> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/obicetrapib-41ee1f14-bdc7-46e1-adcb-5f53d79c7b97
> Record changed: 2026-10-13

# Obicetrapib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

**Drug name**

Obicetrapib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

**Molecular weight**

722.61

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

**Structure (SMILES)**

CCOC(=O)N1c2ccc(C(F)(F)F)cc2\[C@@H\](N(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ncc(OCCCC(=O)O)cn2)C\[C@H\]1CC

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

### Other names (20)

- amg 899
- AMG-899
- casa
- CASA
- dez 001
- DEZ-001
- obicetrapib
- Obicetrapib
- obicetrapib \[INN\]
- OBICETRAPIB \[USAN\]
- Obicetrapib \[WHO-DD\]
- Obicetrapib 10 mg
- Obicetrapib 10mg
- Obicetrapib 5mg
- obicetrapib inn
- obicetrapib usan
- obicetrapib who dd
- ta 8995
- Ta-8995
- TA-8995

## Identifiers

**ATC classification codes**

- C10A

**CAS registry numbers**

- 866399-87-3

**ChEMBL ID**

CHEMBL3785197

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

**InChIKey**

NRWORBQAOQVYBJ-GJZUVCINSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3785197)

**PubChem compound IDs**

- 11498596

**FDA ingredient codes (UNII)**

- 8O74K609HN

## Regulatory information

### European Union

**Status**

opinion

**Status date**

23 Jul 2026

**Approved indications**

Treatment of primary hypercholesterolaemia or mixed dyslipidaemia.

**Product number**

EMEA/H/C/006516

**Authorisation holder**

A. Menarini International Licensing S.A.

**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

- Dyslipidemias
- Hypercholesterolemia

European medicines record

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/ubeslo)

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

obicetrapib

**Type**

Synthetic organic

**Drug name stem**

\-cetrapib

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
cholesteryl ester transfer protein

**Gene symbol**  
CETP

**Protein identifier**  
P11597
- **Mechanism**  
Cholesteryl ester transfer protein inhibitor

**Action type**  
Inhibitor

**Target**  
Cholesteryl ester transfer protein

**Protein identifier**  
P11597

### Open Targets mechanisms

- **Mechanism**  
Cholesteryl ester transfer protein inhibitor

**Action type**  
Inhibitor

**Target**  
Cholesteryl ester transfer protein

### Investigated indications (5)

- **Condition**  
Liver Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0001421

**Subject identifier**  
D008107
- **Condition**  
Atherosclerosis

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003914

**Subject identifier**  
D050197
- **Condition**  
Dyslipidemias

**Highest recorded phase**  
1

**Condition identifier**  
HP:0003119

**Subject identifier**  
D050171
- **Condition**  
Alzheimer Disease

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0004975

**Subject identifier**  
D000544
- **Condition**  
Lipid Metabolism Disorders

**Highest recorded phase**  
2

**Condition identifier**  
Orphanet:309005

**Subject identifier**  
D052439

### Open Targets indications (15)

- **Condition identifier**  
EFO\_0000195

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000319

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0001421

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0003914

**Highest recorded phase**  
3
- **Condition identifier**  
GO\_0006629

**Highest recorded phase**  
1
- **Condition identifier**  
HP\_0003119
- **Condition identifier**  
HP\_0003124

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001336

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002525

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004975

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004995

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005148

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005311

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005439

**Highest recorded phase**  
3
- **Condition identifier**  
Orphanet\_309005

**Highest recorded phase**  
2

### Trial references (9)

- NCT01878474  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01878474)
- NCT01879020  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01879020)
- NCT01970215  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01970215)
- NCT02241759  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02241759)
- NCT02408055  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02408055)
- NCT02523391  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02523391)
- NCT05161715  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05161715)
- NCT05202509  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05202509)
- NCT06048302  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06048302)

## Chemical properties

**Hydrogen bond acceptors**

7

**Hydrogen bond donors**

1

**Polar surface area**

105.09

**Calculated partition coefficient (ALogP)**

8.67

**Calculated partition coefficient (XLogP)**

7.4

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

2

**Rotatable bonds**

11

**Heavy atoms**

50

**Molecular formula**

C32H31F9N4O5

**Monoisotopic mass**

722.21507356

**Natural product**

No

## Evidence counts

**Recorded assays**

3

**Active assays**

0

## Related records

### Trials (26)

- A CCTA Imaging Trial to Evaluate the Effect of Obicetrapib/Ezetimibe on Coronary Plaque
- A Dose-Finding Study in Japanese Patients to Evaluate the Effect of Obicetrapib as an Adjunct to Stable Statin Therapy.
- A Drug-drug Interaction Study Evaluating the PK Effects of Obicetrapib on Atorvastatin and Rosuvastatin
- A Preliminary Drug Drug Interaction Study With TA-8995
- A Study on the Effects of TA-8995 on Lp(a) in Subjects With Elevated Lp(a)
- A Study to Evaluate Drug-Drug Interactions of Obicetrapib Tablets and Ezetimibe Tablets in Healthy Adult Subjects
- 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
- ADME Study in Healthy Male Subjects With TA-8995
- Bioequivalence Study of Capsule and Tablet Formulations of TA-8995
- [Cardiovascular Outcome Study to Evaluate the Effect of Obicetrapib in Patients With Cardiovascular Disease](https://trialight.com/data/trial/cardiovascular-outcome-study-to-evaluate-the-effect-of-a24be9af-323b-4b20-8e8f-bba1227c741b.md)
- Evaluate the Effect of Obicetrapib in Patients With HeFH on Top of Maximum Tolerated Lipid-Modifying Therapies.
- Evaluate the Pharmacokinetics of a Combined Oral Contraceptive (COC) With and Without Obicetrapib
- Evaluation of Obicetrapib on Antioxidant Levels in Plasma and HDL Particles of Healthy Volunteers
- Evaluation of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of TA-8995 After Multiple Doses in Healthy Subjects
- Evaluation of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of TA-8995 With Single, Escalating Doses in Healthy Subjects
- Impact of Obicetrapib and Obicetrapib Plus Repatha on Lp(a) Levels
- Investigating the Effect of Obicetrapib on Lipoprotein Metabolism
- 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
- PK and Safety in Participants Taking Obicetrapib With Moderate Hepatic Impairment Relative to Normal Hepatic Function
- Proof-of-concept, Open-label Study in Patients With Early Alzheimer's Disease

### In development for (6)

- [Alzheimer disease](https://trialight.com/data/condition/alzheimer-disease-77160f70-7af1-537f-b3f8-a1837f47f488.md) Phase 2
- [Atherosclerosis](https://trialight.com/data/condition/atherosclerosis-5dab64e9-1fd4-5dd2-90c2-ce84935652d1.md) Phase 3
- [Cardiovascular disorder](https://trialight.com/data/condition/cardiovascular-disorder-362e433e-88a4-575f-90af-50fe7239dec0.md) Phase 2
- Familial hyperlipidemia Phase 2
- Inherited lipid metabolism disorder Phase 2
- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1

### Targets (1)

- [CETP](https://trialight.com/data/target/cetp-ee67b070-5298-5ba4-a1fa-ad945dfd4897.md) Cholesteryl ester transfer protein inhibitor

---

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