Protein / target

Gastric triacylglycerol lipase

LIPFP07098Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
2
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Triacylglycerol lipase activity

Primary system

Endocrine & metabolic

Strongest disease association

temporomandibular joint disorder

Genetic evidence · score 0.47

Therapeutic maturity

Clinically validated target

2 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

2 approved

30 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Catalyzes the hydrolysis of triacylglycerols to yield free fatty acids, diacylglycerol, monoacylglycerol, and glycerol (PubMed:10358049, PubMed:2243091). Shows a preferential hydrolysis at the sn-3 position of triacylglycerol (PubMed:2243091)

Subcellular location

Secreted
Domains and Gene Ontology detail (9)

Domains & features

AB hydrolase-1

Gene Ontology

  • Cextracellular region
  • Cmitochondrion
  • Flipid binding
  • Fmalate dehydrogenase activity
  • Ftriacylglycerol lipase activity
  • Plipid catabolic process
  • Plipid metabolic process
  • Ptriglyceride metabolic process

398 aa · 45 kDa · 4 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Metabolic enzyme activityGO
View supporting evidence

Metabolic enzyme activity

  • ·malate dehydrogenase activity
  • ·lipid metabolic process
  • ·triglyceride metabolic process
View underlying pathways (1)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

PNLIPPNLIPR…LIPCLPLCELLIPGCLPSPNLIPR…MGLLPNPLA2LIPF

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

1

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

orlistat
Narrow target profileApprovedInhibitor

Gastric lipase inhibitor

Appears in clinical studies involving obesity disorder, Obesity, Infertility, Sleep apnea

Direct interaction with this protein · 1 of 2 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

temporomandibular joint disorder0.47

Genetic · overall 0.28

Proptosis0.41

Genetic · overall 0.25

type 2 diabetes mellitus0.06

Genetic · overall 0.42

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

obesity disorder0.93

Clinical · overall 0.57

Obesity0.89

Clinical · overall 0.54

inherited lipid metabolism disorder0.61

Clinical · overall 0.37

Infertility0.43

Clinical · overall 0.26

hyperlipidemia0.12

Clinical · overall 0.07

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

hypertriglyceridemia0.07

Clinical

polycystic ovary syndrome0.07

Clinical

Show all associations
obesity disorder0.57
Obesity0.54
type 2 diabetes mellitus0.42
inherited lipid metabolism disorder0.37
temporomandibular joint disorder0.28
Infertility0.26
Proptosis0.25
hyperlipidemia0.07
hypertriglyceridemia0.07
polycystic ovary syndrome0.07

Open Targets ranks 118 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 2 total

ORLISTATApproval

obesity disorder · Obesity · Infertility

CETILISTATApproval

Obesity · type 2 diabetes mellitus · inherited lipid metabolism disorder

Tractability

SM · Approved DrugSM · High-Quality PocketSM · Druggable FamilyAB · UniProt loc med confAB · UniProt SigP or TMHMMAB · GO CC med conf

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

Show remaining trials (24)

COMPLETED · via orlistat · NCT02767531

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

obesity disorderModerately supported
0.70
agreement 0.550.86
Clinical98%Literature2%

Open Targets aggregate 0.57 · 2 independent evidence families

ObesityModerately supported
0.67
agreement 0.520.83
Clinical98%Literature2%

Open Targets aggregate 0.54 · 2 independent evidence families

type 2 diabetes mellitusModerately supported
0.53
agreement 0.430.64
Clinical88%Genetic11%Literature1%

Open Targets aggregate 0.42 · 3 independent evidence families

temporomandibular joint disorderLimited support
0.47
agreement 0.350.59
Genetic100%

Open Targets aggregate 0.28 · 1 independent evidence family

inherited lipid metabolism disorderLimited support
0.46
agreement 0.290.62
Clinical100%

Open Targets aggregate 0.37 · 1 independent evidence family

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

8

Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.

  1. New publication2024-03-19
    Exploring the association between suicidal thoughts, self-injury, and GLP-1 receptor agonists in weight loss treatments: Insights from pharmacovigilance measures and unmasking analysis.

    European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2024 · 44 citations · Europe PMC · via orlistat

  2. Safety communication2014-12-11

    Drug Safety Update: Orlistat: theoretical interaction with antiretroviral HIV medicines

    mhra · safety · mhra · via orlistat

  3. New publication2010-01-01
    A randomized trial of a low-carbohydrate diet vs orlistat plus a low-fat diet for weight loss.

    Archives of internal medicine · 2010 · 103 citations · Europe PMC · via orlistat

  4. Regulatory approval2007-07-22

    Approval: Alli (previously Orlistat GSK) (EMA)

    ema · regulatory · ema · via orlistat

  5. New publication2004-03-01
    Efficacy of orlistat as an adjunct to behavioral treatment in overweight African American and Caucasian adolescents with obesity-related co-morbid conditions.

    Journal of pediatric endocrinology & metabolism : JPEM · 2004 · 65 citations · Europe PMC · via orlistat

  6. New publication2002-07-01
    Three-month tolerability of orlistat in adolescents with obesity-related comorbid conditions.

    Obesity research · 2002 · 104 citations · Europe PMC · via orlistat

  7. New publication2002-07-01
    Effects of orlistat on fat-soluble vitamins in obese adolescents.

    Pharmacotherapy · 2002 · 101 citations · Europe PMC · via orlistat

  8. Regulatory approval1998-07-29

    Approval: Xenical (EMA)

    ema · regulatory · ema · via orlistat

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.