MDF topical from Samson Therapeutics

Uh oh, Ron. Now you’ve done it. Prepare for the public flogging to come:-D

I take it that you have not been here before. You MUST see things from our perspective. We get BOMBARDED by magic lotions and potions claiming to be the “next” generation hair loss treatment and NOT ONE has ever come to fruition.

Secondly, you don’t EVER mess with Bryan when it comes to medical literature. He knows more about it than anyone here (including ALL of the doctors who frequent this site). It is just like messing with Texas - it aint done!

» 2. You seem to have contradictory views about effectiveness. You
» (correctly) state that flutamide has shown a systemic effect, but then
» you assert that no local effect can be assumed without clinical studies.
» However, normal pharmacokinetic partitioning requires a drug to traverse
» the dermis (where the hair follicles reside) and cumulate a significant
» concentration there before it can pass into the systemic circulation.
» Therefore, a drug that demonstrates a systemic effect MUST have a local
» effect, if there are susceptible receptors there.

I’m going to explain to you EXACTLY what I mean by a “local” effect, so that there can be no further misunderstanding: when a drug has the intended effect ONLY where it is physically applied and not in any other location, then that is a “local” effect. Take a look at the following graph which is a part of the Chen et al topical flutamide study which I cited in my previous post:

As you can see, they applied three different doses of flutamide ONLY to the right flank organs of the hamsters, while the left flank organs received only a control vehicle without the drug. But both flank organs were reduced IDENTICALLY by the flutamide, and at all three doses!! Clearly, the flutamide was getting absorbed systemically, and then got spread to both flank organs through the bloodstream (and notice that the same thing happened with the topical finasteride). There was no “local” effect at all. And the other topical flutamide study from 1975, which I previously cited, had a similar result.

As I said in my other post, the Sintov study is the only one I know of which claimed to find a “local” effect from the topical application of flutamide, but I find it to be less than fully persuasive. I think it’s rather strange that you and your company would go to so much time and trouble to develop a very expensive product based (mostly) on such rather flimsy evidence as the Sintov study (and I’ll add here that any evidence for using topical dutasteride is ENTIRELY absent from the medical literature).

.

» » 2. You seem to have contradictory views about effectiveness. You
» » (correctly) state that flutamide has shown a systemic effect, but then
» » you assert that no local effect can be assumed without clinical
» studies.
» » However, normal pharmacokinetic partitioning requires a drug to
» traverse
» » the dermis (where the hair follicles reside) and cumulate a significant
» » concentration there before it can pass into the systemic circulation.
» » Therefore, a drug that demonstrates a systemic effect MUST have a local
» » effect, if there are susceptible receptors there.
»
» I’m going to explain to you EXACTLY what I mean by a “local” effect, so
» that there can be no further misunderstanding: when a drug has the
» intended effect ONLY where it is physically applied and not in any other
» location, then that is a “local” effect. Take a look at the following
» graph which is a part of the Chen et al topical flutamide study
» which I cited in my previous post:
»
» ImageShack - Best place for all of your image hosting and image sharing needs
»
» As you can see, they applied three different doses of flutamide ONLY to
» the right flank organs of the hamsters, while the left flank organs
» received only a control vehicle without the drug. But both flank organs
» were reduced IDENTICALLY by the flutamide, and at all three doses!!
» Clearly, the flutamide was getting absorbed systemically, and then got
» spread to both flank organs through the bloodstream (and notice that the
» same thing happened with the topical finasteride). There was no “local”
» effect at all. And the other topical flutamide study from 1975, which I
» previously cited, had a similar result.
»
» As I said in my other post, the Sintov study is the only one I know of
» which claimed to find a “local” effect from the topical application of
» flutamide, but I find it to be less than fully persuasive. I think it’s
» rather strange that you and your company would go to so much time and
» trouble to develop a very expensive product based (mostly) on such rather
» flimsy evidence as the Sintov study (and I’ll add here that any evidence
» for using topical dutasteride is ENTIRELY absent from the medical
» literature).

Bryan,

I don’t see where we disagree. Flutamide has a systemic effect, end of story. But in biological systems, dose is everything. At doses used in dermatologic practice, the distal response has not been demonstrated at the doses used. For example, women taking oral doses of Flutamide at 250 mg or less do not manifest changes in fertility, sexual function or elevated liver function tests, which are the hallmarks of flutamide toxicity–and those systemically absorbed levels are 25 times what we see with topical administration (@62.5 mg).

RonLev

» .

