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.
| Drug | Company | Target |
|---|---|---|
| Approved! | ||
| Vemurafenib | Plexxikon | B-Raf(V600E) |
| Venetoclax | AbbVie/Genentech | Selective Bcl-2 |
| Phase 3 | ||
| Asciminib | Novartis | Bcr-Abl |
| Erdafitinib | J&J/Astex | FGFR1-4 |
| Lanabecestat | AstraZeneca/Lilly/Astex | BACE1 |
| PLX3397 | Plexxikon | CSF1R, KIT |
| Verubecestat | Merck | BACE1 |
| Phase 2 | ||
| AT7519 | Astex | CDK1,2,4,5,9 |
| AT9283 | Astex | Aurora, JAK2 |
| AUY-922 | Vernalis/Novartis | HSP90 |
| AZD5363 | AstraZeneca/Astex/CR-UK | AKT |
| CPI-0610 | Constellation | BET |
| DG-051 | deCODE | LTA4H |
| eFT508 | eFFECTOR | MNK1/2 |
| Indeglitazar | Plexxikon | pan-PPAR agonist |
| LY2886721 | Lilly | BACE1 |
| LY517717 | Lilly/Protherics | FXa |
| Navitoclax (ABT-263) | Abbott | Bcl-2/Bcl-xL |
| Onalespib | Astex | HSP90 |
| PF-06650833 | Pfizer | IRAK4 |
| PF-06835919 | Pfizer | KHK |
| Phase 1 | ||
| ABT-518 | Abbott | MMP-2 & 9 |
| ABT-737 | Abbott | Bcl-2/Bcl-xL |
| ASTX029 | Astex | ERK1,2 |
| ASTX660 | Astex | XIAP/cIAP1 |
| AT13148 | Astex | AKT, p70S6K, ROCK |
| AZD3839 | AstraZeneca | BACE1 |
| AZD5099 | AstraZeneca | Bacterial topoisomerase II |
| BI 691751 | Boehringer Ingelheim | LTA4H |
| ETC-206 | D3 | MNK1/2 |
| GDC-0994 | Genentech/Array | ERK2 |
| IC-776 | Lilly/ICOS | LFA-1 |
| LP-261 | Locus | Tubulin |
| LY2811376 | Lilly | BACE1 |
| MAK683 | Novartis | PRC2 EED |
| Mivebresib | AbbVie | BRD2-4 |
| PLX5568 | Plexxikon | kinase |
| SGX-393 | SGX | BCR-ABL |
| SGX-523 | SGX | Met |
| SNS-314 | Sunesis | Aurora |
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.
This post hasn't even been up a week but it's already out of date: I just learned that ABBV-744, a BD2-selective BET inhibitor derived from the same fragment as ABBV-075, is in Phase 1.
ReplyDeleteSeveral more FBDD-derived drugs of which I've become aware:
ReplyDeleteLY3202626 - Phase 2, Lilly, BACE1, terminated
AMG 510, Phase 1, Amgen, KRAS G12C mutant, active
AZD5991, Phase 1, AztraZeneca, MCL1, active
HTL14242, Phase 1, Heptares, mGlu5 NAM, active
S64315, Phase 1, Servier/Novartis/Vernalis, MCL1, active
And a third approval - erdafitinib!
ReplyDeleteAnd then there were four: pexidartinib (née PLX3397) was approved last year for tenosynovial giant cell tumor.
ReplyDelete