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ACOMPLIA 20 mg film-coated tablets
Each tablet contains 20 mg rimonabant.
 

PHARMACEUTICAL FORM:
Film-coated tablet
Biconvex, teardrop-shaped, white tablets debossed with “20” on one side.
 

Therapeutic indications:
As an adjunct to diet and exercise for the treatment of obese patients (BMI 30 kg/m2), or overweight patients (BMI > 27 kg/m2) with associated risk factor(s), such as type 2 diabetes or dyslipidaemia (see section 5.1).

More information (INCLUDING IMPORTANT SAFTEY INFORMATION) is available at: http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=18283

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Should You Take Acomplia?

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The real dangers of replacing willpower with pill power
by Charles Hirschberg, Men's Health; Photograph by Plamen Petkov
 

Suppose—just suppose—there was a pill that could help you shed 10 percent of your body weight, raise your good cholesterol and lower your triglycerides. Would you take it?

Don't answer yet. Suppose this same pill could help you shrug off any chemical addictions that might be troubling you—your chain-smoking, your problem drinking. Would you take it now?

Don't answer yet. Suppose this same pill had been tried by 10,000 people, and the only reported side effects were tummy trouble and depression. Would you take it now?

The reason I ask, gentlemen, is that there really is such a pill. It's called Acomplia, and if it lives up to a fraction of its promise, you may actually have to decide whether or not to take it.

Let's get one thing straight, right at the top: Acomplia, as of press time, isn't yet on the market. And, in any case, it's nothing like that miracle potion in The Nutty Professor that transformed Eddie Murphy from blimp-butted Sherman Klump into slim hipster Buddy Love. The majority of people who used Acomplia in clinical trials lost at least 5 percent of their body weight in a year, but almost no one lost much more than 10 percent.

Still, the medication could help millions of people resist their most self-destructive cravings and, at the same time, fine-tune their metabolisms. What's more, Acomplia could well be just the first of a whole new class of drugs that work by taking advantage of one of the most intriguing biological discoveries of the past 20 years: the endocannabinoid system.

Larger than Lipitor

So, what do you think now? Would you take it?

"I would," says Peter VanOoyen. In fact, he probably already has. VanOoyen had been trying to quit smoking for 17 years when he saw an ad in a West Virginia paper for a clinical trial of Acomplia and signed up. He may have received a placebo, but he doubts it. "I'd tried everything," he says. "Nicotine patch, nicotine gum, cold turkey. I started on that pill, and I quit within six days. No side effects. Cigarettes just didn't taste right anymore."

And there's more: Most smokers really pack on the lard after quitting. But not VanOoyen. "I didn't gain an ounce," he says delightedly. This is typical of people who quit smoking with Acomplia—some even lose weight.

"I would definitely take it," chimes in Anita Galis, another West Virginian, who struggled with her weight for years before entering a clinical trial. The white capsule she took could also have been a placebo, but she doesn't think so. She experienced absolutely no side effects, lost 20 pounds, and saw her cholesterol improve markedly. Unfortunately, as soon as she stopped taking the capsules, she gained it all back again.

That, too, is typical: Evidently, those who want the full benefits of Acomplia will probably have to take it indefinitely. That's fine with chronic overeaters like Galis. "Oh," she says with gusto, "the second that drug comes out, I'm back on it!"

That reaction presages a glorious payday for Sanofi-Aventis. The French-based company, the third-largest drug manufacturer in the world, has been developing Acomplia since 1992. Financial analysts have giddily predicted sales of $3 billion to $5 billion a year—a blockbuster by any standard. But those analysts assumed that Acomplia would be used merely to treat some of the 60 million Americans who are obese, along with some of the 30 million or so smokers who would like to quit. Now Sanofi-Aventis is suggesting that Acomplia could become "complementary to Lipitor," the cholesterol reducer that is more widely prescribed than any other pill in the United States; $12 billion worth is sold annually.

But here's the catch: No one knows when, or even if, the Food and Drug Administration will approve Acomplia for use by the general public. (The drug is rumored to be on the FDA's agenda for the first half of this year.) Moreover, while nearly all the medical experts interviewed by Men's Health are enthusiastic about Acomplia's potential and expect it to be approved, many of them are urging the public to be cautious about taking it until scientists have had a few more years to study its effects.