» Bryan,
»
» I don’t see where we disagree. Flutamide has a systemic effect, end of
» story. But in biological systems, dose is everything. At doses used in
» dermatologic practice, the distal response has not been demonstrated at
» the doses used.

If I’m understanding you correctly, I think you’re grossly misusing the term “distal response” here! :no:

In the context of whether or not an antiandrogenic drug has a “local” effect where applied topically, flutamide has been demonstrated NOT to have any local effect in most of the existing studies; only in the (questionable?) Sintov study has there been a claim to the contrary.

What you seem to be talking about above is something entirely different, though, which is whether or not you can get a decent antiandrogenic effect from flutamide without nasty side effects of other kinds, REGARDLESS of how you get the flutamide inside you. If that’s really all you’re claiming here, and you’re admitting that flutamide will inevitably go systemic regardless of how you apply it, then there’s no particular reason to use it topically. You might as well just go ahead and SWALLOW it! :wink:

Certain other antiandrogens do in fact have local effects, though. Two obvious examples are spironolactone and RU58841. When those antiandrogens are applied to only one hamster flank organ, ONLY that one flank organ is affected. The other one on the other side isn’t. In other words, there is no “distal response” at the site of the other flank organ, antiandrogenic or otherwise.

» For example, women taking oral doses of Flutamide at 250 mg or
» less do not manifest changes in fertility, sexual function or elevated
» liver function tests, which are the hallmarks of flutamide toxicity–and
» those systemically absorbed levels are 25 times what we see with topical
» administration (@62.5 mg).

Well, there you go: so are you really admitting that topical flutamide (even when used in the form of your new product) has no local effect at all, and it’s entirely systemic?? What exactly is the point of using it topically in the first place?? Why not just go ahead and swallow the proper dose of flutamide? :slight_smile:

.

» » Bryan,
» »
» » I don’t see where we disagree. Flutamide has a systemic effect, end of
» » story. But in biological systems, dose is everything. At doses used
» in
» » dermatologic practice, the distal response has not been demonstrated at
» » the doses used.
»
» If I’m understanding you correctly, I think you’re grossly misusing the
» term “distal response” here! :no:
»
» In the context of whether or not an antiandrogenic drug has a “local”
» effect where applied topically, flutamide has been demonstrated NOT to have
» any local effect in most of the existing studies; only in the
» (questionable?) Sintov study has there been a claim to the contrary.
»
» What you seem to be talking about above is something entirely different,
» though, which is whether or not you can get a decent antiandrogenic effect
» from flutamide without nasty side effects of other kinds, REGARDLESS of how
» you get the flutamide inside you. If that’s really all you’re claiming
» here, and you’re admitting that flutamide will inevitably go
» systemic regardless of how you apply it, then there’s no particular reason
» to use it topically. You might as well just go ahead and SWALLOW it! :wink:
»
» Certain other antiandrogens do in fact have local effects, though. Two
» obvious examples are spironolactone and RU58841. When those antiandrogens
» are applied to only one hamster flank organ, ONLY that one flank organ is
» affected. The other one on the other side isn’t. In other words, there is
» no “distal response” at the site of the other flank organ, antiandrogenic
» or otherwise.
»
» » For example, women taking oral doses of Flutamide at 250 mg or
» » less do not manifest changes in fertility, sexual function or elevated
» » liver function tests, which are the hallmarks of flutamide
» toxicity–and
» » those systemically absorbed levels are 25 times what we see with
» topical
» » administration (@62.5 mg).
»
» Well, there you go: so are you really admitting that topical flutamide
» (even when used in the form of your new product) has no local effect at
» all, and it’s entirely systemic?? What exactly is the point of using it
» topically in the first place?? Why not just go ahead and swallow
» the proper dose of flutamide? :slight_smile:
»
»

Bryan,

It appears that you stand, on principle, that any drug that is systemically absorbed would make topical application worthless since, as you say “you might as well just take it orally” and be done with it. However, that flies in the face of standard dermatologic practice. Drugs in multiple therapeutic classes (all manifesting systemtic absorption) are compounded in topical formulations to concentrate the effect at the point of application. For example, topical corticosteroids all manifest systemic absorption, but dermatologists use topical formulations because they can use lower doses and still obtain effectiveness in the skin (for treating eczema, allergic dermatitis, etc.), GRANTED that some of the steroids will be systemtically absorbed. The same applies to topical antibiotics, et al.

