Drugs in various stages of development targeting TNF/TNFR for the focus IMIDs (phase 2 and above)
| Drug (Trade name) . | Target and action . | Form . | Stage and indications . |
|---|---|---|---|
| TNF axis | |||
| ABBV-3373 | TNF antagonism, glucocorticoid receptor modulation | Adalimumab-GRM steroid conjugate (ADC) | Phase 2: RA |
| Adalimumab (Humira) | TNF antagonism | Human IgG1 κ mAb | Launched: CD, psoriasis, RA, UC |
| Certolizumab pegol (Cimzia) | TNF antagonism | PEGylated anti-TNF F(ab) fragment of humanized IgG1 κ mAb | Launched: CD, psoriasis, RA; Phase 2: UC |
| Etanercept (Enbrel) | TNF antagonism | Fusion of extracellular domain of human TNFR2 and the Fc portion of human IgG1 Ab | Launched: psoriasis, RA |
| Golimumab (Simponi) | TNF antagonism | Human IgG1 κ mAb | Launched: UC, RA; Phase 2: CD |
| Infliximab (Remicade) | TNF antagonism | Humanized IgG1 κ mAb | Launched: CD, psoriasis, RA, UC |
| Ozoralizumab (Nanozora) | TNF antagonism | Humanized trivalent, bispecific nanobody made of two anti–TNFα VHHs and an anti–HSA VHH | Launched: RA (Japan) |
| SAR441566 | TNF antagonism | Small molecule | Phase 2: RA, psoriasis |
| TL1A axis | |||
| RG6631 | TL1A antagonism | Human IgG1 mAb | Phase 2: UC, CD |
| TEV-48574 | TL1A antagonism | Human IgG1 mAb | Phase 2: UC, CD |
| Tulisokibart | TL1A antagonism | Humanized IgG1 mAb | Phase 2: UC, CD |
| CD40/CD40L axis | |||
| Abiprubart | CD40 antagonism | Humanized Fc-silenced IgG4 mAb | Phase 2: RA |
| Dapirolizumab pegol | CD40L antagonism | PEGylated anti-CD40L F(ab’) fragment of humanized mAb | Phase 3: SLE |
| Dazodalibep | CD40L antagonism | Fusion of two tenascin-3 Fnlll domains (Tn3) with human serum albumin | Phase 2: RA |
| Frexalimab | CD40L antagonism | Humanized mAb | Phase 2: SLE |
| Iscalimab | CD40 antagonism | Human Fc-silenced IgG1 mAb | Phase 2: SLE |
| Ravagalimab | CD40 antagonism | Humanized IgG1 mAb | Phase 2: UC |
| OX40/OX40L axis | |||
| Amlitelimab | OX40L antagonism | Human IgG4 mAb | Phase 3: AD, Phase 2: Asthma |
| IMG-007 | OX40 antagonism | Humanized Fc modulated IgG1 mAb | Phase 1/2: AD |
| Rocatinlimab | OX40 antagonism | Human IgG1 mAb | Phase 3: AD |
| Telazorlimab | OX40 antagonism | Humanized IgG1 mAb | Phase 2: AD |
| BAFF/BAFF-R axis | |||
| Belimumab (Benlysta) | BAFF antagonism | Human IgG1 λ mAb | Launched: SLE |
| Ianalumab | BAFF-R antagonism | Human IgG1 κ mAb | Phase 3: SLE |
| Povetacicept | BAFF and APRIL neutralization | Fusion of engineered TACI receptor and the Fc portion of human IgG Ab | Phase 2: SLE |
| Rozibafusp alfa | BAFF and ICOSL antagonism | Bispecific IgG2 Ab-peptide conjugate that targets BAFF and ICOSL | Phase 2: SLE |
| Telitacicept | BAFF and APRIL neutralization | Fusion of the TACI receptor and the Fc portion of human IgG Ab | Phase 3: RA, SLE. Launched: SLE (China) |
