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. 2021 Jun 29;10(7):1629. doi: 10.3390/cells10071629

Table 1.

A summary of clinical trials targeting LPA receptors (LPARs).

No. ClinicalTrials.gov Identifier Mechanism Project Title Study Design Outcome
1 NCT01766817 LPAR1 antagonist (BMS-986020) Safety and efficacy of a lysophosphatidic acid receptor antagonist in idiopathic pulmonary fibrosis Phase 2; parallel-arm, multicenter, randomized, double-blind, placebo-controlled trial; 143 patients with idiopathic pulmonary fibrosis were randomized and treated. BMS-986020 600 mg bid treatment for 26 weeks significantly slowed the lung function decline compared with placebo [124,125].
2 NCT02068053 LPAR1 antagonist (BMS-986020) Absorption, distribution, metabolism, and excretion (ADME) study of BMS-986020 Phase 1; a single group assignment to investigate the pharmacokinetic, biotransformation, routes of elimination, and mass balance of BMS-986020 in humans; 6 healthy participants. It was completed in April 2014. No results were posted [126].
3 NCT02101125 LPAR1 antagonist (BMS-986020) Drug interaction study with Rosuvastatin Phase 1; an open-label, single-sequence study to evaluate the effect of concomitant administration of BMS-986020 on the single-dose pharmacokinetics of Rosuvastatin in healthy subjects; 26 healthy participants. It was completed in May 2014. No results were posted [127].
4 NCT03429933 LPAR1 antagonist (BMS-986278) A study of experimental medication BMS-986278 given to healthy participants Phase 1; a double-blind, placebo-controlled, randomized, single and multiple ascending dose study of oral BMS-986278 administration in healthy participants; 112 healthy participants. It was completed in March 2019. No results were posted [128].
5 NCT04308681 LPAR1 antagonist (BMS-986278) A study measuring the effectiveness, safety, and tolerability of BMS-986278 in participants with lung fibrosis Phase 2; a multicenter, randomized, double-blind, placebo-controlled study; 360 patients with lung fibrosis. It started in July 2020 and is currently still recruiting [129].
6 NCT04069143 LPAR1 tracer (BMT-136088) Safety, tolerability, kinetics, and repeatability of the novel LPA1 PET ligand 18F-BMS-986327 Phase 1; an open-label study; 20 participants (healthy or with idiopathic pulmonary fibrosis). It started in October 2019 and is currently still recruiting [130].
7 NCT01651143 LPAR1 antagonist (SAR100842) Proof of biological activity of SAR100842 in systemic sclerosis Phase 2; a double-blind, randomized, placebo-controlled study; 32 patients with diffuse cutaneous systemic sclerosis. SAR100842 was well tolerated in patients. The modified Rodnan skin thickness score improved during the study, although the difference was not significant [131].