RonLev

I used topical flutamide gel (and NOT MUCH EITHER) for one week once. I had the limp noodle in three days, and no sex drive for the last four days WHATSOEVER. I felt nauseous, had diarreah (every time I went), didn’t feel like working out…in other words, I felt like shiiiit.

This is why topical dutasteride and topical finasteride forumlations need to measure the SERUM LEVELS OF DHT in TESTING before being ALLOWED to be sold. Nobody knows how much is sytemically absorbed. Ive been on finas a long time and can handle it, but obviously a few men really have unpleasant side effects. Flutamide, which can basically chemically block your very manhood, isn’t something to fool with if you want a high quality of life. Unless some entity can perform a big test in humans and prove their topical forulation isn’t sytstemically absorbed…why in the hell would they sell the stuff?

» Bryan,
»
» It appears that you stand, on principle, that any drug that is
» systemically absorbed would make topical application worthless since, as
» you say “you might as well just take it orally” and be done with it.
» However, that flies in the face of standard dermatologic practice. Drugs
» in multiple therapeutic classes (all manifesting systemtic absorption) are
» compounded in topical formulations to concentrate the effect at the point
» of application. For example, topical corticosteroids all manifest systemic
» absorption, but dermatologists use topical formulations because they can
» use lower doses and still obtain effectiveness in the skin (for treating
» eczema, allergic dermatitis, etc.), GRANTED that some of the steroids will
» be systemtically absorbed. The same applies to topical antibiotics, et
» al.

Did you miss the whole point of my previous posts? I demonstrated to you with the graph from the Chen et al study that the effect of the topical flutamide was absolutely, positively NOT concentrated at the point of application. I took pains to point out that the results on both flank organs were IDENTICAL, even though the drug was applied only to one flank organ. Now do you understand the point that I’ve been making all along? The flutamide was acting in those rodent studies EXCLUSIVELY by a systemic route.

.

» » Bryan,
» »
» » It appears that you stand, on principle, that any drug that is
» » systemically absorbed would make topical application worthless since,
» as
» » you say “you might as well just take it orally” and be done with it.
» » However, that flies in the face of standard dermatologic practice.
» Drugs
» » in multiple therapeutic classes (all manifesting systemtic absorption)
» are
» » compounded in topical formulations to concentrate the effect at the
» point
» » of application. For example, topical corticosteroids all manifest
» systemic
» » absorption, but dermatologists use topical formulations because they
» can
» » use lower doses and still obtain effectiveness in the skin (for
» treating
» » eczema, allergic dermatitis, etc.), GRANTED that some of the steroids
» will
» » be systemtically absorbed. The same applies to topical antibiotics, et
» » al.
»
» Did you miss the whole point of my previous posts? I demonstrated to you
» with the graph from the Chen et al study that the effect of the
» topical flutamide was absolutely, positively NOT concentrated at the point
» of application. I took pains to point out that the results on both flank
» organs were IDENTICAL, even though the drug was applied only to one flank
» organ. Now do you understand the point that I’ve been making all along?
» The flutamide was acting in those rodent studies EXCLUSIVELY by a systemic
» route.
»
» Likewise, you are missing my point; I am not concerned about systemic activity at the flank organ–I already acknowledged that flutamide is systemically absorbed. What a dermatologist wants to know is: what is the activity of flutamide at the skin site of administration and what happens to that activity in the skin when the dose is titrated downward so that systemic activity is extinguished? (That was not the objective of Chen’s experiment.)

RonLev

» I used topical flutamide gel (and NOT MUCH EITHER) for one week once. I had
» the limp noodle in three days, and no sex drive for the last four days
» WHATSOEVER. I felt nauseous, had diarreah (every time I went), didn’t feel
» like working out…in other words, I felt like
» shiiiit.
»
»
»
» This is why topical dutasteride and topical finasteride forumlations need
» to measure the SERUM LEVELS OF DHT in TESTING before being ALLOWED to be
» sold. Nobody knows how much is sytemically absorbed. Ive been on finas a
» long time and can handle it, but obviously a few men really have unpleasant
» side effects. Flutamide, which can basically chemically block your very
» manhood, isn’t something to fool with if you want a high quality of life.
» Unless some entity can perform a big test in humans and prove their topical
» forulation isn’t sytstemically absorbed…why in the
» hell would they sell the stuff?