"When I was in medical school, there was an adage: 'Every drug has at least two effects—the one you intended and the one you didn't,' " says Harvard medical school professor Jerry Avorn, M.D., author of Powerful Medicines: The Benefits, Risks and Costs of Prescription Drugs. "It's important to remember that new drugs can be harmful in new ways."

Thank you for pot smoking

If Acomplia pans out, Sanofi-Aventis can thank the American stoner. In his own mellowed-out way, he hastened the dawning of the age of Acomplia.

More than six years ago, 62 pot smokers lucked into an awesome gig: Scientists at the National Institute on Drug Abuse (NIDA) offered to pay them to smoke dope.

The NIDA scientists wanted only seasoned pot smokers for their experiment—connoisseurs, if you will, who could make sophisticated judgments about the quality and intensity of a cannabis experience. Each applicant had to have an IQ higher than 85 (roughly that of Koko, the voluble gorilla) and prove his pot-smoking bona fides by failing a drug test. He also had to answer questions about his past, if he could remember it. Dudes were excluded if they suffered from major psychiatric illnesses, drank more than four beers a day, used hallucinogens, or had ever been knocked out for more than three minutes.

Those who made the cut (they were all males, between 21 and 45) reported to a NIDA laboratory and, after medical tests, received a pill a day later. That pill was either a placebo or a compound then known as SR141716. (It was also called rimonabant.)

Two hours later, each stoner took a seat before a computer screen and fired up a machine-rolled cannabis cigarette weighing 764 milligrams, precisely 2.64 percent of which was THC, marijuana's active ingredient. He was then instructed to commence puffing at a rate of eight inhalations per minute. As the blunt disappeared, the stoner was asked at frequent intervals, "How stoned are you now? How high do you feel now? How strong is the drug effect you feel now?" The questions continued for more than an hour after the joint was gone.

The results were striking. Stoners who received SR141716 experienced major bummerage. They complained of being about 40 percent less stoned than those who took the placebo. Marilyn A. Huestis, Ph.D., chief of NIDA's Chemistry and Drug Metabolism Intramural Research Program, observed, "These findings confirm for the first time in humans the central role of CB1 receptors in mediating the effects of marijuana."

This was doubtless very interesting to Huestis, who hopes someday to use Acomplia, or something like it, to help habitual marijuana users wean themselves off dope. But what does the drug's effect on marijuana smokers have to do with its ability to promote weight loss, improve metabolism and lower the risk of cardiac disease? Everything.

By showing that Acomplia impedes marijuana intoxication, Huestis gave Sanofi-Aventis every reason to hope that the drug could be effective against one of marijuana's loopiest side effects—a phenomenon scientists refer to as hyperphagia and stoners call "the munchies."

Manipulating the munchies

It's estimated that about one in three Americans has tried marijuana at one time or another, and many of them have also subsequently inhaled a five-course breakfast at 4 o'clock in the morning. In college, I myself was once awakened by the screams of some moron who had burned his eyes with hot oil while trying to make popcorn in a frying pan—without a lid. The most irritating moment occurred when I realized that the moron was actually me.

But it was the antics of dope-smoking college morons that led scientists like Raphael Mechoulam, Ph.D., now of Israel's Hebrew University, to wonder how reefer smoke could have such wacky effects on the human brain. In 1964, Mechoulam discovered THC (short for delta-9-tetrahydrocannabinol), the single chemical responsible, and pharmaceutical researchers began wondering whether this discovery might yield a marketable drug. For instance, if they could figure out why and how marijuana gives people the munchies, maybe they could design an anti-munchie drug—an appetite suppressant.

So scientists set out to unravel exactly what happens in people's brains when THC makes them high. "We knew there had to be a receptor," says Allyn C. Howlett, Ph.D., of North Carolina Central University's Julius L. Chambers Biomedical/Biotechnical Research Institute. Every one of the body's trillions of cells, including those in the brain, is dotted with receptors—tiny proteins that lie in wait atop the cell's membrane like docking stations. Each receptor is constructed to bind with a particular type of ligand—a chemical that carries information from one cell to another, provoking particular behaviors.

