27 November 2012

Is this a Fragment?

Fierce Biotech has a listing of the top 15 (potential) late stage blockbusters in development.  I think these lists Fierce put out are very interesting.  The last one on the list is alpharadin.  Its a potential treatment for bone metastases and Bayer just came up with data that it could also be a broad spectrum treatment for prostate cancer.  We typically don't discuss late stage development; so few of us have actually been there its like Oz.  What makes this so interesting to me is the chemical structure of alpharadin: radium-223 dichloride.  RaCl2.  Three atoms or 297 g/mol. 

I realize this is not a fragment in the true sense of what most of us do.  I found it fascinating nonetheless.


Dan Erlanson said...

It is remarkable how effective some truly tiny molecules can be: in my 2011 Introduction to Fragment-Based Drug Discovery I noted that more than 400 approved drugs comply with the Rule of 3. In fact, Astex’s Hsp90 inhibitor AT13387
is derived from the drug ethamivan, which was present in their fragment screening library.

Morten G said...

Not a fragment but BG-12 definitely is.

Dr. Teddy Z said...

Morten G, yes it is! I totally forgot about dimethyl fumarate.

Anonymous said...

I wouldn't really call this a fragment either (at least not in the conventional terms), just like I wouldn't consider cisplatin.