Investigational Drug Details
| Drug ID: | D123 |
| Drug Name: | Emricasan |
| Synonyms: | IDN-6556 |
| Type: | Chemical drug |
| DrugBank ID: | DB05408 |
| DrugBank Description: | Emricasan is the first caspase inhibitor tested in human which has received orphan drug status by FDA. It is developed by Pfizer and made in such a way that it protects liver cells from excessive apoptosis. |
| PubChem ID: | 12000240 |
| CasNo: | 254750-02-2 |
| Repositioning for NAFLD: | No |
| SMILES: | N(C(=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)COc1c(F)c(F)cc(c1F)F)CC(=O)O)C)c1c(C(C)(C)C)cccc1 |
| Structure: |
|
| InChiKey: | SCVHJVCATBPIHN-SJCJKPOMSA-N |
| Molecular Weight: | 569.508 |
| DrugBank Targets: | Caspase-1; Caspase-3; Caspase-7 |
| DrugBank MoA: | IDN-6556 significantly improves markers of liver damage in patients infected with the Hepatitis C virus (HCV), an infection that affects up to 170m patients worldwide. IDN-6556 represents a new class of drugs that protect the liver from inflammation and cellular damage induced by viral infections and other causes. Various studies have also shown that it significantly lowers aminotransferase activity in HCV patients and appeared to be well tolerated. |
| DrugBank Pharmacology: | -- |
| DrugBank Indication: | Investigated for use/treatment in hepatitis (viral, C), liver disease, and transplantation (organ or tissue). |
| Targets: | caspase inhibitor |
| Therapeutic Category: | Anti-inflammatory |
| Clinical Trial Progress: | Phase 2 completed (Emricasan treatment did not improve liver histology in patients with NASH fibrosis despite target engagement and may have worsened fibrosis and ballooning. Caspase inhibition lowered serum alanine aminotransferase in the short-term but may have directed cells to alternative mechanisms of cell death, resulting in more liver fibrosis and hepatocyte ballooning. Clinical trial number: Clinical Trials.gov #NCT02686762.) |
| Latest Progress: | Failed in clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0342 | NCT03439189 | Not applicable | Completed | Has Results | August 28, 2016 | October 22, 2020 | Details |
| L0343 | NCT02686762 | Phase 2 | Completed | No Results Available | January 26, 2016 | August 19, 2019 | Details |
| L0359 | NCT02960204 | Phase 2 | Completed | Has Results | October 17, 2016 | February 11, 2022 | Details |
| L0390 | NCT04806750 | Phase 2 | Not recruiting | No Results Available | 17/03/2021 | 29 March 2021 | Details |
| L0575 | EUCTR2015-004473-32-DE | Not applicable | Not Recruiting | No Results Available | -- | -- | Details |
| L0587 | EUCTR2015-004336-35-ES | Phase 2 | Not Recruiting | No Results Available | 18/03/2016 | 28 February 2019 | Details |
| L0817 | NCT03205345 | Phase 2 | Not recruiting | No Results Available | 20/06/2017 | 12 December 2020 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S13 | Anti-apoptosis | hepatocyte apoptosis; hepatic autophagy; apoptosis | Pan-caspase inhibitor | Emricasan | 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 |
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00695 | 35000120 | Clin J Gastroenterol | The impact of emricasan on chronic liver diseases: current data. | Details |
| A03482 | 33987427 | Ann Transl Med | Non-alcoholic fatty liver disease (NAFLD)/non-alcoholic steatohepatitis (NASH)-related liver fibrosis: mechanisms, treatment and prevention. | Details |
| A05080 | 33385317 | J Dig Dis | Efficacy and safety of drugs for nonalcoholic steatohepatitis. | Details |
| A06011 | 33038432 | J Hepatol | Emricasan to prevent new decompensation in patients with NASH-related decompensated cirrhosis. | Details |
| A08128 | 32237916 | Expert Opin Pharmacother | Current and new pharmacotherapy options for non-alcoholic steatohepatitis. | Details |
| A08933 | 31931543 | Z Gastroenterol | [What is the (right) target for non-alcoholic fatty liver disease (NAFLD)?] | Details |
| A09065 | 31887369 | J Hepatol | A randomized, placebo-controlled trial of emricasan in patients with NASH and F1-F3 fibrosis. | Details |
| A09107 | 31870950 | J Hepatol | Randomized placebo-controlled trial of emricasan for non-alcoholic steatohepatitis-related cirrhosis with severe portal hypertension. | Details |
| A12477 | 30430605 | Aliment Pharmacol Ther | Randomised clinical trial: emricasan versus placebo significantly decreases ALT and caspase 3/7 activation in subjects with non-alcoholic fatty liver disease. | Details |
| A12835 | 30261763 | Expert Rev Gastroenterol Hepatol | An update on the recent advances in antifibrotic therapy. | Details |
| A14771 | 29247356 | J Gastroenterol | Current and future pharmacological therapies for NAFLD/NASH. | Details |
| A17704 | 27646933 | Gut | Current and upcoming pharmacotherapy for non-alcoholic fatty liver disease. | Details |
| A22202 | 24750664 | Liver Int | The pan-caspase inhibitor Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. | Details |
| A29903 | 33296631 | Med Sci (Paris) | [Caspase inhibition: From cellular biology and thanatology to potential clinical agents]. | Details |
| A31754 | 29913280 | Clin Gastroenterol Hepatol | Emricasan Improves Liver Function in Patients With Cirrhosis and High Model for End-Stage Liver Disease Scores Compared With Placebo. | Details |
| A47886 | 30063802 | Hepatology | Emricasan (IDN-6556) Lowers Portal Pressure in Patients With Compensated Cirrhosis and Severe Portal Hypertension. | Details |