The receptor she and others discovered came to be known as CB1 ("CB" for "cannabinoid"). Scientists were astonished to find out that not only is it one of the most plentiful receptors, but it is also found in nearly every major region of the brain.

"It's not very likely that this receptor exists just so people can experience the effects of marijuana," Howlett deadpans. "It had to have other purposes, and some of them were probably important."

In order to uncover these purposes, scientists still had to find the message-carrying chemicals (ligands) for which the receptor was actually meant. These substances, sometimes called "the body's inner dope," are more properly known as endogenous (that is, native to the body) cannabinoids, or endocannabinoids. It was Mechoulam who found the first one, and he named it "anandamide," from the Sanskrit word meaning "bliss."

Its exact role in the emotions is not yet known, but scientists strongly suspect that it is integral to that fine chunk of bliss you feel whenever you satisfy an oral craving—say, when you lick that first, sweet swirl of frosting off the top of your birthday cake. It is a crucial part of an internal reward system that, according to Daniele Piomelli, Ph.D., a professor of pharmacology at the University of California at Irvine, "seems to have been designed to make humans feel good about something they obtain after a long quest."

In other words, the ape-man who chowed down, and fattened up, whenever he tripped over a wildebeest carcass had a better chance of surviving an Ice Age winter than did a fellow who was content with a nosh. The endocannabinoid system that evolved accordingly is a masterpiece of natural selection. Its receptors are located by the millions, not just in the brain, but in the digestive tract, muscle tissue, bladder, liver, fat cells and many other organs. It is a network of spectacular complexity, carrying intricate messages from one cell to another, from one organ to another, from one system to another. The fact that humans stumbled across so vital a part of themselves by way of a smoldering doobie is pretty hilarious, when you think about it.

There's profits in those pills

To the pharmaceutical industry, however, the endocannabinoid system is deadly serious—as serious as money. Nearly all the major companies sniffed profit in a potion that could tamp the system down, but in 1994, Sanofi (at the time a separate company from Aventis) won the race after just two years of research—"one of the quickest cycle times between a target and a drug discovery in the history of the pharmaceutical industry," boasts Douglas Greene, M.D., Sanofi-Aventis's vice president of corporate and regulatory affairs. Pfizer, Merck, Hoffman-La Roche, AstraZeneca and Solvay are among the companies that have patented similar drugs, but none are as far along in development.

By the time NIDA began testing the effects of Acomplia on stoners, the important question was not so much would it work, but to what degree? Think about it: In addition to stimulating the appetite, marijuana also relaxes the mind, soothes the stomach and dulls pain. If Acomplia reverses the munchies, might it not also agitate the mind, roil the stomach and increase sensitivity to pain?

Animal studies suggest that it might. Australian scientists have found that rats treated with Acomplia are more sensitive when you jab their skin or apply heat to their tails. In another study, stiff doses of Acomplia were given to least shrews (mouselike creatures), which caused them to vomit like nobody's business. Elsewhere it was shown that, under certain circumstances, it's much easier to freak out a rat after he's had a dose of Acomplia.

To study these sorts of effects, Sanofi-Aventis tested its potential blockbuster on a huge scale, recruiting more than 13,000 people in both Europe and North America to sample the medicine's effectiveness in smoking cessation, weight loss and the prevention of type-2 diabetes.

The smoking trials were called STRATUS (Studies with Rimonabant and Tobacco Use) and went smoothly enough for Robert Anthenelli, M.D., of the University of Cincinnati, to announce the results with some fanfare at the American College of Cardiology Scientific Sessions in spring 2004. Nearly 800 smokers were given either Acomplia or a placebo for 10 weeks. One-third of the Acomplia users were able to quit for at least a month—double the number who took the placebo. And quitters who used Acomplia were less likely to take up smoking again after a year, even though they had stopped taking the drug.

But it was a two-year trial on more than 1,500 obese or overweight Europeans and Americans that established Acomplia as a potential superstar. According to the Lancet, the amount of blubber people shed was actually fairly modest—an average of about three inches off some very large waistlines. But what got tongues flapping, from the watercoolers of Merrill Lynch to the dieters' chat rooms of cyberspace, was a shocking bonus that no one could have predicted before the endocannabinoid system was properly understood.

