| AVANAFIL POTENTIAL SIDE EFFECTS AND BENEFITS zhion@zhion.com November 21, 2005 |
WHAT IS AVANAFIL? WHAT IS ITS ADVANTAGE?
Avanafil, a PDE5 inhibitor, blocks the activity of a protein that
prevents blood vessels from expanding. According to the news,
avanafil is better at concentrating its activity on PDE5 than other
drugs in its class.
Examples of type V (5) phosphodiesterase inhibitors include, but not
limited to, sildenafil, tadalafil, vardenafil, avanafil, zaprinast RTM,
papaverine and dipyridamole. Other type 5 PDE inhibitors are
disclosed in PCT Publication Nos. WO 94/28902, WO 96/16644, U.S.
Pat. No. 6,338,862 and U.S. Pat. No. 6,476,037.
Avanafil's great advantage is that it acts faster than the other PDE5
inhibitors, taking effect in about 30 minutes, and disappears from the
body faster. Because of the fast action, those men who use it won't
have to wait as long.
Avanafil's relatively quick disappearance from the bloodstream should
lessen its possible side effects. In a study of 295 men, the
effectiveness was "excellent, while the side effects were minimal,
according to the news release.
WHAT ARE PDE INHIBITORS?
Phosphodiesterase (PDE) inhibitors are a class of intracelleular
enzymes which mediate the catabolism of second messengers like
cyclic adenosine monophosphate (cAMP) and cyclic guanosine
monophosphate (cGMP). These enzymes have been classified into at
least eleven groups (types I-XI) and various subclasses based on
their amino acid sequence and substrate specificity (Polson, 1996;
Trophy, 2000). The various PDE differ in their tissue, cellular
distribution, and their specificity towards cAMP or cGMP. (table 1). So
phosphodiesterase inhibitors have applications in a number of
disorders including vascular, neuronal and inflammatory disorders
(Zang 2002, Martin 2002, Grootendorst 2002, Burnouf, 2002). PDE
inhibitors are drug candidates for the treatment of a number of
disorders including heart failure, depression, asthma, inflammation,
sexual dysfunction, and erectile dysfunction. Phoshodiesterase 4D
has been shown to have a role in ischemic stroke (Gretarsdottir,
2003). [1]
WHAT ARE THE POTENTIAL APPLICATIONS OF Phosphodiesterase
PDE5 INHIBITORS?
1. Enhance sexual function in men following prostate surgery.
2. Enhance sexual function in hypogonadal men by combining
testosterone and phosphodiesterase inhibitor.
3. Treatment of premature or rapid ejaculation.
4. Enhance sexual function in women
5. Enhance endothelial function in patients with primary pulmonary
hypertension.
6. Treatment of urinary tract symptoms due to benign prostatic
hyperplasia.
7. Treatment of urinary incontinence.
8. Treatment of sickle cell anemia by combination therapy with
hydroxyurea
9. Enhance sexual function in men and women by combination
therapy with antioxidants, vitamin E, arginine, apomorphine ,
dopamine agonists, alpha adrenergic blocker etc.
10. Prevention and treatment of stroke.
11. Treatment of coronary and cerebral vascular diseases.
12. Treatment of thrombosis
13. Treatment of ocular hypertension
14. Treatment of pregnancy-induced hypertension.
15. Treatment of anal sphincter disorders (Jones, 2002).
16. Treatment of neurodegenerative diseases such as Alzheimer's
disease, Parkinson's disease, amyloid diseases, Prion diseases.
17. Treatment of other diseases where cGMP is implicated to have
beneficial effects.
WHAT ARE THE SIDE EFFECTS OF AVANAFIL?
Not much information has been reported about avanafil side effects.
In general, the side effects of Phosphodiesterase inhibitors include
hypotension, flushing, headache, nasal congestion and heartburn
and these effects are dose dependent (Moreira, 2000). The incidence
of cardiovascular events and deaths have been reported with the use
of PDE 5 inhibitors (Lim, 2002). This may be due to the fact that PDE5
inhibitors dilate the coronary arteries which makes the patient feel
better. This may lead to vigorous physical activity (exercise or
intercourse). Such activity may lead to ischemia and heart attack. Also
interaction with other drugs including nitroglycerine poses substantial
risks. The visual side effects of Phosphodiesterase 5 inhibitors are
due to the inhibition of Phosphodiesterase 6 found in the retina. [1]
ABOUT ERECTILE DYSFUNCTION
Erectile dysfunction, sometimes called "impotence," is the repeated
inability to get or keep an erection firm enough for sexual intercourse.
The word "impotence" may also be used to describe other problems
that interfere with sexual intercourse and reproduction, such as lack
of sexual desire and problems with ejaculation or orgasm. Using the
term erectile dysfunction makes it clear that those other problems are
not involved.
