New Pharmacotherapies for Assisting Smokers in Their Cessation Efforts

Frank Vocci, Ph.D.Director, DPMCDADecember 7, 2005

Varenicline• Partial agonist at the 4ß2 nicotine

receptor• Partial agonists have some effects like

nicotine but can also act like antagonists

• A dual mechanism of action is proposed:– Partial nicotine-like effects– Nicotine blockade from cigarette smoking

Varenicline

Varenicline Phase II Trials- Tonstad study

Drug 12 WeekQuit Rate %

52 WeekQuit Rate %

placebo 18 10

Bupropion 30 16

Varenicline 44 22

Rimonabant

• CB1 inverse agonist/ antagonist• Stratus-US Study ( unpublished)• Quit rates in the 20 mg group were

double that of placebo• Weight gain in the 20 mg group was 0.4

kg for 12 weeks versus 3.6 kg for placebo• The 20 mg group also had attenuated

weight gain 1.5 kg versus and additional 3.5 kg for placebo

Rimonabant

• May be sought after by smokers who want to quit but don’t want to gain weight

• Could be tested with other therapies, especially NRT for additive effects

• Has other metabolic effects which can independently reduce cardiovascular disease risk

Nicotine Vaccine

• Being produced by three companies

• Potential indications:– Aid to cessation– Prevention of relapse– And prevention of smoking

Nicotine Vaccine

Nicotine Vaccine

Nicotine Vaccine Blocks Nicotine Self-

Administration

New Therapies

• Offer new prospects for smokers looking for an assist to quit smoking

• Each may have distinct advantages• The vaccine may be useful for relapse

prevention• Other medications are also being

developed