Table 1.
Summary of GPCR Targeting Clinical Trials for IPF
| Receptor activity | Drug | Outcomes | Status | Trial Number Citation |
|---|---|---|---|---|
| ETA and ETB antagonist | Bosentan | No significant Improvements. | Phase 2/3 (completed) | NCT00071461 [106] |
| ETA and ETB antagonist | Bosentan | No significant Improvements. | Phase 3 (completed) | NCT00391443 [107] |
| ETA antagonist | Ambrisentan | More patients experienced disease progression and death in treatment group compared to placebo. | Phase 3 (terminated) | NCT00768300 [108] |
| ETA and ETB antagonist | Macitentan | No significant Improvements. | Phase 2 (completed) | NCT00903331 [109] |
| LPA1 antagonist | BMS-986020 | Improvement in forced vital capacity for the 600 mg/bid group compared to placebo. | Phase 2 (completed) | NCT01766817 [110] |
| GPR40 agonist and GPR84 antagonist | PBI-4050 | PBI-4050 alone or in combination was well tolerated. | Phase 2 (completed) | NCT02538536 [111] |
| AT1 antagonist | Losartan | Improvement in forced vital capacity. | Pilot Study | NCT00879879 [112] |
| β2 Adrenergic agonist | Formoterol | Treatment significantly improved forced expiratory volume and flow. | Pilot Study | EudraCT: 2013-004404-19 [113] |
| Leukotriene antagonist | Tipelukast | - | Phase 2 (recruiting) | NCT02503657 |
| Prostanoid antagonist | Treprostinil | - | Phase 2 (terminated) | NCT00703339 |
| Prostanoid antagonist | Treprostinil | - | Phase 2 (completed) | NCT00705133 |
| GPR84 antagonist | GLPG1205 | - | Phase 2 (recruiting) | NCT03725852 |
| Smoothened antagonist | Vismodegib | - | Phase 1 (completed) Phase 2 (terminated) | NCT02648048 NCT02168530 |
| Serotonergic and Dopaminergic ligand | RP5063 | - | Phase 2 (planning) | - |