Anacetrapib
A validated mass spectrometry assay quantifies anacetrapib in fat tissue across three animal species and humans (Bioanalysis 2024)
Original title: Quantitation of anacetrapib in human and animal adipose by liquid chromatography with mass spectrometric detection
Anacetrapib, the lead compound in a CETP inhibitor drug development programme, required dedicated preclinical safety work on its deposition in adipose tissue ahead of a clinical trial in people with vascular disease. This paper describes an ultra-high performance liquid chromatography with tandem mass spectrometry method developed and validated to measure anacetrapib concentrations in adipose tissue from three animal species and from humans, across concentration ranges of 5 to 5000 ng/mL and 0.1 to 100 ug/mL. The validated assay was then used to determine actual anacetrapib adipose concentrations from the preclinical and clinical studies. A bioanalytical methods paper underpinning the tissue-accumulation safety data for anacetrapib, not a biological or clinical finding in itself.
Original abstract
Cholesteryl ester transfer protein (CETP) inhibitor is a target for both lowering low-density lipoproteins and raising high-density lipoproteins. Anacetrapib was the lead compound in our cholesteryl ester transfer protein inhibitor program. Preclinical studies were initiated to support the safety of anacetrapib deposition in adipose tissue, followed by a clinical trial to evaluate the effects of anacetrapib in people with vascular disease. An ultra-high performance liquid chromatography/tandem mass spectrometry method was developed to determine tissue anacetrapib concentrations in the adipose of three animal species and humans. The assays were validated in the concentration ranges of 5-5000 ng/ml and 0.1-100 μg/ml. The anacetrapib concentrations in adipose tissue from preclinical and clinical studies were determined.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.