06 October 2018

Fragments in the clinic: 2018 edition

To celebrate FBLD 2018, we're updating the list of FBLD-derived drugs. The current list contains 40 molecules - 25% more than the last compilation two years ago. As always, this table includes compounds whether or not they are still in development (indeed, some of the companies no longer even exist). Drugs reported as still active in clinicaltrials.gov, company websites, or other sources are in bold, and those that have been discussed on Practical Fragments are hyperlinked to the most relevant post.


DrugCompanyTarget
Approved!

VemurafenibPlexxikonB-Raf(V600E)
VenetoclaxAbbVie/GenentechSelective Bcl-2
Phase 3

AsciminibNovartisBcr-Abl
ErdafitinibJ&J/AstexFGFR1-4
LanabecestatAstraZeneca/Lilly/AstexBACE1
PLX3397PlexxikonCSF1R, KIT
VerubecestatMerckBACE1
Phase 2

AT7519AstexCDK1,2,4,5,9
AT9283 AstexAurora, JAK2
AUY-922Vernalis/NovartisHSP90
AZD5363AstraZeneca/Astex/CR-UKAKT
CPI-0610ConstellationBET
DG-051deCODELTA4H
eFT508eFFECTORMNK1/2
IndeglitazarPlexxikonpan-PPAR agonist
LY2886721LillyBACE1
LY517717Lilly/ProthericsFXa
Navitoclax (ABT-263)AbbottBcl-2/Bcl-xL
OnalespibAstexHSP90
PF-06650833PfizerIRAK4
PF-06835919PfizerKHK
Phase 1

ABT-518AbbottMMP-2 & 9
ABT-737AbbottBcl-2/Bcl-xL
ASTX029AstexERK1,2
ASTX660AstexXIAP/cIAP1
AT13148AstexAKT, p70S6K, ROCK
AZD3839AstraZenecaBACE1
AZD5099AstraZenecaBacterial topoisomerase II
BI 691751Boehringer IngelheimLTA4H
ETC-206D3MNK1/2
GDC-0994Genentech/ArrayERK2
IC-776Lilly/ICOSLFA-1
LP-261LocusTubulin
LY2811376LillyBACE1
MAK683NovartisPRC2 EED
MivebresibAbbVieBRD2-4
PLX5568Plexxikonkinase
SGX-393SGXBCR-ABL
SGX-523SGXMet
SNS-314SunesisAurora

I have no doubt that this list is incomplete, particularly in Phase 1. If you know of any others (and can mention them) please leave a comment.

1 comment:

Dan Erlanson said...

This post hasn't even been up a week but it's already out of date: I just learned that ABBV-744, a BD2-selective BET inhibitor derived from the same fragment as ABBV-075, is in Phase 1.