I don’t normally write about the pharmaceutical industry, but I was intrigued by several posts by Derek Lowe (who does cover this area) on the topic of creating new drugs by deuterating existing ones. Thus he covered the first deuterated drug receiving FDA approval last year, having first reviewed the concept back in 2009. So when someone introduced me to sila-haloperidol, I checked to see if Derek had written about it. Apparently not, so here are a few details.
The idea appears to take a well-known drug, in this case haloperidol and selectively replacing a carbon atom with a silicon atom to form silahaloperidol.[1] The compound was actually reported in 2004 (see data citation 10.5517/cc7yhc0) but its drug-like properties were only reported four years later in 2008. Haloperidol itself has some undesirable side-effects, including those due to the metabolic products of the drug and so there are certainly reasons for trying to reduce these. Here are the main conclusions:
These do seem to add up to a promising route for optimising drug activities. The authors themselves note the “great potential” for drug design. A review in 2017[2] concurs. So along with deuterated drugs, perhaps siladrugs are ones to watch in the future!
Postscript. More reports of silicon analogues.[3]
In the mid to late 1990s as the Web developed, it was becoming more obvious…
I have written a few times about the so-called "anomeric effect", which relates to stereoelectronic…
The recent release of the DataCite Data Citation corpus, which has the stated aim of…
Following on from my template exploration of the Wilkinson hydrogenation catalyst, I now repeat this…
In the late 1980s, as I recollected here the equipment needed for real time molecular…
On 24th January 1984, the Macintosh computer was released, as all the media are informing…