Pantethine, a derivative of vitamin B5, offers a safe option for improving lipid profiles and reducing cardiovascular risk beyond what can be obtained with a low-fat diet and lifestyle modification alone.
Used widely by Japanese physicians to treat people with dyslipidemia, pantethine has been evaluated in 28 controlled clinical trials involving Asian patients at high risk for cardiac events. In these studies, it has been shown to reduce total cholesterol by approximately 15%, LDL cholesterol by 20%, and TGL by 32%, while raising HDL by about 8%.
A recent study, the first involving a North American population, showed that at a dose of 600 mg per day, pantethine reduced total cholesterol by 6 mg/dl and LDL by 4 mg/dl, beyond the changes patients experienced on a therapeutic lifestyle diet.
The biologically active metabolite of pantethenic acid (vitamin B5), pantethine is normally produced by the body from B5 in food. An absorbable form of the active metabolite known as Pantesin has been available in Japan for over 30 years. It was recently introduced into the US by Kyowa Hakko as an ingredient for dietary supplements.
Benefits Beyond Diet
In the current study, cardiologist John Rumberger, PhD, MD, and colleagues evaluated the impact of pantethine supplementation in 120 US men and women fitting the ATP-III category 1 and 2 CVD risk profiles. At baseline, subjects had total cholesterols in the range of 108-112 mg/dl, and a median age of 47 years.
All patients adhered to the National Heart, Lung & Blood Institute’s lipid-lowering “TLC” (Therapeutic Lifestyle Change) diet for 4 weeks. This diet limits saturated fat intake to less than 7% of total daily calories. Most subjects showed significant reductions in total cholesterol and LDL from the diet alone, on the order of 5-10 mg/dl).
The study protocol prohibited use of supplemental fiber, plant sterols, or any other lipid-modulating supplements. None of the subjects were on lipid lowering medications.
“The purpose of the TLC diet lead-in phase was to “level the playing field,” so that we could eliminate or minimize any concerns of dietary influences on our results,” explained Dr. Rumberger.
Subjects were then randomized to treatment with placebo or pantethine in tablet form, 600 mg/day (200 mg taken thrice daily), while continuing with the TLC diet for 8 weeks. At the 8-week point, the pantethine dose was increased to 900 mg per day.
By week 16, subjects in the pantethine group had an additional 6 mg/dl reduction in total cholesterol compared with those on placebo. There was also a 4 mg/dl additional decrease in both LDL and apolipoprotein B (Rumberger JA, et al. Nutrition Research. 2011; 31: 608-615)
The cholesterol lowering effect of pantethine was already apparent by the end of the second week during the 600-mg phase, and the dose increase did not produce any further changes. This is in keeping with the dose levels found most effective in the Japanese high-risk studies.
The authors also noted that after 16 weeks, there was a non-significant reduction in TGL in the pantethine group (105 ± 44.6 mg/dL) compared with placebo (120 ± 62.3 mg/dL). Surprisingly, there was no difference in HDL, as was seen in Japanese trials. But because of the reductions in total cholesterol, the TC/HDL ratio did show favorable and significant changes.
The absence of an HDL-raising effect, and the overall smaller LDL and TC reductions are attributable to the fact that subjects in this study were at lower risk and had better LDL and HDL profiles to begin with.
“Pantethine is really good for patients on the cusp of needing lipid lowering medications or as an adjunct along with medications,” said Danielle Citrolo, Pharm.D., technical services director for Kyowa Hakko. “It doesn’t just focus on one lipid parameter but offers a very comprehensive way to positively affect a variety of lipids.”
In an interview with Holistic Primary Care, Ms. Citrolo explained that pantethine inhibits HMG-CoA reductase and acetyl –Coenzyme A, which largely accounts for the observed cholesterol changes. Unlike statin medications, pantethine does not block co-enzyme Q10 and does not produce the dramatic changes in LDL seen with statins.
She believes it makes an excellent complement to omega-3 fatty acids and other nutraceuticals used for cardiovascular health, such as niacin and aged garlic.
Though it does affect HMG-CoA reductase, Dr. Citrolo stressed that pantesin is not a statin substitute, and should not be used in place of statins in high-risk individuals for whom drug therapy is warranted. That said, it might also be helpful in conjunction with statins to avert a dose increase in people for whom low dose statins are no longer effective.
Pantethine has an excellent safety profile. In the Rumberger study, there were more patients reporting side effects in the placebo group than in the pantethine group. Loose stool was the most common pantethine associated problem (n=8 subjects), but it was uncommon and not particularly bothersome.
In his report, Dr. Rumberger noted that while there are no published data showing that pantethine supplementation lowers incidence of CVD events, one can certainly apply statin logic and estimate—as is done in statin meta-analyses—that for each 1% lowering of TC/LDL-C, there is a concomitant lowering of global CVD by at least 1%.
Kyowa Hakko’s branded Pantesin form of pantethine is available in heart health products made by a number of supplement companies, including Integrative Therapeutics, Protocol for Life Balance, Endurance Products , and Pure Encapsulations.
The cost ranges from roughly $11-$27 for a months’ supply, making it a relatively inexpensive adjunct for improving cardiovascular health.