← The Peter Attia Drive

#255 ‒ Latest therapeutics in CVD, APOE's role in Alzheimer's disease and CVD, familial hypercholesterolemia, and more | John Kastelein, M.D., Ph.D.

May 22, 2023 2h 4m 22 insights
<p><a href="https://peterattiamd.com/johnkastelein/?utm_source=podcast-feed&amp;utm_medium=referral&amp;utm_campaign=230522-pod-johnkastelein&amp;utm_content=230522-pod-johnkastelein-podfeed"> View the Show Notes Page for This Episode</a></p> <p><a href="https://peterattiamd.com/subscribe/?utm_source=podcast-feed&amp;utm_medium=referral&amp;utm_campaign=230522-pod-johnkastelein&amp;utm_content=230522-pod-johnkastelein-podfeed"> Become a Member to Receive Exclusive Content</a></p> <p><a href="https://peterattiamd.com/newsletter/?utm_source=podcast-feed&amp;utm_medium=referral&amp;utm_campaign=230522-pod-johnkastelein&amp;utm_content=230522-pod-johnkastelein-podfeed"> Sign Up to Receive Peter's Weekly Newsletter</a></p> <p>John Kastelein is a renowned expert in lipoprotein metabolism and atherosclerotic cardiovascular disease (ASCVD) research. In this discussion, John delves deep into familial hypercholesterolemia (FH), a genetic disorder characterized by high levels of LDL cholesterol in the blood that increases the risk of developing heart disease. He covers its definition, genetic underpinnings, and clinical identification. He then explores the therapeutic options available for the prevention and treatment of cardiovascular disease, including the captivating history of CETP inhibitors. He explains the past shortcomings of previous CETP inhibitors before underscoring the compelling potential of the latest iterations, not only for cardiovascular disease but also for conditions like Alzheimer's disease and type 2 diabetes. Moreover, he unveils the intricate role of APOE, shedding light on why the APOE4 isoform codes for a protein that significantly increases the risk of Alzheimer's disease and cardiovascular disease. Concluding the discussion, John shares a profound sense of optimism, envisioning the possibility of targeted therapeutic interventions for high-risk patients in the near future.</p> <p><strong>We discuss:</strong></p> <ul type="disc"> <li>Familial hypercholesterolemia (FH): a genetic condition [4:30];</li> <li>Differentiating between phenotype and genotype when it comes to FH [9:45];</li> <li>The pathophysiology related to mutations of FH [15:30];</li> <li>Clinical presentations, physical manifestations, and diagnosis of FH [22:00];</li> <li>Why a small fraction of people with FH do not develop premature ASCVD [34:15];</li> <li>Treatment and prevention for those with FH [39:45];</li> <li>Addressing the assertion by some that elevated LDL is not casual in cardiovascular disease [52:45];</li> <li>The history of CETP inhibitors, and the role of the CETP protein [55:45];</li> <li>The thrifty gene hypothesis and why genes underlying FH may have been preserved [1:09:00];</li> <li>The compelling potential of the latest CETP inhibitor (obicetrapib) [1:13:00];</li> <li>Promising results from phase 3 trials exploring obicetrapib [1:27:45];</li> <li>Why the APOE4 allele increases the risk of Alzheimer's disease, and the connection to blood lipids [1:41:30];</li> <li>The role of APOE in cardiovascular disease [1:51:45];</li> <li>Takeaways and looking ahead [1:57:00]; and</li> <li>More.</li> </ul> <p>Connect With Peter on <a href="https://twitter.com/PeterAttiaMD">Twitter</a>, <a href="https://www.instagram.com/peterattiamd/">Instagram</a>, <a href="https://www.facebook.com/peterattiamd/">Facebook</a> and <a href="https://www.youtube.com/channel/UC8kGsMa0LygSX9nkBcBH1Sg">YouTube</a></p>
Actionable Insights

1. Initiate Early FH Treatment in Children

If a child is diagnosed with definite Familial Hypercholesterolemia (FH) based on rigorous criteria, initiate treatment as early as 6-8 years of age to significantly improve long-term outcomes and prevent premature cardiovascular disease.

2. Aggressively Treat Adult FH

For adults with FH, especially those transitioning from pediatric care, aggressively treat with high-intensity statins, ezetimibe, PCSK9 inhibitors, and potentially inclisiran, striving for the lowest possible LDL cholesterol levels to minimize cardiovascular risk.

3. Utilize Dutch Lipid Clinic Criteria for FH

To ensure the most accurate diagnosis of Familial Hypercholesterolemia, utilize the Dutch Lipid Clinic Network (DLCN) criteria, which have been externally and internally validated as highly predictive for FH.

4. Rule Out Secondary Causes of High LDL

Before diagnosing FH, always rule out other medical conditions that can cause elevated LDL cholesterol, such as high triglycerides, type 2 diabetes, untreated thyroid disease, or renal disease.