Benji,

It is regrettable that you experienced sexual side effects from topical dutasteride and finasteride. However, no drug is perfect and I don’t claim otherwise. Every drug presents a profile of desired and undesirable effects; it is how the balance tips in one direction or the other that occurs in each particular patient that determines whether it is worthwhile. It is important to note that GSk admits in its information for healthcare professionals statement that Avodart®–a fully FDA-approved oral version of dutasteride–has detectable side effects (including sexual dysfunction) in many patients taking it and significant sexual side effects in 4.7% of patients (although it does decline to 1% after 12 months, if one can tolerate the waiting time). Is this unusual? Should Avodart (and our topical preparation) be taken off the market? No. Because ALL drugs have risk/benefits. If you are looking for a perfect drug for hair loss, or hypertension, or cholesterol, or whatever–it just doesn’t exist. I wish I could advise you of a better solution now. Hopefully, in the future a nonpharmaceutical treatment for hair loss will make this discussion unnecessary, such as hair cloning.

RonLev

» » Did you miss the whole point of my previous posts?
» » I demonstrated to you with the graph from the Chen
» » et al study that the effect of the topical
» » flutamide was absolutely, positively NOT concentrated
» » at the point of application. I took pains to point out
» » that the results on both flank organs were IDENTICAL,
» » even though the drug was applied only to one flank organ.
» » Now do you understand the point that I’ve been making all along?
» » The flutamide was acting in those rodent studies EXCLUSIVELY
» » by a systemic route.
»
» Likewise, you are missing my point; I am not concerned about systemic
» activity at the flank organ–I already acknowledged that flutamide is
» systemically absorbed. What a dermatologist wants to know is: what is the
» activity of flutamide at the skin site of administration and what happens
» to that activity in the skin when the dose is titrated downward so that
» systemic activity is extinguished? (That was not the objective of Chen’s
» experiment.)

Ahhh…but that was an objective of Chen’s experiment! :wink: I think now you’re also beginning to understand why I made such a big point before of the fact that Chen et al tested THREE separate doses: a large dose which strongly reduced flank organ size (identical effect on both sides); a medium dose which moderately reduced flank organ size (identical effect on both sides); and a small dose which had only a very minimal effect on flank organ size (identical effect on both sides).

Sorry about pressing you on all this, but there’s just no way to put a favorable “spin” of any kind on the animal experiments with topical flutamide. They demonstrate that (1) topical flutamide works EXCLUSIVELY by a systemic route, and (2) titrating the dose up or down doesn’t alter the systemic nature of how it works.

The animal experiments are clearly DISASTROUS for anybody who wants to develop a topical flutamide product for human use. Any rationale one can conjure up for how such a product might be great for humans is soundly contradicted by the results of these animal experiments (with the possible exception of the Sintov study, as I explained before). All you can do now is hope against hope that topical flutamide works by some substantially different mechanism in humans than it does in rodents; and frankly, I consider that to be a pretty weak foundation on which to develop a new product for human use. It doesn’t inspire one with confidence.

.

Topical FLUTAMIDE gave me the limp noodle, diarreah, and no energy, and no sex drive.

RonLev has tried to spin this and accuse to other drugs. I smell dishonesty. Be sure I will check back here again and again and remind others that the quickest path to no erections is TOPICAL or INTERNAL flutamide.

» » » Did you miss the whole point of my previous posts?
» » » I demonstrated to you with the graph from the Chen
» » » et al study that the effect of the topical
» » » flutamide was absolutely, positively NOT concentrated
» » » at the point of application. I took pains to point out
» » » that the results on both flank organs were IDENTICAL,
» » » even though the drug was applied only to one flank organ.
» » » Now do you understand the point that I’ve been making all along?
» » » The flutamide was acting in those rodent studies EXCLUSIVELY
» » » by a systemic route.
» »
» » Likewise, you are missing my point; I am not concerned about systemic
» » activity at the flank organ–I already acknowledged that flutamide is
» » systemically absorbed. What a dermatologist wants to know is: what is
» the
» » activity of flutamide at the skin site of administration and what
» happens
» » to that activity in the skin when the dose is titrated downward so that
» » systemic activity is extinguished? (That was not the objective of
» Chen’s
» » experiment.)
»
» Ahhh…but that was an objective of Chen’s experiment! :wink: I think now
» you’re also beginning to understand why I made such a big point before of
» the fact that Chen et al tested THREE separate doses: a large
» dose
which strongly reduced flank organ size (identical effect on both
» sides); a medium dose which moderately reduced flank organ size
» (identical effect on both sides); and a small dose which had only a
» very minimal effect on flank organ size (identical effect on both sides).
»
» Sorry about pressing you on all this, but there’s just no way to put a
» favorable “spin” of any kind on the animal experiments with topical
» flutamide. They demonstrate that (1) topical flutamide works EXCLUSIVELY
» by a systemic route, and (2) titrating the dose up or down doesn’t alter
» the systemic nature of how it works.
»
» The animal experiments are clearly DISASTROUS for anybody who wants to
» develop a topical flutamide product for human use. Any rationale one can
» conjure up for how such a product might be great for humans is soundly
» contradicted by the results of these animal experiments (with the possible
» exception of the Sintov study, as I explained before). All you can do now
» is hope against hope that topical flutamide works by some substantially
» different mechanism in humans than it does in rodents; and frankly, I
» consider that to be a pretty weak foundation on which to develop a new
» product for human use. It doesn’t inspire one with confidence.
»
» Bryan,

