Summary
Orlistat has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Obesity would be drug repurposing rather than first-in-human development. This does not mean it is approved for Obesity. ClinicalTrials.gov lists 8 registered trials linking Orlistat to Obesity: 1 is active or not yet recruiting; 6 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 4 (NCT05496075). The largest enrolment is 200 participants (NCT00001723). Registration activity spans 1998 to 2026. The literature layer holds 12 publications for this pair: 5 Cochrane reviews, 2 meta-analyses and 5 clinical trial publications. Publication years run from 2024 to 2026. Because at least one synthesis-level source exists (systematic review, meta-analysis or Cochrane review), this pair has been assessed beyond single studies, although the synthesis may concern a different indication.
The RepurpOS disease-intelligence file for Obesity ranks 368 candidate therapeutics from Open Targets, ChEMBL, DGIdb and PubMed; only a minority carry direct clinical evidence, and this page covers one of those. Spontaneous remission context recorded for the condition: Sustained weight loss of >5% without intervention: ~5-10% at 2 years; weight regain almost universal after behavioural intervention alone (95% return to within 5% of starting weight at 5 years on lifestyle alone).
Evidence table
| Evidence tier | A · Strong |
|---|---|
| Evidence score | 74.0 (trials 24.0, literature 30.0, tier 15, approved bonus 5.0) |
| Registered trials | 8 total: 0 recruiting, 1 active / not yet recruiting, 6 completed, 1 other |
| Linked publications | 12 (5 Cochrane reviews, 5 clinical trial publications, 2 meta-analyses) |
| Agent type | Drug (Small molecule) |
| Development stage (any indication) | Approved |
| Mechanism / class | Not recorded |
| Data sources | DGIdb |
| Linked via biomarker / target | CNR1 |
How the evidence score is calculated
- Each registered trial scores by status (recruiting / active / enrolling 3, completed 2.5, not yet recruiting 2, unknown 1, terminated / withdrawn / suspended 0.5) plus a phase bonus (phase 3-4 +2, phase 2 +1, phase 1 +0.5). The trial component is capped at 30.
- Each literature item scores by design (Cochrane review 5, meta-analysis 4, systematic review 3, RCT 3, clinical trial publication 2, curated reference 1.5, other PubMed record 1). The literature component is capped at 30.
- The existing evidence tier adds 15 (A / Strong), 10 (B / Moderate), 5 (C / Preliminary) or 0 (D / Anecdotal).
- Agents approved for any indication (max clinical phase 4) add 5, because an approved agent has an established safety profile that lowers the barrier to repurposing trials.
- The score ranks what has been studied, not what works. It does not read effect sizes or directions of effect.
Registered clinical trials
| NCT ID | Title | Status | Phase | Enrolment |
|---|---|---|---|---|
| NCT00152360 | The Effect of Xenical on Weight and Risk Factors 2005 | completed | Phase 4 | 25 |
| NCT05496075 | Orlistat Reduces Uric Acid in Overweight/Obese Patients With Hyperuricemia 2022 | completed | Phase 4 | 72 |
| NCT00001723 | Safety and Efficacy of Xenical in Children and Adolescents With Obesity-Related Diseases 1998 | completed | Phase 2 | 200 |
| NCT02069197 | Ketogenic Diet Treatment of Obesity With Co-morbid Type 2 Diabetes Mellitus and/or Obstructive Sleep Apnea 2014 | status unknown | Phase 2 | 150 |
| NCT00829283 | Treatment of Obesity and Binge Eating: Behavioral Weight Loss Versus Stepped Care 2008 | completed | Not applicable | 191 |
| NCT01170806 | Study of Fat Malabsorption by Lipiblock Versus Xenical 2009 | completed | Not applicable | 20 |
| NCT00991926 | Growth Factor/Insulin-like Growth Factor (GH/IGF)-1 Axis in Obese Subjects in Treatment With Orlistat 2006 | completed | Not applicable | 20 |
| NCT07437001 | Effect of Electroacupuncture on Central Obesity and Fatty Liver in Postmenopausal Women 2026 | not yet recruiting | Not applicable | 60 |
Published literature
- Cochrane review Pharmacological interventions for the treatment of obesity in children and adolescentsGerardi C, Allocati E, Prutsky G et al. · The Cochrane database of systematic reviews · 2026 · PMID 42125960
- Cochrane review The Effects of Exercise Combined with Pharmacotherapy on Body Composition and Metabolic Parameters in Overweight/Obese Adults: A Meta-Analysis and Network Pharmacology StudyPeng T, Liang W, Wei J et al. · Diabetes, metabolic syndrome and obesity : targets and therapy · 2026 · PMID 42094035