5. Be Aware of FH Physical Signs

Look for physical manifestations of FH, including tendon xanthomas (cholesterol deposits on tendons, especially extensor tendons of hands and Achilles), arcus cornealis (a cholesterol ring in the cornea), and xanthelasmata (deposits on eyelids), as these can aid in early diagnosis.

6. Consider Genetic Testing for FH

If clinical diagnosis of FH is strong, pursue genetic testing to definitively confirm the presence of a mutation, as this provides an unambiguous diagnosis without overlap, unlike cholesterol levels alone.

7. Implement Healthy Lifestyle for FH Children

For children with heterozygous FH, establish a very healthy lifestyle early on, including extensive anti-smoking education, comprehensive dietary counseling for healthy food choices, and regular physical exercise.

8. Start Statin Therapy for FH Children

Despite lifestyle interventions, statin therapy should be initiated in children with FH, typically around age six, as lifestyle measures alone are insufficient to cure the condition.

9. Consider Rosuvastatin for Pediatric FH

When prescribing statins for children with FH, rosuvastatin can be a preferred option due to its ability to be dosed at a low 2.5 mg, making it a tiny, manageable pill for a child.

10. Aim for Lower LDL in FH Children

While conservative guidelines suggest an LDL cholesterol goal of at least below 130 mg/dL for children with FH, recognize that a healthy endothelium ideally has much lower LDL levels, suggesting potential benefit from more aggressive treatment.

11. Utilize Quadruple Therapy for Homozygous FH

For individuals with homozygous FH, implement a state-of-the-art quadruple therapy consisting of high-dose statins, ezetimibe, evolocumab (or similar PCSK9 inhibitor), and evinacumab (an NGPTL3 monoclonal antibody) to achieve relatively normal LDL levels.

12. Advocate for Evinacumab in Pediatric Homozygous FH

For children with severe homozygous FH, advocate for the use of evinacumab, as it is a ‘golden rescue’ that can significantly reduce LDL levels and often obviate the need for LDL apheresis, though currently approved for adults.

13. Do Not Dismiss LDL’s Causal Role in ASCVD

Do not dismiss the causal link between elevated LDL cholesterol and atherosclerotic cardiovascular disease (ASCVD), as evidenced by the severe and often premature outcomes in FH patients with single-gene mutations that solely raise LDL.

14. Reject the HDL Hypothesis for ASCVD Prevention

Do not rely on high HDL cholesterol as a primary protective factor against ASCVD, as clinical trials with CETP inhibitors that only raised HDL without lowering LDL or ApoB showed no reduction in heart attacks or strokes.

15. Prioritize Potent CETP Inhibitors for LDL Lowering

When considering CETP inhibitors, prioritize those that robustly lower LDL cholesterol (e.g., by 50% on top of high-intensity statins) and have a clean safety profile, as LDL lowering is the validated mechanism for cardiovascular benefit.

16. Consider Obicetrapib for Type 2 Diabetes Risk Reduction

Recognize the potential of potent CETP inhibitors like obicetrapib to reduce the risk of type 2 diabetes by improving pancreatic beta-cell function and reducing lipotoxicity, an effect observed across multiple CETP inhibitor trials.

17. Consider Obicetrapib for Sepsis Protection

Understand that potent CETP inhibition may offer protection against septicemia by maintaining high HDL levels, which can function as a sink for endotoxins and other inflammatory mediators during infection.

18. Consider Obicetrapib for Lp(a) Reduction

If you have elevated Lp(a), consider the potential of obicetrapib to significantly lower Lp(a) levels (e.g., by 56% at a 10mg dose), although clinical outcome data specifically for Lp(a) lowering with this drug are still pending.

19. APOE4 Carriers: Raise ApoA1 for Neuroprotection

For APOE4 carriers, consider strategies that substantially raise ApoA1 levels (such as potent CETP inhibitors), as ApoA1 can traverse the blood-brain barrier and potentially offset the detrimental effects of dysfunctional APOE4 on brain cholesterol metabolism and Alzheimer’s risk.

20. APOE4 Carriers: Proactively Manage Risk Factors

If you are an APOE4 carrier, proactively take steps to prevent exacerbating risk factors for Alzheimer’s and cardiovascular disease, as early intervention and comprehensive management can significantly improve your long-term outcomes.

21. APOE4 Carriers: Be Aware of Cardiovascular Risk

If you are an APOE4 carrier, be aware of your increased risk for cardiovascular disease due to higher LDL cholesterol and a pro-inflammatory state, and manage these factors aggressively.

22. Prioritize ApoB and Non-HDL-C as Biomarkers

Prioritize non-HDL cholesterol and ApoB as superior prognostic markers and measures of therapeutic efficacy compared to LDL cholesterol calculated by the Friedewald formula, as they more accurately reflect the total burden of atherogenic lipoproteins.