I appreciate your spirited and scientifically rigorous rebuttals. I would only add as a coda to this discussion that many drugs in this field (and I am including ALL hormonal modulators in this discussion, not just antiandrogens for treatment of hair disorders) are developed with an acknowledgement of some risk as a part of their side effect profile. As I mentioned in response to Benji’s unfortunate experience with finasteride and dutasteride, even well-established, fully FDA-approved drugs will not pass muster by your standard. That is not to say that your standard is wrong, it is just that the state of the art currently puts us in a position where antiandrogenic control cannot be absolutely locally restricted. If you want truly effective control of DHT in the here-and-now, this is the risk that patients and their doctors must weigh, and for most the benefits outweigh the risks.

RonLev

» » Bryan,
»
». As I
» mentioned in response to Benji’s unfortunate experience with finasteride
» and dutasteride, even well-established, fully FDA-approved drugs will not
» pass muster by your standard. BENJI HAS BEEN ON FINASTERIDE FOR 12 YEARS WITH NO PROBLEM. FLUTAMIDE TOPICALLY IS WHAT GAVE HIM NO ERECTIONS, NAUSEA, NO SEX DRIVE, DIARREAH, and you know this…youre simply lying as Ive pointed it out to you the FIRST time you tried to intentionally misinterpret what I clearly stated and blame finasteride…

That is not to say that your standard is
» wrong, it is just that the state of the art currently puts us in a position
» where antiandrogenic control cannot be absolutely locally restricted. If
» you want truly effective control of DHT in the here-and-now, this is the
» risk that patients and their doctors must weigh, and for most the benefits
» outweigh the risks. OF DUTASTERIDE, MAYBE. NOT FLUTAMIDE. You are worried about sales of your product, most people who buy it will only use it a month or two and stop because of the FLUTAMIDE side effects. You should have tried to formulate topical dutasteride and minoxidil along with some topical ketoconazole and the sides would have been small enough for many to keep with it. The FLUTAMIDE sides will make them quit. They will feel like shiiiit. Furthermore, Flutamide probably has to be metabolized to even work directly as Docjo77 has pointed out at HLT. »

The makers of finasteride (MERK) and Dutasteride (Glaxo-Smith-Kline) do not claim that their drugs work by any other means than systemic absorption. They do not sell topical forumlations thereof. No tests anywhere have suggested that these drugs can be used topically and be useful unless serum levels of DHT are also affected by the makers. Some claim that finasteride can be suspended topically in the right vehicle, but its never been proven. Nobody that I know of claims that for dutasteride, but even if it worked, one could just drain dutasteride capsules in a bottle of minoxidil and get the same effect. If you think you have a topical vehicle that can suspend dutasteride topically where it does not cross into the bloodstream and only has local effects, commission a study and treat AGA topically with it and show no serum changes in DHT. But you dont and we both know it.

You are trying to turn a buck on people’s ignorance. Im trying to save men from a pretty miserable month or so of life…which they will have if they use flutamide topically.

