It’s been two years since Practical Fragments updated its list of fragment-derived compounds in the clinic, and since then there have been some nice developments. The table below starts from the previous list and also includes everything new we've managed to find. As before, this 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 (PLX4032) | Plexxikon | B-Raf(V600E) inhibitor |
| Phase 3 | ||
| ABT-199 | Abbott | Selective Bcl-2 inhibitor |
| LEE011 | Novartis/Astex | CDK4 inhibitor |
| MK-8931 | Merck | BACE1 inhibitor |
| Phase 2 | ||
| AT13387 | Astex | HSP90 inhibitor |
| AT7519 | Astex | CDK1,2,4,5 inhibitor |
| AT9283 | Astex | Aurora, Janus kinase 2 inhibitor |
| AUY922 | Vernalis/Novartis | HSP90 inhibitor |
| AZD3293 | AstraZeneca/Astex/Lilly | BACE1 inhibitor |
| AZD5363 | AstraZeneca/Astex/CR-UK | AKT inhibitor |
| Indeglitazar | Plexxikon | pan-PPAR agonist |
| Linifanib (ABT-869) | Abbott | VEGF & PDGFR inhibitor |
| LY2886721 | Lilly | BACE1 inhibitor |
| LY517717 | Lilly/Protherics | FXa inhibitor |
| Navitoclax (ABT-263) | Abbott | Bcl-2/Bcl-xL inhibitor |
| PLX3397 | Plexxikon | FMS, KIT, and FLT-3-ITD inhibitor |
| Phase 1 | ||
| ABT-518 | Abbott | MMP-2 & 9 inhibitor |
| ABT-737 | Abbott | Bcl-2/Bcl-xL inhibitor |
| AT13148 | Astex | AKT, p70S6K inhibitor |
| AZD3839 | AstraZeneca | BACE1 inhibitor |
| AZD5099 | AstraZeneca | Bacterial topoisomerase II inhibitor |
| DG-051 | deCODE | LTA4H inhibitor |
| IC-776 | Lilly/ICOS | LFA-1 inhibitor |
| JNJ-42756493 | J&J/Astex | FGFr inhibitor |
| LP-261 | Locus | Tubulin binder |
| LY2811376 | Lilly | BACE1 inhibitor |
| PLX5568 | Plexxikon | kinase inhibitor |
| (RG-7129) | Roche | BACE1 inhibitor |
| SGX-393 | SGX | Bcr-Abl inhibitor |
| SGX-523 | SGX | Met inhibitor |
| SNS-314 | Sunesis | Aurora inhibitor |
| Undisclosed | Vernalis/Servier | Bcl-2 inhibitor |
The current list contains more than 30 clinical-stage drugs but is certainly incomplete, particularly in Phase I. If you know of any others (and can mention them) please leave a comment.
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5 comments:
As a reminder, AStex was acquired by Otsuka, so updates may be less frequent but may show up here:
http://www.otsuka.com/en/rd/pharmaceuticals/pipeline/
Also, Novartis recently returned rights to AUY922 to Vernalis, placing its future highly in doubt given the shift in corporate strategy by Vernalis.
Navitoclax should be de-bolded. It was halted due to dose-dependent thrombocytopenia. Its successor is ABT-199 (venetoclax), which also had a rocky time a couple of years ago when deaths due to tumor lysis syndrome triggered a clinical hold, but that problem seems to have been surmounted.
Just a few updates: PLX3397 is now in Phase 3, and Vernalis has an open phase 2 trial for their FAAH inhibitor V158866.
Another update: ABL001, an allosteric Abl inhibitor from Novartis, is in a Phase 1 trial for CML and ALL - stay tuned for more details!
Fresh from Pacifichem, ASTX660, Astex's cIAP/XIAP inhibitor, is now in a Phase 1-2 trial for advanced solid tumors and lymphomas.
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