07 September 2010

Fragments in the Clinic: 2010 Edition

It’s been a while since we last tried to tabulate all the drugs derived from fragment-based drug discovery that have entered the clinic. Below is an attempt, culled together from a variety of sources. Those that have been covered on Practical Fragments are hyperlinked to the relevant post.

I realize that some of these 18 drugs have been quietly discontinued, but I’m also sure I’m missing others that have entered the clinic. If you know of any, please add them in the comments.

Phase 3
PLX-4032 Plexxikon B-RafV600E inhibitor

Phase 2
ABT 263 Abbott Bcl-2/Bcl-xL inhibitor
ABT 869 Abbott VEGF & PDGFR inhibitor
AT9283 Astex Aurora inhibitor
LY-517717 Lilly/Protherics FXa inhibitor
Indeglitazar Plexxikon PPAR agonist
VER-52296/NVP-AUY-922 Hsp90 inhibitor

Phase 1
ABT-518 Abbott MMP-2 & 9 inhibitor
ABT-737 Abbott Bcl-2/Bcl-xL inhibitor
AT13387 Astex Hsp90 inhibitor
AT-7519 Astex CDK1,2,4,5 inhibitor
DG-051 deCODE LTA4H inhibitor
IC-776 Lilly/ICOS LFA-1 inhibitor
LP-261 Locus Tubulin inhibitor
PLX-5568 Plexxikon Kinase inhibitor
SGX-393 SGX Bcr-Abl inhibitor
SGX-523 SGX Met inhibitor
SNS-314 Sunesis Aurora inhibitor

1 comment:

Anonymous said...

ABT-869 is not in the clinic anymore...