In the US we're about to celebrate Thanksgiving. One of the things I'm thankful for is the discovery of new medicines, so this seems like an appropriate time to update our tally of fragment-derived drugs.
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 58 molecules, up from 52 last year, with more than 40% approved or in active trials: not bad given that only about 10% of drugs that make it into the clinic are ultimately approved.
Drugs reported
as still active in clinicaltrials.gov, company websites, or other sources are in bold, and the 36 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 |
| 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 | ||
| Capivasertib | AstraZeneca/Astex/CR-UK | AKT |
| 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 |
| 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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