| Drug (Trade name) . | Target and action . | Form . | Stage and indications . |
|---|---|---|---|
| TNF axis | |||
| ABBV-3373 | TNF antagonism, glucocorticoid receptor modulation | Adalimumab-GRM steroid conjugate (ADC) | Phase 2: RA |
| Adalimumab (Humira) | TNF antagonism | Human IgG1 κ mAb | Launched: CD, psoriasis, RA, UC |
| Certolizumab pegol (Cimzia) | TNF antagonism | PEGylated anti-TNF F(ab) fragment of humanized IgG1 κ mAb | Launched: CD, psoriasis, RA; Phase 2: UC |
| Etanercept (Enbrel) | TNF antagonism | Fusion of extracellular domain of human TNFR2 and the Fc portion of human IgG1 Ab | Launched: psoriasis, RA |
| Golimumab (Simponi) | TNF antagonism | Human IgG1 κ mAb | Launched: UC, RA; Phase 2: CD |
| Infliximab (Remicade) | TNF antagonism | Humanized IgG1 κ mAb | Launched: CD, psoriasis, RA, UC |
| Ozoralizumab (Nanozora) | TNF antagonism | Humanized trivalent, bispecific nanobody made of two anti–TNFα VHHs and an anti–HSA VHH | Launched: RA (Japan) |
| SAR441566 | TNF antagonism | Small molecule | Phase 2: RA, psoriasis |
| TL1A axis | |||
| RG6631 | TL1A antagonism | Human IgG1 mAb | Phase 2: UC, CD |
| TEV-48574 | TL1A antagonism | Human IgG1 mAb | Phase 2: UC, CD |
| Tulisokibart | TL1A antagonism | Humanized IgG1 mAb | Phase 2: UC, CD |
| CD40/CD40L axis | |||
| Abiprubart | CD40 antagonism | Humanized Fc-silenced IgG4 mAb | Phase 2: RA |
| Dapirolizumab pegol | CD40L antagonism | PEGylated anti-CD40L F(ab’) fragment of humanized mAb | Phase 3: SLE |
| Dazodalibep | CD40L antagonism | Fusion of two tenascin-3 Fnlll domains (Tn3) with human serum albumin | Phase 2: RA |
| Frexalimab | CD40L antagonism | Humanized mAb | Phase 2: SLE |
| Iscalimab | CD40 antagonism | Human Fc-silenced IgG1 mAb | Phase 2: SLE |
| Ravagalimab | CD40 antagonism | Humanized IgG1 mAb | Phase 2: UC |
| OX40/OX40L axis | |||
| Amlitelimab | OX40L antagonism | Human IgG4 mAb | Phase 3: AD, Phase 2: Asthma |
| IMG-007 | OX40 antagonism | Humanized Fc modulated IgG1 mAb | Phase 1/2: AD |
| Rocatinlimab | OX40 antagonism | Human IgG1 mAb | Phase 3: AD |
| Telazorlimab | OX40 antagonism | Humanized IgG1 mAb | Phase 2: AD |
| BAFF/BAFF-R axis | |||
| Belimumab (Benlysta) | BAFF antagonism | Human IgG1 λ mAb | Launched: SLE |
| Ianalumab | BAFF-R antagonism | Human IgG1 κ mAb | Phase 3: SLE |
| Povetacicept | BAFF and APRIL neutralization | Fusion of engineered TACI receptor and the Fc portion of human IgG Ab | Phase 2: SLE |
| Rozibafusp alfa | BAFF and ICOSL antagonism | Bispecific IgG2 Ab-peptide conjugate that targets BAFF and ICOSL | Phase 2: SLE |
| Telitacicept | BAFF and APRIL neutralization | Fusion of the TACI receptor and the Fc portion of human IgG Ab | Phase 3: RA, SLE. Launched: SLE (China) |
ICOSL, inducible T cell costimulator ligand; VHH, variable region of heavy-chain-only antibody.