Table 1.
Examples of fragment-based ligand/lead discovery (FBLD)-derived drugs/compounds (adapted from [35]).
| Drug | Company | Target name, Function |
|---|---|---|
| Approved | ||
| Vemurafenib/ZELBORAF | Plexxikon/Roche | BRAF, protein kinase (mutation V600E) |
| Venetoclax/VENCLEXTA | AbbVie/Genentech | BCL-2, apoptosis suppressor protein |
| Erdafitinib/BALVERSA | Janssen Pharmaceutical Companies | FGFRs, fibroblast growth factor receptors |
| Phase III | ||
| Asciminib/ABL001 | Novartis | Bcr-Abl, oncoprotein |
| Lanabecestat 1 | AstraZeneca/Eli Lilly and Company | BACE-1, β-site amyloid precursor protein-cleaving enzyme 1 |
| Pexidartinib/TURALIOTM | Plexxikon/Daiichi Sankyo | CSF1R, colony stimulating factor 1 receptor KIT, proto-oncogene receptor tyrosine kinase |
| Verubecestat 1 | Merck | BACE-1, β-site amyloid precursor protein-cleaving enzyme 1 |
| Phase II | ||
| AT7519 2 | Astex | CDKs, cyclin-dependent kinases |
| AT9283 | Astex | Aurora and JAK2, kinases |
| Luminespib/AUY-922 1 | Vernalis/Novartis | HSP90, heat shock protein |
| Capivasertib/AZD5363 | AstraZeneca/Astex | AKT, serine/threonine protein kinase |
| CPI-0610 | Constellation | BET, bromodomain and extra-terminal protein |
| DG-051 2 | deCODE | LTA4H, leukotriene A4 hydrolase |
| eFT508 | eFFECTOR | MNK1/2, kinases |
| Indeglitazar 2 | Plexxikon | PPARs, peroxisome proliferator-activated receptors |
| LY2886721 2 | Eli Lilly and Company | BACE-1, β-site amyloid precursor protein-cleaving enzyme 1 |
| LY517717 2 | Eli Lilly and Company | FXa, Factor Xa |
| Navitoclax/ABT-263 | Abbott | BCL-2/BCL-XL, apoptosis suppressor proteins |
| Onalespib/AT13387 | Astex | HSP90, heat shock protein |
| PF-06650833 | Pfizer | IRAK4, interleukin-1 receptor-associated kinase |
| PF-06835919 | Pfizer | KHK, ketohexokinase |
| Phase I 3 |
1 Compounds for which the corresponding clinical phase has failed or has been discontinued; 2 Compounds whose development status is unknown; 3 In October 2018, at least nineteen fragment-based ligand/lead discovery (FBLD)-derived drugs were in Phase I.