Table 1.
Novel targeted therapies
| Target | Agent | Company | Administration | Phase |
|---|---|---|---|---|
| Targeting signaling events in tumor cell development | ||||
| FGFR3 | SU5402 | Sugen Inc. | ||
| SU10991 | Sugen Inc. | |||
| PD173074 | Pfizer | |||
| CHIR-258 | Novartis/Chiron | p.o. | I/II | |
| PRO-001 (hu-anti-FGFR3 Fab) | ProChon Biotech Ltd. | |||
| HDAC | SAHA (Vorinostat) | Merck | i.v. | I |
| NVP-LAQ824 | Novartis | p.o. | ||
| LBH 589 | Novartis | p.o. | II | |
| romidepsin (depsipeptide, FK228) | Gloucester Pharm. | i.v. | I/II | |
| ITF2357 | Italfarmaco | p.o. | ||
| PXD101 | CuraGen | i.v. | II | |
| belinostat | TopoTarget AIS | p.o. | II | |
| MS-275/SNDX-275 | Bayer Schering, Syndax | p.o. | I | |
| HDAC6 | tubacin | Broad Institute | ||
| telomerase | GRN163 | Geron Corp. | i.v. | I |
| TMPyP4 | ||||
| Telomestatin | ||||
| microtubuli | Epothilone B (KOS-862) | Novartis | i.v. | |
| CDKs | Flavopiridol/alvocidib | NCI | i.v. | II |
| PD 0332991 | Pfizer | p.o. | I/II | |
| Targeting the cell membrane | ||||
| HMG-CoA | Statins: | Merck | p.o. | I/II |
| Lovastatin | ||||
| Fluvastatin | ||||
| Simvastatin | ||||
| Targeting cytokines, growth factors and their receptors | ||||
| IL-6 | CNT328 | Centocor | i.v. | I/II |
| Sant7 | Sigma-Tau | i.v. | ||
| VEGF | PTK787/ZK222584 (vatalanib) | Novartis | p.o. | II |
| Pazopanib (GW786034B) | GlaxoSmithKline | p.o. | II | |
| Sorafenib (BAY43-9006/nexavar) | Bayer and Onyx | p.o. | I | |
| Avastin | Genentech | i.v. | I/II | |
| ZD6474 | Astra Zeneca | p.o. | II | |
| SU5416 | Sugen Inc. | i.v. | II | |
| Sunitinib (SU011248) | Pfizer | p.o. | II | |
| PI-88 | Progen | s.c. | ||
| XL999 | Exelixis | i.v. | II | |
| Neovastat (AE-941) | Aeterna Zentaris | p.o. | II | |
| FGF, VEGF | BIBF100 | Boehringer Ingelheim | p.o. | |
| SDF-1 | AMD3100/perixafor/JM3100 | Genzyme | i.v. | II/III |
| CD40 | SGN-40 | Seattle Genetics | i.v. | I |
| Chir12-12 | Chiron | i.v. | ||
| TRAIL-R1 | HGS-ETR1 (mapatumumab) | Human Genoma | s.c. | II |
| TACI-Ig | Atacicept | ZymoGenetics | i.v. | |
| IGF-1 | NVP-ADW742 | Novartis | p.o. | |
| CP-571871 | Pfizer | i.v. | ||
| JB-1 | Chiron | i.v. | ||
| CD56 | BB-10901 | ImmunoGen | I.v. | I |
| Targeting downstream signaling pathways | ||||
| FT | R115777 (tipifarnib/zarnestra) | J&J | p.o. | I/II |
| SCH66336 (lonafarnib) | Schering- Plough | p.o. | ||
| Raf-1 | Sorafenib (BAY43-9006/nexavar) | Bayer | p.o. | I/II |
| MEK1/2 | AZD6244 (ARRY-14886) | Astra Zeneca | p.o. | |
| Akt | Perifosine (KRX-0401) | Keryx | p.o. | I/II |
| mTOR | Rapamycin, P70S6 | Genentech | p.o. | |
| CCI-779 (temsirolimus) | Wyeth | i.v. | II | |
| RAD001 (everolimus) | Novartis | p.o. | II | |
| AP23573 (deforolimus) | Ariad | i.v. | II | |
| JAK/Stat | Atiprimod | Callisto Pharm. | p.o. | I/II |
| SAPK/JNK | Aplidin (plitidepsin) | PharmaMar | i.v. | II |
| p38 | SCIO-469 | SCIOS Inc. | p.o. | II |
| NFkB, IkK | PS-1145 | Millenium | p.o. | |
| BAY11-7082 | Biomol | |||
| RTA 402 (CDDO-Me) | Reata | p.o. | I | |
| AS602868 | Merck | p.o. | ||
| MLN120B | Millenium | |||
| ACHP | Bayer | |||
| Wnt | PKF115-584 | |||
| PKC | Enzastaurin | Eli Lilly | p.o. | I/II |
| Midostaurin (PKC412) | Novartis | p.o. | ||
| HSP90 | Tanespimycin (KOS-953) | Kosan Biosciences | p.o. | II |
| Geldanamycin (17-AAG) | Kosan | i.v. | II | |
| Inducing MM cell apoptosis | ||||
| Smac agonists | LBW242 | Novartis | ||
| SOD | 2ME2 | EntreMed | p.o. | II |
| Bcl2 | B3139 (Genasense)/oblimersen | Genta Incorp. | i.v. | III |
| Targeting MM cells and the MM BM microenvironment | ||||
| proteasome | NPI-0052 | Nereus | i.v. | I |
| PR-171 | Cephalon | i.v. | I | |
| CEP-18770 | Cephalon | i.v. | ||
| Thal | Thalidomide | Celgene | p.o. | |
| IMiD | Lenalidomide | Celgene | p.o. | |
| Treating MM bone disease | ||||
| RANKL: Fc | RANKL: Fc | J&J | p.o. | I/II |
| OPG: Fc | OPG: Fc | Schering- Plough | p.o. | |
| OPG | AMGN-0007 | Bayer | p.o. | |
| HDAC | PXD101 (belinostat) | Astra Zeneca | p.o. | II |
| MEK | AZD6244/ARRY- 142886 | Keryx | p.o. | |
| - | Resveratrol | Genentech | p.o. | |
| CCR1 | MLN3897 | Wyeth | i.v. | |
| COX | SDX-308 | Novartis | p.o. | |
| IMiDs | IMiDs: CC-4047, Lenalidomide | Callisto Pharm. | i.v. | |
| Proteasome | Bortezomib | PharmaMar | i.v. | |
| DKK-1 | ||||