licofelone 5lox new drug

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Novel type of painkiller promising

New anti-inflammatory may ease aches, pains of arthritis

ASSOCIATED PRESS

June 14 — A new type of anti-inflammatory painkiller is showing promise

in experiments on people with arthritis in their knees. Research

presented at a conference in Stockholm this week indicated the drug

works just as well for arthritis as traditional nonsteroidal

anti-inflammatory drugs such as aspirin and ibuprofen, but is gentler on

the stomach.

EXPERTS say the medication, licofelone, could offer an

alternative to newer arthritis drugs, such as Vioxx and Celebrex, which

have recently come under suspicion of increasing certain people’s heart

risks.

Licofelone, being developed by German pharmaceutical manufacturer

Merckle, works in a slightly different way from other anti-inflammatory

painkillers and some scientists suspect it might have benefits beyond

pain relief.

“It’s extremely encouraging and it will provide another option

for treatment for arthritis patients, which we desperately need,” said

Dr. Jean-Pierre Pelletier, head of the osteoarthritis research unit at

the University of Montreal’s Central Hospital, who was not connected

with the research.

Conventional nonsteroidal anti-inflammatories work by shutting

off production of prostaglandins, inflammation-causing substances. They

do this by blocking the action of the enzyme cox, which produces

prostaglandins.

Rheumatoid arthritis, or RA, involves inflammation in the lining of

the joints and/or other internal organs. RA typically affects many

different joints. It can be chronic or can be a disease of flares and

remissions.

RA, which affects the entire body, is characterized by the

inflammation of the membrane lining the joint, which causes pain,

stiffness, warmth, redness and swelling. The inflamed joint lining can

invade and damage bone and cartilage. Inflammatory cells release enzymes

that may digest bone and cartilage. The involved joint can lose its

shape and alignment, resulting in pain and loss of movement.

Major symptoms include inflammation of joints, swelling, difficulty

moving and pain. Pain and swelling may occur in the same joints on both

sides of the body and will usually start in the hands or feet. RA

affects the wrist and many of the hand joints, but usually not the

joints that are closest to the fingernails (except the thumb). RA also

can affect elbows, shoulders, neck, knees, hips and ankles. It tends to

persist over prolonged periods of time, and over time, inflamed joints

may become damaged.

Other symptoms include: loss of appetite, fever, loss of energy,

anemia and rheumatoid nodules (lumps of tissue under the skin.

* Rheumatoid arthritis affects 2.1 million Americans, mostly women

* Onset is usually in middle-age, but often occurs in the 20s and 30s

* 1.5 million women have rheumatoid arthritis compared to 600,000 men

The cause of rheumatoid arthritis is not yet known. However, it is

known that RA is an autoimmune disease. The body's natural immune system

does not operate as it should, resulting in the immune system attacking

healthy joint tissue and causing inflammation and subsequent joint

damage.

Researchers suspect that virus-like agents may trigger RA in some

people who have an inherited tendency for the disease. Many people with

RA share a certain genetic marker.

If you have any of these signs in or around a joint for more than two

weeks, see your doctor.

* Pain

* Stiffness

* Swelling

* Difficulty moving joint

Highly effective drug treatments exist for rheumatoid arthritis. Early

treatment is critical. Current treatment methods focus on relieving

pain, reducing inflammation, stopping or slowing joint damage, and

improving patient function and well-being. Medications can be divided

into two groups

* Symptomatic medications, such as NSAIDs and aspirin, analgesics, and

glucocorticoids, help reduce joint pain, stiffness and swelling. These

drugs may be used in combination.

* Disease-modifying medications include low doses of methotrexate,

leflunomide, D-Penicillamine, sulfasalazine, gold therapy, minocycline,

azathioprine, hydroxychloroquine (and other antimalarials), cyclosporine

and biologic response modifiers.

People with moderate to severe RA who have not responded well to

disease modifying anti-rheumatic drugs may opt to try Prosorba therapy.

In addition, treatment most often involves some combination of

exercise, rest, joint protection, and physical and occupational therapy.

Surgery is available for joints that are damaged and painful.

* Exercise regularly

* Use correct posture to help your joints stay aligned properly

* Listen to your body for signals that it needs to rest

* Use assistive devices such as splints and braces to help stabilize

joints, provide strength and reduce pain and inflammation

* Ask your doctor about hot tub therapy

* Get enough sleep

* Consider massage

* Practice relaxation techniques

In the late 1980s, scientists discovered there were two varieties

of the cox enzyme. They found that while cox-2 causes pain and

inflammation as part of the body’s repair process, cox-1 protects the

lining of the stomach.

That explained why the painkillers caused stomach upsets. The

discovery led to drugs designed to relieve pain but spare the stomach.

That type of pill, including Vioxx and Celebrex, blocks only

cox-2 rather than both cox enzymes, and is known as a cox-2 inhibitor.

However, recent studies have suggested that some cox-2 blockers

might increase the risk of blood clots. Scientists speculate it may be

because the two cox enzymes are out of balance. As well as protecting

the stomach lining, cox-1 plays a role in blood clotting.

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The new drug, licofelone, blocks both cox-1 and cox-2, like the older

painkillers, but also interferes with the action of another enzyme

involved in pain and inflammation, called 5-lox.

The study, presented at the European Congress of Rheumatology in

Stockholm, found that licofelone worked as well as the older drugs, was

gentle on the stomach and showed no trace of side effects that could

cause heart problems.

It involved 710 people with arthritic knees, followed for a year.

One-third received a low dose of the new drug, one-third a high

dose and the others got naproxen, a conventional nonsteroidal

anti-inflammatory.

The study’s lead investigator, Dr. Jean-Yves Reginster of the

University of Liege, said the new drug was as effective as the old one.

In each of the three arms of the study, two-thirds of the patients had

significant improvements in pain and inflammation.

Those on the new drug were 80 percent less likely than the others

to get a stomach ulcer.

Reginster said the study did not directly address heart safety,

but that swelling in the feet and ankles, and elevated blood pressure —

both side effects suggested in studies of cox-2 blockers — did not

affect patients taking the new drug.

Pelletier said he doesn’t expect to see any heart problems with

the new drug because its cox enzyme blocking action is balanced.

The fact that the new drug also blocks the enzyme 5-lox may give

it extra appeal, Pelletier added.

There is preliminary evidence that 5-lox may play a role in

deterioration of the joints and licofelone is being investigated as a

possible disease-slowing drug, he said.

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