Investigational Drug Details
| Drug ID: | D136 |
| Drug Name: | Firsocostat |
| Synonyms: | GS-0976; GS-ACC; ND-630; NDI-010976; Firsocostat |
| Type: | Chemical drug |
| DrugBank ID: | DB16166 |
| DrugBank Description: | Firsocostat is under investigation in clinical trial NCT02781584 (Safety, Tolerability, and Efficacy of Selonsertib, Firsocostat, and Cilofexor in Adults With Nonalcoholic Steatohepatitis (NASH)). |
| PubChem ID: | 71528744 |
| CasNo: | 1434635-54-7 |
| Repositioning for NAFLD: | No |
| SMILES: | C([C@H](OC1CCOCC1)c1c(OC)cccc1)n1c2c(c(=O)n(c1=O)C(C(=O)O)(C)C)c(c(s2)c1ncco1)C |
| Structure: |
|
| InChiKey: | ZZWWXIBKLBMSCS-FQEVSTJZSA-N |
| Molecular Weight: | 569.636 |
| DrugBank Targets: | -- |
| DrugBank MoA: | -- |
| DrugBank Pharmacology: | -- |
| DrugBank Indication: | -- |
| Targets: | ACC inhibitor |
| Therapeutic Category: | Enhance lipid metabolism |
| Clinical Trial Progress: | Phase 2 completed (In a randomized placebo-controlled trial of patients with NASH, we found 12-week administration of GS-0976 20 mg decreased hepatic steatosis, selected markers of fibrosis, and liver biochemistry. ClinicalTrials.gov ID NCT02856555.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0130 | NCT02781584 | Phase 2 | Completed | Has Results | June 13, 2016 | March 16, 2022 | Details |
| L0196 | NCT04971785 | Phase 2 | Recruiting | No Results Available | August 9, 2021 | March 11, 2022 | Details |
| L0198 | NCT03987074 | Phase 2 | Completed | Has Results | July 29, 2019 | July 15, 2021 | Details |
| L0213 | NCT03449446 | Phase 2 | Completed | Has Results | March 21, 2018 | December 3, 2020 | Details |
| L0246 | NCT02856555 | Phase 2 | Completed | Has Results | August 8, 2016 | July 24, 2020 | Details |
| L0311 | NCT02891408 | Phase 1 | Completed | Has Results | September 23, 2016 | December 17, 2020 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S02 | Enhance lipid metabolism | triglyceride-lowering; lipid tolerance; lipid metabolism | 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor; Decreases intestinal cholesterol absorption; FXR agonist; ACC inhibitor; FAS inhibitor; DGAT2 inhibitor; SCD-1 inhibitor | Atorvastatin; Ezetimibe; Obeticholic Acid; GS-9674; GS-0976; TVB-2640; IONIS-DGAT2rx; Aramchol; | Details |
| S03 | Anti-fibrosis | fibrosis | Angiotensin Receptor Blocker (ARB); CCR2/CCR5 antagonist; Thyroid receptor β agonist; PEGylated human FGF21 analogue; Monoclonal antibody to lysyl oxidase-like 2 (LOXL2); Galectin-3 inhibitor; FGF19 variant | Losartan; Cenicriviroc; VK-2809; MGL-3196; Pegbelfermin; Simtuzumab; GR-MD-02; NGM282 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A01245 | 34815444 | Sci Rep | A 3D primary human cell-based in vitro model of non-alcoholic steatohepatitis for efficacy testing of clinical drug candidates. | Details |
| A01422 | 34754150 | World J Gastroenterol | Acetyl-CoA carboxylase inhibitors in non-alcoholic steatohepatitis: Is there a benefit? | Details |
| A02701 | 34278169 | Hepatol Commun | Improvements of Fibrosis and Disease Activity Are Associated With Improvement of Patient-Reported Outcomes in Patients With Advanced Fibrosis Due to Nonalcoholic Steatohepatitis. | Details |
| A03845 | 33849361 | Expert Opin Drug Discov | The identification of farnesoid X receptor modulators as treatment options for nonalcoholic fatty liver disease. | Details |
| A05661 | 33169409 | Hepatology | Combination Therapies Including Cilofexor and Firsocostat for Bridging Fibrosis and Cirrhosis Attributable to NASH. | Details |
| A07720 | 32376414 | J Hepatol | Acetyl-CoA carboxylase inhibition disrupts metabolic reprogramming during hepatic stellate cell activation. | Details |
| A08772 | 31990961 | PLoS One | Acetyl-CoA carboxylase 1 and 2 inhibition ameliorates steatosis and hepatic fibrosis in a MC4R knockout murine model of nonalcoholic steatohepatitis. | Details |
| A09983 | 31536725 | Eur J Pharmacol | Farnesoid X nuclear receptor agonists for the treatment of nonalcoholic steatohepatitis. | Details |
| A10031 | 31519114 | Expert Opin Investig Drugs | GS-0976 (Firsocostat): an investigational liver-directed acetyl-CoA carboxylase (ACC) inhibitor for the treatment of non-alcoholic steatohepatitis (NASH). | Details |
| A28794 | 34999207 | Clin Gastroenterol Hepatol | Fenofibrate Mitigates Hypertriglyceridemia in Nonalcoholic Steatohepatitis Patients Treated With Cilofexor/Firsocostat. | Details |
| A43318 | 31984804 | Expert Opin Investig Drugs | NASH and NAFLD: emerging drugs, therapeutic targets and translational and clinical challenges. | Details |
| A50298 | 35439567 | J Hepatol | Safety and efficacy of combination therapy with semaglutide, cilofexor and firsocostat in patients with non-alcoholic steatohepatitis: A randomised, open-label phase II trial. | Details |
| A51118 | 35668318 | Hormones (Athens) | Semaglutide, cilofexor, and firsocostat for nonalcoholic steatohepatitis: a dance that may need more than one dancer. | Details |
| A51306 | 35735253 | Hepatol Commun | Combinations of an acetyl CoA carboxylase inhibitor with hepatic lipid modulating agents do not augment antifibrotic efficacy in preclinical models of NASH and fibrosis. | Details |