A new wonder drug is born

People who took Acomplia saw their triglycerides drop by about 15 percent, while their "good" cholesterol shot up some 23 percent—improvements that were fully "twice that which would be expected from the degree of weight loss achieved," according to Columbia University's Xavier Pi-Sunyer, M.D., who conducted his own two-year study of the drug. By one estimate, the jump in HDL cholesterol alone could reduce the risk of heart disease by 50 percent.

But "what is truly remarkable," says Jean-Pierre Després, Ph.D., of Quebec's Laval University, whose study of Acomplia's effect on lipids was recently published in the New England Journal of Medicine, is that the drug "appears to have a direct effect on fat cells." By that, he means it may quiet the body's fat-storage mechanism, as well as lessen the appetite that feeds it.

If he's right, the instant Acomplia is approved, it's likely to become the most effective long-term weight-loss drug ever introduced. Of course, that's not saying much—at the moment, there are only two long-term drugs, and neither has many fans. There's Meridia, which works by suppressing the appetite, but in so doing, often raises blood pressure, which is about the last side effect an overweight person needs. And then there's Xenical, which just won over-the-counter approval from the FDA. But look before you take that leap. The drug works by preventing the absorption of certain fats—but at the prescription dosage, at least, it also causes as many as 9 percent of its users to soil their underpants.

Acomplia, in contrast, both suppresses the appetite and alters the metabolism. Nausea and a feeling of fullness in the belly are not unusual side effects, but the kinds of disasters that put the "ick" in Xenical are rare.

"For the first time," says Louis Aronne, M.D., a past president of the North American Association for the Study of Obesity, "there appears to be part of a solution to obesity and cardio-metabolic risk by getting to the root of why people put on excess weight. Acomplia may be a sign of a completely new era in the treatment of obesity."

Even as Dr. Aronne and all the rest await the FDA's final word, the Internet clamor has already begun. Weight-loss junkies chat and post, breathlessly asking one another whether or not Acomplia might, at last, be the holy grail—a pill that makes you not only thin, but healthy and happy, too. The anxiety side effects are the last thing on their minds.

But Mechoulam hopes both the public and Sanofi-Aventis will be prudent. "So far," says the scientist who, more than any other, is responsible for the discovery of the endocannabinoid system, "[Acomplia] seems to be quite free of dangers." But, he adds, "in view of the importance of the endocannabinoid system, I would have expected more serious side effects. I sincerely hope that none are noted when many thousands start using it over long periods of time."

Many thousands of users over long periods of time—that's the only way to really judge the safety of a drug like Acomplia. And what concerns physicians like Dr. Avorn is that "many people still assume that once the FDA has approved a drug, that means it's safe, or at least that its benefits outweigh its risks. And that's just not the case."

In fact, the FDA's trials are devoted primarily to proving that a drug is more effective than a placebo—or, to put it another way, that it is better than nothing. Of course, its negative side effects in clinical trials must be noted and the public warned. But, according to Dr. Avorn, even large trials of the sort used to test Acomplia may be too small to detect certain rare and potentially lethal side effects.

Shooting for a bigger target

For men who are morbidly obese, have tried everything else and just can't seem to control their appetites, Acomplia may well prove to be a godsend. But the large-guy market is a little too small for executives at Sanofi-Aventis. They're itching to broaden the drug's portfolio. Research suggests that, like cholesterol-fighting Lipitor, Acomplia could be effective in fighting the "metabolic syndrome" that afflicts 50 million of us—a combination of excess abdominal flab, dangerous levels of cholesterol and triglycerides, elevated blood pressure and early symptoms of type-2 diabetes that often leads to heart disease or stroke.

"It took 15 years before drugs like Lipitor evolved to become as widely used as they are today," says Sanofi-Aventis's Dr. Greene. "Had we fully understood their potency and the number of people who would benefit from them, it would have been nice to have brought that process along much quicker. And so it's our hope to be able to do that [with Acomplia]." Dr. Greene's belief in the therapeutic value of the drug is obviously sincere. But mingled with his impatience is the fact that sales of Lipitor are running in the neighborhood of $1 billion a month.

