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A few years ago pharmaceutical companies made billions of US$ when chiral drugs were declared sufficiently novel to patent, thus chiral forms of drugs discovered long ago as blends of chiral forms are permitted fresh patent status as pure chiral forms.
The new thing here swaps just one or a few carbon
atoms out with Si or Ge atoms to create pharmaceuticals that are based on the vast number of preexisting drugs yet have a patentable novel difference; this is a multibillion dollar opportunity.
When Si or Ge replaces a C at a molecule depending on the location it creates longer circulation times from resistance to P450 enzymatic modification; it also creates the possibility of changing the rate of motion between various bendy shapes known as conformations; changes to these conformations modulates drug effect
Molecular mass effects may also be used to keep SiOrganics or GeOrganics on the body side of the blood brain barrier minimizing side effects.
Imagine a depo provera drug that is oral where one pill lasts more than a month; not only is this a form of birth control, depo provera has been shown to reduce the behavior of pedophiles 95 pt; creating a durable oral version creates new treatment options
technologically either the C at the reactive groups or the <:=:> structural part of cyclic areas can be modified to create effects; there is even the fresh possibility of making one side of a symmetric molecule more labile (motional)than the other promoting new drug effects
<;=;> where (, = C) ( . = Si or Ge)
Thus anyone with the pharmaceutical industry is urged to create a few standard swap outs then create fresh long lasting profitable new drugs
[link]
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83% capitalization efficiency - this is a personal best,
Beany! |
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(a) slower degradation may in many cases correspond to
lower pharmacological activity, particularly for the many
drugs that are given as pre-active compounds or which act
by participating in various reactions. |
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Again, these pills of yours would be easier to swallow if
they weren't written as conclusive reports on an inevitably
successful strategy, and if they weren't padded with
irrelevant detail - it's a bit like trying to convince people
that your spaceship design will work by describing the
precise shape of the cup-holders.
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I'm sure there must be a fatal flaw in this, somewhere, but it
sure *sounds* plausible ... [+] |
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Does anyone else think it's a shame the Daedalus column isn't in New Scientist any more? |
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One problem i can see with this is that liver enzymes are unlikely to metabolise them and they will accumulate. If a drug is prescribed for a particular action and it continues to exert that action beyond the point where the patient is asymptomatic, it will push it the other way. For instance, suppose the carbon next to the amino group in thyroxine were to be replaced with silicon (which may be impossible for all i know), and this then gives it a longer half-life. Someone has an underactive thyroid, so they're given this compound, which has the same action as thyroxine, which again is not necessarily so: similar compounds sometimes have reverse actions, for instance antifolates or warfarin. It then hangs around in the bloodstream and continues to stimulate thyroid receptors, because it's not being broken down by the liver. It may or may not down-regulate TSH. If it doesn't, the patient is now hyperthyroid. |
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Then again, it's fairly normal for halogens to replace hydrogens on drugs, but they're monovalent. They don't have to stick a number of atoms together. Also, just as there are only a few chlorinated or fluorinated biochemical compounds but loads of drugs, i am open to the idea that compounds using a group IV element could be pharmacologically active, though i don't think their actions would be predictable as simply as you suggest. It'd be more a question of testing a compound synthesised from scratch, maybe to fit a particular receptor, and taking it through the whole drug development process. |
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Siloxanes are used medicinally of course, as breast implant goo. |
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bean, can you link some precedent or science for this? Long hang times are desirable as you point out but I am not aware of any drug which produces this effect using Si. |
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I'm not a chemist or a doctor, so I honestly have no idea how plausible this is. But I will say that the entire motive of tweaking the formula just enough to re-patent and eek out another billion dollars is one of the biggest factors of this mess we are in. These companies are not using patents to protect themselves, they are using them to stifle innovation and hold out monopolies as long as possible. The length of time it takes a patent to run it's course is an eternity to the medical field, and the FDA is just another enabler. Even "generic" versions of drugs are still quite expensive. If the effect is the same, just lasts longer.. then it won't really be providing monopoly-like gains, it will just be an improved version, therefore much more fair to the way our market works. |
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