Erectile dysfunction can be a total inability to achieve erection, an
inconsistent ability to do so, or a tendency to sustain only brief
erections. These variations make defining erectile dysfunction and
estimating its incidence difficult. Estimates range from 15 million to 30
million, depending on the definition used. According to the National
Ambulatory Medical Care Survey (NAMCS), for every 1,000 men in the
United States, 7.7 physician office visits were made for erectile
dysfunction in 1985. By 1999, that rate had nearly tripled to 22.3.
The increase happened gradually, presumably as treatments such as
vacuum devices and injectable drugs became more widely available
and discussing erectile function became accepted. Perhaps the most
publicized advance was the introduction of the oral drug sildenafil
citrate (Viagra) in March 1998. NAMCS data on new drugs show an
estimated 2.6 million mentions of Viagra at physician office visits in
1999, and one-third of those mentions occurred during visits for a
diagnosis other than erectile dysfunction.
In older men, erectile dysfunction usually has a physical cause, such
as disease, injury, or side effects of drugs. Any disorder that causes
injury to the nerves or impairs blood flow in the penis has the
potential to cause erectile dysfunction . Incidence increases with
age: About 5 percent of 40-year-old men and between 15 and 25
percent of 65-year-old men experience erectile dysfunction . But it is
not an inevitable part of aging.
ABOUT VIVUS INC.
VIVUS, Inc. was founded in 1991 by Virgil A. Place, M.D., to research,
develop and commercialize therapies to restore male sexual function.
VIVUS' first product, MUSE®, was based on the discovery that
certain vasodilating agents, some of which are used to treat
hypertension, can be applied in the urethra and absorbed into the
erectile tissues, causing an erection in males. Today, VIVUS continues
to develop innovative therapies to restore male sexual function and is
at the forefront of pioneering therapies for women's sexual health.
THIS ARTICLE IS FOR YOUR REFERENCE ONLY. YOU SHOULD CONSULT WITH
YOUR DOCTOR IF YOU HAVE ANY MEDICAL PROBLEMS. YOU SHOULD
CONSULT WITH YOUR INVESTMENT ADVISOR, BEFORE ANY TRANSACTION.
YOU SHOULD CONSULT WITH A SCIENTIST IF YOU ARE DEVELOPING A
RELATED PRODUCT. PUBLISHER DOES NOT GUARANTEE THE ACCURACY OF
THIS ARTICLE. ALL RIGHT RESERVED 2005 zhion inc. DO NOT COPY NOR
TRANSFER TO OTHER WEBSITES OR OTHER TYPES OF PUBLICATIONS.
SOURCES VIVUS Announces Presentation of Positive Results From Five Key
Avanafil Studies at the Sexual Medicine Society Fall Meeting Press Release
Nov. 18 2005 National Institute of Diabetes and Digestive and Kidney Diseases
[1] Methods and compositions to enhance the efficacy of phosphodiesterase
inhibitors US PATENT APPLICATION NUMBER 20050009835
Avanafil, a PDE5 inhibitor, blocks the activity of a protein that
prevents blood vessels from expanding. According to the news,
avanafil is better at concentrating its activity on PDE5 than other
drugs in its class.
Examples of type V (5) phosphodiesterase inhibitors include, but not
limited to, sildenafil, tadalafil, vardenafil, avanafil, zaprinast RTM,
papaverine and dipyridamole. Other type 5 PDE inhibitors are
disclosed in PCT Publication Nos. WO 94/28902, WO 96/16644, U.S.
Pat. No. 6,338,862 and U.S. Pat. No. 6,476,037.
Avanafil's great advantage is that it acts faster than the other PDE5
inhibitors, taking effect in about 30 minutes, and disappears from the
body faster. Because of the fast action, those men who use it won't
have to wait as long.
Avanafil's relatively quick disappearance from the bloodstream should
lessen its possible side effects. In a study of 295 men, the
effectiveness was "excellent, while the side effects were minimal,
according to the news release.
WHAT ARE PDE INHIBITORS?
Phosphodiesterase (PDE) inhibitors are a class of intracelleular
enzymes which mediate the catabolism of second messengers like
cyclic adenosine monophosphate (cAMP) and cyclic guanosine
monophosphate (cGMP). These enzymes have been classified into at
least eleven groups (types I-XI) and various subclasses based on
their amino acid sequence and substrate specificity (Polson, 1996;
Trophy, 2000). The various PDE differ in their tissue, cellular
distribution, and their specificity towards cAMP or cGMP. (table 1). So
phosphodiesterase inhibitors have applications in a number of
disorders including vascular, neuronal and inflammatory disorders
(Zang 2002, Martin 2002, Grootendorst 2002, Burnouf, 2002). PDE
inhibitors are drug candidates for the treatment of a number of
disorders including heart failure, depression, asthma, inflammation,
sexual dysfunction, and erectile dysfunction. Phoshodiesterase 4D
has been shown to have a role in ischemic stroke (Gretarsdottir,
2003). [1]
WHAT ARE THE POTENTIAL APPLICATIONS OF Phosphodiesterase
PDE5 INHIBITORS?
