Investigational Drug Details
| Drug ID: | D268 |
| Drug Name: | PF-05221304 |
| Synonyms: | -- |
| Type: | Chemical drug |
| DrugBank ID: | -- |
| DrugBank Description: | -- |
| PubChem ID: | -- |
| CasNo: | 2248008-98-0 |
| Repositioning for NAFLD: | No |
| SMILES: | O=C(O)C=1C=CC(=CC1)C2=NC(OC)=CC(=C2)C(=O)N3CCC4(CC(=O)C5=C(C=NN5C(C)C)C4)CC3 |
| Structure: |
|
| InChiKey: | LXZMHBHEXAELHH-UHFFFAOYSA-N |
| Molecular Weight: | 502.56 |
| DrugBank Targets: | -- |
| DrugBank MoA: | -- |
| DrugBank Pharmacology: | -- |
| DrugBank Indication: | -- |
| Targets: | ACC inhibitor |
| Therapeutic Category: | Enhance lipid metabolism |
| Clinical Trial Progress: | Phase 2 completed (NCT03248882: AEs were reported for 10/28 (36%) patients after co-administered PF-05221304 and PF-06865571, with no discontinuations due to AEs, and the ACC inhibitor-mediated effect on serum triglycerides was mitigated, suggesting that PF-05221304 and PF-06865571 co-administration has the potential to address some of the limitations of ACC inhibition alone.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0025 | NCT03776175 | Phase 2 | Completed | Has Results | January 4, 2019 | September 23, 2020 | Details |
| L0042 | NCT03248882 | Phase 2 | Completed | Has Results | August 22, 2017 | December 9, 2020 | Details |
| L0122 | NCT04399538 | Phase 2 | Recruiting | No Results Available | August 10, 2020 | December 14, 2021 | Details |
| L0133 | NCT04321031 | Phase 2 | Recruiting | No Results Available | June 15, 2020 | March 18, 2022 | Details |
| L0134 | NCT04395950 | Phase 1 | Withdrawn | No Results Available | December 2020 | August 25, 2021 | Details |
| L0426 | EUCTR2019-004775-39-SK | Phase 2 | Authorised | No Results Available | 01/06/2020 | 7 February 2022 | 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 |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A01728 | 34635855 | Nat Med | ACC inhibitor alone or co-administered with a DGAT2 inhibitor in patients with non-alcoholic fatty liver disease: two parallel, placebo-controlled, randomized phase 2a trials. | Details |
| A06611 | 32809824 | J Med Chem | Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting. | Details |
| A07361 | 32526482 | Cell Mol Gastroenterol Hepatol | Acetyl-CoA Carboxylase Inhibition Improves Multiple Dimensions of NASH Pathogenesis in Model Systems. | Details |
| A47778 | 32065514 | Clin Pharmacol Drug Dev | Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Liver-Targeting Acetyl-CoA Carboxylase Inhibitor (PF-05221304): A Three-Part Randomized Phase 1 Study. | Details |
| A50524 | 35354614 | BMJ Open | Efficacy and safety of an orally administered DGAT2 inhibitor alone or coadministered with a liver-targeted ACC inhibitor in adults with non-alcoholic steatohepatitis (NASH): rationale and design of the phase II, dose-ranging, dose-finding, randomised, placebo-controlled MIRNA (Metabolic Interventions to Resolve NASH with fibrosis) study. | Details |