For Acomplia to approach that number, a lot of doctors will need to suggest it to a lot of patients to help with metabolic syndrome. Says Dr. Greene, "I would expect, in a day-to-day physician-to-patient relationship, that this will very likely start before we have all of the hard outcome data."

Here's what that means: The moment Acomplia is approved for smoking cessation and obesity, physicians can prescribe it off-label for just about anything they like. And if they want to start prescribing it for metabolic syndrome, for instance, Sanofi-Aventis would not exactly object. Plenty of doctors seem prepared to do just that—but some researchers are not so sure.

"My mother takes Lipitor," says Piomelli, "but I would never, never let her take [Acomplia] with it. She tends to be very anxious, and I'd be afraid she could have a potentially dangerous reaction."

Piomelli is currently experimenting with a promising treatment for depression that works essentially by provoking an effect opposite to the one Acomplia creates in the brain. He has closely studied the relationship between the endocannabinoid system and emotions, and he wonders if the clinical trials might have undercounted the depression and anxiety Acomplia can cause.

For instance, in one trial involving more than 1,500 obese and overweight people, 7 percent of those treated with Acomplia—as opposed to 5 percent of those who took a placebo—were said to have experienced psychiatric disorders, including depression and anxiety. But a disconcerting 20 percent of the Acomplia patients dropped out before the study was completed, for reasons described by researchers as "poor compliance," "patient request," or "lost to follow-up." Could a substantial percentage of this group also have suffered from Acomplia-induced emotional distress? Scientists readily admit that they simply don't know.

Underestimating the risk

What concerns Piomelli is that many internists—perhaps even internists like the one Dr. Greene imagines, conscientiously prescribing Acomplia for metabolic syndrome "before we have all the hard data results"—might underestimate the risk of depression. In the real world, Piomelli points out, "most people are not much more likely to discuss depression with their internists than they are to discuss their lipids with their psychiatrists."

Mind you, Piomelli has nothing against Acomplia—in fact, he's a fan. "For a large percentage of patients, I think it could be fantastic," he says. "But that is precisely why I worry. Imagine if, say, 50 to 100 of the men who take [Acomplia] become depressed, don't realize what's happening, and, like so many men, instead of seeing a psychiatrist, deal with it by going to the gym to work on their abs. If even just a few of those were to commit suicide, it not only would be a tragedy, but could result in the drug being removed from the market. And not just this drug, but the whole class of drugs, with all its promise and potential."

That potential seems virtually limitless. As you read this, scientists are conducting experiments that could lead to endocannabinoid-based treatments for tumors, sexual dysfunction, Parkinson's disease, liver disease, respiratory illnesses and many other disturbances. And that is why nearly every medical expert interviewed for this story practically begged Men's Health to tell its readers, "If you don't need Acomplia for health reasons, don't take it."

Eric Topol, M.D., a renowned cardiologist at Ohio's Cleveland Clinic, has just launched the most comprehensive study of Acomplia yet. Appropriately titled CRESCENDO (Comprehensive Rimonabant Evaluation Study of Cardiovascular Endpoints and Outcomes), it will follow 17,000 men and women 55 and older for three years, to determine whether the weight and lipid improvements Acomplia brings actually translate to fewer heart attacks and strokes. "We will also be carefully monitoring depression and anxiety," says Dr. Topol. Like nearly everyone, he is optimistic about the potential of Acomplia. "But I do not think it should be prescribed for metabolic syndrome" until the CRESCENDO study is complete, he says. "I would also hope the company would refrain from direct advertising" until that time.

That's not likely. A spokesman for Sanofi-Aventis says the company reserves its right to exercise "all of our options" in order to "educate" the public about Acomplia.

The sad fact is, Americans have had a long, humiliating love affair with diet pills, and the results have been almost uniformly disastrous. In the 1930s, an estimated 100,000 Americans chugged weight-loss preparations containing dinitrophenol—a chemical also used in weed killers—before it was found to cause cataracts and death. Then, in the pill-popping 1960s, amphetamines became the weight-loss drug of choice, to the tune of about 2 billion pills in a single year. Their most famous user, and victim, was poor Elvis Presley, who took so many amphetamines to tame his ravenous appetite that his body ballooned and shrank like an inflatable doll. Finally, one night, Presley's heart gave out, and he died on the bathroom floor—a grisly warning on the dangers of both overeating and overmedicating.

