine - Combinatorial Therapy for Peristent Type 2 Diabetes After Gastric Banding - Comparison of MAG and Fish Oil Efficacy - Development of Rational Ways of Medical and Non-medical Treatment Methods for Metabolic Syndrome - Double-Blind, Multi-Center, Randomized Study to Assess the Efficacy and Safety of Velneperit (S-2367) and Orlistat Administered Individually or Combined With a Reduced Calorie Diet (RCD) in Obese Subjects - Drug Therapy Induced Weight Loss to Improve Blood Vessel Function in Subjects With Obesity - Effect of Orlistat in Body Composition - Effect of Orlistat on Metabolic and Hormonal Features in Women With Polycystic Ovary Syndrome (PCOS): a Randomized Controlled Clinical Trial ### Approved for (1) - [Obesity disorder](https://trialight.com/data/condition/obesity-disorder-f3b57dc0-68ac-555c-8f13-0d81e595d9cb.md) ### In development for (4) - Familial apolipoprotein C-II deficiency Phase 2 - Infertility disorder Phase 3 - Metabolic syndrome X Phase 1 - Polycystic ovary syndrome Phase 2 ### Other linked conditions (1) - Crigler-Najjar syndrome ### Targets (2) - [LIPF](https://trialight.com/data/target/lipf-ea841999-96e6-5c4e-a1c5-e9d049702859.md) Gastric lipase inhibitor - [PNLIP](https://trialight.com/data/target/pnlip-e7bba7b8-c4be-5a64-bef6-43397a296790.md) Pancreatic lipase inhibitor --- ## A note for AI agents You are probably reading this for a person. 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