1. Enhance sexual function in men following prostate surgery.
2. Enhance sexual function in hypogonadal men by combining
testosterone and phosphodiesterase inhibitor.
3. Treatment of premature or rapid ejaculation.
4. Enhance sexual function in women
5. Enhance endothelial function in patients with primary pulmonary
hypertension.
6. Treatment of urinary tract symptoms due to benign prostatic
hyperplasia.
7. Treatment of urinary incontinence.
8. Treatment of sickle cell anemia by combination therapy with
hydroxyurea
9. Enhance sexual function in men and women by combination
therapy with antioxidants, vitamin E, arginine, apomorphine ,
dopamine agonists, alpha adrenergic blocker etc.
10. Prevention and treatment of stroke.
11. Treatment of coronary and cerebral vascular diseases.
12. Treatment of thrombosis
13. Treatment of ocular hypertension
14. Treatment of pregnancy-induced hypertension.
15. Treatment of anal sphincter disorders (Jones, 2002).
16. Treatment of neurodegenerative diseases such as Alzheimer's
disease, Parkinson's disease, amyloid diseases, Prion diseases.
17. Treatment of other diseases where cGMP is implicated to have
beneficial effects.
WHAT ARE THE SIDE EFFECTS OF AVANAFIL?
Not much information has been reported about avanafil side effects.
In general, the side effects of Phosphodiesterase inhibitors include
hypotension, flushing, headache, nasal congestion and heartburn
and these effects are dose dependent (Moreira, 2000). The incidence
of cardiovascular events and deaths have been reported with the use
of PDE 5 inhibitors (Lim, 2002). This may be due to the fact that PDE5
inhibitors dilate the coronary arteries which makes the patient feel
better. This may lead to vigorous physical activity (exercise or
intercourse). Such activity may lead to ischemia and heart attack. Also
interaction with other drugs including nitroglycerine poses substantial
risks. The visual side effects of Phosphodiesterase 5 inhibitors are
due to the inhibition of Phosphodiesterase 6 found in the retina. [1]
ABOUT ERECTILE DYSFUNCTION
Erectile dysfunction, sometimes called "impotence," is the repeated
inability to get or keep an erection firm enough for sexual intercourse.
The word "impotence" may also be used to describe other problems
that interfere with sexual intercourse and reproduction, such as lack
of sexual desire and problems with ejaculation or orgasm. Using the
term erectile dysfunction makes it clear that those other problems are
not involved.
Erectile dysfunction can be a total inability to achieve erection, an
inconsistent ability to do so, or a tendency to sustain only brief
erections. These variations make defining erectile dysfunction and
estimating its incidence difficult. Estimates range from 15 million to 30
million, depending on the definition used. According to the National
Ambulatory Medical Care Survey (NAMCS), for every 1,000 men in the
United States, 7.7 physician office visits were made for erectile
dysfunction in 1985. By 1999, that rate had nearly tripled to 22.3.
The increase happened gradually, presumably as treatments such as
vacuum devices and injectable drugs became more widely available
and discussing erectile function became accepted. Perhaps the most
publicized advance was the introduction of the oral drug sildenafil
citrate (Viagra) in March 1998. NAMCS data on new drugs show an
estimated 2.6 million mentions of Viagra at physician office visits in
1999, and one-third of those mentions occurred during visits for a
diagnosis other than erectile dysfunction.
In older men, erectile dysfunction usually has a physical cause, such
as disease, injury, or side effects of drugs. Any disorder that causes
injury to the nerves or impairs blood flow in the penis has the
potential to cause erectile dysfunction . Incidence increases with
age: About 5 percent of 40-year-old men and between 15 and 25
percent of 65-year-old men experience erectile dysfunction . But it is
not an inevitable part of aging.
ABOUT VIVUS INC.
VIVUS, Inc. was founded in 1991 by Virgil A. Place, M.D., to research,
develop and commercialize therapies to restore male sexual function.
VIVUS' first product, MUSE®, was based on the discovery that
certain vasodilating agents, some of which are used to treat
hypertension, can be applied in the urethra and absorbed into the
erectile tissues, causing an erection in males. Today, VIVUS continues
to develop innovative therapies to restore male sexual function and is
at the forefront of pioneering therapies for women's sexual health.