Despite this warning, America just got fatter—and all the more desperate for pharmacological help. In the 1990s, a cocktail of fenfluramine and phentermine—fen-phen—was anointed as savior. That is, until researchers identified two fatal risks associated with the "fen" part of the cocktail: pulmonary hypertension—a potentially fatal high blood pressure in the arteries of the lungs—and dangerous heart-valve abnormalities. In 1997, the drug was yanked off the market, and, at last count, Wyeth had paid more than $20 billion in fen-phen-related damages—another sort of grisly warning.

You see where this is going: The appetite for Acomplia is already huge, and the table is set for another disaster. Only this time, a genuinely beneficial drug could be taken off the market simply because it is prescribed too widely, too quickly.

"It all comes down to the big D—discipline," says Dr. Topol. "People want a pill to do it for them. The healthiest thing, by far, is to do it for yourself."

Provided by Men's Health

Acomplia Cuts Diabetes Patients' Risks

Experimental Weight Loss Drug May Have Benefits for Type-2 Diabetes By Daniel DeNoon
WebMD Medical News Reviewed By Louise Chang, MD
on Monday, June 12, 2006
 

June 12, 2006 -- Acomplia, an experimental weight lossweight loss drug, helps obese people with type 2 diabetesdiabetes lose weight, reduce waist size, and even control blood sugar and blood fats.

Surprisingly, Acomplia's beneficial effect on blood sugars and fats went 57% beyond the benefit that would have been expected from weight loss alone. The drug, which affects the body's cannabinoid system, appears to reduce interrelated risks for heart and metabolic diseases.

The benefits seen were in addition to the benefits of standard, ongoing treatment with Glucophage or the family of diabetes drugs called sulfonylureas. Researcher André Scheen, MD, PhD, head of diabetes at the University of Liège in Belgium, reported the findings at this week's annual meeting of the American Diabetes Association, held June 9-13 in Washington.

"These findings support the use of [Acomplia] for reducing cardiometabolic risk in patients with type 2 diabetes, and show that the benefits achieved are additional to those of background oral antidiabetic therapy," Scheen and colleagues wrote in their presentation abstract.

The findings come from an international clinical trial of more than 1,000 men and women with diabetes. The average study patient was 56 years old and obese, with a 43.3-inch waistline. At study entry, patients' average hemoglobin A1c (HbA1c) level was 7.5%. HbA1c measures average blood sugar levels over the past three months. Normal HbA1c levels range from 4% to 6%.

Acomplia lowered HbA1c levels by 0.6%. That may not sound like much, but recent studies indicate every 1% increase in HbA1c raises the risk of death -- from all causes -- by 24% for men and 28% for women.


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SOURCES: Scheen, A. X. Presentation to the Annual Scientific Sessions of the American Diabetes Association, Washington, June 9-13, 2006; Abstract 560-P. Khaw, K.-T. Annals of Internal Medicine, Sept. 21, 2004; vol 141: pp 413-420.



Pharmaceuticals
Page 3 of 13 from Cardiovascular Drugs To Watch
Matthew Herper and Robert Langreth, 08.05.05, 11:15 AM ET
 

Sales Potential: $$$
Novelty: ++++

Acomplia appears to help patients lose weight and quit smoking, but that's just the beginning. The drug, which works by blocking off the same hunger-causing receptors that marijuana stimulates, cut 3.5 inches off patients' waistlines, helping them shed an average of 20 pounds. Additionally, the drug doubles patients' likelihood of quitting smoking within ten weeks. Acomplia also appears to work directly on fat cells, reducing several important risk factors for heart disease. For instance, it raises HDL, the good cholesterol, by 27%--about as much as any available drug. In new data presented at a medical meeting on June 12, the drug also controlled blood sugar as effectively as many diabetes drugs. But it does have side effects, including anxiety and nausea. An FDA submission was made in June 2005, and a decision is expected in a year.
 

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