Our Science

Overview

Our lead investigational candidate, obicetrapib, is a novel, selective inhibitor that targets the cholesteryl ester transfer protein (CETP).

CETP transports cholesterol from good high-density lipoprotein cholesterol (HDL-C) to low-density lipoprotein cholesterol (LDL-C). Obicetrapib works by blocking this transfer.

Obicetrapib has been shown in clinical trials to date to:

  • Significantly reduce LDL cholesterol

  • Significantly reduce Apolipoprotein B (ApoB)

  • Substantially increase HDL cholesterol

  • Substantially increase Apolipoprotein A1 (ApoA1)

We believe by transforming the ratio of good versus bad cholesterol in the body, obicetrapib holds transformative treatment potential for patients.

Genetic and Clinical Results Confirmed

Numerous deep genomic analyses have shown that lowering LDL-C by inhibiting CETP is a mechanism for lowering the risk of negative cardiovascular outcomes and other pathologies. This genetic mechanism has translated to observations in recent clinical trials of tens of thousands of patients.

 

Obicetrapib has the potential to be a safe, convenient, low-dose, once-daily oral therapy that can meaningfully improve the landscape of treatment for metabolic diseases.

  • ROBUST GENETIC TARGET

    Blocking CETP exhibits a strong genetic linkage to human metabolic diseases.

    • CETP loss of function is considered a longevity gene,

    • People with CETP loss-of-function are significantly less likely to develop metabolic diseases such as coronary artery disease, diabetes, and Alzheimer’s disease.

    • Gain-of-function mutations in CETP are associated with significant increases in the risk for these diseases.

  • CLINICALLY OBSERVED MECHANISM

    Obicetrapib’s mechanism of action has also been observed clinically to decrease the risk of adverse cardiovascular outcomes and diabetes.

    • In the REVEAL trial of 30,000 hyperlipidemia patients, anacetrapib demonstrated that LDL-lowering with a CETP inhibitor reduced cardiovascular outcomes in patients by 9% after 4.1 years and 20% after 6.4 years.

    • This observed clinical benefit is consistent with expectations based on magnitude of LDL decrease.

    • Four prior CETP inhibitors have all demonstrated clinical benefit in diabetes in clinical trials with more than 90,000 patients.

    • Obicetrapib is differentiated from these prior compounds given its improved selectivity and potency for CETP as well as its safety and tolerability profile observed to date.

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