26 July 2009


Two reviews in the July issue of Drug Discovery Today provide an update on the state of FBDD.

The first, from researchers at the VU University, Amsterdam, and IOTA Pharmaceuticals, discusses 23 examples. Many of these have been reviewed elsewhere, but the paper also describes some studies that are unpublished or just reported at meetings. It’s a nice, thorough introduction to the field, and the organization of the review, by institution, gives a flavor of the diversity of approaches.

The second review, from researchers at Astex Therapeutics, provides a historical perspective and clinical focus. There are also useful tables of commercial suppliers of fragments as well as FBDD-derived compounds that have made it into clinical development.

In an accompanying editorial, Mark Whittaker of Evotec asks whether fragment-based drug discovery (FBDD) should really be called fragment-assisted drug discovery (FADD):

This is more than just a difference in semantics, but is, in fact, a broader question of when and how to apply fragment approaches to lead generation, either on their own or in concert with other hit finding techniques.

He goes on to explain that although fragment-based methods can be used by themselves to generate leads, they can also be complementary to other approaches to assess target druggability or focus later hit-finding. This conclusion is consistent with Practical Fragments’ latest poll, in which 85% of respondents reported that, far from being a fad, FBDD (or, if you like, FADD) is integrated in the hit finding stage at their company.

1 comment:

James said...

Do we really care if it's based on fragments or assisted by fragments - do they work is the question!! There's enough discussion and disagreement around the nomenclature for ligand efficiency, lets not muddy the waters even more with another FLA (or Four Letter Accrynym for the uninitiated), lets just get on with the job of trying to discover some new value adding drug candidates.