THIS ARTICLE IS FOR YOUR REFERENCE ONLY. YOU SHOULD CONSULT WITH
YOUR DOCTOR IF YOU HAVE ANY MEDICAL PROBLEMS. YOU SHOULD
CONSULT WITH YOUR INVESTMENT ADVISOR, BEFORE ANY TRANSACTION.
YOU SHOULD CONSULT WITH A SCIENTIST IF YOU ARE DEVELOPING A
RELATED PRODUCT. PUBLISHER DOES NOT GUARANTEE THE ACCURACY OF
THIS ARTICLE. ALL RIGHT RESERVED 2005 zhion inc. DO NOT COPY NOR
TRANSFER TO OTHER WEBSITES OR OTHER TYPES OF PUBLICATIONS.
SOURCES VIVUS Announces Presentation of Positive Results From Five Key
Avanafil Studies at the Sexual Medicine Society Fall Meeting Press Release
Nov. 18 2005 National Institute of Diabetes and Digestive and Kidney Diseases
[1] Methods and compositions to enhance the efficacy of phosphodiesterase
inhibitors US PATENT APPLICATION NUMBER 20050009835
| AVANAFIL POTENTIAL BENEFITS Avanafil (made by Vivus Inc.) may be a potentially faster-acting competitor on the horizon for Viagra (and Levitra and Cialis) in the battle against impotence. It could be marketed by about 2007, if it can enter the Phase III study next year. |
PHARMCEUTICAL
INDUSTRY
Foundamental
Science
Colloidal
Stabilization
Drug Product
Development
Patent Application
Product
Development
Product
Ingredients
Colorant
Scale up a batch 1
Drug Delivery
Industry
Drug Delivery -
Smart Bomb
Lotion, Cream,
Preps
Enteric
Coating-Eudragit
Enteric
Coating-Nutrateric
SR
Coating-Aquacoat
Drug Industry
Drug
Competitions
Drug in
Development
Cholesterol-loweri
ng
Drug-Terminologi
es
Packaging
Materials
Market
Drug Dev- 2004
Drug Dev -
2005Q1
Drug Dev- 2005Q2
Drug
Dev-2005Summer
Drug Dev-2005Q3
Orphan Drug
Protein Drug
Niche Market
Novo Norkdisk
R&D
Equipment
Blenders
CONTRACT
MANUFACT.
Nutrition
Supplements
NEW DRUGS
Arranon
Actoplus Met
Alfuzosin
Ambien CR
Avastin
Asmanex(R)
Erbitux
(cetuximab)
Gardasil
GRN163
Herceptin
Increlex (rhIGF-1)
Lidoerm
(Lidocaine)
Liraglutide
Lyrica (pregabalin)
Rozerem
Sorafenib
Sutent
Tamsulosin
Torcetrapib
Zometa
OLD DRUGS
Lithium Carbonate
DRUG NOTES
[CONSTRUCT]
Clinical Research
Terminologies
FDA ALERTS
Protein Drug
Market
Niche Market
Orphan Drug
levothyroxine
Protein Drug 1
Protein Drug2
Double-blind
Study
INDUSTRY
Foundamental
Science
Colloidal
Stabilization
Drug Product
Development
Patent Application
Product
Development
Product
Ingredients
Colorant
Scale up a batch 1
Drug Delivery
Industry
Drug Delivery -
Smart Bomb
Lotion, Cream,
Preps
Enteric
Coating-Eudragit
Enteric
Coating-Nutrateric
SR
Coating-Aquacoat
Drug Industry
Drug
Competitions
Drug in
Development
Cholesterol-loweri
ng
Drug-Terminologi
es
Packaging
Materials
Market
Drug Dev- 2004
Drug Dev -
2005Q1
Drug Dev- 2005Q2
Drug
Dev-2005Summer
Drug Dev-2005Q3
Orphan Drug
Protein Drug
Niche Market
Novo Norkdisk
R&D
Equipment
Blenders
CONTRACT
MANUFACT.
Nutrition
Supplements
NEW DRUGS
Arranon
Actoplus Met
Alfuzosin
Ambien CR
Avastin
Asmanex(R)
Erbitux
(cetuximab)
Gardasil
GRN163
Herceptin
Increlex (rhIGF-1)
Lidoerm
(Lidocaine)
Liraglutide
Lyrica (pregabalin)
Rozerem
Sorafenib
Sutent
Tamsulosin
Torcetrapib
Zometa
OLD DRUGS
Lithium Carbonate
DRUG NOTES
[CONSTRUCT]
Clinical Research
Terminologies
FDA ALERTS
Protein Drug
Market
Niche Market
Orphan Drug
levothyroxine
Protein Drug 1
Protein Drug2
Double-blind
Study
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