Obicetrapib

Summary

Obicetrapib (CHEMBL3785197) is a phase-3 clinical-stage small molecule targeting CETP; indicated across 5 conditions including atherosclerosis and alzheimer disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (CETP)
• Indications: 5 conditions
• Clinical trials: 28
• Chemistry: 722.6 Da · C32H31F9N4O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3785197
Name	Obicetrapib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11498596
Molecular formula	C32H31F9N4O5
Molecular weight	722.6
InChIKey	NRWORBQAOQVYBJ-GJZUVCINSA-N

SMILES: CC[C@@H]1C[C@@H](C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C4=NC=C(C=N4)OCCCC(=O)O

IUPAC name: 4-[2-[[3,5-bis(trifluoromethyl)phenyl]methyl-[(2R,4S)-1-ethoxycarbonyl-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinolin-4-yl]amino]pyrimidin-5-yl]oxybutanoic acid

Also known as: AMG-899, CASA, DEZ-001, Obicetrapib, Ta-8995, TA-8995, OBICETRAPIB

Parent form; salt/anhydrous children: CHEMBL6068417

Patent coverage: 96 distinct patent families (252 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CETP	cholesteryl ester transfer protein	Inhibition		0.2%	P11597

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): CETP.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
LDL remodeling	1	CETP
HDL remodeling	1	CETP
NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux	1	CETP

Dominant GO biological processes

GO term	Targets
triglyceride metabolic process	1
lipid transport	1
cholesterol metabolic process	1
negative regulation of macrophage derived foam cell differentiation	1
regulation of cholesterol efflux	1
cholesterol transport	1
positive regulation of cholesterol transport	1
triglyceride transport	1
very-low-density lipoprotein particle remodeling	1
low-density lipoprotein particle remodeling	1
high-density lipoprotein particle remodeling	1
cholesterol homeostasis	1
reverse cholesterol transport	1
phosphatidylcholine metabolic process	1
lipid homeostasis	1

Indications & clinical

Indications

5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
atherosclerosis	3	MONDO:0005311	EFO:0003914
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
liver disorder	1	MONDO:0005154	EFO:0001421

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 28.

Phase distribution

Phase	Trials
PHASE1	11
PHASE2	7
PHASE3	6
Not specified	3
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05202509	PHASE3	ACTIVE_NOT_RECRUITING	Cardiovascular Outcome Study to Evaluate the Effect of Obicetrapib in Patients With Cardiovascular Disease
NCT07219602	PHASE3	RECRUITING	A Study to Evaluate the Effect of Obicetrapib/Ezetimibe 10 mg Fixed-Dose Combination or Obicetrapib 10 mg Daily on Top of Guideline-Recommended Lipid-Lowering Therapy in Participants With Type 2 Diabetes and/or Metabolic Syndrome
NCT07614958	PHASE3	RECRUITING	Phase 3 Clinical Study Evaluating Efficacy, Safety, and Tolerability of Obicetrapib Vs Bempedoic Acid to Treat Dyslipidemia in Adults With Primary Non-familial Hypercholesterolemia or Mixed Dyslipidemia at High to Very High Cardiovascular Risk, During a Treatment Period of Approximately 84 Days
NCT05142722	PHASE3	COMPLETED	Randomized Study to Evaluate the Effect of Obicetrapib on Top of Maximum Tolerated Lipid-Modifying Therapies
NCT05425745	PHASE3	COMPLETED	Evaluate the Effect of Obicetrapib in Patients With HeFH on Top of Maximum Tolerated Lipid-Modifying Therapies.
NCT06005597	PHASE3	COMPLETED	Study of Obicetrapib & Ezetimibe Fixed Dose Combination on Top of Maximum Tolerated Lipid-Modifying Therapies
NCT06982508	PHASE2	RECRUITING	Evaluation of Obicetrapib on Antioxidant Levels in Plasma and HDL Particles of Healthy Volunteers
NCT01970215	PHASE2	COMPLETED	TA-8995: Its Use in Patients With Mild Dyslipidaemia (TULIP)
NCT02241772	PHASE1/PHASE2	COMPLETED	A Study on the Effects of TA-8995 on Lp(a) in Subjects With Elevated Lp(a)
NCT04753606	PHASE2	COMPLETED	Randomized Study of Obicetrapib as an Adjunct to Statin Therapy
NCT04770389	PHASE2	COMPLETED	Randomized Study of Obicetrapib in Combination With Ezetimibe
NCT05161715	PHASE2	COMPLETED	Proof-of-concept, Open-label Study in Patients With Early Alzheimer’s Disease
NCT05266586	PHASE2	COMPLETED	Study to Evaluate the Effect of Obicetrapib in Combination With Ezetimibe as an Adjunct to HIS Therapy
NCT05421078	PHASE2	COMPLETED	A Dose-Finding Study in Japanese Patients to Evaluate the Effect of Obicetrapib as an Adjunct to Stable Statin Therapy.
NCT05972278	PHASE1	ACTIVE_NOT_RECRUITING	Investigating the Effect of Obicetrapib on Lipoprotein Metabolism
NCT01878474	PHASE1	COMPLETED	Evaluation of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of TA-8995 With Single, Escalating Doses in Healthy Subjects
NCT01879020	PHASE1	COMPLETED	Evaluation of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of TA-8995 After Multiple Doses in Healthy Subjects
NCT02124954	PHASE1	COMPLETED	A Preliminary Drug Drug Interaction Study With TA-8995
NCT02241759	PHASE1	COMPLETED	Study of the Electrocardiographic Effects of TA-8995
NCT02408055	PHASE1	COMPLETED	ADME Study in Healthy Male Subjects With TA-8995
NCT02523391	PHASE1	COMPLETED	Bioequivalence Study of Capsule and Tablet Formulations of TA-8995
NCT06048302	PHASE1	COMPLETED	PK and Safety in Participants Taking Obicetrapib With Moderate Hepatic Impairment Relative to Normal Hepatic Function
NCT06081166	PHASE1	COMPLETED	A Drug-drug Interaction Study Evaluating the PK Effects of Obicetrapib on Atorvastatin and Rosuvastatin
NCT06250205	PHASE1	COMPLETED	Evaluate the Pharmacokinetics of a Combined Oral Contraceptive (COC) With and Without Obicetrapib
NCT06547359	PHASE1	COMPLETED	A Study to Evaluate Drug-Drug Interactions of Obicetrapib Tablets and Ezetimibe Tablets in Healthy Adult Subjects
NCT01739686	Not specified	COMPLETED	Collaborative Care to Alleviate Symptoms and Adjust to Illness in Chronic Heart Failure (CASA) Trial
NCT02136680	Not specified	COMPLETED	CASA: Care and Support Access in HIV Disease
NCT02702570	Not specified	COMPLETED	Committed Actions for Successful Aging

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

5 molecules share ≥1 primary target. Top 5 by shared-target count:

Molecule	Source	Status	Shared targets
ANACETRAPIB	ChEMBL	Phase 3	CETP
DALCETRAPIB	ChEMBL	Phase 3	CETP
EVACETRAPIB	ChEMBL	Phase 3	CETP
TORCETRAPIB	ChEMBL	Phase 3	CETP
URSOLIC ACID	ChEMBL	Phase 2	CETP