Table 3.
Current and novel biologics to the treatment of inflammatory bowel diseases.
| Drug | Manufacturer | Target | Admin | Development status |
||
|---|---|---|---|---|---|---|
| Crohn’s disease | Ulcerative colitis | |||||
| BLOCKADE PRO-INFLAMMATORY CYTOKINES | ||||||
| TNF | Infliximab | MSD | TNF | IV | Approved in EU and USA | Approved in EU and USA |
| Adalimumab | Abbvie | TNF | SC | Approved in EU and USA | Approved in EU and USA | |
| Certolizumab pegol | UCB Pharma. | TNF | SC | Approved in USA | – | |
| Golimumab | MSD | TNF | SC | – | Approved in EU and USA | |
| CT-P13 | Celltrion, Hospira | TNF | IV | Approved in EU | Approved in EU | |
| TNF-Kinoid | Neovacs | TNF | IV | Phase II (-) | – | |
| HMPL-004 (Andrographis paniculata extract) | Hutchison Medipharma Limited | TNF and IL-1β | Oral | Ongoing Phase III | Ongoing Phase III | |
| IL-12/IL-23 | Ustekinumab | Janssen | IL-12/IL-23 (p40 subunit) | IV/SC | Ongoing Phase III | – |
| AMG139 | Amgen | IL-23/IL-23R interaction | IV | Ongoing Phase II | – | |
| BI 655066 | Boehringer Ingelheim | IL-23 (p19 subunit) | SC | Ongoing Phase II | – | |
| IL-6 | PF-04236921 | Pfizer | IL-6 | SC | Ongoing phase I/II | – |
| IL-13 | Tralokinumab | AstraZeneca | IL-13 | SC | – | Phase II (-) |
| Anrukinzumab | Pfizer | IL-13 receptor | IV | – | Phase II (-) | |
| QAX576 | Novartis Pharmaceuticals | IL-13 | IV | Ongoing phase II | – | |
| Bertilimumab | Immune Pharmaceuticals | Eotaxin-1 | IV | – | Ongoing phase II | |
| IL-17 | Vidofluidimus | 4SC AG | IL-17 release | Oral | Phase II (+) | Phase II (+) |
| IL-21 | ATR-107 (PF0530900) | Pfizer | IL-21 receptor | IV/SC | Ongoing phase I | – |
| NNC0114-0006 | Novo Nordisk A/S | IL-21 | IV | Ongoing phase II | – | |
| BLOCKADE OF THE DOWNSTREAM SIGNALLING PATHWAYS MEDIATED BY CYTOKINE | ||||||
| JAK/STAT pathway | Tofacitinib | Pfizer | JAK1, 2 and 3 | Oral | Ongoing phase III | Ongoing phase III |
| Peficitinib (JNJ-54781532) | Janssen | JAK1 | Oral | – | Ongoing phase II | |
| GLPG0634 | Galapagos NV | JAK1 | Oral | Ongoing phase II | – | |
| TGF-β | GED0301 | Giuliani | Smad7 antisense oligonucleotide | Oral | Phase I (+) | – |
| IP-10 antagonists | BMS-936557 | Bristol-Myers Squibb | IP-10 | IV | Ongoing phase II | Phase II (±) |
| Tyrosine kinase receptor | Masitinib (AB1010) | AB science | c-kit, PDGFR α/β; Lck, Lyn, FGFR-3; FAK | Ongoing phase II | – | |
| ANTI-ADHESION MOLECULES | ||||||
| Natalizumab | Tysabri, Biogen Idec | α4 | IV | Approved in USA | – | |
| Vedolizumab | Millennium Pharma . | α4β7 | IV | Phase III (±) | Phase III (+) | |
| Etrolizumab | Genentech | β7 | IV/SC | – | Phase II (+) | |
| PF-00547659 | Pfizer | MadCAM-1 | IV/SC | Ongoing phase II | Ongoing phase II | |
| AJM300 | Ajinomoto | α4 | Oral | – | Phase II (+) | |
| Alicaforsen | ISIS Pharma. | ICAM-1 | Oral/intrarectal | Phase II (-) | Phase II (+) | |
| Vatelizumab | Sanofi | α2β1 integrin | SC | – | Ongoing phase II | |
| firategrast (SB-683699) (formerly T-0047) | GlaxoSmithKline | α4 | Oral | Ongoing phase II | – | |
| GLPG0974 | Galapagos NV | FFA-2 | Oral | – | Ongoing phase II | |
| TRK-170 | Toray Industries, Inc. | β7 | Oral | Ongoing phase II | – | |
| ADMINISTRATION OF ANTI-INFLAMMATORY CYTOKINE | ||||||
| IL-2 | Low dose IL-2 | ILTOO Pharma | IL-2 | SC | Ongoing phase II | Ongoing phase II |
| BLOCKADE OF T-CELL STIMULATION AND INDUCTION OF APOPTOSIS | ||||||
| SB012 | Sterna Biologicals GmbH & Co. KG | GATA-3 | Intrarectal | – | Ongoing phase I/II | |
| VB-201 | VBL Therapeutics | TLR2 dependent innate cell activation | Oral | – | Ongoing phase II | |
| GSK1399686 | GSK | Ribosomal 50S subunit | Oral | – | Ongoing phase II | |
| Laquinimod | Teva Pharmaceutical Industries | ? | Oral | Phase II (+) | – | |
| NNC 0142-0000-0002 | Novo Nordisk A/S | NKG2D | Ongoing phase II | – | ||
| DIMS0150 | InDex Pharmaceuticals | TLR9 | Intrarectal | – | Ongoing phase III | |
| OTHER MECHANISM | ||||||
| Fingolimod | Mitsubishi Tanabe Pharma Corporation | sphingosine 1-phosphate 1 receptor | Oral | Ongoing phase I | – | |
| RPC1063 | Receptos, Inc. | sphingosine 1-phosphate 1 receptor | Oral | – | Ongoing phase II | |
| GSK1399686 | GSK | Ribosomal 50S subunit | Oral | – | Ongoing phase 2 | |
FFA-2, free fatty acid receptor-2; ICAM-1, InterCellular Adhesion Molecule-1; infliximab; Ig, immunoglobulin; IL, interleukin; IP-10, interferon-γ-inducible protein-10; IV, intravenous; JAK, Janus kinase; Lck, lymphocyte-specific kinase; Lyn, Lck/Yes-related protein; MadCAM-1, mucosal address in cell adhesion molecule 1; NZB, natalizumab; NKG2D, natural killer group 2, member D; PDGFR α/β, platelet-derived growth factor receptor-α/β; SC, subcutaneous; TNF, tumor necrosis factor; TGF, transforming growth factor; TLR, Toll-like receptor.