Protein / target

Cholesteryl ester transfer protein

Encoded byCETPP11597Homo sapiensSwiss-Prot

UniProt: P11597 Ensembl: ENSG00000087237 HGNC: HGNC:1869 NCBI Gene: 1071

Clinical-stage

Therapeutic maturity

Clinical candidates

Clinical trials

Small-molecule tractable

Druggability

Advanced Clinical

Protein at a glance

Biological role

Phospholipid transporter

Strongest disease association

Metabolic Syndrome

Via encoding gene CETP · Genetic evidence · score 0.94

Therapeutic position

Clinically advancing target

Small molecules

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 overview

Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride, among lipoprotein particles.

View complete UniProt function annotation

Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride, among lipoprotein particles. Allows the net movement of cholesteryl ester from high density lipoproteins/HDL to triglyceride-rich very low density lipoproteins/VLDL, and the equimolar transport of triglyceride from VLDL to HDL (PubMed:24293641, PubMed:3281933, PubMed:3600759). Regulates the reverse cholesterol transport, by which excess cholesterol is removed from peripheral tissues and returned to the liver for elimination (PubMed:17237796)

Subcellular location

Secreted

Domains and Gene Ontology detail (29)

Gene Ontology

Cextracellular exosome
Cextracellular region
Cextracellular space
Chigh-density lipoprotein particle
Cvesicle
Fcholesterol binding
Fcholesterol transfer activity
Flipid binding
Fphosphatidylcholine binding
Fphospholipid transporter activity
Ftriglyceride binding
Pcholesterol homeostasis

493 aa · 55 kDa · 2 isoforms

Biological roles

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

Lipid & lipoprotein metabolismUniProt · GO

View supporting evidence

Lipid & lipoprotein metabolism

·Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride…
·high-density lipoprotein particle
·cholesterol binding
·cholesterol transfer activity

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

Drugs targeting this protein

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

Dalcetrapib

Narrow target profilePhase 3Inhibitor

Cholesteryl ester transfer protein inhibitor

Direct interaction with this protein · Only this protein recorded as a target

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

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene CETP

Gene-level evidence surfaced through the gene CETP that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Metabolic Syndrome

0.96Well supported

Genetic evidence dominant · Open Targets 0.65

Macular Degeneration

0.94Well supported

Genetic evidence dominant · Open Targets 0.57

Coronary Artery Disease

0.87Well supported

Genetic evidence dominant · Open Targets 0.66

Metabolic Diseases

0.87Well supported

Genetic evidence dominant · Open Targets 0.53

Hyperlipidemias

0.84Well supported

Genetic evidence dominant · Open Targets 0.52

View evidence synthesis (5)

Metabolic SyndromeWell supported

0.96

agreement 0.86–1.00

Genetic68%Clinical23%Literature9%

Open Targets aggregate 0.65 · 3 independent evidence families

Macular DegenerationWell supported

0.94

agreement 0.80–1.00

Genetic89%Literature11%

Open Targets aggregate 0.57 · 2 independent evidence families

Coronary Artery DiseaseWell supported

0.87

agreement 0.77–0.98

Genetic56%Clinical34%Literature11%

Open Targets aggregate 0.66 · 3 independent evidence families

Metabolic DiseasesWell supported

0.87

agreement 0.73–1.00

Genetic98%Literature2%

Open Targets aggregate 0.53 · 2 independent evidence families

HyperlipidemiasWell supported

0.84

agreement 0.74–0.95

Genetic81%Literature10%Clinical9%

Open Targets aggregate 0.52 · 3 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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 per-type scores above show the calculation.

Show all associations

Coronary Artery Disease0.66

Metabolic Syndrome0.65

Macular Degeneration0.57

Metabolic Diseases0.53

Hyperlipidemias0.52

Drug development

6 compounds recorded · 6 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph: these count different sets and are not a subset relation.

View all recorded compounds (6)

ROCACETRAPIBPhase 2

OBICETRAPIBPhase 3

EVACETRAPIBPhase 3

DALCETRAPIBPhase 3

ANACETRAPIBPhase 3

TORCETRAPIBPhase 3

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small molecules — Strong

Advanced Clinical and Structure with Ligand support this modality.

Antibodies — Emerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degraders — Emerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (9)

SM · Advanced ClinicalSM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

cardiovascular disease eventsClinPGx

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

Phase III, Double-blind, Randomized Placebo-controlled Study to Evaluate the Effects of Dalcetrapib on Cardiovascular (CV) Risk in a Genetically Defined Population With a Recent Acute Coronary Syndrome (ACS)PHASE3

RECRUITING · via Dalcetrapib · NCT05918861

A Phase III, Double-blind, Randomized Placebo-controlled Study to Evaluate the Effects of Dalcetrapib on Cardiovascular (CV) Risk in a Genetically Defined Population With a Recent Acute Coronary Syndrome (ACS): The Dal-GenE TrialPHASE3

COMPLETED · via Dalcetrapib · NCT02525939

A Phase 3b, Multi-Center, Double-Blind, Placebo-Controlled, Parallel Group, Study to Evaluate the Effect of Dalcetrapib 600 mg on Cardiovascular (CV) Events in Adult Patients With Stable Coronary Heart Disease (CHD), CHD Risk Equivalents or at Elevated Risk for Cardiovascular Disease (CVD).PHASE3

COMPLETED · via Dalcetrapib · NCT01516541

A Phase III, Double-blind, Randomized, Placebo-controlled, Multi-center Study Evaluating the Efficacy and Safety of Dalcetrapib on Lipids, Lipoproteins, Apolipoproteins and Markers of Cardiovascular (CV) Risk in Patients Hospitalized for an Acute Coronary Syndrome (ACS) When Treatment is Initiated Within 1 Week After an ACS (Dal-ACUTE)PHASE3

COMPLETED · via Dalcetrapib · NCT01323153

View all trials (10)

A Multi-Center, Double-blind, Randomized, Placebo Controlled, Parallel Group Study of the Effect of Dalcetrapib on Atherosclerotic Disease Progression As Measured by Coronary Intravascular Ultrasound, Carotid B-Mode Ultrasound and Coronary AngiographyPHASE3

TERMINATED · via Dalcetrapib · NCT01059682

A Randomized, Double-blind, Placebo-controlled Study Assessing the Effect of RO4607381 on Cardiovascular Mortality and Morbidity in Clinically Stable Patients With a Recent Acute Coronary SyndromePHASE3