As I write this, more than 350,000 people worldwide have tested positive for SARS-CoV-2. More than 15,000 of them have died.
It is important to stay aware of what's going on and take appropriate measures to stop the spread of COVID-19. But to paraphrase Nietzsche, one can spend too much time staring into the abyss. In the spirit of hope, Practical Fragments offers an updated list of FBLD-derived drugs.
The current list contains 47 molecules, 7 more than the last compilation, with 4 approved. 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 list contains a higher proportion of compounds that are no longer progressing. 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. The list is almost certainly incomplete, particularly for Phase 1 compounds. If you know of any others (and can mention them) please leave a comment.
It is important to stay aware of what's going on and take appropriate measures to stop the spread of COVID-19. But to paraphrase Nietzsche, one can spend too much time staring into the abyss. In the spirit of hope, Practical Fragments offers an updated list of FBLD-derived drugs.
The current list contains 47 molecules, 7 more than the last compilation, with 4 approved. 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 list contains a higher proportion of compounds that are no longer progressing. 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. The list is almost certainly incomplete, particularly for Phase 1 compounds. If you know of any others (and can mention them) please leave a comment.
| Drug | Company | Target |
|---|---|---|
| Approved! | ||
| Erdafitinib | Astex/J&J | FGFR1-4 |
| Pexidartinib | Plexxikon | CSF1R, KIT |
| Vemurafenib | Plexxikon | B-RAFV600E |
| Venetoclax | AbbVie/Genentech | Selective BCL-2 |
| Phase 3 | ||
| Asciminib | Novartis | BCR-ABL |
| Lanabecestat | Astex/AstraZeneca/Lilly | BACE1 |
| Verubecestat | Merck | BACE1 |
| Phase 2 | ||
| AMG 510 | Amgen | KRASG12C |
| ASTX660 | Astex | XIAP/cIAP1 |
| AT7519 | Astex | CDK1,2,4,5,9 |
| AT9283 | Astex | Aurora, JAK2 |
| AUY-922 | Vernalis/Novartis | HSP90 |
| AZD5363 | AstraZeneca/Astex/CR-UK | AKT |
| AZD5991 | AstraZeneca | MCL1 |
| CPI-0610 | Constellation | BET |
| DG-051 | deCODE | LTA4H |
| eFT508 | eFFECTOR | MNK1/2 |
| Indeglitazar | Plexxikon | pan-PPAR agonist |
| LY2886721 | Lilly | BACE1 |
| LY3202626 | Lilly | BACE1 |
| LY517717 | Lilly/Protherics | FXa |
| MAK683 | Novartis | PRC2 EED |
| Navitoclax (ABT-263) | Abbott | BCL-2/BCLxL |
| Onalespib | Astex | HSP90 |
| PF-06650833 | Pfizer | IRAK4 |
| PF-06835919 | Pfizer | KHK |
| Phase 1 | ||
| ABBV-744 | Abbott | BD2-selective BET |
| ABT-518 | Abbott | MMP-2 & 9 |
| ABT-737 | Abbott | BCL-2/BCLxL |
| ASTX029 | Astex | ERK1,2 |
| 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 |
| HTL0014242 | Sosei Heptares | mGlu5 NAM |
| IC-776 | Lilly/ICOS | LFA-1 |
| LP-261 | Locus | Tubulin |
| LY2811376 | Lilly | BACE1 |
| Mivebresib | AbbVie | BRD2-4 |
| Navoximod | New Link/Genentech | IDO1 |
| PLX5568 | Plexxikon | RAF |
| S64315 | Vernalis/Servier/Novartis | MCL1 |
| SGX-393 | SGX | BCR-ABL |
| SGX-523 | SGX | MET |
| SNS-314 | Sunesis | Aurora |
We live in scary times. But, as this list demonstrates, by working together we can still achieve marvels.
Phase 1/2A clinical trial of VK-2019 (that targets EBNA1) in patients with EBV-positive advanced nasopharyngeal carcinoma. (https://clinicaltrials.gov/ct2/show/NCT03682055). Molecule was discovered and developed by the Wistar Institute and licensed by Cullinan Oncology. (https://www.cullinanoncology.com/2019/01/30/cullinan-to-develop-ebna1-inhibitor/)
ReplyDeleteHi Troy,
ReplyDeleteCongratulations - is this related to your work that we profiled here?
And via LinkedIn, Alastair Donald noted that AZD5363 (capivasertib) is actually already in Phase 3.
So out of date in less than a day - in a good way!
I am surprised that you list Verubecestat and Lanabecestat, both BACE1 inhibitors.
ReplyDeleteAs far as I know the plug has been pulled on them due to inefficacy, or even
making things worse.
Also, LY2811376 has been dropped.
ReplyDeleteThanks Unknown. As I write above, "As always, this table includes compounds whether or not they are still in development..."
ReplyDelete