» » » Bryan,
» »
» ». As I
» » mentioned in response to Benji’s unfortunate experience with
» finasteride
» » and dutasteride, even well-established, fully FDA-approved drugs will
» not
» » pass muster by your standard. BENJI HAS BEEN ON
» FINASTERIDE FOR 12 YEARS WITH NO PROBLEM. FLUTAMIDE TOPICALLY IS WHAT GAVE
» HIM NO ERECTIONS, NAUSEA, NO SEX DRIVE, DIARREAH, and you know
» this…youre simply lying as Ive pointed it out to you the FIRST
» time you tried to intentionally misinterpret what I clearly stated and
» blame finasteride…

»
» That is not to say that your standard is
» » wrong, it is just that the state of the art currently puts us in a
» position
» » where antiandrogenic control cannot be absolutely locally restricted.
» If
» » you want truly effective control of DHT in the here-and-now, this is
» the
» » risk that patients and their doctors must weigh, and for most the
» benefits
» » outweigh the risks. OF DUTASTERIDE, MAYBE. NOT
» FLUTAMIDE. You are worried about sales of your product, most people who buy
» it will only use it a month or two and stop because of the FLUTAMIDE side
» effects. You should have tried to formulate topical dutasteride and
» minoxidil along with some topical ketoconazole and the sides would have
» been small enough for many to keep with it. The FLUTAMIDE sides will make
» them quit. They will feel like shiiiit. Furthermore, Flutamide probably has
» to be metabolized to even work directly as Docjo77 has pointed out at HLT.
»
»
»
»
»
»
» The makers of finasteride (MERK) and Dutasteride
» (Glaxo-Smith-Kline) do not claim that their drugs work by any other means
» than systemic absorption. They do not sell topical forumlations thereof. No
» tests anywhere have suggested that these drugs can be used topically and be
» useful unless serum levels of DHT are also affected by the makers. Some
» claim that finasteride can be suspended topically in the right vehicle, but
» its never been proven. Nobody that I know of claims that for dutasteride,
» but even if it worked, one could just drain dutasteride capsules in a
» bottle of minoxidil and get the same effect. If you think you have a
» topical vehicle that can suspend dutasteride topically where it does not
» cross into the bloodstream and only has local effects, commission a study
» and treat AGA topically with it and show no serum changes in DHT. But you
» dont and we both know it.

»
»
»
» You are trying to turn a buck on people’s ignorance. Im trying to save men
» from a pretty miserable month or so of life…which they will
» have if they use flutamide topically.

Benji,

Hold your horses. I never claimed that MDF was not systemically absorbed. The point I want to make is that your treatment with these FDA-approved products by Glaxo TAKEN AS DIRECTED was responsible for significant sexual side effects, yet you direct all of your criticism at MDF. The one claim we can make (aside from the development of a stable solution of these components, which was quite difficult) is that the systemic exposure of these components is lower with MDF than with oral doseforms (10.3 mg of flutamide topically vs. 62.5 mg orally; and 0.25 mg of dutasteride vs. 0.5 mg orally). One issue that mystifies me is why you obsess over flutamide when, on a dose-response basis, there is a greater likelihood of experiencing sexual side effects from dutasteride (since both agents are in MDF, I can comment on this issue without bias).

I regret that you had such a poor experience with dutasteride (and finasteride, as you noted earlier). While you appear to be quite sensitive to antiandrogens, others who have less sensitivity may experience fewer side effects from MDF. Notice I said “may”, not “will”.

RonLev

Three Time Ron Lev has tried to claim I had bad experiences with dutasteride/finasteride. Ive had no bad experiences with either and have used finasteride internally for more than a decade.

I had a bad experiment with TOPICAL FLUTAMIDE, which he is putting in his topical

Finasteride has never given me any problems whatsoever.

Im not going anywhere Ron, and since youve pissed me off by lying about what Ive stated three times now…I’ll be sure to stay right at it right here. I’ll check back every couple of days.

Flutamide is systemically abosorbed, and probably would not work unless it IS SYSTEMICALLY absorbed and metabolized anyway.

And one more thing…you are a liar, dont think that people who have followed this board for many many years will take your word over mine.

Let me shine in since I am the only person on these boards taking DUT (oral, 0.5mg a day for 4 years) and topical Flutamide (1% Flutagel) at the same time.
According to what I noticed in my own human test on myself…flutamide works great to stop aggressive hairloss and does work topically.
I noticed very clearly that hair was getting thicker, darker and growing faster at the hairline and shedding stopped, and this after only 3 weeks of daily application.
I even took pics & made many posts about this on the other forums (same ID).

Absolutely no libido effects were noticed at that time and up to until 2.5 months after starting the treatement.
I did not have major, constant libido issues on oral DUT 0.5mg a day except for a few weeks when I started.
Never had anything on FIN (previous 6 years)

Now, at the 2.5 months mark on Flutamide, libido has cleary taken a hit, in a constant manner over the day.

My personnal conclusion is that a small amount of Flutmide is systemically absorbed everyday and this BUILDS UP everyday until the amount is such that it starts to influences libido.
This amount varies from person to person.
Flutamide has a very short half-life, so when I stopped using it for 2-3 days the libido improved.

