Thalidomide

Delancey

Is it true that Thalidomide is still in use ( albeit not for treating morning sickness as originally designed ) ? What illnesses is it used to treat ?

opinion guy

So far as I know its under trial as an anti-cancer drug against a couple of types of cancer.

Lung cancer for one:
http://news.bbc.co.uk/2/hi/health/8154021.stm

Some others also I believe thou i don't know which cancers.

Tree

It's now separated into its respective entantiamers (sp?), two mirror forms of the same compound. The one that was causing birthdefects was opposite to the one with therapeutic value, but both are produced by the manufacturing process

Delancey

Tree wrote: »

It's now separated into its respective entantiamers (sp?), two mirror forms of the same compound. The one that was causing birthdefects was opposite to the one with therapeutic value, but both are produced by the manufacturing process

Thanks for that info - does this mean that it is possible to separate the ' bad ' compound that causes birth defects ?

nesf

There are plenty of tetrogenic drugs being used so it wouldn't be surprising if it was still in use. It's only really a problem when it's not known to be tetrogenic.

Woden

I recall studying thalidomide as a classic example of chirality/enantiomers.

At the time we where told that even though you can split the enantiomers and administer the safe one in vivo there will be racemisation.

This topic has always interested me and I have been looking over this paper since I stumbled across the thread

From http://www.k-faktor.com/contergan/fi...cemization.pdf

Putative differences in therapeutic or adverse effects between (+)-(R)- and
(-)-(S)-thalidomide would to a large extent be abolished by rapid interconversion in vivo.

So you can split it into the R enantiomer (good) and the S enantiomer (bad) but in the body it is going to convert into both. I am not sure what they mean that adverse effects would be abolished by rapid interconversion in the body. Surely this is not true from experience?

SomeDose

Thalidomide (along with it's newer derivative, lenalidomide) is currently licensed for treatment of multiple myeloma. It may also be in trials for other treatments, but I don't know for sure. For obvious reasons, there are extremely tight prescribing restrictions surrounding its use. The pharmaceutical drug is a mixture of both R and S enantiomers, so it's still highly teratogenic. In theory, however, there is no risk of these effects actually occuring since it's essentially illegal to use in pregnant women and can only be used in women of child-bearing potential if there is virtually zero chance of them becoming pregnant.

anotherlostie

I'm pretty sure that it is also licensed in some jurisdictions for the treatment of leprosy but again, there would need to be precautions taken to prevent women of child bearing age becoming pregnant.

Another teratogenic drug used is misoprostol, indicated for prevention of gastric ulcers when taking NSAID's. It is also an abortifacient and a ripening agent (a case where what is the side effect in one case, is the target action in another). Any woman of child bearing age on the drug for ulcer prevention must ensure she doesn't become pregnant.