It has been more than a year since our last list of fragment-derived clinical compounds. Since then capivasertib has been approved, bringing the number of marketed drugs to seven. There have also been a few other changes.
As always, this table includes compounds whether or
not
they are still in development (indeed, some of the companies no longer
even exist). Because of this, the Phase 1 section contains a higher
proportion of compounds that are no longer progressing. The full list contains 59 molecules, up slightly from 2022, with just under 40% approved or in active trials.
Drugs reported
as still active in clinicaltrials.gov, company websites, or other sources are in bold, and the 37 that have been discussed on Practical Fragments are hyperlinked to the most relevant post. The list is almost certainly
incomplete, particularly for Phase 1 compounds. If you know of others please leave a comment.
| Drug | Company | Target |
|---|---|---|
| Approved! | ||
| Asciminib | Novartis | BCR-ABL1 |
| Capivasertib | AstraZeneca/Astex/CR-UK | AKT |
| Erdafitinib | Astex/J&J | FGFR1-4 |
| Pexidartinib | Plexxikon | CSF1R, KIT |
| Sotorasib | Amgen | KRASG12C |
| Vemurafenib | Plexxikon | B-RAFV600E |
| Venetoclax | AbbVie/Genentech | Selective BCL-2 |
| Phase 3 | ||
| Lanabecestat | Astex/AstraZeneca/Lilly | BACE1 |
| Navitoclax (ABT-263) | Abbott | BCL-2/BCLxL |
| Pelabresib (CP-0610) | Constellation | BET |
| Verubecestat | Merck | BACE1 |
| Phase 2 | ||
| ASTX029 | Astex | ERK1,2 |
| ASTX660 | Astex | XIAP/cIAP1 |
| AT7519 | Astex | CDK1,2,4,5,9 |
| AT9283 | Astex | Aurora, JAK2 |
| AUY-922 | Vernalis/Novartis | HSP90 |
| AZD5991 | AstraZeneca | MCL1 |
| DG-051 | deCODE | LTA4H |
| eFT508 | eFFECTOR | MNK1/2 |
| Indeglitazar | Plexxikon | pan-PPAR agonist |
| LY2886721 | Lilly | BACE1 |
| LY3202626 | Lilly | BACE1 |
| LY3372689 | Lilly | OGA |
| LY517717 | Lilly/Protherics | FXa |
| LYS006 | Novartis | LTA4H |
| MAK683 | Novartis | PRC2 EED |
| MK-8189 | Merck | PDE10A |
| Onalespib | Astex | HSP90 |
| PF-06650833 | Pfizer | IRAK4 |
| PF-06835919 | Pfizer | KHK |
| PLX51107 | Plexxikon | BET |
| S64315 | Vernalis/Servier/Novartis | MCL1 |
| VK-2019 | Cullinan Oncology / Wistar | EBNA1 |
| Phase 1 | ||
| AG-270 | Agios/Servier | MAT2A |
| ABBV-744 | Abbott | BD2-selective BET |
| ABT-518 | Abbott | MMP-2 & 9 |
| ABT-737 | Abbott | BCL-2/BCLxL |
| AT13148 | Astex | AKT, p70S6K, ROCK |
| AZD3839 | AstraZeneca | BACE1 |
| AZD5099 | AstraZeneca | Bacterial topoisomerase II |
| BI 1823911 | Boehringer Ingelheim | KRASG12C |
| BI 691751 | Boehringer Ingelheim | LTA4H |
| CFTX-1554 | Confo Therapeutics | AT2 receptor |
| ETC-206 | D3 | MNK1/2 |
| GDC-0994 | Genentech/Array | ERK2 |
| HTL0014242 | Sosei Heptares | mGlu5 NAM |
| HTL0018318 | Sosei Heptares | M1-receptor partial agonist |
| HTL9936 | Sosei Heptares | M1-receptor partial agonist |
| IC-776 | Lilly/ICOS | LFA-1 |
| LP-261 | Locus | Tubulin |
| LY2811376 | Lilly | BACE1 |
| Mivebresib | AbbVie | BRD2-4 |
| MRTX1719 | Mirati | PRMT5•MTA |
| Navoximod | New Link/Genentech | IDO1 |
| PLX5568 | Plexxikon | RAF |
| SGX-393 | SGX | BCR-ABL |
| SGX-523 | SGX | MET |
| SNS-314 | Sunesis | Aurora |
| TAK-020 | Takeda | BTK |
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