My feedback to Ron Lev: unfortunalty there is a high possibility that many users will have severe libido issues due to Flutamide AFTER SOME TIME, but if they decrease the dosage/frequency, libido should come back fairly quickly.

» Bryan,
»
» I appreciate your spirited and scientifically rigorous rebuttals. I
» would only add as a coda to this discussion that many drugs in this field
» (and I am including ALL hormonal modulators in this discussion, not just
» antiandrogens for treatment of hair disorders) are developed with an
» acknowledgement of some risk as a part of their side effect profile. As I
» mentioned in response to Benji’s unfortunate experience with finasteride
» and dutasteride, even well-established, fully FDA-approved drugs will not
» pass muster by your standard. That is not to say that your standard is
» wrong, it is just that the state of the art currently puts us in a position
» where antiandrogenic control cannot be absolutely locally restricted. If
» you want truly effective control of DHT in the here-and-now, this is the
» risk that patients and their doctors must weigh, and for most the benefits
» outweigh the risks.

I must take issue with your claim that “even well-established, fully FDA-approved drugs will not pass muster” by my standard. I’m astonished that you would try to take some of the heat off (topical) flutamide by implying that all other antiandrogens are going to have similar risks with systemic absorption. But such is not the case! :stuck_out_tongue: I’m sure you’re aware that topical spironolactone has been thoroughly tested in both animals and humans, and been found to have no detectable systemic absorption (one study applied a spiro cream to literally HALF the entire body surface area of some human test subjects, with no ill effects). Topical spiro may not be all that powerful an antiandrogen, but one feature it does have that topical flutamide apparently doesn’t is that all-important “local” antiandrogenic effect.

And what about topical RU58841?? That substance has been thoroughly tested in animals (and at least privately in humans), and probably has the greatest ratio of local-to-sytemic antiandrogenic effect of any substance ever discovered. It has NO known risk of a systemic antiandrogenic effect when applied topically, yet has a very potent “local” effect which has been described as “castration-like” in some of the animal studies.

So I think you’re being rather disingenuous by trying to make us believe that all other antiandrogens are going to have the same issues and problems as flutamide, when used topically. But that is clearly NOT the case. When anybody makes an objective comparison of the animal studies with flutamide and the animal studies with (say) RU58841, a huge gulf is seen to exist between the two which stretches out like the Grand Canyon. And yet you’re trying to convince us that your new flutamide product is going to be about as good as one can get with the current state of the art. I don’t believe that, and I doubt that very many other people believe it, either. The difference between flutamide and RU58841 (at the very least in the animal studies, and that carries a LOT of weight with me) is like the difference between day and night.

.

» » Bryan,
» »
» » I appreciate your spirited and scientifically rigorous rebuttals. I
» » would only add as a coda to this discussion that many drugs in this
» field
» » (and I am including ALL hormonal modulators in this discussion, not
» just
» » antiandrogens for treatment of hair disorders) are developed with an
» » acknowledgement of some risk as a part of their side effect profile. As
» I
» » mentioned in response to Benji’s unfortunate experience with
» finasteride
» » and dutasteride, even well-established, fully FDA-approved drugs will
» not
» » pass muster by your standard. That is not to say that your standard
» is
» » wrong, it is just that the state of the art currently puts us in a
» position
» » where antiandrogenic control cannot be absolutely locally restricted.
» If
» » you want truly effective control of DHT in the here-and-now, this is
» the
» » risk that patients and their doctors must weigh, and for most the
» benefits
» » outweigh the risks.
»
» I must take issue with your claim that “even well-established, fully
» FDA-approved drugs will not pass muster” by my standard. I’m astonished
» that you would try to take some of the heat off (topical) flutamide by
» implying that all other antiandrogens are going to have similar risks with
» systemic absorption. But such is not the case! :stuck_out_tongue: I’m sure you’re aware
» that topical spironolactone has been thoroughly tested in both animals and
» humans, and been found to have no detectable systemic absorption (one study
» applied a spiro cream to literally HALF the entire body surface area of
» some human test subjects, with no ill effects). Topical spiro may not be
» all that powerful an antiandrogen, but one feature it does have that
» topical flutamide apparently doesn’t is that all-important “local”
» antiandrogenic effect.
»
» And what about topical RU58841?? That substance has been thoroughly
» tested in animals (and at least privately in humans), and probably has the
» greatest ratio of local-to-sytemic antiandrogenic effect of any substance
» ever discovered. It has NO known risk of a systemic antiandrogenic effect
» when applied topically, yet has a very potent “local” effect which has been
» described as “castration-like” in some of the animal studies.
»
» So I think you’re being rather disingenuous by trying to make us believe
» that all other antiandrogens are going to have the same issues and problems
» as flutamide, when used topically. But that is clearly NOT the case. When
» anybody makes an objective comparison of the animal studies with flutamide
» and the animal studies with (say) RU58841, a huge gulf is seen to exist
» between the two which stretches out like the Grand Canyon. And yet you’re
» trying to convince us that your new flutamide product is going to be about
» as good as one can get with the current state of the art. I don’t believe
» that, and I doubt that very many other people believe it, either. The
» difference between flutamide and RU58841 (at the very least in the animal
» studies, and that carries a LOT of weight with me) is like the difference
» between day and night.
»
» Bryan,