- Cochrane review Comparison of pharmacotherapies for obesity with sleeve gastrectomy: a network meta-analysis and systematic reviewOmeh Z, Khan T, Uthman O et al. · Expert review of endocrinology & metabolism · 2026 · PMID 41968780
- Cochrane review Effect of bariatric surgery and pharmacological treatments on cardiovascular risk factors for adults with overweight and obesity: a systematic review and network meta-analysisYang Y, Cheng X, Chen S et al. · International journal of surgery (London, England) · 2026 · PMID 41738616
- Cochrane review Long-Term Effects of Orlistat on Lipid Metabolism and Anthropometric Indices: A Meta-Analysis of Clinical TrialsKhodadadiyan A, Khazraei Y, Kamali M et al. · Journal of obesity · 2026 · PMID 41737647
- Meta-analysis Weight-Lowering Drugs and Natural Female Fertility-A Systematic Review and Meta-AnalysisAlnaimi SJ, Alsugeir DM, Wei L et al. · Clinical obesity · 2026 · PMID 42307450
- Meta-analysis Weight Loss Medications for Adult Patients With Obesity and Binge Eating-A Systematic Review and Meta-analysisViolante-Cumpa JR, Rios-Ortega AG, Sánchez-García A et al. · Endocrine practice : official journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists · 2026 · PMID 41513086
- Clinical trial publication Diet strategies for maintaining substantial therapeutic weight loss: 78-week mixed methods randomised trialBrosnahan N, Hankey C, Leeds A et al. · Clinical nutrition (Edinburgh, Scotland) · 2025 · PMID 40934815
- Clinical trial publication The Supportive Effect of Acarbose to Orlistat in Weight Management-A Randomized, Double-Blind, Multiarm Phase 2 TrialHolmbäck U, Grudén S, Kuusk S et al. · Obesity (Silver Spring, Md.) · 2025 · PMID 40769876
- Clinical trial publication A Comparative Analysis of the Pharmacodynamic and Pharmacokinetic Properties of 2 Controlled-Release Formulations Versus a Marketed Orlistat ProductGrudén S, Forslund A, Litorp H et al. · Clinical pharmacology in drug development · 2025 · PMID 39783852
- Clinical trial publication Effect of Silibinin on Human Pancreatic Lipase Inhibition and Gut Microbiota in Healthy Volunteers: A Randomized Controlled TrialPonce Martínez C, Murcia García E, Pérez Sánchez H et al. · International journal of molecular sciences · 2024 · PMID 39684564
- Clinical trial publication Efficacy and safety of orlistat in male patients with overweight/obesity and hyperuricemia: results of a randomized, double-blind, placebo-controlled trialLiu S, Lin X, Tao M et al. · Lipids in health and disease · 2024 · PMID 38468241
Mechanism and notes
No mechanism of action is recorded for this pair in the source databases.
OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in DGIdb, in this case via the biomarker or target CNR1. The tier describes how well the drug-disease link is documented, not how well the drug works.
Frequently asked questions
Is Orlistat approved for Obesity?
Orlistat has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Obesity would be drug repurposing rather than first-in-human development. This does not mean it is approved for Obesity. Approval status for the specific indication should always be confirmed with the relevant regulator and prescribing information.
Is Orlistat in clinical trials for Obesity?
ClinicalTrials.gov lists 8 registered trials linking Orlistat to Obesity: 1 is active or not yet recruiting; 6 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 4 (NCT05496075). The largest enrolment is 200 participants (NCT00001723). Registration activity spans 1998 to 2026.
What does the evidence show for Orlistat in Obesity?
Orlistat has both completed registered trials and synthesis-level publications linked to Obesity. That is the strongest profile in this database, but the summaries here do not extract effect sizes, so read the linked reviews for direction and magnitude of benefit. OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in DGIdb, in this case via the biomarker or target CNR1. The tier describes how well the drug-disease link is documented, not how well the drug works.
Cite this page
Data: ClinicalTrials.gov, PubMed, Open Targets, ChEMBL, DGIdb and the OSMF therapeutic agent database. Last updated 2026-07-05. Page built 2026-10-07.