In studies directly comparing spironolactone and flutamide,flutamide has been shown to be a more potent antiandrogen (Moghetti, P: J. Clin. Endocrinol. Metab. 85(1) 2000). But more importantly from a practical perspective, spironolactone has an objectionable odor especially when combined with minoxdil and requires a viscid base to remain stable in solution. This imposes a dilemma on patients: they must either tolerate the odor or messyness (most do not) or separate the spironolatone application from the minoxidil application–a ritual that quickly becomes too bothersome for the patient, who eventually looks for another type of treatment.

RU58841 is a wonderful drug that will never see the light of day because of the disinterest of Roussel Uclaf (now a part of Aventis) to pursue the expense of an FDA approval. (Compounders don’t need an FDA approval for hair loss, but we are legally bound to use components that are FDA approved for some legitimate indication.)

Bryan, of course we looked at alternatives that you consider worthy, and there is a reason why we rejected them.

RonLev

» Let me shine in since I am the only person on these boards taking DUT
» (oral, 0.5mg a day for 4 years) and topical Flutamide (1% Flutagel) at
» the same time.
» According to what I noticed in my own human test on myself…flutamide
» works great to stop aggressive hairloss and does work topically.
» I noticed very clearly that hair was getting thicker, darker and growing
» faster at the hairline and shedding stopped, and this after only 3 weeks of
» daily application.
» I even took pics & made many posts about this on the other forums (same
» ID).
»
» Absolutely no libido effects were noticed at that time and up to until 2.5
» months after starting the treatement.
» I did not have major, constant libido issues on oral DUT 0.5mg a day
» except for a few weeks when I started.
» Never had anything on FIN (previous 6 years)
»
» Now, at the 2.5 months mark on Flutamide, libido has cleary taken a hit,
» in a constant manner over the day.
»
El Duterino,

» My personnal conclusion is that a small amount of Flutmide is systemically
» absorbed everyday and this BUILDS UP everyday until the amount is such that
» it starts to influences libido.
» This amount varies from person to person.
» Flutamide has a very short half-life, so when I stopped using it for 2-3
» days the libido improved.
»
» My feedback to Ron Lev: unfortunalty there is a high possibility that many
» users will have severe libido issues due to Flutamide AFTER SOME TIME, but
» if they decrease the dosage/frequency, libido should come back fairly
» quickly.

El Duterino,

Your experiences with flutamide concur with what our early patients experienced. There is a tradeoff between effectiveness and side effects which you thoroughly understand and have control over. This is the mitigating feature of using flutamide–it has a halflife of only 6 hours in the bloodstream. It is important for people considering the use of MDF or other flutamide-containing compounds to look at your experience (and ours) and to have some skepticism about the hysterics that abound on this forum about flutamide. Another point I should mention is that, when using a topical agent, you can also restrict the amount and coverage to just the most severe areas of hairloss–this is a form of dose control that you do not have with an oral agent.

RonLev

» RU58841 is a wonderful drug that will never see the light of day because
» of the disinterest of Roussel Uclaf (now a part of Aventis) to pursue the
» expense of an FDA approval. (Compounders don’t need an FDA approval for
» hair loss, but we are legally bound to use components that are FDA approved
» for some legitimate indication.)
»
» Bryan, of course we looked at alternatives that you consider worthy, and
» there is a reason why we rejected them.
»
» RonLev

http://www.strakan.com/topicalantiandrogen.html

That company currently owns the patent to RU58841 and the page says that its available for licensing. RonLev, why don’t you guys go ahead with that instead?